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Deficiency of Vitamin D is very common in Pakistan, even among healthy asymptomatic individuals [1], [2]. Recent studies have shown that the risk of contracting COVID-19 was increased to two-fold, and consequent mortality to 4-fold if the person is Vitamin D deficient [3]. Health care workers including the nursing and administration staff are at a high risk of contracting SARS-CoV2 due to increased regular exposure in a health care setting [4]. Consequently, a convergence of the COVID-19 pandemic, the deficiency of Vitamin D, and the increased exposure can render the health care workers at an additional risk to COVID-19 infection. Our objective was to determine the prevalence of vitamin D deficiency in healthy asymptomatic front-line health care workers and to analyze the change in serum level by loading oral dose of SunnyD STAT softgel capsules (200000 IU Vitamin D3). We followed single centered, cross-sectional, cohort study with subsequent randomized placebo-controlled design for supplementation and follow up. Serum level of 25-hydroxyvitamin D (25OHD) was the main outcome variable, with anthropometric data, nutritional intake, and lifestyle variables analyzed for potential association as risk factors for the outcome. Severe Vitamin D deficiency was found to be prevalent among front line health care workers in this urban hospital-based sample. Serum level of Vitamin D was found to be significantly associated with designation and presence of high blood pressure. The likelihood of increased serum Vitamin D levels was observed with increasing monthly income, higher designation, increasing age and supplementation intake. Mean increase in the serum 25(OH)D3 level after 2 doses of SunnyD STAT softgel capsule (200000 IU Vitamin D3) was 34.22 ng/ml. Public health interventions regarding Vitamin D supplementation and awareness are needed, especially amid COVID-19 pandemicDeficiency of Vitamin D is very common in Pakistan, even among healthy asymptomatic individuals [1], [2]. Recent studies have shown that the risk of contracting COVID-19 was increased to two-fold, and consequent mortality to 4-fold if the person is Vitamin D deficient [3]. Health care workers including the nursing and administration staff are at a high risk of contracting SARS-CoV2 due to increased regular exposure in a health care setting [4]. Consequently, a convergence of the COVID-19 pandemic, the deficiency of Vitamin D, and the increased exposure can render the health care workers at an additional risk to COVID-19 infection. Our objective was to determine the prevalence of vitamin D deficiency in healthy asymptomatic front-line health care workers and to analyze the change in serum level by loading oral dose of SunnyD STAT softgel capsules (200000 IU Vitamin D3). We followed single centered, cross-sectional, cohort study with subsequent randomized placebo-controlled design for supplementation and follow up. Serum level of 25-hydroxyvitamin D (25OHD) was the main outcome variable, with anthropometric data, nutritional intake, and lifestyle variables analyzed for potential association as risk factors for the outcome. Severe Vitamin D deficiency was found to be prevalent among front line health care workers in this urban hospital-based sample. Serum level of Vitamin D was found to be significantly associated with designation and presence of high blood pressure. The likelihood of increased serum Vitamin D levels was observed with increasing monthly income, higher designation, increasing age and supplementation intake. Mean increase in the serum 25(OH)D3 level after 2 doses of SunnyD STAT softgel capsule (200000 IU Vitamin D3) was 34.22 ng/ml. Public health interventions regarding Vitamin D supplementation and awareness are needed, especially amid COVID-19 pandemic.

What is known and objective There is limited information on acceptability of solid dosage forms by young patients with neuromuscular disorders such as Duchenne muscular dystrophy (DMD). Capsule size selection and ability to swallow the NF-κB inhibitor edasalonexent were assessed in males 4-7 years of age with DMD enrolled in clinical trials for a new therapeutic. Methods The Phase 3 PolarisDMD randomized, double-blind, placebo-controlled trial enrolled 131 patients from 8 countries. The Phase 2 MoveDMD trial enrolled 31 patients in the United States. As part of enrolment criteria, these trials assessed the ability to swallow softgel 100 mg (~10 mm) or 250 mg (~15 mm) capsules formulated with a phosphatidylcholine-containing coating. Supportive strategies included pill-swallowing techniques and aids. Results Most (97%; 175/181) patients screened were able to swallow capsules. In Phase 2 and 3, respectively, 77% (24/31) and 61% (80/131) of enrolled patients selected the larger capsule and among those selecting the smaller capsule, most transitioned to the larger capsule. There were no obvious geographical differences in ability to swallow capsules and size selection was not correlated with age. Compliance was high (92%-98%) through 52 weeks of dosing with no discontinuations due to capsule burden. What is new and conclusion Swallowing of capsules was not a barrier for drug administration in young patients with DMD. Capsule formulations may be an acceptable alternative to liquid formulations for children as young as 4 years of age.

Hypothyroidism is a common endocrine disorder affecting 3-15% of the adult population in subclinical form and 0.3-0.8% as overt disease. The mainstay of treatment is replacement monotherapy with levothyroxine (LT4). Currently several oral LT4 formulations including tablets, softgel capsules, and liquid formulations are available. Liquid LT4 is manufactured as LT4 solution in 85% glycerol and 96% ethanol and as LT4 solution in purified water and glycerol. The latest formulation, Tirosint SOL, gained FDA approval in 2017. To evaluate the clinical utility of liquid LT4 we reviewed the literature using three databases: PubMed/MEDLINE, Scopus, and Embase and found 405 articles among which 23 prospective and two retrospective studies were further evaluated. Finally, several case reports on rare clinical conditions were discussed. Our review demonstrated that liquid LT4 was more effective than tablet formulation in patients with malabsorption caused by interfering diseases, drugs, and bariatric surgery. The better pharmacokinetics of liquid LT4 was also confirmed in subjects without malabsorption: patients on replacement or suppressive therapy, who switched from tablet to liquid formulation in equivalent dose, gained better hormonal control, and required less frequent TSH measurements. The drug also appeared effective and easy to handle in patients fed by enteric tube. Liquid LT4 appeared equally effective whenever taken before or during breakfast. The analysis of the drug utility in particular populations including newborns, pregnant women, and the elderly confirmed the high value and safety of liquid LT4. However, in neonates the higher incidence of TSH suppression on liquid in comparison to tablet LT4 therapy was noted, and particular attention to avoid over-treatment must be paid. Concluding: the literature review revealed that liquid LT4 is especially advantageous in patients with malabsorption and the critically ill, but it seems also very promising in common therapy. The lack of alcohol content in the new formulation makes Tirosint SOL especially attractive.

