盐酸多潘立酮透皮缓释贴剂治疗晕动病的配方及疗效评价

M. Asif Jamshaid, Muqarab Abbas, M. Yousaf, Mahnoor Younas, Hajra Muzaffar, Talib Hussain, Rais A. Nawaz
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引用次数: 0

摘要

目的:经皮给药途径避免了首过效应,保证了患者更好的依从性,减少了给药频率,尤其是缓释制剂,使用方便,优于口服给药途径。盐酸多潘立酮是DA2受体拮抗剂,用于预防恶心和呕吐。目的是制定多潘立酮盐酸缓释经皮给药系统治疗晕动病。方法:采用不同的溶剂(甲醇和二氯甲烷)和聚合物(HPMC和Eudragitl-100),采用溶剂蒸发法制备5种不同的配方。每个贴片中加入500mg盐酸多潘立酮,并加入邻苯二甲酸二丁酯作为增塑剂。采用3% w/v的聚乙烯醇层作为衬底。对各制剂的理化性质(重量变化、厚度、折叠耐力、抗拉强度)、体外药物释放、药物含量测定、FTIR和DSC法测定药物与辅料的不相容性、皮肤刺激性等进行评价。结果:各制剂具有良好的理化性能,24 h内释药率分别为79.3%、97.1%、96.8%、74.7%和59.7%。F-YM体外释放量最大。优化后的配方(F-YM)符合Korsmeyer Peppas释放模型,n=0.383,符合溶出依赖性药物释放。DSC和FTIR均未检测到药物与辅料之间的相互作用。未检测到皮肤刺激。结论:制备了治疗晕动病的多潘立酮缓释透皮贴剂,F-YM处方表现出最佳的体外释药效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and evaluation of sustained releasedomperidone hydrochloride transdermal patches to treat motion sickness
Objective: Transdermal route of drug delivery is superior than oral route because it avoids first pass effect, ensures better patient compliance, reduce dosing frequency especially in extended-release formulation and is easy to use. Domperidone HCl is DA2 receptor antagonistic and is used to prevent nausea and vomiting. The objective was to formulate a domperidone HCl extended-release transdermal drug delivery system to treat motion sickness. Methods: Five different formulations were formed using different solvents (methanol and dichloromethane) and polymers (HPMC and Eudragitl-100) by solvent evaporation method. 500mg of domperidone HCl was added in each patch and dibutyl phthalate was added as plasticizer. A 3%  w/v PVA layer was used as backing. All these formulations were evaluated for their physicochemical properties (weight variation, thickness, folding endurance and tensile strength), in-vitro drug release, drug contents determination, any incompatibility between drug and excipients by FTIR and DSC and skin irritation. Results: All formulations exhibited good physicochemical properties and percentage drug release during 24 hours was 79.3%, 97.1%, 96.8%, 74.7% and 59.7% respectively. F-YM showed maximum in-vitro drug release. The optimized formulation (F-YM) followed Korsmeyer Peppas release model with n=0.383 showing that the system was following dissolution dependent drug release. No interaction between drug and excipients was detected by DSC and FTIR. No skin irritation was detected. Conclusion: The extended release transdermal patches of domperidone HCl to treat motion sickness were prepared and formulation F-YM showed optimized behavior with maximum in vitro drug release.
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