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This study explores the impact of varying temperatures on the release behavior of Triptorelin Acetate (TA) from a PLGA-based in-situ forming implant (ISFI) and polymer degradation. Formulations were prepared using the in situ forming method in an acetate buffer (pH = 6.8) and then exposed to temperatures of 4 to 60 °C. The drug release and polymeric depot behavior were evaluated using HPLC, SEM, GPC, Rheometer, and pH measurements. A modified Gallagher-Corrigan Model-based mathematical model was applied to fit the in-vitro data, and the activation energy for peptide release in diffusional and erosional phases was calculated using the Arrhenius equation. The results revealed that matrices formed at 37, 45, and 53 °C exhibited a highly porous structure, resulting from rapid phase inversion and surface pore closing. This led to a reduction in TA burst release, observed as 38%, 27%, and 15% at 37 °C, 45 °C, and 53 °C respectively. Conversely, matrices at 4 and 25 °C demonstrated a faster initial release, followed by the formation of dense structures. The accelerated drug release profiles at 45 and 53 °C showed a shortened ultimate drug release duration and a good correlation with the real-time results at 37 °C. Due to the discernible PLGA matrices degradation at different temperatures, biphasic and tri-phasic release patterns were observed. The experimental release results aligned well with the proposed mathematical model, and the drug release kinetic parameters were estimated. Thus, in in-vitro studies, the release medium temperature plays a significant role in the drug-release behavior of ISFIs. [ABSTRACT FROM AUTHOR]

Abstract Background The preservation of fertility and integrity of the reproductive organs has increasingly been of concern to most women with adenomyosis. Adenomyomectomy is conservative surgery that is now widely applied; however, relapse is a serious problem after the operation. Postoperative treatment, such as gonadotropin-releasing hormone agonist (GnRHa) has been suggested to result in reducing the rate of disease recurrence. However, there is still a lack of evidence from randomized clinical trials examining the efficacy of GnRHa in decreasing the postoperative recurrence rate. Method/design Relapse after conservative surgery combined with triptorelin acetate versus conservative surgery only in women with focal adenomyosis is a multicenter, prospective, randomized controlled trial. The primary outcome is relapse assessed using a visual analogue scale (VRS) and numeric rating scale (NRS), pictorial blood loss assessment chart (PBAC) score, and the size of the uterus and the lesion as measured by two/three-dimensional color doppler ultrasonography (2D/3D-CDUS) or magnetic resonance imaging (MRI). The secondary outcomes include quality of life, clinical pregnancy, ovarian reserve, adverse events, assessment by the Short Form (36) Health Survey and Female Sexual Function index, serum follicle-stimulating hormone, estradiol levels, and anti-Muellerian hormone and so on. All these indexes are measured at 3, 6, 12, 18, 24, 30, and 36 months after conservative surgery. Discussion The result of this large, multicenter randomized trial will provide evidence for one of the strategies of long-term management in focal adenomyosis after conservative operation. Trial registration Chinese Clinical Trial Registry: ChiCTR1800014340 . Registered on 6 January 2018.

The work is a continuation of the research on the use of NMR spectroscopy in the quality control of natural peptide hormone-based active substances and their synthetic analogues. The aim of the paper was to develop identification test methods for triptorelin acetate and goserelin acetate substances using NMR spectroscopy that does not require reference standards ‒ with the aim of using the newly developed test methods in pharmacopoeial analysis. Materials and methods: the procedure was developed using two-dimensional NMR spectroscopy (1H-1H gCOSY, 1H-13C gHSQC, 1H-13C gHMBC). Results: thestudy made it possible to assign 1H and 13C NMR signals to a specific molecular fragment, and to determine the amino acid composition of each oligopeptide. Conclusions: the authors drew up a table showing structural assignment of NMR signals, which makes it possible to use the NMR method for identification testing of triptorelin acetate and goserelin acetate substances without the use of pharmacopoeial reference standards. The study helped to determine the optimal temperature conditions for recording 13C NMR spectra (27 °С and 50 °С for triptorelin acetate and goserelin acetate, respectively). It was demonstrated that 13C NMR spectroscopy could be used for identification testing in pharmacopoeial analysis.