Introduction Vulvar and vaginal atrophy (VVA) affects up to two thirds of postmenopausal women, with symptoms of vaginal dryness, dyspareunia, and vulvar/vaginal irritation. Despite the availability of various treatments, women express dissatisfaction with their options. An estradiol (E2; 4-µg and 10-µg) softgel vaginal insert was approved by the Food and Drug Administration (FDA) to treat moderate to severe dyspareunia, a symptom of VVA, due to menopause. These inserts were designed to treat VVA effectively and safely while avoiding some of the drawbacks of other administration methods. Areas covered This article reviews the physical characteristics and pharmacokinetic data of the E2 softgel vaginal insert. Primary and secondary efficacy endpoints and safety data are reviewed from the pivotal REJOICE trial (NCT02253173), and substudies that explore response rates, changes in vaginal epithelium by visual assessment, efficacy in patient subgroups, effects on sexual function, and patient satisfaction compared with other treatments. Expert opinion The E2 insert shows that vaginal drug delivery is an optimal route of administration for locally treating VVA. This E2 softgel vaginal insert is a safe and effective treatment for symptoms of postmenopausal VVA. The E2 insert's pharmacokinetic characteristics are related to its unique formulation, rapid dissolution, and minimal systemic absorption. Abbreviations AE: adverse event; AUC: area under the concentration-time curve; BMI: body mass index; Cavg: average concentration; CI: confidence interval; Cmax: maximum concentration; Cmin: minimum concentration; E2: estradiol; FDA: Food and Drug Administration; FSFI: Female Sexual Function Index; GSM: genitourinary symptoms of menopause: MBS: most bothersome symptom; NAMS: North American Menopause Society; OR: odds ratio; PI: pulsatility index; PK: pharmacokinetic; REVIVE: Real Women's Views of treatment options for menopausal Vaginal changEs; RI: resistance index; ROC: receiver operating characteristic; TEAE: treatment-emergent adverse event; tmax: time to maximum concentration; VVA: vulvar and vaginal atrophy.

Background. The unresponsiveness to conventional pharmacological treatments and their side effects have led patients with irritable bowel syndrome (IBS) to use complementary and alternative medicine such as herbal remedies. Beside, Zataria multiflora Boiss (ZM), Trachyspermum ammi L. (TA), and Anethum graveolens L. (AG) are being used as an antiseptic, carminative, and antispasmodic in traditional medicine. This trial investigated the efficacy and safety of a combination of ZM, AG, and TA essential oils in the treatment of IBS. Method. The present study was a randomized double-blind clinical trial with parallel groups in Iran. Patients in the control arm received three tablets of 10 mg hyoscine butylbromide daily for two weeks, and the intervention arm was daily treated with two 250 mg softgel capsules containing 180 mg of essential oils of ZM, AG, and TA for two weeks. Primary outcomes were the response rates based on the IBS Symptom Severity Scale (IBS-SSS), IBS Adequate Relief (IBS-AR), and IBS Global Assessment Improvement (IBS-GAI) at the end and two weeks after the end of the intervention. Secondary outcomes were the improvement rates in IBS-SSS scores, improving the quality of life, safety, and tolerability. Results. The posttreatment improvement percentage based on IBS-AR, IBS-GAI, and IBS-SSS scales was 83.9%, 75%, and 87% in the intervention group and 37.9%, 27.5%, and 34.4% in the control group, respectively (P<0.001). Also, the improvement of the quality of life in the herbal medicine arm was significantly more than that in the control arm (P<0.001). Conclusions. According to the results, the herbal medicine investigated in this study can be considered an appropriate alternative treatment for IBS.

Type III lipid-based formulations (LBFs) combine poorly water-soluble drugs with oils, surfactants, and cosolvents to deliver the drugs into the systemic circulation. However, the solubility of the drug can be influenced by the colloidal phases formed in the gastrointestinal tract as the formulation is dispersed and makes contact with bile and other materials present within the GI tract. Thus, an understanding of the phase behavior of LBFs in the gut is critical for designing efficient LBFs. Molecular dynamics (MD) simulation is a powerful tool for the study of colloidal systems. In this study, we modeled the internal structures of five type III LBFs of loratadine containing poly(ethylene oxide) nonionic surfactants polysorbate 80 and polyoxyl hydrogenated castor oil (Kolliphor RH40) using long-timescale MD simulations (0.4-1.7 μs). We also conducted experimental investigations (dilution of formulations with water) including commercial Claritin liquid softgel capsules. The simulations show that LBFs form continuous phase, water-swollen reverse micelles, and bicontinuous and phase-separated systems at different dilutions, which correlate with the experimental observations. This study supports the use of MD simulation as a predictive tool to determine the fate of LBFs composed of medium-chain lipids, polyethylene oxide surfactants, and polymers.

Midostaurin (MDS) is used for the treatment of acute myeloid leukemia, myelodysplastic syndrome, and advanced systemic mastocytosis. MDS softgel capsule samples were subjected to stress testing per International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines for impurity profiling study. MDS underwent extensive degradation under stress testing (acid, alkaline, oxidative, photolytic, thermolytic, and hydrolysis conditions) and formed four degradation products (DPs). MDS and its DPs were separated well from one another with good resolution using reserved-phase HPLC using an Inertsil ODS-3V column (250 × 4.6 mm, 5 μm) and a mobile phase of ammonium formate (40 mM) and acetonitrile. The stability-indicating characteristic of the newly developed method was proven for the estimation of MDS assay, and its organic impurities were free from interference. The validated method exhibited excellent linearity, accuracy, precision, specificity, detection limit, and quantitation limit within 25 min run time. Stress testing, robustness, and solution stability were performed to ensure the continuous performance of the developed method. The peak fractions of DPs formed under stress testing were isolated and characterized using LC-MS, 1 H and 13 C NMR, IR, and UV-Vis. The structure of the major DPs was predicted as DP1 based on the spectral data. The proposed method is effectively used for MDS in bulk drug and finished formulations in the pharmaceutical industry.

Objective: TX-004HR is a low-dose estradiol (E2) softgel vaginal insert designed to be rapidly dissolving and mucoadhesive. This report describes the physical attributes and pharmacokinetic parameters of the softgel vaginal insert evaluated for the treatment of moderate to severe dyspareunia due to menopausal vulvar and vaginal atrophy. Methods: In vitro dissolution studies with 25-μg E2 inserts were performed and media samples were analyzed for E2 by high-performance liquid chromatography. Effects of body position on E2 bioavailability were assessed in a phase 1, randomized trial of the 25-μg softgel capsule versus a reference product in which women remained supine after dosing (n = 16), and in a substudy (n = 16) in which women were ambulatory or seated after dosing. Estradiol Cmax, AUC0-24, and tmax were measured by high-performance liquid chromatography-tandem mass spectroscopy. A phase 2, randomized study (n = 50) of 10-μg E2 versus placebo inserts assessed timing of capsule disintegration at days 1 and 15. Results: In vitro testing detected more than 80% of E2 in the dissolution medium by 15 minutes (first time point measured). In the phase 1 studies, baseline-corrected E2 plasma levels were not significantly different regardless of supine versus ambulatory/seated position after dosing: Cmax, 24.1 versus 34.3 pg/mL; AUC0-24, 77.6 versus 93.7 h · pg/mL; and tmax, 2.1 versus 1.9 hours, respectively. In the phase 2 study, no remnants of the softgel capsule were found at day 1 (6 hours) after dosing and day 15. Vaginal discharge was minimal (1/48 women; 2.1%). Conclusions: The presented data support rapid dissolution of the softgel capsule and similar E2 pharmacokinetic parameters regardless of body position after dosing.

