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治疗高血压的洛沙坦透皮系统的药效学。

Pharmacodynamics of a losartan transdermal system for the treatment of hypertension.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

出版信息

Drug Dev Ind Pharm. 2010 Apr;36(4):385-92. doi: 10.3109/03639040903188471.

DOI:10.3109/03639040903188471
PMID:20205600
Abstract

AIMS

Transdermal therapeutic systems were developed using the polymers, Eudragit E 100 and polyvinyl pyrrolidone VA 64 in a film casting assembly. The medicated films were evaluated for physical properties, in vitro drug release studies, in vitro skin permeation studies, and pharmacodynamic studies.

RESULTS

The physical parameters were found to be very satisfactory with high drug content (>99%). The in vitro drug release studies were performed using paddle-over-disc assembly specified in USP XXIII. The pharmacodynamic studies were carried out using tail cuff method in Wistar albino rats. Hypertension was induced by methyl prednisolone acetate subcutaneously for 2 weeks. The developed matrix patch was found to decrease the blood pressure (25.42% reduction in mean systolic blood pressure of rats) significantly (P < 0.001) in proximity of the normal value and it was maintained for 24 hours.

CONCLUSION

It can be concluded that the developed transdermal matrix patch holds promise for the management of hypertension that needs to be validated by clinical trials.

摘要

目的

采用聚合物 Eudragit E 100 和聚乙烯吡咯烷酮 VA 64 制成涂膜组件,开发经皮治疗系统。对含药膜进行物理性质、体外药物释放研究、体外皮肤渗透研究和药效学研究评估。

结果

药物含量(>99%)非常高,物理参数非常令人满意。体外药物释放研究采用 USP XXIII 规定的桨碟装置进行。药效学研究采用 Wistar 白化大鼠尾套法进行。通过皮下注射醋酸甲泼尼龙诱导高血压 2 周。所开发的基质贴剂显著降低血压(大鼠收缩压平均降低 25.42%)(P <0.001),接近正常值,并维持 24 小时。

结论

可以得出结论,所开发的经皮基质贴剂有望用于高血压的管理,需要通过临床试验进行验证。

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