Background and objectives: Prostate cancer is the second leading cause of mortality among men worldwide, and the eighth cancer-related cause of death in Iran. Male sex hormones (androgens) are the main cause of prostate cancer cells. Triptorelin is considered a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) in the treatment of prostate cancer. This study aimed to evaluate the methods to deal with the constraints in use of lipid nanoarchaeosomes. Due to their adjuvant feature and presence of ether links, archaeosomes are more stable in blood, compared to other lipid-based formulations. In the present study, the effects of nanoarchaeosomes containing triptorelin acetate on the cellular toxicity of the PC3 prostate cancer cell line were evaluated. Methods: Halobacterium salinarum bacteria were cultured in HS medium, and their polar lipids of the membrane were removed applying the Blight&Dye technique in order to obtain nanoarchaeosome containing membrane polar lipids. In the next stage, nanoarchaeosomes were prepared by the hydration of polar lipids. In addition, cell viability was evaluated using the MTT assay on the PC3 cell line. Results: In this research, mean diameter of the drug-containing nanoarchaeosomes was estimated at 263 nm using the ZetaSizer device. Moreover, drug loading efficiency of nanoarchaeosomes was estimated at 98%. Furthermore, the toxicity of the free and nanoarchaeosome drugs was assessed via the MTT assay, results of which were indicative of a mean of IC 50 0.22 µg/ml in this regard. Conclusion: According to the results of the study, archaeosomes extracted from polar lipids were produced with high concentration and purity on the nanoscale. Considering the high stability, ease of production, level of drug loading, and toxic effect on cancer cells, nanoarchaeosomes can be used as a suitable technique for targeted drug delivery in future studies.

Context. GnRHa treatment has been a standard of care in progressive early puberty (EP). Choice of the GnRHa formulation is dependent on the preference of the clinician. Objective. To compare the effects of triptorelin acetate (TA) and leuprolide acetate (LA) on anthropometry in girls with EP. Design. A descriptive observational study. Subjects and Methods. Girls diagnosed with central EP and treated with GnRHa at least for one year were included; treated with TA (n=46) and LA (n=35). First year anthropometric response and final height were evaluated. Results. The mean age at the initiation of GnRHa treatment of girls was 8.5±0.5 years. The ratio of obesity and of overweight was 7.4 and 25.9%, respectively. In both TA and LA groups, anthropometric data of the patients at initiation and at the first year of treatment were similar. Although growth velocity was similar in each group, in LA group height SDS at the first year of the treatment showed a significant decrease (p=0.045), but not in TA group (p=0.317). No significant ΔBMI was observed with treatment. The differences between FH -- PAH at initiation (height gain) in TA and LA groups were 2.9±4.7 and 4.0±5.8 cm, respectively (p=.316). Height gain per treatment year was 1.7±3.0 cm. Conclusions. There was a significant decrease in height SDS at the first year of leuprolid treatment, but not in triptorelin. Although these two analogs show similar effects on treatment, a not significant but slightly better benefit in leuprolide was observed. [ABSTRACT FROM AUTHOR]

Background: The preservation of fertility and integrity of the reproductive organs has increasingly been of concern to most women with adenomyosis. Adenomyomectomy is conservative surgery that is now widely applied; however, relapse is a serious problem after the operation. Postoperative treatment, such as gonadotropin-releasing hormone agonist (GnRHa) has been suggested to result in reducing the rate of disease recurrence. However, there is still a lack of evidence from randomized clinical trials examining the efficacy of GnRHa in decreasing the postoperative recurrence rate.Method/design: Relapse after conservative surgery combined with triptorelin acetate versus conservative surgery only in women with focal adenomyosis is a multicenter, prospective, randomized controlled trial. The primary outcome is relapse assessed using a visual analogue scale (VRS) and numeric rating scale (NRS), pictorial blood loss assessment chart (PBAC) score, and the size of the uterus and the lesion as measured by two/three-dimensional color doppler ultrasonography (2D/3D-CDUS) or magnetic resonance imaging (MRI). The secondary outcomes include quality of life, clinical pregnancy, ovarian reserve, adverse events, assessment by the Short Form (36) Health Survey and Female Sexual Function index, serum follicle-stimulating hormone, estradiol levels, and anti-Muellerian hormone and so on. All these indexes are measured at 3, 6, 12, 18, 24, 30, and 36 months after conservative surgery.Discussion: The result of this large, multicenter randomized trial will provide evidence for one of the strategies of long-term management in focal adenomyosis after conservative operation.Trial Registration: Chinese Clinical Trial Registry: ChiCTR1800014340. Registered on 6 January 2018. [ABSTRACT FROM AUTHOR]

