氨氯地平/氯沙坦联合应用胃保留漂浮微球治疗高血压

Rubab Ali, Muhammad Naeem Aamir, Nayab Khalid, Muhammad Bilal
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引用次数: 1

摘要

背景:高血压是影响数百万人的严重全球健康问题之一,如果不及时治疗,将导致心血管损伤。目前已有多种降压药物问世,但单药难以达到较好的降压效果,因此本研究开发了持续有效的联合降压药物。方法:配制苯磺酸氨氯地平和氯沙坦钾胃保留漂浮微球,以增加药物在上胃肠道的滞留时间,最终延长药物释放时间。以乌拉吉特RS100为控释剂。采用溶剂萃取法制备微球。配制微球后,通过FTIR药物和聚合物相容性、尺寸分析和包封效率测试,评估流动性能、浮力(%)、产率、药物释放、表面形貌。利用累积释放数据进行释放动力学研究。结果:在1.2 pH的缓冲液中,所有制剂在12小时内保持浮力。还发现药物从制剂中释放时间延长,表明剂型持续有效。其他结果均令人满意,并发现随着聚合物浓度的增加,配方的包封效率也有所提高。在此基础上,选择药聚合物比为1:1的配方1为最佳配方。结论:胃保留性漂浮微球是延长给药系统释放的最佳途径之一。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan
Background: Hypertension is one of the serious global health issues that affect millions of people and leads to cardiovascular damage if remain untreated. Various antihypertensive drugs have been developed but it is difficult to achieve better control of blood pressure by using mono-therapy so in this research work, combination therapy having sustained effect for the treatment of hypertension was developed. Method: Gastroretentive floating microspheres of amlodipine besylate and losartan potassium were formulated for the purpose of increasing the time of retention of drugs in the upper gastrointestinal tract and ultimately extend drug release. Eudragit RS100 was used as release controlling agent. The method adopted to prepare microspheres was solvent extraction. Formulated microspheres after that tested for assessing flow properties, buoyancy (%), percentage yield, drug release, surface morphology, by FTIR drug and polymer compatibility, size analysis and entrapment efficiency. Release kinetics on cumulative release data were applied. Results: It was observed from the findings that all the formulation remained buoyant in 1.2 pH buffer up to 12 hrs. It was also found that release of drug from formulation was prolonged which indicates sustained effect of dosage form. All the other results were satisfactory and it was also found that entrapment efficiency of formulation increased when concentration of polymer increased. On the basis of results, formulation 1 with 1:1 drug polymer ratio was selected as optimum formulation. Conclusion: It was concluded from the study that gastroretentive floating microspheres could be a one of best approach to extend the release of drug delivery system.
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