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Beta-blockers have been prohibited by the World Anti-Doping Agency (WADA) in certain sports, but insufficient research data make it difficult to distinguish between therapeutic uses or misuses. This study aimed at investigating the urinary excretion pattern following beta-blocker ophthalmic drops and the potential risk of constituting an adverse analytical finding (AAF) in sports. Prescribed timolol and carteolol ophthalmic drops were used in healthy participants and glaucoma patients. The urine samples were then collected to investigate the urinary excretion pattern following acute and chronic administration of the above beta-blocker ophthalmic drops. The liquid chromatograph-tandem mass spectrometry method was applied for measuring urinary beta-blockers. Our results demonstrated that the levels of both urinary timolol and carteolol exceeded the minimum reporting levels (MRL) following acute and chronic administration. The highest levels of urinary timolol and carteolol observed in the present study were 255.7 and 923.8 ng/ml, respectively. Regarding the acute administration of timolol ophthalmic drop, 26.19 (11/42) of urine samples were detected with timolol higher than the MRL in timed and random sampling. In contrast, the acute administration of carteolol ophthalmic drops made the carteolol levels higher than the MRL among most urine samples. On the other hand, 36.36% (4/11) of urine samples were detected with beta-blockers higher than the MRL during the chronic administration of timolol and carteolol ophthalmic drops. In the context of receiving ophthalmic beta-blocker medications, the present study has highlighted the potential risk of constituting an AAF in specific sports and suggests strengthening athletes' awareness of therapeutic use exemptions.

In the fight against sports doping, the Athlete Biological Passport (ABP) system aims to indirectly unveil the doping incidents by monitoring selected biomarkers, however, several unexplored extrinsic factors may dampen a fair interpretation of ABP profiles. Chinese herbal medicine (CHM) plays a pivotal role in the health care system, and some remedies have a long history of being used to treat anaemia. In this study, we addressed the concerns of whether the CHM administration could yield a measurable effect on altering the ABP haematological variables. Forty-eight healthy volunteers were randomly assigned to receive two-week oral administration of one of the six selected CHM products that are commonly prescribed in Taiwan (eight subjects per group). Their blood variables were determined longitudinally in the phases of baseline, intervention, and recovery over 5 weeks. Blood collection and analyses were carried out in strict compliance with relevant operating guidelines. In the groups receiving Angelicae Sinensis Radix, Astragali Radix, and Salviae Miltiorrhizae Radix et Rhizoma, a significant increased reticulocyte percentage and decreased OFF-hr Score were manifested during the intervention, and such effects even sustained for a period of time after withdrawal. All other variables, including haemoglobin and Abnormal Blood Profile Score, did not generate statistical significance. Our results show that the use of CHM may impact the ABP haematological variables. As a consequence, we recommend athletes, particularly those who have been registered in the testing pool, should be aware of taking specific Chinese herbal-based treatment or supplementation, and document any of its usage on the anti-doping forms.

Higenamine is a β2 -agonist that has been prohibited in sports by the World Anti-Doping Agency. Higenamine could potentially promote anabolism and lipolysis; however, its crucial pharmacokinetics data, particularly muscle distribution, remain unavailable. The present study aims to investigate the blood-to-muscle distribution as well as the urinary excretion of higenamine in laboratory rats. In the first experiment, the microdialysis technique was employed to continuously measure free, protein-unbound concentrations in blood and muscle for 90 min (sampling at a 5-min interval) after rats received IV infusion of higenamine. The mean half-lives of higenamine in blood and muscle were 17.9 and 19.0 min, respectively. The blood-to-muscle distribution ratio (AUCmuscle /AUCblood ) of higenamine was estimated to be 22%. In the second experiment, rats were orally administered with a single-dose higenamine, and their urine samples were profiled at a 12-h interval for up to 48 h. Results showed only a small portion of total consumption (1.44%, ranging 0.71%-2.50%) was excreted in the urine. Among these time points, about 43% cumulative amount of higenamine was eliminated within the first 12 h. Our data suggested that one-quarter of the unbound higenamine rapidly penetrates from the vessels into muscle, distributes to the interstitial fluid, then eliminates from the rat in a short span of time. The muscle tissue is likely to have a low binding affinity for higenamine, and renal excretion plays a minor role in its elimination. Together, our findings provide valuable pharmacokinetics data that may gain deeper insights into higenamine's role in skeletal muscle functions.