Objective: In the REPLENISH trial, women receiving TX-001HR—an oral, softgel capsule, combining 17β-estradiol (E2) and progesterone (E2 mg/P4 mg 1/100, 0.5/100), had significantly improved vasomotor symptoms, while having their endometrium protected from hyperplasia. The objective here was to describe P4 levels sufficient to counteract the potential endometrial effects of 1 or 0.5 mg oral E2 with TX-001HR. Methods: In REPLENISH (phase 3; NCT01942668), serum P4, E2, and estrone (E1) levels were characterized in postmenopausal women treated with TX-001HR (E2 mg/P4 mg: 1/100, 0.5/100, [0.5/50, 0.25/50 and placebo not reported here]) at baseline, week 12, and month 12 for P4, and at baseline, weeks 4 and 12, and months 6, 9, and 12 for E2 and E1. In a phase 1 study, pharmacokinetic parameters were assessed after 7 daily doses of oral E2 mg/P4 mg (1/100 and 0.5/100). Results: In REPLENISH (n = 1,835), mean P4 levels were 0.39 to 0.55 ng/mL with 100-mg P4 doses; E2 levels were 42.3 to 45.6 pg/mL and 23.0 to 27.4 pg/mL for the 1-mg and 0.5-mg E2 doses, respectively; E1 levels were 214 to 242 pg/mL and 114 to 129 pg/mL for the 1-mg and 0.5-mg E2 doses. In the phase 1 study (n = 40; day 7), mean Cavg for P4 was 0.66 ng/mL with 100-mg P4 doses; E2 was 38.1 pg/mL and 29.2 pg/mL for 1 mg and 0.5 mg E2, respectively; and E1 was 211 and 106 pg/mL for 1 mg and 0.5 mg E2. All three analytes reached steady state within 7 days; accumulation ratios were 1.36 to 1.94. Conclusions: P4 levels observed with TX-001HR were similar in the phase 1 and 3 studies, and were associated with no endometrial hyperplasia with either E2 daily dose over 1 year in the REPLENISH phase 3 study, which showed significant improvements in menopausal vasomotor symptoms.

In postmenopausal women under L-T4 therapy, which was subsequently accompanied by calcium carbonate (CC) supplementation taken 6–8 h after tablet L-T4, TSH levels were greater than prior to adding CC. Total cholesterolemia [CHOL], fasting glycemia [FG], systolic and diastolic blood pressure [SBP, DBP] were also greater than baseline. Our aim was to explore the effects of either liquid or softgel capsule L-T4, while maintaining CC ingestion 6–8 h, later on TSH levels, CHOL, FG, SBP, and DBP. We proposed to 50 hypothyroid postmenopausal women under tablet L-T4 therapy, to switch to either liquid or softgel capsule L-T4 at the same daily dose while maintaining CC ingestion 6–8 h later. Sixteen women accepted [group I; liquid (n = 9), capsule (n = 7)], while 34 continued tablet L-T4 [group II, (n = 34)]. After 3 months, in group I, TSH decreased significantly (1.23 ± 0.49 vs. 1.80 ± 0.37 mU/L, P

Objective: This study aimed to evaluate improvement of dyspareunia and associated vaginal dryness with a 17β-estradiol softgel vaginal insert (TX-004HR; TherapeuticsMD, Boca Raton, FL, USA)...

The softgel, vaginal 17β-estradiol (E2) insert (TX-004HR) significantly improved the maturation index of the vaginal epithelium, dyspareunia and vaginal dryness in menopausal women with vulvar and vaginal atrophy (VVA) and moderate to severe dyspareunia, without histological changes to the endometrium (Constantine G et al, Menopause 2017;24:409-416). The 4-μg and 10-μg E2 doses were FDA approved as Imvexxy® (TherapeuticsMD, Boca Raton, FL), for the treatment of moderate to severe dyspareunia, a symptom of VVA, due to menopause. The progesterone receptor (PR) is an estrogen-regulated gene with expression that is very sensitive to E2 exposure (Xiao CW and Goff AK, J Reprod Fertil.1999;115:101-109). Endometrial PR expression in the biopsies of women using the softgel vaginal 4-µg E2 insert was used as a marker of E2 exposure to determine whether sufficient E2 applied with the vaginal insert reaches the endometrium to upregulate PR expression. Our hypothesis posits that there would be insufficient E2 from the 4-µg E2 insert to stimulate an increase in endometrial PR expression. In this post hoc analysis of the REJOICE trial, endometrial biopsies from 25 women who had a normal baseline biopsy, an on-therapy biopsy after study day 70, and tissue readings from all pathologists were randomly selected from the 4-µg E2 vaginal insert and placebo groups. Endometrial tissue sections were stained to visualize PR expression using PgR1294 (Agilent; Santa Clara, CA). Cell staining was quantified using a trainable feature-recognition algorithm and mean expression levels between baseline and week 12 were analyzed by 2-sided t-tests. Acceptable PR expression results were available for 22 women in the 4-µg E2 group (three had insufficient tissue for analysis) and 25 women in the placebo group. For the 4-µg E2 group, mean ± SD (pmol/mg) PR expression was 0.455 ± 0.203 at baseline and 0.506 ± 0.226 at week 12. For the placebo group, mean PR expression was 0.579 ± 0.196 at baseline and 0.563 ± 0.213 at week 12. Mean PR expression levels at baseline and week 12 were not significantly different from each other within the 4-µg E2 (P=0.438) or placebo (P=0.783) group. No meaningful difference in endometrial PR expression was observed with the vaginal 4-µg E2 insert at week 12. These data support our hypothesis and the assertion that low-dose, local vaginal E2 exposure with the insert placed in the lower part of the vagina, does not pose an endometrial safety issue in postmenopausal women.

A new sildenafil analog has been identified in the softgel shell of a dietary supplement. The compound was investigated by UV spectroscopy and high-resolution MS analysis, leading to the proposed structure 1-methyl-5-{5-[2-(4-methylpiperazin-1-yl)acetyl]-2-propoxyphenyl}-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one. A synthetic reference compound with the proposed structure was prepared, and the two sets of analytical data were compared, confirming the structure of the new compound. The compound was named propoxyphenyl noracetildenafil from its structure and similarity with the known compound.

