Study On The Transdermal Therapeutic System For Nitrendipine

Transdermal delivery system is designed to provide controlled continuous therapeutic system of drugs via administration across skin. It is well known as the third generation formulation after oral delivery and injection, because of its avoidance of the toxicity affection of gastrointestinal physiological function, it is deeply welcomed by medical affairs people and sufferers. Especially for some side affection medicals, the use of controlled membrane will get better effect. We choose nitrendipine as the research medicine because it is a 1,4-dihydropyridine derivative calcium channel blocker, is a potent peripheral vasodilator which effectively reduces blood pressure, when given at dosed of 5-20 mg/day. It readily crosses blood brainer. The oral bioavailability is about 15-45% because of the extensive first-pass metabolism in the liver and lipid solubility. The flux of drugs through the skin can be increased with transdermal penetration enhancers. This paper consists of four chapters.Chapter one: The recent progress of transdermal delivery system has been reviewed with the relative references of 59.Chapter two: The permeability percutaneous absorption of nitrendipine cream was studied using modified Franz diffusion cell and isolated rat skin as permeation barrier. The penetration enhancer could obviously enhance the percutaneous permeation of nitrendipine cream and the accumulative permeation quantity of nitrendipine cream containing oleic acid increased remarkably compared with that of mtrendipine cream without enhancer.Chapter three: Nitrendipine film was prepared using two bases (Chinese PVA-1788 and Japanese PVA-124) and compared the differences of the two nitrendipine films at content determination and stability. Its transdermal delivery was studied with Chinese PVA-1788 as base using diffusion equipment and rat skin. The experimental results indicated that the two films had no differences at content determination and stability. Nitrendipine film can be prepared with Chinese polyvinylalcohol (PVA-1788) as base instead of Japanese polyvinyl alcohol (PVA-124). The accumulative permeation quantity of nitrendipine film can be enhanced by glycerin.Chapter four: The permeability of nitrendipine through rat skin in vitro was examined using the self-made Franz diffusion cell. Accumulative permeation quantity (0 and steady percutaneous speed (k1) were determined. Steady percutaneous speed of nitrendipine suspension with glycerol and 1,2-propylene increased 3.73 and 2.62 times, respectively. The percutaneous mechanism of nitrendipine suspension was studied.