Objective: To analysis the clinical effect of progesterone combined with triptorelin acetate in the treatment of endometriosis. Methosds: Selected 398 patients with endometriosis who were treated in our hospital from January 2015 to December 2017 were enrolled in the order of admission. They were divided into two groups according to the odd-even method, each group of 199 cases. The control group was given didrogesterone orally only after operation, one tablet per time, two times per day, for 6 months. The observation group was treated with desdrogesterone combined with triptorelin acetate after operation, i.e. intramuscular injection of triprillin acetate, 3.75 mg/time, once a month, for 6 consecutive times. The curative effect, serological index, dysmenorrhea, pelvic pain and degree of sexual intercourse pain before and after treatment were compared between the two groups. Results: After treatment, the total effective rate of the observation group was significantly higher than that of the control group (P<0.05). After treatment, the levels of luteinizing hormone (LH) and Follicle-stimulating hormone (FSH) did not change significantly in the two groups (P>0.05), while the levels of serum estradiol (E2), carbohydrate antigen 125 (Carbohydrate antigen, CA125) and vascular endothelial growth factor (VEGF) were significantly lower than those before treatment (P<0.05). The scores of dysmenorrhea, pelvic pain and sexual pain in the two groups were significantly lower than those before treatment (P<0.05), and the observation group was significantly lower than the control group (P<0.05). Conclusion: Postoperative treatment of endometriosis with dydrogesterone combined with triptorelin acetate has a significant therapeutic effect, and can effectively alleviate the pain symptoms of patients, improve serum related indicators, and effectively improve endometriosis. [ABSTRACT FROM AUTHOR]

The aim of this study is to compare the clinical and biochemical outcomes of triptorelin acetate (TPA) versus triptorelin pamoate (TPP) treatment in girls with central precocious puberty. A total of 60 patients with idiopathic CPP were retrospectively recruited. Thirty girls were treated with triptorelin acetate 3.75 mg/month (TPA group) and thirty girls in a second group received triptorelin pamoate 3.75 mg/4 weeks (TPP group). Patient follow-up at 12 and 24 months included GnRH Test at 12 months and baseline LH at 24 months. Patients were monitored with pelvic ultrasound, X-Ray of the hand and wrist and anthropometric evaluations. A total of 60/60 girls showed a good response to both formulations. Significant reductions in basal and LH peaks, estradiol values, breast pubertal stage, progression of bone age and growth velocity rate after 12 months treatment were obtained in both groups, demonstrating the equivalence of the two formulations in regulating the hypothalamic–pituitary-gonadal (HPG) axis. Triptorelin pamoate provided a more effective and significant reduction in LH peak after 12 months in comparison with triptorelin acetate more effective in reducing ovarian volume and endometrial thickness. Both formulations were equivalent, even though the LH peak was significantly lower in girls treated with triptorelin pamoate [ABSTRACT FROM AUTHOR]

The objective of these studies was to investigate the efficacy of an intravaginal triptorelin acetate (TA) gel as an ovulation-inducing agent in mares. In Exp. 1, 24 mares were blocked using a combination of parity and age and randomly assigned to 1 of 3 treatment groups: 5 mL TA gel (TA5), 10 mL TA gel (TA10), or 5 mL vehicle gel only (CON). Following the appearance of a follicle ≥ 25 mm, a blood sample was obtained for measurement of LH from each mare every 24 h until treatment administration. When a follicle ≥ 35 mm was observed, treatments were administered intravaginally. Following treatment, blood samples were collected for measurement of LH and ovaries were scanned via ultrasonography every 12 h until 48 h post-ovulation. Mares in both TA5 and TA10 tended (P = 0.08) to experience a brief surge in LH by 12 h post-treatment. There was a treatment by time interaction (P < 0.005). The interval from treatment to ovulation was not different between groups (P > 0.05). We hypothesized that duration of elevated LH was not sufficient to induce ovulation in most mares. In Exp. 2, 23 mares were blocked by parity/age and randomly assigned to 3 treatment groups: the CON (n = 7) and TA5 (n = 8) treatment groups remained the same, but the TA10 treatment was split into two 5-mL doses administered 24 h apart (TA5×2; n = 8). Blood collection and ultrasonography occurred every 12 h on detection of a follicle ≥ 25 mm in diameter. Once a follicle ≥ 35 mm was detected, treatment was administered and ultrasonography and blood collection for measurement of LH occurred every 6 h until 48 h post-ovulation to get a more robust characterization of the effect of TA on LH and a more accurate timeframe in which ovulation was occurring. Mares in both TA5 and TA5×2 had an increase (P < 0.05) in LH by 6 h post-treatment, which was declining by 12 h post-treatment. Following the second dose in TA5×2, another rise in LH occurred, but to a lesser magnitude (P > 0.05) compared with the initial dose. Again there was a treatment by time interaction (P < 0.005) and in Exp. 2 the interval from treatment to ovulation was shorter in TA5 (61.5 ± 8.8 h) and TA5×2 (61.5 ± 9.6 h) compared with CON (123.1 ± 21.7 h; P < 0.01). In Exp. 2, administration of TA gel increased LH concentrations and hastened the interval from treatment to ovulation in mares, without an advantage in the timing of ovulation noted between the 5 or 10-mL doses, or administration of two 5-mL doses given 24 h apart. [ABSTRACT FROM AUTHOR]

