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基于气体形成技术的盐酸普萘洛尔漂浮型骨架剂型:研制与体外评价

Floating matrix dosage form for propranolol hydrochloride based on gas formation technique: development and in vitro evaluation.

作者信息

Chaturvedi Kiran, Umadevi S, Vaghani Subhash

机构信息

P. E. S. College of Pharmacy, Bangalore, India.

出版信息

Sci Pharm. 2010 Oct-Dec;78(4):927-39. doi: 10.3797/scipharm.0909-02. Epub 2010 Sep 26.

DOI:10.3797/scipharm.0909-02
PMID:21179326
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3007615/
Abstract

Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ânâ value of the formulations ranged from 0.5201 to 0.7367 (0.5<n<1.0) which indicated anomalous (non-Fickian) transport mechanism. Formulation containing 27.5% HPMC K15M, 29% DCP, 3.75% citric acid and 18.75% sodium bicarbonate seemed most desirable. FTIR, DSC and XRPD studies indicated the absence of any significant chemical interaction within dug and excipients. Stability study of optimized formulation revealed no significant change and found to be stable.

摘要

采用直接压片法,以柠檬酸和碳酸氢钠作为泡腾剂,研制了盐酸普萘洛尔胃内滞留片。使用羟丙基甲基纤维素(HPMC K15M)制备漂浮片,以延缓药物在胃内12小时的释放。加入羧甲基纤维素钠(NaCMC)或卡波姆934P以改变药物释放曲线或制剂的尺寸稳定性。磷酸氢钙(DCP)用作填充剂。对制剂进行了漂浮滞后时间、漂浮持续时间、尺寸稳定性、药物含量和体外药物释放曲线的评价。发现制剂的漂浮滞后时间小于1分钟。发现制剂的尺寸稳定性随着溶胀剂浓度的增加而增加。基于Peppas和Higuchi模型评价了盐酸普萘洛尔从漂浮片中的释放机制。制剂的“n”值范围为0.5201至0.7367(0.5<n<1.0),这表明为非菲克(非Fickian)转运机制。含有27.5% HPMC K15M、29% DCP、3.75%柠檬酸和18.75%碳酸氢钠的制剂似乎是最理想的。傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和X射线粉末衍射(XRPD)研究表明药物与辅料之间不存在任何显著的化学相互作用。优化制剂的稳定性研究表明没有显著变化,且发现是稳定的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/ff211d30e37e/scipharm-2010-78-927f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/62317d2ffd39/scipharm-2010-78-927f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/f65ef2aac5ea/scipharm-2010-78-927f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/ebbb65598887/scipharm-2010-78-927f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/8e10536cfec9/scipharm-2010-78-927f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/ff211d30e37e/scipharm-2010-78-927f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/62317d2ffd39/scipharm-2010-78-927f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/f65ef2aac5ea/scipharm-2010-78-927f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/ebbb65598887/scipharm-2010-78-927f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/8e10536cfec9/scipharm-2010-78-927f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1215/3007615/ff211d30e37e/scipharm-2010-78-927f5.jpg

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