Background Vaginal microbicides are a promising means to prevent the transmission of HIV and other sexually transmitted infections, by empowering women to initiate use prophylactically when they perceive themselves to be at risk. However, in clinical trials, microbicides have shown mixed results, with the consistent finding that effectiveness varies substantially as a function of user adherence. Methods Based on the assumption that adherence is driven, at least in part, by product properties that influence acceptability, we used softgel technology to develop vaginal drug delivery systems in the intermediate texture space between solids and liquids to overcome potential shortcomings of current dosage forms. Here, we used focus groups and surveys to determine women’s initial reactions (i.e., acceptance and willingness-to-try) for semisoft vaginal suppositories intended for HIV and STI prevention, with a specific focus on how perception of and preferences for vaginal suppositories may be influenced by product characteristics such as size, shape, and firmness. Results Via focus groups, we identified intrinsic and extrinsic factors relevant to acceptability of semisoft suppository prototypes. Willingness-to-try depended on factors like intended functionality, anticipated leakage, type of sex, recommended frequency of use, type of sexual partner, and perceived risk. When handled ex vivo, shape, size, and firmness of suppositories communicated information about ease of imagined insertion and handling, perceived effectiveness, anticipated awareness and comfort of the product in the body. These impressions were partly based on prior experience with vaginal products. Conclusions Sensory attributes appear to play a substantial role in women’s preferences and willingness to try the semisoft suppositories. Using these methods during preclinical development should help efficiently optimize a final product that is both biologically efficacious and preferred by women, toward a goal of enhancing adherence and effectiveness.

Objective: TX-004HR is an investigational, muco-adhesive, vaginal, softgel capsule containing low-dose, solubilized, 17β-estradiol designed to treat postmenopausal vulvar and vaginal atrophy (VVA) and improve user experience without an applicator and less mess. Methods: As part of the 12-week, placebo-controlled, double-blind, phase 3 REJOICE trial evaluating the efficacy/safety of 4-, 10-, and 25-μg TX-004HR in 764 postmenopausal women with VVA, a five-question product survey was administered. Pearson correlation coefficients were used to evaluate correlations between clinical endpoints (vaginal physiology, dyspareunia, and vaginal dryness) and patient acceptability and satisfaction. Results: Majority of the women receiving TX-004HR or placebo reported that the product was easy to use (85.4%-92.1%) and rated ease of capsule insertion as “good” to “excellent” (75.0%-82.6%). A significantly greater percentage of women reported being “very satisfied” or “satisfied” with TX-004HR (68.6%-76.3%) than with placebo (56.8%, P

Capsule is the most versatile of all dosage forms. Capsules are solid dosage forms in which one or more medicinal and inert ingredients are enclosed in a small shell or container usually made of gelatin. There are two types of capsules, “hard” and “soft”. The hard capsule is also called “two pieces” as it consists of two pieces in the form of small cylinders closed at one end, the shorter piece is called the “cap” which fits over the open end of the longer piece, called the “body”. The soft gelatin capsule is also called as “one piece”. Capsules are available in many sizes to provide dosing flexibility. Unpleasant drug tastes and odors can be masked by the tasteless gelatin shell. The administration of liquid and solid drugs enclosed in hard gelatin capsules is one of the most frequently utilized dosage. This proves the oral bioavailability of poorly soluble compounds, delivery of low and ultra-low doses of a compound using softgel also ensures decreased plasma variability. This has led to the commercial pharmaceutical and nutraceutical industries opting for the development of alternative shell forming materials instead of the traditional capsule shell material gelatin. This review discusses establishment and the ongoing development of the manufacturing technology for liquid and semisolid capsules with focus on progress and challenges of soft and hard gelatin capsules formulation in oral administration for improved solubility and as an absorption-enhancing technique. These considerations form a basis for new applications in oral drug delivery.

This study focuses on a novel liquid chromatographic approach that has been developed and approved for the quantitative determination of bexarotene (BXT), its potential impurities in drug substances and drug products. Chromatographic separation was developed on a Symmetry C8 (150 × 4.6) mm 5-µm column with a mobile phase containing an isocratic mixture of acetonitrile:DI water:glacial acetic acid (650:350:7.5) v/v/v at a flow rate of 1.2 mL min−1, and quantitation was carried out using ultraviolet detection at 262 nm for BXT and 290 nm for BHA with a column temperature of 35 °C. The resolution among butylated hydroxyanisole (BHA), BXT and its process-related impurity-A was found to be greater than 5. Regression analysis confers an R value (correlation coefficient) higher than 0.998 for BHA, BXT and impurity-A. The detection level for BXT impurities was found at a level below 0.03% (0.18 µg mL−1). The inter- and intra-day precisions for BHA, BXT and impurities were evaluated and found to have a %RSD of less than 3.0.

Oral lipid-based formulations provide a significant opportunity to address the poor and variable gastrointestinal absorption associated with poorly water soluble drugs. It is useful to discuss how a formulation can strategize various options creatively to overcome some of the challenges posed by the softgel dosage form development of a highly hydrophobic drug with large dose. Etodolac (ETO) was formulated in different lipid vehicle according to Lipid Formulation Classification System (LFCS) to optimize the appropriate fill composition and was subjected to different tests for characterization. Water migration studies, rupture test and mechanical properties of softgels were also performed to investigate the effect of the formulation materials on the integrity, physical stability of the prepared capsules and on the dissolution characteristics of drug. Selected formulations were assessed for in vitro dissolution profile and rupture test for softgel before and after accelerated and shelf stability for 3 months. Results revealed a correlation between the composition of the softgel core fill liquid and drug dissolution parameters. Application of hydrophilic surfactants showed a remarkable enhancement in the dissolution rate of drug. The extent of migration of a solute between a fill and a shell depends on the hydrophilicity of the solute, composition of the shell formulation. Antioxidants should be added to formulations containing hydrophilic surfactants which composed of polyoxyethylene moiety. Nominated formula containing polyethylene glycol/poloxamar 407 showed a good and stable dissolution results after accelerated and shelf stability in addition to better mechanical results.

