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首页> 外文期刊>Journal of Young Pharmacists >Preparation and in vitro Evaluation of Ethylcellulose Coated Egg Albumin Microspheres of Diltiazem Hydrochloride
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Preparation and in vitro Evaluation of Ethylcellulose Coated Egg Albumin Microspheres of Diltiazem Hydrochloride

机译：盐酸地尔硫ze的乙基纤维素包膜蛋清微球的制备及体外评价

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The aim of the present investigation was to develop sustained release ethylcellulose-coated egg albumin microspheres of diltiazem hydrochloride (DH) to improve patient compliance. The microspheres were prepared by the w/o emulsion thermal cross-linking method using different proportion of the polymer to drug ratio (1.0:1.0, 1.0:1.5 and 1.0:2.0). A 32 full factorial design was employed to optimize two independent variables, polymer to drug ratio (X1) and surfactant concentration (X2) on dependent variables, namely % drug loading, % drug release in 60 min (Y60) and the time required for 80 % drug release (t80) were selected as dependable variable. Optimized formulation was compared to its sustained release tablet available in market. The polymer to drug ratio was optimized to 1:1 at which a high drug entrapment efficiency 79.20% 6 0.7% and the geometric mean diameter 47.30 6 1.5 mm were found. All batches showed a biphasic release pattern; initial burst release effect (55% DH in 1 h) and then were released completely within 6 h. In situ coating of optimized egg albumin DH microspheres using 7.5% ethylcellulose significantly reduced the burst effect and provided a slow release of DH for 8-10 h. Finally, it was concluded that ethylcellulose-coated egg albumin DH microspheres is suitable for oral SR devices in the treatment of angina pectoris, cardiac arrhythmias, and hypertension due to their size and release profile.
机译：本研究的目的是开发缓释盐酸地尔硫卓（DH）的乙基纤维素包衣的蛋清蛋白微球，以改善患者的依从性。通过w / o乳液热交联法使用不同比例的聚合物与药物的比例（1.0：1.0、1.0：1.5和1.0：2.0）制备微球。采用3 2 全因子设计来优化两个独立变量，即聚合物与药物的比例（X 1 ）和表面活性剂浓度（X 2 ）根据相关变量，即载药量百分比，60分钟内的药物释放百分比（Y 60 ）和80％药物释放所需的时间（t 80 ）作为可靠变量变量。将优化配方与其市售的缓释片剂进行比较。将聚合物与药物的比例优化为1：1，在该比例下，发现较高的药物截留效率79.20％6 0.7％和几何平均直径47.30 6 1.5 mm。所有批次均显示出双相释放模式;最初的爆发释放效果（1小时内55％的DH），然后在6小时内完全释放。使用7.5％乙基纤维素原位包被的优化蛋清蛋白DH微球可显着降低破裂效应，并在8-10小时内缓慢释放DH。最后，得出的结论是，由于乙基纤维素包被的卵清蛋白DH微球的大小和释放特性，它们适用于口服SR装置治疗心绞痛，心律不齐和高血压。

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