含阿司匹林和甘油的新型乳剂治疗缺血性脑卒中的配方开发与评价

Koteswari Poluri, Swetha Tippani, Laxmi Prasanna P, Swapna Saha, A. D., Sana Saneela
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摘要

当部分大脑的血液供应中断或减少,导致脑组织无法获得氧气和营养物质时,就会发生缺血性中风。脑细胞在几分钟内开始死亡。缺血性中风可立即使用抗血小板药物如阿司匹林治疗,可预防血栓形成,促进中风后的康复。甘油也被用于减少缺血性中风的水肿。本研究的目的是开发一种含有阿司匹林的甘油油乳剂的新配方,用于缺血性中风的治疗和体外评估。采用高剪切均质法制备甘油乳状液中的油脂,并对其粒径、药物含量、体外释药及稳定性进行了评价。根据阿司匹林的log P值,选择橄榄油作为油相,用吐温80作为乳化剂。共制备了10种配方f1 ~ F10,其中f1 ~ f6相在24 h内分离,F8 ~ F10相稳定1周后形成膏状,可再分散。通过光学显微镜测定F8、F9和F10的平均粒径分别为6.04、3.38和7.8µm。F8、F9、F10的含量分别为68±3.95%、108±5.816%、103±4.61%。药物释放速度符合一级动力学,并在15分钟内观察到立即爆发释放效应。结果表明,制备出了含阿司匹林的橄榄油甘油乳剂,并对其进行了评价。阿司匹林和甘油联合给药治疗缺血性脑卒中是一种很有前途的配方方法。这些配方在物理和化学上都是稳定的。今后将在合适的动物模型上进行体内应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation Development and Evaluation of a Novel Emulsion Composition Embracing Aspirin and Glycerol in the Treatment of Ischemic Stroke
An ischemic stroke occurs when the blood supply to part of the brain is interrupted or reduced, preventing brain tissue from getting oxygen and nutrients. Brain cells begin to die in minutes. Ischemic stroke can be treated by using Antiplatelet drug such as aspirin as an immediate treatment which may prevent blood clots and improve recovery after stroke. Glycerol is also used as it decreases the edema in ischemic stroke. The aim of the present investigation is to develop a novel formulation of oil in Glycerol emulsion comprising aspirin in the treatment of ischemic stroke and in vitro evaluation. The oil in glycerol emulsion was prepared by high shear homogenization and prepared emulsions were evaluated for particle size, drug content, in vitro drug release and stability. Based on log P values of aspirin, olive oil is selected as oil phase and tween 80 was used as emulsifying agent. Total 10 formulations F1to F10 were prepared and among these, in F1-F6 phase separation was observed within 24 hrs whereas F8 to F10 were stable for one week and later creaming was observed and it is re-dispersible. The particle size was determined by optical microscopy and the average particle size for F8, F9 and F10 were 6.04, 3.38 and 7.8 µm respectively. Drug content was determined as 68±3.95%,108±5.816%, 103±4.61% respectively in compositions F8, F9 and F10. Rate of drug release followed first order kinetics and an immediate burst release effect was observed within 15 minutes. It is concluded that olive oil and glycerol emulsions containing aspirin is prepared successfully and evaluated. It is a promising formulation approach for co administration of aspirin and glycerol in the treatment of ischemic stroke. The formulations were physically and chemically stable. In vivo application of this formulation will be done in suitable animal models in future.
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