Anaphylaxis is an acute, potentially life-threatening allergic multisystemic hypersensitivity reaction. Although the anaphylaxis incidence is not clearly known, serious reactions are seen at a rate of approximately 1-3 per 10,000. Drugs are among the most common causes of anaphylactic reactions. Triptorelin acetate treatment aims to alleviate the clinical symptoms of early pubertal development, the psychological consequences and the effects on growth. Triptorelin acetate is major long-acting gonadotropin releasing hormone (GnRH) analogue. Our case diagnosed with central precocious puberty was being followed up by the pediatric endocrinology department when anaphylaxis occurred following an injection at the 18th month of treatment. Anaphylaxis with Triptorelin acetate has been reported in only two cases in the literature. Although the risk of anaphylaxis with this drug is low, the possibility should be considered and appropriate measures taken. [ABSTRACT FROM AUTHOR]

Purpose: To compare the efficacy of the oral dienogest versus triptorelin acetate injection for treatment of premenopausal menorrhagia and pelvic pains in women with uterine adenomyosis.Methods: A total of 41 patients with adenomyosis suffering from pelvic pains and menorrhagia were recruited. First group was managed with oral dienogest (2 mg/day, orally) while the second group received triptorelin acetate (3.75 mg/4 weeks, subcutaneous injection) for 16 weeks. Outpatient follow-up was undertaken after 8 weeks but mean values were calculated at baseline and after 16 weeks (end of treatment).Results: A total of 41 women were allocated to treatment with dienogest (n = 22) or triptorelin acetate (n = 19); 19 (86.4 %) and 18 (94.7 %) % of the respective groups completed the trial. Significant reductions in pelvic pains after 16 weeks treatment were obtained in both groups demonstrating the equivalence of dienogest relative to triptorelin acetate. Triptorelin acetate was more effective in controlling of menorrhagia and reduction of uterine volume.Conclusions: Dienogest may be a valuable alternative to depot triptorelin acetate for treatment of premenopausal pelvic pains in women with uterine adenomyosis. [ABSTRACT FROM AUTHOR]

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Triptorelin acetate-loaded poly(lactide- co-glycolide) (PLGA) microspheres have been prepared in binary solvent mixtures composed of dichloromethane (DCM) and acetone (AC). The surface morphology of PLGA microspheres was examined by scanning electron microscopy with varying solvent composition, and the size distribution of PLGA microspheres was measured using a particle size analyzer. Triptorelin acetate is a luteinizing hormonereleasing hormone analog that is used as a model peptide drug. With the increase of AC content in the binary solvent mixture, PLGA microspheres with smooth surface were obtained and this led to an increased loading efficiency with the decreased particle size. For the application of PLGA microspheres as a controlled drug delivery system, the release pattern of triptorelin acetate was observed and the stability of triptorelin acetate-loaded PLGA microspheres was observed with or without mannitol. The sustained release pattern was observed after the initial burst effect and the improved stability of PLGA microspheres was observed with mannitol. [Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

Objective: To compare the clinical effect of triptorelin acetate and megestrol acetate tablets in the treatment of idiopathic central precocious puberty. Methods: select our hospital since 2014 February 2015 during February were idiopathic central precocious puberty in 92 cases of children. According to the random number table method, they were divided into 2 groups, 46 cases of children only accept megestrol acetate tablets in the treatment (control group), 46 patients received triptorelin acetate treatment (observation group). After 6 months treatment, compared the growth index and hormone level changes and statistical the adverse reaction between two groups. Results: After treatment, the weight, height.growth rate,prediction of height, BA/CA growth index of observation group was better than that of the control group (P<0.05): compared with before tr eatment, the E2. LH and FSF1 levels of two groups had improved significantly after treatment(P<0.05); and the E2. LH and FSH levels of observation group was better than that of control group (P<0.05); No obvious adverse reactions were found in the two groups. Conclusion: Comparing with megestrol acetate tablets, the clinical effect of triptorelin acetate in the treatment of idiopathic central precocious puberty in childr en was more better, delay the maturation of bone age of children, reduce the level of sex hormone, which has good application value in clinical. [ABSTRACT FROM AUTHOR]