Astragalus membranaceus (AM) is classified as a high-class traditional herbal medicine, which has strengthened vitality and multifunctional pharmacological activities, but limited empirical evidence is available to support its effects in muscular hypertrophy. It evokes skeletal muscle hypertrophy by increasing anabolic pathway, which is essential to prevent sarcopenia in elderly population. In this study, we examined the effects of AM on skeletal muscle hypertrophy by focusing on the molecular mechanism. We employed an in vitro model to investigate whether AM-treated skeletal muscle, as represented by myotube C2C12 cells, was hypertrophic, and to further investigate the efficacy of AM-activated phosphorylation of PI3K/Akt/mTOR signaling that must occur prior to myotube hypertrophy. The results showed that the myotubes formed larger multinucleated myotubes with increased diameter and thickness (1.16-fold relative to control group, p < 0.05). Administration of PI3K and mTOR inhibitors abolished AM-induced muscular hypertrophy. Moreover, AM-induced PI3K-mediated myotube hypertrophy was accompanied by the activation of Akt and mTOR signaling. We concluded that the AM is a nutritional activator to enhance muscular hypertrophy by increasing PI3K/Akt/mTOR signaling phosphorylation. As the AM is effective in myotube hypertrophy, AM and its derivatives may be promising candidates for ergogenic aid to prevent sarcopenia.

This paper reviews gas chromatography-mass spectrometry (GC-MS) methods for the analysis of amphetamines, ketamines, opioids, cocaine, and other abused drugs in urine that were developed by authors in Taiwanese institutions, and published during the 2000 to early 2008 period. Information on sample preparation, derivatization, internal standard, GC column, detection mode, and validation data for the reported methods are summarized in table format to facilitate readers' reference and adaptation.

In order to understand the quality of ampicillin capsules, fifty samples (46 domestic, 4 imported) were purchased from different counties and cities in Taiwan during 1991 fiscal year. All of the samples were investigated for appearance, mean weight, weight uniformity, identification of drug, potency, dissolution, content uniformity, and loss on drying. The results showed that 5 samples (10.0%) failed to meet the potency requirement of the official regulation (90-120%) and the contents of uniformity. Besides, there were three samples (6.0%) did not meet the specification of dissolution test.

A sensitive and specific gas chromatography-mass spectrometry (GC-MS) method using selected ion monitoring (SIM) has been developed for quantification of pentazocine in urine. This method uses solid-solid extraction (SPE) and N, O-bis (trimethylsilyl) trifluoroacetamide with 1% trimethylchlorosilane derivatization, followed by GC-MS analysis using dextromethorphan as the internal standard. The method was linear between 125 and 1500 ng/mL (r^2=0.997). The limit of quantification and limit of detection were 125 and 62.5 ng/mL, respectively. The intraday accuracy and precision were -6.3~4.7% and 3.6~11.2%, respectively. The interday accuracy and precision were -7.5~7.0% and 6.2~10.0%, respectively. These data showed that the GC-MS method was suitable for the determination of pentazocine in urine. This method was further applied to an interlaboratory study. The collaborative study was given by the Association of Official Analytical Chemists International (AOAC International). Nine drug abuse urine testing laboratories in Taiwan participated to analyze 3 samples in duplicate. The repeatability relative standard deviation (RSDr) and reproducibility relative standard deviation (RSDR) values were 3.0~5.2% and 6.8~10.3%, respectively. The method showed acceptable reproducibility, as evidenced by HORRAT values of 1.1 to 1.5. The method recommended for use by the drug abuse urine testing laboratories in Taiwan.

A gas chromatography-mass spectrometry method for the analysis of phencyclidine (PCP) in urine was subjected to an inter-laboratory study. The collaborative study followed the guidelines provided by the Association of Official Analytical Chemists International. Ten laboratories participated, analyzing 3 samples of PCP-spiked urine as blind duplicate. The repeatability relative standard deviation (RSD(subscript r)) and the reproducibility relative standard deviation (RSD(subscript R)) were between 2.1%-3.6% and 4.2%-7.3%, respectively. HORRAT values for the reproducibility showed 0.4-0.7, indicating acceptable precision between laboratories. The method was thus proposed to be used by the drug-abuse urine testing laboratories in Taiwan.

A previously published gas chromatography-mass spectrometry (GC-MS) method for the analysis of 7-aminoflunitrazepam(7-amino-FM2) in urine was subjected to an inter-laboratory collaborative study. The method was rigorously defined in termsof performance requirements, yet allowed some degrees of flexibility to individual analysts. The collaborative study followedthe guidelines provided by the Association of Official Analytical Chemists International (AOAC International). Each of ninedrug-abuse urine testing laboratories in Taiwan participated in the study to analyze 3 samples in duplicate. The repeatabilityrelative standard deviation (RSD(subscript r)) and the reproducibility relative standard deviation (RSD(subscript R)) of the measurements of 7-amino-FM2 in urine were determined to be less than 9.91% and 14.84%, respectively. The method showed acceptable reproducibility, asevidenced by HORRAT values of 0.6 to 0.7. The method was thus proposed to be used by the testing laboratories in Taiwan.

Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 &plusmn, 0.5 &deg, C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS (F10) formulation comprising glyceryl trioctanoate, polyoxyethylene castor oil, and Tween 20 at a ratio of 10:10:80 (w/w/w) was the optimal formulation. This formulation maintained over 90% of its contents in different storage environments for 12 weeks. After the self-emulsification of SNEDDS, the SSM dispersed droplet size was 66.4 &plusmn, 31.4 nm, intestinal permeability increased by more than three-fold, relative bioavailability increased by approximately 12.9-fold, and absolute bioavailability increased from 0.3% to 4.4%. Accordingly, the developed SNEDDS formulation can preserve SSM&rsquo, s solubility, permeability, and bioavailability. Therefore, this SNEDDS formulation has great potential for the oral administration of SSM, which can enhance its pharmacological application value.

Andrographolide (AG), a major diterpene lactone isolated from Andrographis paniculata (Burm. f.) Nees (Acanthaceae), possesses a wide spectrum of biological activities. However, its poor water solubility and low bioavailability limit its clinical application. Therefore, this study aimed to develop a solid dispersion (SD) formulation to increase the aqueous solubility and dissolution rate of AG. Different drug-polymer ratios were used to prepare various SDs. The optimized formulation was characterized for differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffraction. The analysis indicated that the optimized SD enhanced AG solubility and dissolution rates by changing AG crystallinity to an amorphous state. The dissolution behaviors of the optimum SD composed of an AG-polyvinylpyrrolidone K30-Kolliphor EL ratio of 1:7:1 (w/w/w) resulted in the highest accumulated dissolution (approximately 80%). Pharmacokinetic studies revealed that Cmax/dose and the AUC/dose increased by 3.7-fold and 3.0-fold, respectively, compared with AG suspension. Furthermore, pretreatment using the optimized AG-SD significantly increased the swimming time to exhaustion by 1.7-fold and decreased the plasma ammonia level by 71.5%, compared with the vehicle group. In conclusion, the optimized AG-SD formulation appeared to effectively improve its dissolution rate and oral bioavailability. Moreover, the optimized AG-SD provides a promising treatment against physical fatigue.

Since 2017, higenamine has been added to the World Anti-Doping Agency (WADA) prohibited list as a &beta, 2-agonist prohibited at all times for sportspersons. According to WADA&rsquo, s report, positive cases of higenamine misuse have been increasing yearly. However, higenamine occurs naturally in the Chinese herb lotus plumule&mdash, the green embryo of lotus (Nelumbo nucifera Gaertn) seeds&mdash, commercially available as concentrated powder on the Asian market. This study evaluated the major phytochemical components of lotus plumule products using an appropriate extraction method, followed by a human study in which the products were orally administered in multiple doses to investigate the risk of doping violations. Comparing various extraction methods revealed that optimized microwave-assisted extraction exhibited the highest extraction efficiency (extraction time, 26 min, power, 1046 W, and temperature, 120 &deg, C). Subsequently, the alkaloids in lotus plumule products were quantitatively confirmed and compared. Human study participants (n = 6) consumed 0.8 g of lotus plumule (equivalent to 679.6 &mu, g of higenamine) three times daily for three consecutive days. All participants&rsquo, urinary higenamine concentrations exceeded the WADA reporting cut-off of 10.0 ng/mL. Accordingly, lotus plumule consumption may engender adverse analytical findings regarding higenamine. Athletes should avoid consuming lotus plumule-containing products during in- and out-of-competition periods.

Background/Objective: Although the functional movement screen (FMS) has been widely applied for screening athletes, no previous study has used FMS scores to examine the association between distinct training seasons in high school baseball players. The aims of this study were to ascertain the functional movement screen (FMS) scores differences between the preparative period (PPP) and the competitive period (CPP) among high school baseball players and further determine whether FMS can be used as a tool to predict injuries during two major periods. Methods: Fifty-five male high school baseball players (age 15.3 ± 1.7 years; height 1.7 ± 0.8 m; weight 64.6 ± 11.5 kg) volunteered. Athletic injuries were reported through a self-report questionnaire. Players performed the FMS during the PPP and the CPP. A receiver operator characteristic (ROC) curve to calculate a cutoff total composite score ≤ 14 for the relationship between the FMS score and injury. Sensitivity, specificity, positive predictive value (PPV), negative predictive value (NPV) and an area under the curve (AUC) were calculated. Results: FMS individual task score and total composite score were significantly lower in the CPP than in the PPP. However, a cutoff total composite score ≤14 for risk of injury, determined through a ROC curve, represented a low sensitivity of 58%, NPV of 66%, an AUC of 69%, specificity of 79%, and PPV of 71%. Conclusion: Although the low sensitivity and NPV and AUC scores indicated that the FMS does not accurately predict the risk of injury, the FMS individual task and total composite scores differed significantly between the PPP and CPP. Therefore, FMS could be used as a tool to identify physical deficiencies between distinct training seasons; however, utilizing the FMS as a screening tool for injury prediction in particular during the CPP in this population would not be recommended. Keywords: Functional movement screen, Assessment, Athlete

