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一种新型协同半乳甘露聚糖单位剂型,用于阿卡波糖的缓释。

A novel synergistic galactomannan-based unit dosage form for sustained release of acarbose.

机构信息

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

AAPS PharmSciTech. 2012 Mar;13(1):262-75. doi: 10.1208/s12249-011-9724-9. Epub 2012 Jan 11.

Abstract

In the current study, the potential of a novel combination of a galactomannan with acarbose (100 mg) was evaluated for attaining a desired hypoglycaemic effect over a prolonged period of time. Three major antidiabetic galactomannans viz., fenugreek gum, Boswellia gum, and locust bean gum were selected in order to achieve a synergistic effect in the treatment along with retardation in drug release. In vitro studies indicated that batches containing various proportions of fenugreek gum (AF40-60) were able to control drug release for a longer duration of approximately 10-12 h. In contrast, the matrices prepared using Boswellia and locust bean gum were able to sustain the release for relatively shorter durations. Drug release mainly followed first-order release kinetics owing to the highly soluble nature of the drug. In vivo study depicted a significant reduction (p < 0.001) in the postprandial blood glucose and triglyceride levels in the diabetic rats on treatment with formulation AF40. Thus, the developed system provides a better control of the postprandial glycaemic levels and it also obviates the need of conventional multiple dosing of acarbose. Furthermore, it also reduces the occurrence of side effects like diarrhea and loss of appetite.

摘要

在当前的研究中,评估了一种新型半乳甘露聚糖与阿卡波糖(100mg)联合使用的潜力,以在较长时间内达到所需的降血糖效果。选择了三种主要的抗糖尿病半乳甘露聚糖,即葫芦巴胶、乳香胶和槐豆胶,以在治疗中达到协同作用,并延缓药物释放。体外研究表明,含有不同比例葫芦巴胶(AF40-60)的批次能够控制药物释放更长时间,约为 10-12 小时。相比之下,使用乳香胶和槐豆胶制备的基质能够维持相对较短的释放时间。药物释放主要遵循一级释放动力学,这是由于药物具有高度的可溶性。体内研究表明,在糖尿病大鼠中,用制剂 AF40 治疗后,餐后血糖和甘油三酯水平显著降低(p<0.001)。因此,开发的系统提供了更好的餐后血糖控制,并且避免了阿卡波糖常规多次给药的需要。此外,它还减少了腹泻和食欲不振等副作用的发生。

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