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新型卡维地洛黏膜黏附颊贴片对异丙肾上腺素诱发心动过速的影响。

Effect of novel mucoadhesive buccal patches of carvedilol on isoprenaline-induced tachycardia.

作者信息

Verma Navneet, Chattopadhyay Pronobesh

机构信息

Department of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India.

Defence Research Laboratory, DRDO, Tezpur, Assam, India.

出版信息

J Adv Pharm Technol Res. 2014 Apr;5(2):96-103. doi: 10.4103/2231-4040.133436.

Abstract

The main aim of the study was designed to develop bioadhesive buccal patches of carvedilol (CR) and evaluate for isoprenaline-induced tachycardia. Buccal patches of carvedilol were prepared by using chitosan (CH), sodium salt of carboxy methyl cellulose (NaCMC), and polyvinyl alcohol (PVA) as mucoadhesive polymers. The solvent evaporation method was used for the preparation of buccal patches. The patches were evaluated for their physical characteristics like patch thickness, weight variation, content uniformity, folding endurance, surface pH, residence time, in vitro drug release, and in vivo pharmacodynamic study. The swelling index of the patches was found to be proportional to the polymer concentration, whereas surface pH of all the formulated bioadhesive patches was found to lie between neutral ranges. In-vitro release study shows that 94.75% drug was release in 8 hours from the patch, which containing 2% w/v chitosan. The folding endurance result shows good elasticity in all the patches. Application of buccal patches on buccal mucosa of rabbit shows a significant result in % inhibition of isoprenaline-induced tachycardia. Prepared buccal patches of chitosan, NaCMC, and PVA containing Carvedilol meet the ideal requirement for the delivery of cardiovascular drugs and inhibit the isoprenaline tachycardia.

摘要

本研究的主要目的是开发卡维地洛(CR)生物黏附性口腔贴片,并评估其对异丙肾上腺素诱发的心动过速的作用。以壳聚糖(CH)、羧甲基纤维素钠(NaCMC)和聚乙烯醇(PVA)作为黏膜黏附聚合物制备卡维地洛口腔贴片。采用溶剂蒸发法制备口腔贴片。对贴片的物理特性进行评估,如贴片厚度、重量差异、含量均匀度、耐折性、表面pH值、滞留时间、体外药物释放和体内药效学研究。发现贴片的溶胀指数与聚合物浓度成正比,而所有配制的生物黏附性贴片的表面pH值均在中性范围内。体外释放研究表明,含2% w/v壳聚糖的贴片中94.75%的药物在8小时内释放。耐折性结果表明所有贴片中均具有良好的弹性。将口腔贴片应用于兔颊黏膜对异丙肾上腺素诱发的心动过速有显著的抑制作用。制备的含壳聚糖、NaCMC和PVA的卡维地洛口腔贴片满足心血管药物递送的理想要求,并能抑制异丙肾上腺素诱发的心动过速。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27bb/4065471/295e484629b1/JAPTR-5-96-g003.jpg

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