Hsu, CC, Fong, TH, Chang, HM, Su, B, Chi, CP, Kan, NW, and Hsu, MC. Low second-to-fourth digit ratio has high explosive power? A prepubertal study. J Strength Cond Res 32(7): 2091-2095, 2018-A recent study reported that lower limb explosive power had no correlation with the index finger: ring finger (2D:4D) ratio. However, many studies hypothesized that a lower 2D:4D ratio (reflecting a relative higher testosterone exposure) predicts higher physical fitness. The aim of this study was to replicate the study of explosive power and the 2D:4D ratio in a sample of Taiwanese children. A total of 541 Taiwanese prepubertal children (257 girls and 284 boys aged 9-10 years) participated in this study. This study analyzed the relationship between the 2D:4D ratio and explosive power. Explosive power of the lower limbs was assessed using the standing long jump (SLJ) test. The lengths of the second and fourth fingers of the right hand were measured to calculate the 2D:4D ratio. The SLJ length was correlated with the 2D:4D ratios (r = -0.144, p = 0.015) in boys. After controlling for age and the body mass index, this correlation remained significant (r = -0.134, p = 0.024). For girls, 2D:4D ratios were not significantly correlated with SLJ scores. These results indicate that the SLJ distance was negatively correlated with the 2D:4D ratio in boys, but not in girls. These findings might suggest that prenatal testosterone exposure is negatively correlated with the explosive power in men, but not in women.

Triamcinolone (T) is a glucocorticoid commonly used to relieve inflammation and treat arthritis, severe allergies, and asthma; however, it is banned by the World Anti-Doping Agency in competition for athletes when administered orally, intravenously, intramuscularly, or rectally. The minimum required performance limit (MRPL) for urinary T is 30 ng/mL. However, the data about the urinary excretion of T after oral administration is limited. We investigate the elimination profile and determine whether single-dose administration of T would cause a positive doping result. Twelve healthy volunteers received a single-dose of 4-mg T rally, and urine samples were collected for 24 hours. A validated liquid chromatography-tandem mass spectrometry method was used to determine urinary T levels. Non-compartmental modeling was used to estimate the pharmacokinetic parameters. All the urinary T concentrations were much higher than the MRPL. The peak urinary T concentration was 3211.4 ± 860.3 ng/mL (mean ± SD), time to peak concentration was 1.7 ± 0.9 hours, and the estimated elimination half-life was 4.4 ± 2.8 hours. About 27.76% of the consumed dose was eliminated via urine within 24 hours of intake. After a single-dose oral administration, urinary T concentrations still exceeded the MRPL after 24 hours. This information could be useful for limiting the misuse of T. Athletes should be aware when using T in competition and acquire approval for a therapeutic use exemption prior to use. Moreover, the elimination profile of orally administered T may be crucial information for distinguishing different dosage routes.

Globally, the proportion of older adults is increasing. Older people face chronic conditions such as sarcopenia and functional decline, which are often associated with disability and frailty. Proteomics assay of potential serum biomarkers of frailty in older adults. Older adults were divided into non-frail and frail groups (n = 6 each; 3 males in each group) in accordance with the Chinese-Canadian Study of Health and Aging Clinical Frailty Scale. Adults were measured for grip power and the 6-min walk test for physical activity, and venous blood was sampled after adults fasted for 8 h. Ultra-high-performance liquid chromatography-tandem mass spectrometry was used for proteomics assay. The groups were compared for levels of biomarkers by t test and Pearson correlation analysis. Non-frail and frail subjects had mean age 77.5±0.4 and 77.7±1.6 years, mean height 160.5±1.3 and 156.6±2.9 cm and mean weight 62.5±1.2 and 62.8±2.9 kg, respectively. Physical activity level was lower for frail than non-frail subjects (grip power: 13.8±0.4 vs 26.1±1.2 kg; 6-min walk test: 215.2±17.2 vs 438.3±17.2 m). Among 226 proteins detected, for 31, serum levels were significantly higher for frail than non-frail subjects; serum levels of Ig kappa chain V-III region WOL, COX7A2, and albumin were lower. The serum levels of ANGT, KG and AT were 2.05-, 1.76- and 2.22-fold lower (all p < 0.05; Figure 1A, 2A and 3A) for non-frail than frail subjects and were highly correlated with grip power (Figure 1B, 2B and 3B). Our study found that ANGT, KG and AT levels are known to increase with aging, so degenerated vascular function might be associated with frailty. In total, 226 proteins were revealed proteomics assay; levels of angiotensinogen (ANGT), kininogen-1 (KG) and antithrombin III (AT) were higher in frail than non-frail subjects (11.26±2.21 vs 5.09±0.74; 18.42±1.36 vs 11.64±1.36; 22.23±1.64 vs 9.52±0.95, respectively, p < 0.05). These 3 factors were highly correlated with grip power (p < 0.05), with higher correlations between grip power and serum levels of ANGT (r = -0.89), KG (r = -0.90), and AT (r = -0.84). In conclusion, this is the first study to demonstrate a serum proteomic profile characteristic of frailty in older adults. Serum ANGT, KG and AT levels could be potential biomarkers for monitoring the development and progression of frailty in older adults.

