Study on Transdermal Delivery of Nicardipine Hydrochloride from Microemulsions

• Main Authors: Yei-Huan Lin, 林怡慧
• Other Authors: none
• Format: Others
• Language: zh-TW
• Published: 2005
• Online Access: http://ndltd.ncl.edu.tw/handle/15249089087017889836

碩士 === 高雄醫學大學 === 藥學研究所碩士班 === 93 === Nicardipine hydrochloride, a calcium channel blocker with dihydropyridine structure, is widely used in the clinical treatment of hypertension and angina pectoris. Although it is rapidly absorbed after oral administration, it undergoes extensive first-pass elimination in the liver. Therefore, it is suitable for developing the transdermal delivery system. In this study, we have developed a microemulsion system consisted of Tween 80, Tween 20, Span 80, and Span 20 as surfactant phase, isopropyl myristate as oil phase, doubled-distilled water as aqueous phase, and ethanol as co-surfactant phase for transdermal delivery of nicardipine. According to the result of solubility test, it proved that microemulsion system has the ability to elevate the drug solubility of formulation. The droplet size of microemulsion formulations was below 150 nm, and the polydispersity index was around 0.2. Most of these microemulsion formulations belonged to water-in-oil type, except for the formulation D5-3, D6-31, D7-31, D8-31 and D9-31. The in vitro permeation data indicated that the main affecting factor on flux was the increase of drug content of the microemulsion formulation. And the effect of microemulsion formulation on permeation depended upon the properties of formulation itself, especially the stability of formulation and its solubility of drug. Besides, the use of enhancer did not show much effect on permeation. In most cases, it contrarily caused the decrease of drug release, which may be concerned with the competitive release mechanism. The in vivo study result showed that the pharmacokinetic data conformed to the two-compartment model. Transderaml administration of these formulations could maintain a constant plasma concentration through a sustained drug release. In addition, the results measured by colorimeter exhibited that microemulsion formulations didn’t cause obvious skin irritation.