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用于控释给药的加蓬油桃木(欧文氏油桃木)(奥罗克)保形物聚合物基质系统。

Irvingia gabonensis (O'Rorke) Bail polymer matrix system for controlled drug delivery.

作者信息

Patani Bernard O, Akin-Ajani Olufunke Dorothy, Kumaran Arul, Odeku Oluwatoyin Adepeju

机构信息

Department of Pharmaceutics and Industrial Pharmacy, University of Ibadan, Nigeria.

KTN College of Pharmacy, Kerala, India.

出版信息

Polim Med. 2022 Jul-Dec;52(2):67-76. doi: 10.17219/pim/153521.

Abstract

BACKGROUND

Irvingia gabonensis kernel polymer has gained attention in drug delivery systems because of its compatibility and degradation under natural and physiological conditions.

OBJECTIVES

This study aimed to evaluate Irvingia gabonensis polymer as a matrix system for the controlled delivery of ibuprofen in comparison to xanthan gum and hydroxypropylmethylcellulose (HPMC).

MATERIAL AND METHODS

Irvingia gabonensis polymer was extracted using established methods and dried using the ovenand freeze-drying methods. Ibuprofen tablets were prepared by direct compression and the effects of polymer concentration (10-50%), excipients (lactose, microcrystalline cellulose and dicalcium phosphate dihydrate) and polymers (xanthan gum and HPMC) on the mechanical and drug release properties of the tablets were evaluated. Density measurements and the Heckel and Kawakita equations were used to determine the compression properties of the tablets. Friability, crushing strength and the crushing strength-friability ratio (CSFR) were used to evaluate the mechanical properties of the tablets, while dissolution times were used to evaluate drug release from the matrices. The drug release mechanisms were determined by fitting the dissolution data into classic kinetic equations.

RESULTS

Irvingia gabonensis polymer deformed plastically with a fast onset and a high amount of plastic deformation compared with xanthan gum and HPMC. This polymer was directly compressible and formed intact non-disintegrating tablets; the mechanical and dissolution properties of Irvingia gabonensis polymer tablets generally decreased with increasing concentration of ibuprofen. The ranking of dissolution times was xanthan gum > freeze-dried Irvingia gabonensis > HPMC > oven-dried Irvingia gabonensis. The addition of the excipients improved the mechanical properties of the tablets, aided ibuprofen release, and altered the release kinetics, which was largely defined by the Korsmeyer-Peppas model. Increasing the proportion of xanthan gum and HPMC in the matrices resulted in a decreased amount of ibuprofen released after 9 h, with xanthan gum having a greater effect.

CONCLUSIONS

Irvingia gabonensis polymer matrices may be effective in the preparation of controlled release tablets, and their right combination with xanthan gum or HPMC could provide a time-independent release for longer durations.

摘要

背景

加蓬腰果树仁聚合物因其在自然和生理条件下的相容性及降解性,在药物递送系统中受到关注。

目的

本研究旨在评估加蓬腰果树聚合物作为布洛芬控释基质系统的效果,并与黄原胶和羟丙基甲基纤维素(HPMC)进行比较。

材料与方法

采用既定方法提取加蓬腰果树聚合物,并通过烘箱干燥法和冷冻干燥法进行干燥。通过直接压片制备布洛芬片剂,评估聚合物浓度(10 - 50%)、辅料(乳糖、微晶纤维素和二水磷酸氢钙)以及聚合物(黄原胶和HPMC)对片剂机械性能和药物释放性能的影响。使用密度测量以及Heckel和Kawakita方程来确定片剂的压缩性能。通过脆碎度、抗压强度和抗压强度 - 脆碎度比(CSFR)评估片剂的机械性能,同时使用溶出时间评估药物从基质中的释放情况。通过将溶出数据拟合到经典动力学方程来确定药物释放机制。

结果

与黄原胶和HPMC相比,加蓬腰果树聚合物发生塑性变形,起始迅速且塑性变形量大。这种聚合物可直接压片并形成完整不崩解的片剂;加蓬腰果树聚合物片剂的机械性能和溶出性能通常随布洛芬浓度的增加而降低。溶出时间排序为:黄原胶>冷冻干燥的加蓬腰果树聚合物>HPMC>烘箱干燥的加蓬腰果树聚合物。辅料的添加改善了片剂的机械性能,有助于布洛芬释放,并改变了释放动力学,这在很大程度上由Korsmeyer - Peppas模型定义。增加基质中黄原胶和HPMC的比例会导致9小时后布洛芬释放量减少,其中黄原胶的影响更大。

结论

加蓬腰果树聚合物基质在制备控释片剂方面可能有效,其与黄原胶或HPMC的合理组合可为更长时间提供与时间无关的释放。

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