Two Sustained Release Membranes Used in Formulating Low Strength Testosterone Reservoir Transdermal Patches.

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery Pub Date : 2024-01-01 DOI:10.2174/1567201820666230316115921

Ria Vashishth, Monica C Chuong, Juan Chang Duarte, Yadnya Gharat, Stephen G Kerr

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Abstract

Introduction: Several Testosterone Replacement Therapies exist for hypogonadism, but an in-depth analysis of these products reveals a high dosing frequency and a high drug loading, up to 120 mg for a potent drug like Testosterone. This may lead to patient non-compliance and toxicity problems if used improperly. Androderm^® is the only 24-hour marketed transdermal patch. Testopel pellets are another extended-release product given subcutaneously every 3-6 months. But it requires surgical implantation and is associated with severe adverse effects. For this reason, the development of other extended- release testosterone products is needed. The study aims at using different excipients for the exploration of sustained-release patches.

Methods: Reservoir formulations were prepared using Carbomer 941 and HPMC K100M as the sustained- release polymers plus CoTran™ 9702 and CoTran™ 9712 as the release membranes. The formulated patches were subjected to in vitro dissolution for 24 h. The amount of drug release at each time point was determined using the developed HPLC assay. FDA Similarity Factor, f₂, t-test, and ANOVA were applied to all nine-point collected samples.

Results: CoTran™ 9712 membrane was found to be a better candidate than CoTran™ 9702. The in vitro release profiles of the four formulations were compared (Carbomer vs. HPMC, and CoTran™ 9702 vs. CoTran™ 9712).

Conclusion: CoTran™ 9702 releases testosterone significantly lower. Carbomer and CoTran™ 9712 were the best formulation among all with the highest drug release of 2.16 ± 0.36 mg.

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两种缓释膜用于配制低强度睾酮库透皮贴剂。

介绍:目前已有几种睾酮替代疗法用于治疗性腺功能减退，但对这些产品的深入分析表明，它们的给药频率高，药物负荷大，如睾酮等强效药物的给药频率高达120毫克。如果使用不当，可能会导致患者不依从性和毒性问题。Androderm®是唯一一个24小时上市的透皮贴剂。Testopel微丸是另一种缓释产品，每3-6个月皮下注射一次。但它需要手术植入，并伴有严重的副作用。因此，需要开发其他缓释睾酮产品。本研究旨在利用不同赋形剂对缓释贴剂进行探索。方法:以卡波默941和HPMC K100M为缓释聚合物，以CoTran™9702和CoTran™9712为释放膜制备储层制剂。体外溶出24h，采用HPLC法测定各时间点的药物释放量。采用FDA相似因子、f2、t检验和方差分析对所有9点采集的样本进行分析。结果:CoTran™9712膜优于CoTran™9702膜。比较四种剂型的体外释放谱(Carbomer与HPMC, CoTran™9702与CoTran™9712)。结论:CoTran™9702释放睾酮显著降低。其中，卡波莫和CoTran™9712为最佳处方，释药量最高，为2.16±0.36 mg。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.