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采用 32 析因设计研制和优化溴甲东莨菪碱胃滞留漂浮片。

Development and Optimization of Methscopolamine Bromide Gastroretentive Floating Tablets Using 32 Factorial Design.

机构信息

CT Institute of Pharmaceutical Sciences, Shahpur, Jalandhar Punjab.

MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University) Mullana -Ambala.

出版信息

Drug Res (Stuttg). 2020 Dec;70(12):576-582. doi: 10.1055/a-1249-8186. Epub 2020 Sep 29.

Abstract

PURPOSE

The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability.

METHOD

Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide.: Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets.

RESULT

The prepared tablets were evaluated for thickness, hardness, weight variation, floating lag time, swelling index and in-vitro drug release. All the formulations showed less than 10% of weight variation. The hardness and thickness of all the formulations were within the range of 3.7-4.2 kg/cm and 3.63-3.83 mm respectively. Floating lag time for all the formulations was reported in seconds. The degree of swelling was reported in range of 82.10-85.83%. In vitro release was carried out for 24 h. The maximum release was shown by F1 (93.947%) while the minimum release was observed for F4 (90.420%). The best formulation was optimized on the basis of percentage cumulative drug release, floating lag time and swelling index. F1 found to be the best formulation. Further on analyzing the drug release mechanism, F1 found to exhibit korsmeyer peppas model of drug release.

CONCLUSION

Floating gastroretentive tablet of methscopolamine bromide was successfully developed using direct compression method with potential to enhance the drug absorption and effective treatment of peptic ulcer.

摘要

目的

本研究旨在制备盐酸美沙醇的漂浮型药物传递系统,以增加其胃滞留时间,进一步提高药物吸收和总体生物利用度。

方法

采用直接压片法制备盐酸美沙醇的漂浮型药物传递系统:使用不同量的 HPMC、PVP K25 和 MCC 制备片剂。

结果

对制备的片剂进行了厚度、硬度、重量变化、漂浮滞后时间、溶胀指数和体外药物释放的评估。所有配方的重量变化均小于 10%。所有配方的硬度和厚度均在 3.7-4.2 kg/cm 和 3.63-3.83 mm 范围内。所有配方的漂浮滞后时间均以秒为单位报告。溶胀度报告范围为 82.10-85.83%。体外释放进行了 24 小时。F1 显示最大释放(93.947%),而 F4 显示最小释放(90.420%)。根据累积药物释放百分比、漂浮滞后时间和溶胀指数对最佳配方进行了优化。发现 F1 是最佳配方。进一步分析药物释放机制,发现 F1 符合 Korsmeyer-Peppas 药物释放模型。

结论

采用直接压片法成功制备了盐酸美沙醇漂浮型胃滞留片,具有提高药物吸收和有效治疗消化性溃疡的潜力。

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