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一种抗高血压药物口腔黏附性液固系统的设计与表征

Design and Characterization of Buccoadhesive Liquisolid System of an Antihypertensive Drug.

作者信息

Kala Nilesh P, Shastri Divyesh H, Shelat Pragna K

机构信息

Department of Pharmaceutics & Pharmaceutical Technology, K. B. Institute of Pharmaceutical Education & Research, Sector 23, Gandhinagar, Gujarat 382023, India.

出版信息

J Drug Deliv. 2015;2015:574247. doi: 10.1155/2015/574247. Epub 2015 Oct 22.

Abstract

Nifedipine is an antihypertensive BCS class II drug which has poor bioavailability when given orally. The objective of the present study was to increase the bioavailability of nifedipine, by formulation and evaluation of a buccoadhesive liquisolid system using magnesium aluminium silicate (Neusilin) as both carrier and coating material and dissolution media were selected based on the solubility studies. A mixture of carboxymethylcellulose sodium and carbomer was used as mucoadhesive polymers. Buccoadhesive tablets were prepared by direct compression. FTIR studies confirmed no interaction between drug and excipients. XRD studies indicated change/reduction in crystallinity of drug. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial specifications. The dissolution studies for liquisolid compacts and tablet formulations were carried out and it was found that nifedipine liquisolid tablets formulated from bioadhesive polymers containing 49% liquisolid system, 17.5% carbomer, and 7.5% carboxymethylcellulose sodium showed the best results in terms of dissolution properties. Prepared formulation batches were evaluated for swelling, bioadhesion strength, ex vivo residence time, and permeability studies. The optimized batch was showing promising features of the system. Formulating nifedipine as a buccoadhesive tablet allows reduction in dose and offers better control over the plasma levels.

摘要

硝苯地平是一种抗高血压的BCS II类药物,口服时生物利用度较差。本研究的目的是通过使用硅酸镁铝(Neusilin)作为载体和包衣材料来制备和评价一种口腔黏附性液固系统,从而提高硝苯地平的生物利用度,并根据溶解度研究选择溶出介质。羧甲基纤维素钠和卡波姆的混合物用作黏膜黏附聚合物。通过直接压片制备口腔黏附片。傅里叶变换红外光谱(FTIR)研究证实药物与辅料之间无相互作用。X射线衍射(XRD)研究表明药物的结晶度发生了变化/降低。通过不同的流动参数对粉体特性进行评估,以符合药典规范。对液固型压制片和片剂制剂进行了溶出度研究,结果发现,由含49%液固系统、17.5%卡波姆和7.5%羧甲基纤维素钠的生物黏附聚合物制成的硝苯地平液固片在溶出性能方面表现出最佳效果。对制备的制剂批次进行了溶胀、生物黏附强度、离体滞留时间和渗透性研究。优化后的批次显示出该系统具有良好的特性。将硝苯地平制成口腔黏附片可减少剂量,并能更好地控制血浆水平。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f0f4/4633565/e69c6a0692f9/JDD2015-574247.001.jpg

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