A serious disease occurs when the pancreas produce insufficient insulin is called diabetes. A various complications that affected to eyes, heart, and nervous system caused by diabetes. The use of synthetic drugs both oral and injection can cause a serious side effects like hypoglycemia. Based on these reasons, many researchers try to develop an anti-diabetic drugs derived from natural resources.One of the plants which potential to decrease glucose level in diabetic patients is Cinnamon (Cinnamomun zeylanicum). Cinnamon extract is very potent to decreases the glucose level in diabetic conditions. Based on this, the cinnamon extract will formulate in softgel forms. The manufacturing process occurs by encapsulate the extract with gelatin film as a shell material. Gelatin is a chewy shell material. The addition of plasticizer in gelatin is very important because its can affected to flexibility of capsule. The encapsulation process with rotary die method occurs using a special machine. The encapsulation process occurs by create a contract manufacture with third person. To ensure theproduct quality, a various test like organoleptic, weight-content uniformity, and rupture test was conducted.

The softgel 17β-estradiol (E2) vaginal inserts (4 and 10 μg; Imvexxy; TherapeuticsMD, Boca Raton, FL) are FDA approved for treating moderate to severe dyspareunia associated with postmenopausal vulvar and vaginal atrophy (VVA). The objective here was to determine responder rates at week 2 and whether week-2 findings predicted week-12 responders in the REJOICE trial.Postmenopausal women received E2 vaginal inserts 4, 10, or 25 μg, or placebo for 12 weeks. Proportion of responders (having ≥2 of the following: vaginal superficial cells5%, vaginal pH5.0, or dyspareunia improvement of ≥1 category) were calculated. Odds ratios (ORs) for positive response at week 12 given a positive response at week 2 were determined in the efficacy evaluable (EE) population.The responder rate (in EE population [n = 695]) was 74% to 82% with E2 inserts versus 24% with placebo at week 2, and 72% to 80% versus 33% at week 12. Positive treatment responses were 9- to 14-fold higher with vaginal E2 than with placebo at week 2, and 5- to 8-fold higher at week 12. Response at week 2 predicted response at week 12 in the total population (OR 13.1; 95% CI, 8.8-19.7) and with active treatment only (OR 7.9; 95% CI, 4.7-13.2).A high percentage of postmenopausal women with moderate to severe dyspareunia responded with the E2 softgel vaginal insert at week 2, and a positive response at week 2 predicted a positive response at week 12.

Objective: Evidence indicates that L-T4 in liquid and softgel capsule are absorbed better than tablets in hypothyroid patients, even when patients are under medications that impair the intestinal absorption of L-T4. However, no study has evaluated all three L-T4 formulations in the same hypothyroid patients. This study aims to fill this gap. The outcome was the degree of TSH change in the liquid and softgel formulations, using tablet L-T4 as the reference, regardless of sequence of formulation and regardless of whether patients were co-ingesting with interfering medications. Methods: We recorded serum TSH levels in two groups of L-T4 replaced patients with primary hypothyroidism (23 subjects who did not co-ingest interfering medications, and 20 subjects who did). Either group of patients took one formulation of L-T4 at a time with variable sequences. In the first group, the median durations of exposure to tablet, liquid or softgel L-T4 were 14, 9 and 10 months, respectively. In the second group the corresponding durations were 13, 11 and 10 months, during which patients co-ingested interfering medications. Results: In the 23 patients, there were 78, 74 or 101 TSH determinations during liquid, softgel capsule or tablet L-T4 regimens. Serum TSH levels associated with liquid, capsule or tablet L-T4 were 1.62 ± 0.51, 1.77 ± 0.44 mU/L (P = 0.049 vs liquid) or 2.38 ± 0.69 mU/L (P

The Vitamin D Assessment (ViDA) study is a randomised, double-blind, placebo-controlled trial to evaluate the efficacy of monthly vitamin D supplementation in reducing the incidence of a range of acute and chronic diseases and intermediate outcomes.The study was carried out in Auckland, New Zealand, among 5110 adults, aged 50-84 years, who were followed for a median 3.3 years. The intervention was vitamin D3 (2.5 mg or 100,000 IU) or placebo softgel oral capsules, mailed monthly to participants' homes, with two capsules sent in the first mail-out post-randomisation (i.e. 200,000 IU bolus, or placebo), followed 1 month later (and thereafter monthly) with 100,000 IU vitamin D3 or placebo capsules. Outcomes were monitored through routinely collected health data and self-completed questionnaires.The results showed no beneficial effect of vitamin D supplementation on incidence of cardiovascular disease, falls, non-vertebral fractures and all cancer. However, beneficial effects from vitamin D supplementation were seen: for persistence with taking statins in participants on long-term statin therapy; and also in bone mineral density and arterial function in participants with low 25-hydroxyvitamin D levels, and in lung function among ever smokers (especially if vitamin D deficient). The latter findings are consistent with several previous studies, CONCLUSION: Monthly high-dose vitamin D supplementation does not prevent a range of diseases, but may be beneficial for some intermediate outcomes in people who are vitamin D deficient.Australian New Zealand Clinical Trials Registry identifier: ACTRN12611000402943.

A consensus industrial reference was necessary to be established for meeting the U.S. Food and Drug Administration’s current Good Manufacturing Practice Compliance for the manufacture and quality control of dietary ingredients and supplements that contain ginger rhizome, dry extract, and/or purified nonvolatile ginger constituents. An analytical method has been developed, validated, and previously published for identifying and quantifying 6-,8- and 10-gingerols, 6-, 8- and 10-shogaols, 6-paradol, and zingerone. HPLC with UV-Vis detector was used for the determination of nonvolatile ginger constituents by following AOAC Guidelines for Single-Laboratory Validation. Sample was accurately weighed and diluted with acidified water and methanol mixture. The sample solution was then sonicated and filtered through a PTFE filter and analyzed under a linear gradient scheme instrument condition. A reverse-phase superficially porous particle C18 column and an absorption wavelength of 230 nm were used for analyte separation and determination. The method was demonstrated to be selective, linear (R2 > 0.999), specific, accurate (91.1–103.2% spike recovery rate), and precise (RSDr < 5%, RSDR < 8%) and therefore met all AOAC Standard Method Performance Requirements (2017.012) criteria. With a relatively short run time (12 min) and optimized extraction solvent system, the method has been validated to simultaneously determine nonvolatile ginger constituents in a variety of dietary ingredients and dietary supplements matrices including dry extract, powder, tablet, capsule, liquid capsule, softgel capsule, and oleoresin.

