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速溶条:一种维拉帕米给药的新方法。

Fast dissolving strips: A novel approach for the delivery of verapamil.

作者信息

Kunte S, Tandale P

机构信息

Department of Pharmaceutics School of Pharmacy and Technology Management, NMIMS, Vile Parle (West), Mumbai, India.

出版信息

J Pharm Bioallied Sci. 2010 Oct;2(4):325-8. doi: 10.4103/0975-7406.72133.

Abstract

OBJECTIVE

Fast dissolving drug delivery system offers a solution for those patients having difficulty in swallowing tablets/capsules etc. Verapamil is a calcium channel blocker used as an antianginal, antiarrhythmic, and antihypertensive agent with extensive first pass metabolism which results in less bioavailability. This work investigated the possibility of developing verapamil fast dissolving strips allowing fast, reproducible drug dissolution in the oral cavity; thus bypassing first pass metabolism.

MATERIALS AND METHODS

The fast dissolving strips were prepared by solvent casting technique with the help of HPMC E6 and maltodextrin. The strips were evaluated for drug content uniformity, film thickness, folding endurance, in vitro disintegration time, in vitro dissolution studies, surface pH study, and palatability study.

RESULTS

Official criteria for evaluation parameters were fulfilled by all formulations. Disintegration time showed by formulations was found to be in range of 20.4-28.6 sec. Based on the evaluation parameters, the formulation containing 2% HPMC E6 and 3.5% maltodextrin showed optimum performance against other formulations.

CONCLUSION

It was concluded that the fast dissolving strips of verapamil can be made by solvent casting technique with enhanced dissolution rate, taste masking, and hence better patient compliance and effective therapy.

摘要

目的

速溶药物递送系统为那些吞咽片剂/胶囊等有困难的患者提供了一种解决方案。维拉帕米是一种钙通道阻滞剂,用作抗心绞痛、抗心律失常和抗高血压药物,具有广泛的首过代谢,导致生物利用度较低。本研究探讨了开发维拉帕米速溶条的可能性,该速溶条可在口腔中实现快速、可重复的药物溶解;从而绕过首过代谢。

材料与方法

采用溶剂浇铸技术,借助羟丙甲纤维素E6和麦芽糊精制备速溶条。对速溶条进行了药物含量均匀度、膜厚度、折叠耐久性、体外崩解时间、体外溶出度研究、表面pH值研究和适口性研究。

结果

所有制剂均符合评价参数的官方标准。制剂的崩解时间在20.4 - 28.6秒范围内。基于评价参数,含有2%羟丙甲纤维素E6和3.5%麦芽糊精的制剂相对于其他制剂表现出最佳性能。

结论

得出结论,维拉帕米速溶条可通过溶剂浇铸技术制备,具有提高的溶出速率、掩味效果,从而具有更好的患者依从性和有效的治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45e3/2996061/22f2ab5d9d48/JPBS-2-325-g001.jpg

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