Developing a single fixed-time artificial insemination (FTAI) protocol would benefit small-scale and niche market pork producers by decreasing semen costs and labor associated with detection of estrus. The objective of this study was to test the efficacy of an AI breeding system using triptorelin acetate, a GnRH agonist (OvuGel; JBS United Animal Health, LLC, Sheridan, IN) that induces ovulation. A total of 92 sows (parity, 3.5 ± 0.2; BCS, 2.5 ± 0.08) were weaned (h 0) after a 25.0 ± 0.6 d lactation on five participating small pig farms and allocated to one of four treatment groups: 1) OvuGel applied intravaginally at h 96 and AI at h 120 (n = 23); 2) P.G. 600 (400 IU eCG and 200 IU hCG, Merck Animal Health, Inc., De Sota, KS) applied i.m. at weaning, OvuGel at h 96 and AI at h 120 (n = 23); 3) AI at 0 and 24 h after first detection of estrus (n = 23); and 4) P.G. 600 at weaning, and AI at 0 and 24 h after onset of estrus (n = 23). Treatments 1 and 2 were FTAI protocols with sows being inseminated without regards to estrus onset. Treatments 3 and 4 were consistent with current industry AI practices. The proportion of females displaying estrus by day 7 post-weaning was greater (P = 0.02) for sows that received OvuGel (93.9 ± 0.07%) compared to sows that did not (81.0 ± 0.07%). There were no effects (P > 0.05) of P.G. 600 or P.G. 600 x Ovugel on females displaying estrus by day 7. Weaning to estrus interval was decreased (P = 0.04) for sows that received P.G. 600 (4.9 ± 0.4 d) compared to sows that did not (5.4 ± 0.4 d). There were no effects (P > 0.05) of Ovugel or P.G. 600 x Ovugel on the weaning-to-estrus interval. There were no effects of P.G. 600, Ovugel or P.G. 600 x Ovugel (P > 0.1) on pregnancy rate (59%), total litter size (11.8), born live (10.8), or born dead (0.9). These results suggest that FTAI protocols may be employed on small-scale pig farms without compromising reproductive performance. [ABSTRACT FROM AUTHOR]

Developing a single fixed-time artificial insemination (FTAI) protocol would benefit small-scale and niche market pork producers by decreasing semen costs and labor associated with detection of estrus. The objective of this study was to test the efficacy of an AI breeding system using triptorelin acetate, a GnRH agonist (OvuGel; JBS United Animal Health, LLC, Sheridan, IN) that induces ovulation. A total of 92 sows (parity, 3.5 ± 0.2; BCS, 2.5 ± 0.08) were weaned (h 0) after a 25.0 ± 0.6 d lactation on five participating small pig farms and allocated to one of four treatment groups: 1) OvuGel applied intravaginally at h 96 and AI at h 120 (n = 23); 2) P.G. 600 (400 IU eCG and 200 IU hCG, Merck Animal Health, Inc., De Sota, KS) applied i.m. at weaning, OvuGel at h 96 and AI at h 120 (n = 23); 3) AI at 0 and 24 h after first detection of estrus (n = 23); and 4) P.G. 600 at weaning, and AI at 0 and 24 h after onset of estrus (n = 23). Treatments 1 and 2 were FTAI protocols with sows being inseminated without regards to estrus onset. Treatments 3 and 4 were consistent with current industry AI practices. The proportion of females displaying estrus by day 7 post-weaning was greater (P = 0.02) for sows that received OvuGel (93.9 ± 0.07%) compared to sows that did not (81.0 ± 0.07%). There were no effects (P > 0.05) of P.G. 600 or P.G. 600 x Ovugel on females displaying estrus by day 7. Weaning to estrus interval was decreased (P = 0.04) for sows that received P.G. 600 (4.9 ± 0.4 d) compared to sows that did not (5.4 ± 0.4 d). There were no effects (P > 0.05) of Ovugel or P.G. 600 x Ovugel on the weaning-to-estrus interval. There were no effects of P.G. 600, Ovugel or P.G. 600 x Ovugel (P > 0.1) on pregnancy rate (59%), total litter size (11.8), born live (10.8), or born dead (0.9). These results suggest that FTAI protocols may be employed on small-scale pig farms without compromising reproductive performance. [ABSTRACT FROM AUTHOR]