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多潘立酮胃内漂浮片的处方及体外评价研究

Studies on formulation and in vitro evaluation of floating matrix tablets of domperidone.

作者信息

Prajapati S T, Patel L D, Patel D M

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Shri Sarvajanik Pharmacy College, Mehsana-384 001, India.

出版信息

Indian J Pharm Sci. 2009 Jan;71(1):19-23. doi: 10.4103/0250-474X.51944.

DOI:10.4103/0250-474X.51944
PMID:20177450
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2810042/
Abstract

Floating matrix tablets of domperidone were developed to prolong gastric residence time and thereby increased drug bioavailability. Domperidone was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by wet granulation technique, using polymers such as hydroxypropylmethylcellulose K4M, carbopol 934P, and sodium alginate, either alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, % friability, floating capacity, weight variation and content uniformity. Further, tablets were evaluated for in vitro release characteristics for 24 h. In vitro release mechanism was evaluated by linear regression analysis. Floating matrix tablets based on combination of three polymers namely; hydroxypropylmethylcellulose K4M, carbopol 934P and sodium alginate exhibited desired floating and prolonged drug release for 24 h. Carbopol loading showed negative effect on floating properties but were found helpful to control the release rate of drug.

摘要

开发了多潘立酮漂浮型骨架片以延长胃滞留时间,从而提高药物的生物利用度。选择多潘立酮作为模型药物,因为它在下消化道吸收较差。片剂采用湿法制粒技术制备,使用诸如羟丙基甲基纤维素K4M、卡波姆934P和海藻酸钠等聚合物单独或组合使用,以及其他标准辅料。对片剂的物理特性即硬度、脆碎度百分比、漂浮能力、重量差异和含量均匀度进行了评估。此外,对片剂进行了24小时的体外释放特性评估。通过线性回归分析评估体外释放机制。基于羟丙基甲基纤维素K4M、卡波姆934P和海藻酸钠三种聚合物组合的漂浮型骨架片表现出所需的漂浮性能并能使药物释放延长24小时。卡波姆的用量对漂浮性能有负面影响,但发现有助于控制药物的释放速率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/98eba9d1141b/IJPhS-71-19-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/a972ccac6bc2/IJPhS-71-19-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/704ed029d99d/IJPhS-71-19-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/f186110358c9/IJPhS-71-19-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/4279521c4aea/IJPhS-71-19-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/98eba9d1141b/IJPhS-71-19-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/a972ccac6bc2/IJPhS-71-19-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/704ed029d99d/IJPhS-71-19-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/f186110358c9/IJPhS-71-19-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/4279521c4aea/IJPhS-71-19-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fa4/2810042/98eba9d1141b/IJPhS-71-19-g005.jpg

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