Cornu cervi pantotrichum (CCP), used in traditional Chinese medicine, is a well-known yang-invigorating agent with multifunctional bioactivities. We previously showed, through an acute exercise challenge, that short-term CCP supplementation improved physical activities and fatigue-associated biochemical indices. Questions about the long-term effects of CCP treatment on exercise performance and physical fatigue, as well as safety, with intensive exercise training need further research. ICR-strain mice were randomly assigned to three groups: (1) sedentary control and vehicle treatment (SC); (2) exercise training with vehicle treatment (ET); and (3) ET with CCP treatment at 4,108 mg/kg/day (ET+CCP). We assessed the physical performance, body compositions, and serum levels of lactate, ammonia, glucose and creatine kinase (CK) after an acute exercise challenge. The ET and ET+CCP groups had significantly increased grip strength and endurance swimming time, and decreased serum lactate and ammonia levels after the acute exercise challenge than the SC group. Moreover, serum ammonia and CK levels in the ET+CCP group were significantly decreased when compared to that of the ET only group. In regard to the body composition, the ET+CCP group inhibits the decrease in fat tissue, and related biochemical changes induced by the high intensity endurance training CCP supplementation combined with high-intensity endurance exercise could significantly improve the physiological adaptions related to fatigue or energy consumption and maintain the fat composition when compared to treatment with training only. Therefore, CCP may potentially improve the physiological adaptions in intensive exercise training.

Ubiquinol (QH), a reduced form of coenzyme Q10, is a lipid antioxidant that is hydro-soluble and is commonly formulated in commercial supplements. Ubiquinol has been increasingly reported to exert antioxidant functions, in addition to its role in the cell energy-producing system of mitochondria and adenosine triphosphate (ATP) production. The aim of this study was to assess the potential beneficial effects of QH on anti-fatigue and ergogenic functions following physiological challenge. Forty 8-week-old male Institute of Cancer Research (ICR) mice were divided into four groups (n = 10 for each group): Group 1 (vehicle control or oil only), Group 2 (1X QH dose or 102.5 mg/kg), Group 3 (2X QH dose or 205 mg/kg), Group 4 (6X QH dose or 615 mg/kg). Anti-fatigue activity and exercise performance were studied using the forelimb grip strength experiment and exhaustive weight-loaded swimming time, and levels of serum lactate, ammonia, glucose, BUN (blood urea nitrogen), creatine kinase (CK), and free fatty acids (FFA) after an acute exercise challenge. The forelimb grip strength and exhaustive weight-loaded swimming time of the QH-6X group were significantly higher than those of the other groups. QH supplementation dose-dependently reduced serum lactate, ammonia, and CK levels and increased the FFA concentration after acute exercise. In addition, QH increased the liver and muscle glycogen content, an important energy source during exercise. Therefore, the results suggest that QH formulation is a safe dietary supplement for amelioration of fatigue and for promoting exercise performance.

Lycopene, a natural, hydrophobic compound derived from tomatoes, has attracted considerable attention due to its various benefits such as being an anti-oxidant, anti-cancer, and anti-hyperlipidemic agent. The insolubility of lycopene is a major obstacle that leads to poor bioavailability. We aimed to optimize a straightforward, promising approach utilizing a solid dispersion technique, named the dripping pill delivery system, for improving the absorption of lycopene. The polyethylene glycol 6000-based dripping pills were prepared by the hot melt method with rapid cooling. A 32 full factorial design was employed to optimize the effects of the independent variables, Cremophor EL and Tween 80, on the solubility, dissolution, and stability tests. The physicochemical characteristics and interaction were investigated by the disintegration test, scanning electron microscope, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The in vivo experiment was carried out to verify the usefulness of the developed formulae. The optimal dripping pill formulae elevated the solubility and dissolution of lycopene, which was confirmed to be formed in an amorphous state. Furthermore, the optimal dripping pill exhibited an approximate 6-fold improvement in bioavailability.

Hemp nuts are mature cannabis seeds obtained after hulling and stir-frying that are commonly used in traditional Chinese medicine for treating functional constipation. In this work, we screened hemp nut products, classified them, and verified the legality of consuming them. A total of 18 products were purchased from Taiwan, China and Canada. Validated high-performance liquid chromatography with tandem mass spectrometry methods were developed for analyzing the cannabinoid (i.e., Δ9-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol) content of the products and the concentration of urinary 11-nor-9-carboxy-THC. Chemometric techniques, namely hierarchical clustering analysis (HCA) and principal component analysis (PCA), were applied for rapidly classifying 11 concentrated powder products in Taiwan. A pilot human study comprising single and multiple administrations of a product with 1.5 µg/g of THC was conducted to examine the urinary 11-nor-9-carboxy-THC concentration. Through optimization of 32 full factorial design, using 60% isopropanol as the extraction solvent exhibited the highest yield of cannabinoids and was applied as the optimal condition in further analysis. The results of HCA and PCA on quality evaluation were in well agreement; however, the tested products possessed distinct CBD-to-THC ratios which ranged widely from 0.1:1 to 46.8:1. Particularly, the products with CBD-to-THC ratios higher than 1:1 were the majority in Taiwan. Our data suggested that all the tested hemp nut products met the Taiwan restriction criteria of 10 µg/g of THC. We propose a usual consumption amount of hemp nut products in Taiwan would unlikely to violate the cut-off point of 15 ng/mL of urinary 11-nor-9-carboxy-THC. This article is protected by copyright. All rights reserved.