Background and objective Echinacea angustifolia DC. and Zingiber officinale Roscoe are two natural products with documented immunomodulatory activity, both able to modulate the expression of important immune-related genes. Thus, their use in combination seems to be particularly promising. In this context, we have considered the oral supplementation of a highly standardized lipophilic extract combining both above-mentioned phytocomplexes, formulated in attractive softgel capsules, with two objectives: on the one hand to study oral pharmacokinetic of main active extracts’ components and on the other hand to examine the immunomodulation and anti-inflammatory properties by gene expression profiling. Methods Softgel capsules containing a combination of E. angustifolia DC. and Z. officinale Roscoe (5 mg and 25 mg, respectively) were given by oral administration to 10 healthy volunteers. The plasma concentrations of dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) for E. angustifolia DC., 6-gingerol and 6-shogaol (free and glucuronide) for Z. officinale Roscoe were determined by LC-MS analysis, and the pharmacokinetic analysis was performed. To understand the functional mechanisms responsible for the documented health benefits, we also examined the overall transcriptional remodeling induced in the peripheral blood mononuclear cells and performed an integrative functional analysis on the generated gene expression. Results All bioactive components were absorbed very rapidly, and their tmax were detected in plasma from 30 min to 1.40 h. The peak concentrations of tetraene, 6-gingerol, 6-shogaol and their glucuronide metabolites were 14.74, 5.66, 9.25, 29.2 and 22.24 ng/ml, respectively. Integrated analysis performed on the generated gene expression data highlighted immunomodulatory and anti-inflammatory effects similar to those exerted by hydrocortisone. Conclusion These data demonstrated that the bioactive ingredients are highly and rapidly absorbed from softgel capsules containing the combination of the above-mentioned lipophilic extracts, providing evidence to support their immunomodulatory and anti-inflammatory properties. These data also help in defining the mechanistic pathways underlying the health benefits of these plant-derived bioactive compounds.

The post-prandial satiety response and "second-meal effect" of a viscous fibre supplement PolyGlycopleX(®) (PGX(®)) was evaluated in a single-blind, randomised controlled crossover study of 14 healthy adult women. The two hour post-prandial satiety response, expressed as the area under the curve (AUC) of perceived hunger/fullness score versus post-prandial time, of a standardised evening meal with concurrent intake of either PGX softgel or rice flour softgel (control) was determined. On the following morning, after an overnight fast, the four hour satiety response to a standardised breakfast with no softgel supplementation was assessed. A significantly higher satiety response (AUC) to the standard dinner for the PGX-supplemented dinner compared with the control dinner (p=0.001) was found. No significant difference (p=0.09) was observed in the satiety response (AUC) of the breakfast regardless of which supplemented-dinner had been consumed prior, however the p value indicated a trend towards a higher response to the breakfast following the PGX-supplemented dinner. The fullness scores of the breakfast following the PGX-supplemented dinner at 15, 30, 90, 120, 150, 180, 210 and 240min post-prandial were significantly higher than those for the breakfast following the control dinner (p=

Background: The aerobic vaginitis (AV) is characterized by increased levels of aerobic bacteria, vaginal inflammation and depressed levels of lactobacilli. Objective: The purpose of this study was to investigate the therapeutic efficacy of SilTechTM vaginal softgel capsules, containing new microcrystals of silver monovalent ions, for aerobic vaginitis (AV). Methods: This prospective study enrolled 32 women diagnosed with AV. All recruited women were treated with SilTechTM vaginal softgel capsules once daily for 7 days (one course). Therapeutic efficacy was evaluated based on clinical and microscopic criteria, and cure rates were calculated. Women who were improved (but not cured) received a second course of therapy. Patients classified with clinical and microscopic failure were treated using other strategies. Results: After one course of therapy, 59.2% (19/32) of women were cured, 19.0% (6/32) were improved (but not cured) and 21.8% (7/32) failed to respond to the therapy. After two courses of therapy, clinical improvement was achieved in additional two women. The therapy was very well tolerated, and during the entire study no drop out related to the SylTechTM vaginal capsules treatment was observed; only two patients (6.2%) experienced a mild transient burning after application. Conclusion: SylTechTM vaginal capsules is an effective therapeutic option for patients with AV, and most women with AV were cured with one course of therapy.

Fish oil is a source of unsaturated fatty acids, especially the content of omega-3 fatty acids, omega-6 and omega-9. Freshwater fish oil omega-3 content is relatively low. but the high content of omega-9, is one of those derived from patin oil. Sea fish oil has a relatively high content of omega-3 fatty acids, one of which comes from shark liver. Oil is not only comes from fish but also from plants. One of the vegetable oils from palm oil that is beneficial for health is red palm oil which has a relatively high carotenoid content which is a source of vitamin A. These three types of oil have excess and deficiencies in the composition of fatty acids, so they can be combined to improve their functional properties in the form of softgel capsule.The mixture of these three oils in the form of capsule softgel is functional food. The research method of mixing the three oils with a certain ratio of F1 (45 patin oil, 25 red plam oil, and 30 shark liver oil), F2 (.45 patin oil: 30 red plam oil: 25 shark liver oil. and F2 (45 patin oil: 35 red plam oil:20 shark liver oil) was analyzed the composition of fatty acids. The selected F 1 formulation is used as a softgel capsule. The analysis results show that the quality characteristics of the three oils are in accordance with IFOS standards (peroxide number and free fatty acids. The composition of sofgel fatty acids produced with F1 formula, produced omega-3 (0.47%), Omega-6 (32.87%), and omega-9 (26.97%), Besides the high omega-3,6 and 9 content, the saturated fatty acid content is also low.

To review safety, efficacy and pharmacokinetic (PK) data from the phase 3 REJOICE trial, which evaluated a 17β-estradiol (E2) softgel vaginal insert approved in 2018 for moderate to severe dyspareunia associated with menopausal vulvar and vaginal atrophy (VVA).REJOICE (Clinicaltrials.gov: NCT02253173) was a randomized, double-blind, placebo-controlled trial in which women with moderate to severe dyspareunia due to menopausal VVA received 4 µg, 10 µg or 25 µg of an E2 vaginal insert or placebo for 12 weeks. The published data for the recently approved 4 µg and 10 µg doses of the E2 vaginal insert, including four co-primary efficacy endpoints (change from baseline to week 12 in percentages of superficial and parabasal cells, vaginal pH and severity of dyspareunia), safety and PK (which included serum E2 levels measured by gas chromatography and tandem mass spectrometry), are summarized here.Women were randomized to receive the E2 vaginal insert (4 µg [n = 186] or 10 µg [n = 188]; ImvexxyThe recently FDA-approved E2 softgel vaginal insert (4 µg and 10 µg) was safe and effective over 12 weeks for treating moderate to severe dyspareunia due to menopausal VVA with minimal systemic E2 levels.

