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双胍类抗糖尿病药物新型脉冲给药系统的设计与表征

Design and characterization of novel pulsatile delivery system of biguanide antidiabetic drug.

作者信息

Pandey Rahul, Selvamurthy William

机构信息

Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India.

出版信息

J Pharm Bioallied Sci. 2020 Jul-Sep;12(3):356-368. doi: 10.4103/jpbs.JPBS_203_19. Epub 2020 Jul 18.

DOI:10.4103/jpbs.JPBS_203_19
PMID:33100797
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7574743/
Abstract

AIM

This work shows the development of pulsatile capsular pellets of metformin hydrochloride and its characterisation.

MATERIAL AND METHODS

The novel drug delivery system consisted of hydroxy propyl cellulose Type H. It has a lag time modifier and Eudragit L-100 and Eudragit S-100 in different concentrations as pH-dependent release modifier in the gastrointestinal tract. The pellets were subjected to release studies using USP dissolution apparatus type-II in distilled water, phosphate buffer of pH 6.8, and 0.1 N HCl and methanol. Ultraviolet (UV), infrared (IR), high-performance liquid chromatography (HPLC), and mass spectroscopy were performed for active pharmaceutical ingredients and formulations.

RESULT

The study was characterized by the complete release of the drug in pulses after a well-defined lag time of 6 h (±0.20) (period of no drug release) for the treatment of type II diabetes mellitus.

CONCLUSION

The stability studies on the selected formulation of Metformin were found to be stable, with shelf life of 1.94 years. Hence it may be concluded that the newly formulated pulsatile drug delivery systems of Metformin Hydrochloride, when ingested at the bed time in the night, produce effective control of the increased blood glucose level after intake of meals by allowing the drug to release after a lag time of 6 h (after meals).

摘要

目的

本研究展示了盐酸二甲双胍脉冲型胶囊微丸的研发及其特性。

材料与方法

新型药物递送系统由H型羟丙基纤维素组成。它具有滞后时间调节剂以及不同浓度的Eudragit L - 100和Eudragit S - 100作为胃肠道pH依赖型释放调节剂。使用美国药典II型溶出装置，在蒸馏水、pH 6.8的磷酸盐缓冲液、0.1 N盐酸和甲醇中对微丸进行释放研究。对活性药物成分和制剂进行了紫外（UV）、红外（IR）、高效液相色谱（HPLC）和质谱分析。

结果

该研究的特点是在明确的6小时（±0.20）滞后时间（无药物释放期）后，药物以脉冲形式完全释放，用于治疗II型糖尿病。

结论

所选二甲双胍制剂的稳定性研究表明其稳定，保质期为1.94年。因此可以得出结论，新配制的盐酸二甲双胍脉冲型药物递送系统，在夜间就寝时服用，通过使药物在6小时滞后时间（餐后）后释放，能够有效控制餐后血糖水平升高。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/c471da4b726c/JPBS-12-356-g018.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/c471da4b726c/JPBS-12-356-g018.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/f1924d9e1a00/JPBS-12-356-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/ab6f71d264e5/JPBS-12-356-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/f315efcc4fa2/JPBS-12-356-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/afd514642597/JPBS-12-356-g015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/218a5db9f4bf/JPBS-12-356-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/88f136975709/JPBS-12-356-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55fa/7574743/c471da4b726c/JPBS-12-356-g018.jpg

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