Resveratrol (3,4′,5-trihydroxy-trans-stilbene; RES) produces a variety of pharmacological effects; however, its oral bioavailability (BA) approaches zero. In this study, grape peel extract (GPE) was incorporated into a solid dispersion delivery system to improve the solubility, dissolution and oral absorption of RES. The dripping pill (DP) oral delivery system was developed through the hot-melt method, and the optimal formulation consisted of GPE, propylene glycol monocaprylate, poloxamer 188, polyoxyl 35 castor oil and polyethylene glycol 6000. The DPs enhanced the (mean ± SD) dissolution of RES from 23.3 ± 1.0 to 67.8 ± 0.4 %. The pharmacokinetic profiles in the rats revealed that the DPs increased the oral BA of RES from 0.9 ± 0.1 to 10.5 ± 0.9 %; this represented an approximately 12-fold increase in absorption. Our results indicated that the DP formulation improves the dissolution and oral BA of RES. Thus, this could be an effective and practical technique for food and pharmaceutical applications.

This study was to investigate the protective and recovery effects of Danggui Buxue Tang (DBT) supplementation on exercise performance, hepcidin, iron status, and other related biochemical parameters after being challenged by a single bout of intense aerobic exercise. A total of 36 recreationally active males were pair-matched and randomly assigned to receive DBT or a placebo for 11 days, while using clusters based on their aerobic capacities. On the eighth day of the supplementation, the participants performed a 13-km run with maximal effort. Blood and urine samples were collected and analysed before treatment (Pre-Tre) and immediately after (Post-Ex), 24 h after (24-h Rec), and 72 h after (72-h Rec) the run. DBT supplementation dramatically shortened the finish times by 14.0% (12.3 min) when compared with that in the placebo group. Significant group &times, time effects were observed in serum hepcidin and iron levels. DBT supplementation repressed hepcidin levels at Post-Ex and 24-h Rec, thereby causing a significant increase in iron levels by 63.3% and 31.4% at Post-Ex and 72-h Rec, respectively. However, DBT supplementation had no significant anti-inflammatory or haemolysis-preventative effects. Short-term DBT supplementation shortened the running time and repressed exercise-induced hepcidin levels, thereby boosting iron levels and accelerating iron homeostasis during recovery.

Resveratrol (RES), a natural polyphenolic compound, exerts anti-fatigue activity, but its administration is complicated by its low water solubility. To improve RES bioavailability, this study developed a self-nanoemulsifying drug delivery system (SNEDDS) for RES and evaluated its anti-fatigue activity and rat exercise performance by measuring fatigue-related parameters, namely lactate, ammonia, plasma creatinine phosphokinase, and glucose levels and the swimming time to exhaustion. Through solubility and emulsification testing, the optimized SNEDDS composed of Capryol 90, Cremophor EL, and Tween 20 was developed; the average particle size in this formulation, which had favorable self-emulsification ability, was approximately 41.3 ± 4.1 nm. Pharmacokinetic studies revealed that the oral bioavailability of the optimized RES-SNEDDS increased by 3.2-fold compared with that of the unformulated RES-solution. Pretreatment using the RES-SNEDDS before exercise accelerated the recovery of lactate after exercise; compared with the vehicle group, the plasma ammonia level in the RES-SNEDDS group significantly decreased by 65.4%, whereas the glucose level significantly increased by approximately 1.8-fold. Moreover, the swimming time to exhaustion increased by 2.1- and 1.8-fold, respectively, compared with the vehicle and RES-solution pretreatment groups. Therefore, the developed RES-SNEDDS not only enhances the oral bioavailability of RES but may also exert anti-fatigue pharmacological effect.

