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用于全身给药途径的泮托拉唑钠微球及其评价

Pantoprazole Sodium Loaded Microballoons for the Systemic Approach: and Evaluation.

作者信息

Gupta Pravin, Kumar Manish, Kaushik Darpan

机构信息

Department of Pharmaceutics, Agra Public Pharmacy College, Agra (U.P.), India.

Department of Pharmaceutics, Maharishi Markandeshwar College of Pharmacy, Maharishi Markandeshwar University, Mullana-Ambala (Haryana), India.

出版信息

Adv Pharm Bull. 2017 Sep;7(3):461-467. doi: 10.15171/apb.2017.055. Epub 2017 Sep 25.

Abstract

Various floating and pulsatile drug delivery systems suffer from variations in the gastric transit time affecting the bioavailability of drugs. The objective of the study was to develop Pantoprazole Sodium (PAN) microballoons that may prolong the gastric residence time and could enhance the drug bioavailability. Microballoons were prepared using EudragitL100 by adopting emulsion solvent diffusion method with non-effervescent approach, in vitro studies were performed and the in vivo evaluation was carried out employing ethanol induced ulceration method. Optimization and validation were carried out through Design Expert software. The results demonstrate an increase in percentage yield, buoyancy, encapsulation efficacy and swelling. Particles were in the size range 80-100 µm following zero order release pattern. SEM study revealed their rough surface with spherical shape, internal cavity and porous walls. DSC thermo gram confirms the encapsulation of drug in amorphous form. Significant anti ulcer activity was observed for the prepared microballoons. The calculated ulcer index and protection were 0.20±0.05 and 97.43 % respectively for LRS-O (optimized formulation). This kind of pH dependent drug delivery may provide an efficient dosage regimen with enhanced patient compliance.

摘要

各种漂浮和脉动给药系统都存在胃转运时间变化的问题,这会影响药物的生物利用度。本研究的目的是开发泮托拉唑钠(PAN)微球,以延长胃滞留时间并提高药物生物利用度。采用乳液溶剂扩散法和非泡腾方法,用EudragitL100制备微球,进行体外研究,并采用乙醇诱导溃疡法进行体内评价。通过Design Expert软件进行优化和验证。结果表明产率、浮力、包封率和溶胀率均有所提高。颗粒大小在80 - 100 µm范围内,呈零级释放模式。扫描电子显微镜研究显示其表面粗糙,呈球形,有内腔和多孔壁。差示扫描量热法热谱图证实药物以无定形形式被包封。所制备的微球具有显著的抗溃疡活性。LRS - O(优化配方)的计算溃疡指数和保护率分别为0.20±0.05和97.43%。这种pH依赖性给药方式可能提供一种有效的给药方案,提高患者的依从性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f60c/5651068/d1f9f0c6b420/apb-7-461-g001.jpg

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