Background. Levothyroxine sodium (LT4) is the therapy of choice for hypothyroidism. In the last decade new LT4 formulations, such as liquid and soft gel capsules, became available. Even if some evidence has been reached in the efficacy of liquid LT4 in patients with suboptimal TSH on tablet LT4, the usefulness of soft gel LT4 has been rarely studied. This study aimed at evaluating the effect of switching from tablet to soft gel LT4 patients without increased need for LT4. TSH was used as proxy of LT4 bioavailability and effectiveness. Methods. During the period from April to August 2017, 19 patients on tablet LT4 treatment for hypothyroidism, mostly due to autoimmune thyroiditis, were enrolled. Subjects with causes of malabsorption or increased requirement of LT4 were previously excluded. Patients finally included were asked to switch from tablet to soft gel LT4 formulation at unchanged dose and ingestion fashion (30 minutes before breakfast). TSH was measured with chemiluminescence immunoassays. Results. According to exclusion and inclusion criteria, 19 patients were finally selected. One of these had headache four days later and come back to tablet LT4, and 18 of them (16W/2M; mean age=55 years; BMI 22.7 kg/m2) completed the study. They were treated with a median LT4 dose of 88 µg/day and showed a median TSH value of 3.33 mIU/L. The rate of cases with TSH ≤4mU/l was 61.1% (11/18 cases). When patients were re-evaluated after three months of soft gel LT4, we observed that TSH reached levels under 4.0 mIU/L in 16/18 (88.9%) patients, TSH was lower in 11 cases, and in 6 out of 7 patients with pre-switch TSH values over the normal range. Overall, TSH values on soft gel LT4 (median 1.90 mIU/L) was significantly lower from that observed during tablet LT4 (p = 0.0039). Conclusions. These data show that hypothyroid patients with no proven malabsorption may have an improved TSH following three months from the switch from tablet to soft gel LT4 preparation at unchanged dose.

Soft capsules are also commonly known as soft or elastic, one-piece, gelatin capsules, softgel capsules or softgels. Soft capsules are different from liquid-filled hard capsules in that the soft capsule is formed, filled and sealed in a single operation. This chapter will focus on pharmaceutical applications for the dosage form, from a platform technology point of view, rather than focusing heavily on what can be achieved with fill formulations, such as lipid technology. The chapter briefly describes recent advances in technology to use materials other than gelatin as the shell polymer. The author celebrated 30 years in softgel technology in 2016.

The oral bioavailability of diclofenac potassium 50 mg administered as a soft gelatin capsule (softgel capsule), powder for oral solution (oral solution), and tablet was evaluated in a randomized, open-label, 3-period, 6-sequence crossover study in healthy adults. Plasma diclofenac concentrations were measured using a validated liquid chromatography-mass spectrometry/mass spectrometry method, and pharmacokinetic analysis was performed by noncompartmental methods. The median time to achieve peak plasma concentrations of diclofenac was 0.5, 0.25, and 0.75 hours with the softgel capsule, oral solution, and tablet formulations, respectively. The geometric mean ratio and associated 90%CI for AUCinf, and Cmax of the softgel capsule formulation relative to the oral solution formulation were 0.97 (0.95-1.00) and 0.85 (0.76-0.95), respectively. The geometric mean ratio and associated 90%CI for AUCinf and Cmax of the softgel capsule formulation relative to the tablet formulation were 1.04 (1.00-1.08) and 1.67 (1.43-1.96), respectively. In conclusion, the exposure (AUC) of diclofenac with the new diclofenac potassium softgel capsule formulation was comparable to that of the existing oral solution and tablet formulations. The peak plasma concentration of diclofenac from the new softgel capsule was 67% higher than the existing tablet formulation, whereas it was 15% lower in comparison with the oral solution formulation.

Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free flowing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in softgels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen different softgel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution pattern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.

Objective To evaluate the bioequivalence of five 0.1 mg dutasteride capsules to one 0.5 mg dutasteride capsule in healthy adult male subjects under fasting conditions. Methods This was a single-center, open-label, randomized, single dose, two-way cross-over study (ClinicalTrials.gov identifier NCT01929330). Thirty-six healthy male subjects aged 18–65 years received 5 × 0.1 mg dutasteride softgel capsules and 1 × 0.5 mg dutasteride softgel capsule in a randomized order, with a minimum washout of 28 days between each drug administration. Serial blood samples were collected for the measurement of serum dutasteride concentrations by a validated HPLC-MS/MS method. Dutasteride pharmacokinetic parameters were calculated using non-compartmental analysis. Maximum concentration (Cmax) and area under the concentration-time curve to the last quantifiable concentration (AUC[0–t]) were compared between treatments. Safety and tolerability were monitored throughout the study. Results Five 0.1 mg dutasteride capsules were demonstrated to be bioequivalent to 1 × 0.5 mg dutasteride capsule, as the 90% confidence intervals for Cmax and AUC were within the accepted bioequivalence range of 0.80–1.25. The geometric least squares means ratios and associated 90% confidence intervals for 5 × 0.1 mg capsules vs 1 × 0.5 mg capsule were 1.01 (0.97–1.05) for Cmax and 0.91 (0.84–1.00) for AUC(0–t). Adverse events (AEs) were reported for 42% (15/36) and 36% (12/33) of subjects in the 5 × 0.1 mg and 1 × 0.5 mg dosing sessions, respectively. The most frequent AE for both treatments was headache. No subject had a serious AE. Conclusions Five 0.1 mg dutasteride capsules were shown to be bioequivalent to one 0.5 mg dutasteride capsule in healthy adult male subjects under fasted conditions, suggesting that the two dose strengths can be interchanged. Both treatments were generally well tolerated in healthy male subjects.

Four types of materials, type I collagen coat (Coat), acid-soluble type I collagen gel (Hardgel), pepsin-treated acid-soluble type I collagen gel (Softgel), and an extract of extracellular matrix of the murine Engelbreth-Holm-Swarm sarcoma (Matrigel), were used as matrices to culture rat hepatic parenchymal cells, and their morphological changes and adhesion were compared to the matrices by electron microscopic observations. Hepatic parenchymal cells cultured on Coat and Hardgel were extended and flattened, whereas cells cultured on Softgel and Matrigel assembled and formed aggregates. Such aggregates consisted of several hepatic parenchymal cells, with a recognizable bile duct-like alveolus on the inside. Morphologically, the aggregates were more spherical on Matrigel and oval shaped on Softgel. Microvilli of the cell surface were parallel to the matrix on Matrigel, but invaded into the gel on Softgel. Subsequently, investigation into how these morphological features affected the liver-specific functions, including secretion of albumin and induction of P450 by 3-methylcholanthrene, demonstrated that a high level of liver function was maintained in a long-term culture in hepatic parenchymal cells on Softgel. These results suggest that hepatic parenchymal cell interactions were stronger with Softgel than with Matrigel, and that Softgel appears to closely mimic the in vivo environment.