Consumption of Ephedra alkaloids has been prohibited in-competition by the World Anti-Doping Agency (WADA). In Taiwan, colds are often treated with Chinese herbal formulae containing Herba Ephedrae. We screened the products sold in Taiwan and preliminarily assessed their relationships with WADA threshold violations. Fifty-six concentrated powder products, including 19 Chinese herbal formulae that contained Herba Ephedrae, were collected. The content of Ephedra alkaloids, namely ephedrine (E), methylephedrine (ME), norpseudoephedrine (NPE; cathine), pseudoephedrine (PE), and norephedrine (NE; phenylpropanolamine), was determined using a validated high-performance liquid chromatography method. The results revealed that the phenotypic indicators of the collected products, E/PE and E/total ratios, were 1.52–4.70 and 0.49–0.72, respectively, indicating that the Herba Ephedrae species in these products was probably E. sinica or E. equisetina, but not E. intermedia. The contents of E, ME, NPE, PE, and NE and the total alkaloid contents in the daily doses of the products were 0.45–34.97, 0.05–4.87, 0.04–3.61, 0.15–12.09, and 0.01–2.00 mg and 0.68–53.64 mg, respectively. The alkaloid contents followed a relatively consistent order (E > PE > ME ≈ NPE > NE), even for products from different manufacturers. We calculated that single doses of 50.0% and 3.6% of the products would result in the WADA thresholds of E and NPE being exceeded, respectively. Our data provide critical information for athletes and medical personnel, who should be wary of using complex Chinese herbal formulae in addition to over-the-counter products.

Cornu cervi pantotrichum (CCP), used in traditional Chinese medicine, is a well-known yang-invigorating agent with multifunctional bioactivities. We previously showed, through an acute exercise challenge, that short-term CCP supplementation improved physical activities and fatigue-associated biochemical indices. Questions about the long-term effects of CCP treatment on exercise performance and physical fatigue, as well as safety, with intensive exercise training need further research. ICR-strain mice were randomly assigned to three groups: (1) sedentary control and vehicle treatment (SC); (2) exercise training with vehicle treatment (ET); and (3) ET with CCP treatment at 4,108 mg/kg/day (ET+CCP). We assessed the physical performance, body compositions, and serum levels of lactate, ammonia, glucose and creatine kinase (CK) after an acute exercise challenge. The ET and ET+CCP groups had significantly increased grip strength and endurance swimming time, and decreased serum lactate and ammonia levels after the acute exercise challenge than the SC group. Moreover, serum ammonia and CK levels in the ET+CCP group were significantly decreased when compared to that of the ET only group. In regard to the body composition, the ET+CCP group inhibits the decrease in fat tissue, and related biochemical changes induced by the high intensity endurance training CCP supplementation combined with high-intensity endurance exercise could significantly improve the physiological adaptions related to fatigue or energy consumption and maintain the fat composition when compared to treatment with training only. Therefore, CCP may potentially improve the physiological adaptions in intensive exercise training.

BACKGROUND Weekly training volumes for triathlete are typically higher and may cause fatigue and musculoskeletal injury risk. High-intensity interval training (HIT) is a potent time-efficient strategy to induce adaptations normally associated with traditional endurance training. Therefore, the aim of this study was to investigate the effect of two weeks of in-season HIT on exercise capacity and hormonal responses in young triathletes. METHODS Twelve adolescent triathletes performed 18 sessions of HIT over 2 weeks including swim, cycle, and run events. The 6-day training blocks were separated by 1 day of recovery. Pre- and post-training, peak oxygen uptake (VO2peak) and exercise performance were assessed, and blood samples were obtained to detect changes in hormone and metabolite levels. RESULTS VO2peak was significantly higher (P=0.02) post-training (56.4±8.1 mL·min-1·kg-1) versus pre-training (55.1±7.5 mL·min-1·kg-1). Mean power and total work during 6×10 s repeated-sprint tests significantly increased (P=0.03) after HIT. Additionally, 750 m swim time (pre- vs. post: 689.7±102.5 s vs. 662.0±75 s, P=0.01) and 20 km cycling time (pre- vs. post: 1856.6±274.8 s vs. 1705.4±266.8 s, P=0.02) were significantly lower post-training compared to pre-training, but there was no significant difference in 5 km run time after HIT (pre- vs. post: 1315.8±81.3 s vs. 1292.0±112.9 s, P=0.31). In contrast to pre-training, ammonia concentration was significantly increased (P

Triamcinolone acetonide (TA) is classified as an S9 glucocorticoid in the 2014 Prohibited List published by the World Anti-Doping Agency, which caused it to be prohibited in-competition when administered orally, intravenously, intramuscularly or rectally. The Minimum Required Performance Level (MRPL) for the detection and identification of glucocorticoids is 30 ng/mL. Other common local injection routes, such as intraarticular, intratendinous, or intrabursal injection, are not prohibited. The purpose of this study was to analyze the TA and triamcinolone (T) concentrations in urine after a single injection of TA in patients to determine if it would produce a positive result. This study was performed on 40 patients with sports injuries or joint pains. TA was administered locally (doses varied from 12 to 80 mg). Samples were extracted using a solid-phase extraction column, followed by hydrolysis and liquid extraction using diethyl ether. The elution solvents were collected and dried. The dried residue was reconstituted and assayed by performing liquid chromatography–tandem mass spectrometry (LC–MS/MS) in positive ionization mode using electrospray ionization and multiple-reaction monitoring as the acquisition mode. The results demonstrated that the concentrations of both TA and T in urine exceeded the MRPL (30 ng/mL) after a single local injection. We obtained positive results for TA in 25 patients, and a positive result for T in one patient. Furthermore, the metabolic situation of TA, a long-acting glucocorticoid, was not an exact linear model. The highest concentrations of TA and T appeared 1–4 h after injection. This information could be useful for limiting the misuse of TA by athletes. We suggest that athletes be aware when using TA injections during a competition period and obtain approval for therapeutic use exemption prior to using TA.

