马来酸丙氯哌嗪口腔速溶贴剂的研制及其对呕吐的有效控制

YMER Digital Pub Date : 2022-08-05 DOI:10.37896/ymer21.08/13
Shailesh Sharma
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引用次数: 0

摘要

本研究的目的是通过制造马来酸丙氯哌嗪(用于治疗恶心和呕吐)的口腔贴片来提高口服生物利用度并避免其第一次代谢。丙氯哌嗪是BCS II的成员,口服生物利用度为11 - 15%。以HPMC E-15、壳聚糖(成膜剂)、甘油(增塑剂)、吐温80(渗透增强剂)、柠檬酸(唾液刺激剂)、甘露醇(甜味剂)、乙基纤维素(背膜)为辅助剂,采用溶剂铸造法制备马来酸丙氯佩拉嗪口腔贴片。采用不同数量的聚合物制备了12个总配方,并对配方的重量变化、厚度、折叠耐力、药物含量、体外扩散、体外粘附时间、水分损失率、溶胀率和稳定性进行了评价。结果表明,口腔补片(F4)具有提高生物利用度的作用。关键词:马来酸丙氯哌嗪;口腔贴剂;生物利用度
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Development of Fast Dissolving Buccal Patches of Prochlorperazine Maleate for Effective Management of Emesis
The goal of this research was to increase the oral bioavailability and avoid the first pass metabolism of Prochlorperazine Maleate (used to treat nausea and vomiting) by creating its buccal patches. Prochlorperazine is a member of BCS II and has an oral bioavailability of 11– 15%. Prochlorperazine maleate buccal patches were made by solvent casting with the aid of HPMC E-15 and Chitosan (film-forming agents), Glycerol (plasticizer), Tween 80 (penetration enhancer), Citric Acid (saliva stimulating agent), Mannitol (sweetening agent), and Ethyl Cellulose (Backing membrane). Twelve total formulations was made by using different quantities of polymers and formulation was evaluated for weight variation, thickness, folding endurance, drug content, in- vitro diffusion, in vitro, bio-adhesion time, percent moisture loss, % swelling index and stability study. Based on results it was concluded that buccal patches (F4) showed enhanced bioavailability. Keywords: Prochlorperazine maleate, Buccal Patches, Bioavailability, Stability
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