Fish oils are the primary dietary source of ω-3 polyunsaturated fatty acids (PUFA), but these compounds are prone to oxidation, and commercial fish oil supplements sometimes contain less PUFA than claimed. These supplements are predominantly sold in softgel capsules. In this work, we show that Fourier transform (FT)–Raman spectra of fish oils (n = 5) and ω-3 PUFA concentrates (n = 6) can be acquired directly through intact softgel (gelatin) capsules. These spectra could be used to rapidly distinguish supplements containing ethyl esters from those containing triacylglyceride oils. Raman spectroscopy calibrated with partial least-squares regression against traditional fatty acid methyl ester analyses by gas chromatography–mass spectrometry could be used to rapidly and nondestructively quantitate PUFA and other fatty acid classes directly though capsules. We also show that FT–Raman spectroscopy can noninvasively detect oxidation with high sensitivity. Oils with peroxide values of as low as 10 mequiv kg–1, wh...

In this double-blind, parallel trial, 93 healthy adults with hypertriglyceridemia (triacylglycerols [TAG] 150-499 mg/dL) were randomized to receive either a nutritional oil derived from marine algae (DHA-O; 2.4 g/day docosahexaenoic acid [DHA] and eicosapentaenoic acid [EPA] in a 2.7:1 ratio), fish oil (FO; 2.0 g/day DHA and EPA in a 0.7:1 ratio), or a corn oil/soy oil control as 4-1g softgel capsules/day with meals for 14 weeks; and were instructed to maintain their habitual diet. Percent changes from baseline for DHA-O, FO, and control, respectively, were TAG (-18.9, -22.9, 3.5; p

A well-controlled clinical trial previously demonstrated the efficacy of a novel softgel dietary supplement providing 1.8 g/day esterified plant sterols and stanols, as part of the National Cholesterol Education Program Therapeutic Lifestyle Changes diet, to improve the fasting lipid profile of men and women with primary hypercholesterolemia (fasting low-density lipoprotein [LDL] cholesterol ≥ 130 and220 mg/dL [≥ 3.37 and5.70 mmol/L]). The purpose of this randomized, double blind, placebo-controlled crossover study (conducted July 2011 to January 2012) was to support these previous findings in a similar, but independent, sample with a different lead investigator and research site. Repeated measures analysis of covariance was used to compare outcomes for sterol/stanol and placebo treatment conditions using the baseline value as a covariate. Forty-nine subjects were screened and 30 (8 men and 22 women) were randomized to treatment (all completed the trial). Baseline (mean ± standard error of the mean) plasma lipid concentrations were: total cholesterol 236.6 ± 4.2 mg/dL (6.11 ± 0.11 mmol/L), high-density lipoprotein (HDL) cholesterol 56.8 ± 3.0 mg/dL (1.47 ± 0.08 mmol/L), LDL cholesterol 151.6 ± 3.3 mg/dL (3.92 ± 0.09 mmol/L), non-HDL cholesterol 179.7 ± 4.6 mg/dL (4.64 ± 0.12 mmol/L), and triglycerides 144.5 ± 14.3 mg/dL (1.63 ± 0.16 mmol/L). Mean placebo-adjusted reductions in plasma lipid levels were significant (P0.01) for LDL cholesterol (-4.3%), non-HDL cholesterol (-4.1%), and total cholesterol (-3.5%), but not for triglycerides or HDL cholesterol. These results support the efficacy of 1.8 g/day esterified plant sterols/stanols in softgel capsules, administered as an adjunct to the National Cholesterol Education Program Therapeutic Lifestyle Changes diet, to augment reductions in atherogenic lipid levels in individuals with hypercholesterolemia.

Raised blood lipid levels are associated with a risk of a cardiovascular disease (CVD). Moderate reductions in several CVD factors such as total, low-density lipoprotein (LDL) cholesterol and non-high-density lipoprotein (non-HDL) cholesterol concentrations may be more effective in reducing overall risk than a major reduction in just one. A blind, randomised controlled trial was conducted with 120 healthy overweight (BMI 25&ndash, 30) adults aged 25&ndash, 70 years who were non-smokers, not diabetic and of low risk of cardiovascular disease, as assessed by the Framingham risk equation. Participants consumed 4.5 g PolyGlycopleX (PGX) as softgel capsules (PGXS) or 5 g PGX granules (PGXG) or 5 g rice flour (RF) with meals three times a day for 12 weeks. Total, LDL and non-HDL cholesterol were all significantly reduced (&minus, 6%, &minus, 5% and &minus, 3.5%, respectively) post the PGX granule treatment, however, PGX in softgel capsule form did not affect blood lipid profiles. Daily consumption of PGX granules in overweight low CVD risk adults produced lipid changes indicating a CVD preventative benefit.

Background Consumption of soybean oil enriched with stearidonic acid was previously shown to increase eicosapentaenoic acid (EPA) in red blood cells (RBC). Objective This study was designed to evaluate the effect of stearidonic acid oil used as a food ingredient in baked products and beverages on the RBC fatty acid profile. Design This was a randomized, double-blind, controlled, parallel-arm study. Participants Healthy men and women 21 to 65 years of age were included. Intervention Participants consumed either negative control (1.5 g/day high-oleic sunflower ethyl ester oil softgel capsules+foods containing 7 g/day high-oleic sunflower oil), positive control (1.5 g/day EPA oil ethyl ester softgel capsules+foods containing 7 g/day high-oleic sunflower oil), or active (1.5 g/day high-oleic sunflower ethyl ester oil softgel capsules+foods containing 7 g/day stearidonic acid soybean oil) for 12 weeks. Main outcome measures RBC membrane fatty acid profile (at weeks 0, 2, 4, 6, 8, 10, and 12); fasting serum lipids (weeks −2, 0, 6, 10, and 12); and fasting plasma glucose and insulin (weeks −2, 0, 10, and 12) were assessed. Statistical analyses performed A repeated measures analysis of covariance was used for continuous variables, and pair-wise comparisons between treatments were adjusted using a step-down Bonferroni method. Fisher's exact or χ 2 tests were used for categorical data. Results RBC %EPA throughout the 12-week study were significantly different between all groups. Means at 12 weeks were 0.50%±0.03%, 2.17%±0.21%, and 0.85%±0.05% for control, EPA, and stearidonic acid, respectively. Other efficacy outcome measures were not significantly different among treatment groups. Conclusions Consumption of stearidonic acid-enriched soybean oil incorporated into common foods increased RBC %EPA in healthy men and women. Stearidonic acid soybean oil, a sustainable and accessible source of long-chain n-3, can effectively be used to increase EPA in RBC.

ObjectiveThis randomized, placebo-controlled, crossover trial assessed the lipid-altering efficacy of a softgel capsule dietary supplement, providing esterified plant sterols/stanols 1.8 g/d, in 28 participants (∼75% women) with primary hypercholesterolemia (fasting low-density lipoprotein cholesterol [LDL-C] levels ≥130 and