Astragalus membranaceus (AM) is a popular “Qi-tonifying” herb with a long history of use as a Traditional Chinese Medicine with multiple biological functions. However, evidence for the effects of AM on exercise performance and physical fatigue is limited. We evaluated the potential beneficial effects of AM on ergogenic and anti-fatigue functions following physiological challenge. Male ICR strain mice were randomly assigned to four groups (n = 10 per group) for treatment: (1) sedentary control and vehicle treatment (vehicle control); (2) exercise training with vehicle treatment (exercise control); and (3) exercise training with AM treatment at 0.615 g/kg/day (Ex-AM1) or (4) 3.075 g/kg/day (Ex-AM5). Both the vehicle and AM were orally administered for 6 weeks. Exercise performance and anti-fatigue function were evaluated by forelimb grip strength, exhaustive swimming time, and levels of serum lactate, ammonia, glucose, and creatine kinase after 15-min swimming exercise. Exercise training combined with AM supplementation increased endurance exercise capacity and increased hepatic and muscle glycogen content. AM reduced exercise-induced accumulation of the byproducts blood lactate and ammonia with acute exercise challenge. Moreover, we found no deleterious effects from AM treatment. Therefore, AM supplementation improved exercise performance and had anti-fatigue effects in mice. It may be an effective ergogenic aid in exercise training.

Panax quinquefolium L. (American Ginseng, AG) is one of the most popular herbal medicines in the World. We aimed to investigate whether chronic (28-day) supplementation with AG could protect against ethanol-induced ulcer in gastric tissue. Furthermore, we investigated the possible molecular mechanisms leading to AG-mediated gastric mucosal protection. We randomized 32 male Wistar rats into four groups for treatment (n = 8 per group): supplementation with water (vehicle) and low-dose (AG-1X), medium-dose (AG-2X) and high-dose (AG-5X) AG at 0, 250, 500, and 1250 mg/kg, respectively. In the first experiment, animals were fed vehicle or AG treatments for 4 weeks. At day 29, 75% ethanol was given orally to each animal at 10 mL/kg to induce gastric ulceration for 2 h. In a second experiment, animals were pretreated orally with each treatment for 1 hr before a single oral administration of ethanol (70%, 10 mL/kg). Trend analysis revealed that AG treatments inhibited ethanol-induced gastric mucosal damage. AG supplementation dose-dependently decreased the pro-inflammatory levels of interleukin 1β and cyclooxygenase 2 and the expression of pro-apoptotic proteins tBid, cytochrome C, and caspases-9 and -3 and increased the levels of anti-apoptotic proteins Bcl-2, Bcl-xL and p-Bad. AG could have pharmacological potential for treating gastric ulcer.

Ixora parviflora, a species of the Rubiaceae, is rich in polyphenols and flavonoids, and has been traditionally used as a folk medicine. An I. parviflora extract (IPE) has great antioxidant activity in vitro, including a scavenging effect on superoxide radicals, reducing power, and ferrous ion-chelating ability. However, whether IPE is efficacious against oxidative damage in vivo is not known. The purpose of this study was to determine the protective effects of IPE treatment on hepatic oxidative stress and antioxidant defenses after exhaustive exercise in mice. Fifty male C57BL/6 mice (6 week old) were randomly divided into five groups and designated a sedentary control with vehicle (C), and exhaustive exercise with vehicle (IPE0), low dosage (IPE10), medium dosage (IPE50) and high dosage (IPE100) of IPE at 0, 10, 50, and 100 mg/kg, respectively. After a single bout of exhaustive swimming exercise challenge, levels of blood ammonia and creatine kinase (CK), and hepatic superoxide dismutase (SOD) protein expression, thiobarbituric acid-reactive substance (TBARS), and gp91(phox), p22(phox), and p47(phox) subunits of nicotinamide adenine dinucleotide phosphate (NADPH) oxidase expressions in the IPE0 group were significantly affected compared to those of the C group, but they were all significantly inhibited by the IPE treatments. Results of the present in vivo study in mice indicate that I. parviflora extract possesses antioxidative and hepatoprotective potential following exhaustive exercise.

Hemp nuts are mature cannabis seeds obtained after shelling and that are commonly used in traditional Chinese medicine for treating functional constipation. In this work, we screened hemp nut products, classified them, and verified the legality of consuming them. A total of 18 products were purchased from Taiwan, China, and Canada. Validated high-performance liquid chromatography with tandem mass spectrometry methods were developed for analyzing the cannabinoid (i.e., Δ