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天然胶作为缓控释载体:盐酸齐拉西酮胃滞留型给药系统的研制。

Natural gums as sustained release carriers: development of gastroretentive drug delivery system of ziprasidone HCl.

机构信息

Department of Pharmaceutics, Acharya & BM Reddy College of Pharmacy, Soladevanahally Hesaraghatta road, Bangalore, 560090, India.

出版信息

Daru. 2012 Oct 17;20(1):58. doi: 10.1186/2008-2231-20-58.

Abstract

BACKGROUND

Objective of this study is to show the potential use of natural gums in the development of drug delivery systems. Therefore in this work gastro retentive tablet formulations of ziprasidone HCl were developed using simplex lattice design considering concentration of okra gum, locust bean gum and HPMC K4M as independent variables. A response surface plot and multiple regression equations were used to evaluate the effect of independent variables on hardness, flag time, floating time and drug release for 1 h, 2 h, and 8 h and for 24 h. A checkpoint batch was also prepared by considering the constraints and desirability of optimized formulation to improve its in vitro performance. Significance of result was analyzed using ANOVA and p < 0.05 was considered statistically significant.

RESULTS

Formulation chiefly contains locust bean gum found to be favorable for hardness and floatability but combined effect of three variables was responsible for the sustained release of drug. The in vitro drug release data of check point batch (F8) was found to be sustained well compared to the most satisfactory formulation (F7) of 7 runs. The 'n' value was found to be between 0.5 and 1 suggesting that release of drug follows anomalous (non-fickian) diffusion mechanism indicating both diffusion and erosion mechanism from these natural gums. Predicted results were almost similar to the observed experimental values indicating the accuracy of the design. In vivo floatability test indicated non adherence to the gastric mucosa and tablets remain buoyant for more than 24 h.

CONCLUSIONS

Study showed these eco-friendly natural gums can be considered as promising SR polymers.

摘要

背景

本研究的目的是展示天然胶在药物传递系统开发中的潜在用途。因此,在这项工作中,使用 simplex 格子设计,考虑 okra 胶、刺槐豆胶和 HPMC K4M 的浓度作为独立变量,开发了 ziprasidone HCl 的胃滞留片剂制剂。使用响应面图和多元回归方程来评估独立变量对硬度、标志时间、漂浮时间和 1 h、2 h 和 8 h 以及 24 h 的药物释放的影响。还考虑优化制剂的约束和理想性制备了检查点批次,以提高其体外性能。使用 ANOVA 分析结果的显著性,p < 0.05 被认为具有统计学意义。

结果

制剂主要含有刺槐豆胶,发现有利于硬度和漂浮性,但三个变量的综合效应负责药物的持续释放。检查点批次(F8)的体外药物释放数据与 7 次运行中最满意的制剂(F7)相比,发现持续效果更好。n 值介于 0.5 和 1 之间,表明药物释放遵循异常(非菲克)扩散机制,表明这些天然胶具有扩散和侵蚀机制。预测结果与观察到的实验值非常相似,表明设计的准确性。体内漂浮性试验表明,药物不会粘附在胃黏膜上,并且片剂在 24 小时以上保持浮力。

结论

研究表明,这些环保型天然胶可以被认为是有前途的 SR 聚合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cb6/3556007/5cf8b0966113/2008-2231-20-58-1.jpg

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