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司他夫定口腔崩解片用于艾滋病治疗:一种新的技术方法。

Oral Disintegration Tablets of Stavudine for HIV Management: A New Technological Approach.

作者信息

Sankar V, Ramakrishna B, Devi P Shalini, Karthik S

机构信息

Department of Pharmaceutics, PSG College of Pharmacy, Coimbatore-641 004, India.

出版信息

Indian J Pharm Sci. 2012 Nov;74(6):556-63. doi: 10.4103/0250-474X.110602.

Abstract

Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets.

摘要

司他夫定口腔崩解片的配方旨在最大程度地减少苦味并降低肝脏首过代谢。测定了粉末混合物的各种压片前参数,如休止角、堆密度、压缩指数和豪斯纳比。在本研究中,采用直接压片法制备了14种司他夫定口腔崩解片配方。对片剂进行了重量差异、脆碎度百分比、崩解时间、硬度、湿润时间和吸水率的评估。批次S1(司他夫定+交联聚维酮+羟丙基淀粉)的体外溶出研究结果令人鼓舞,因为其达到了最高溶出率(100分钟内99.2%)和最短崩解时间(56秒)。在兔子身上进行了体内药物释放研究,发现配方S1的相对生物利用度比传统片剂高2.83倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a07/3687926/2363ff44bdbf/IJPhS-74-556-g004.jpg

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