Design, Development and Evaluation of Sumatriptan Succinate Transdermal Patches

نویسندگان

  • Gururaj S. Kulkarni
  • Narasinha Reddy
چکیده

Most of the therapeutic agents are recommended through an oral route, but oral route has disadvantages like first pass metabolism, liver toxicity, etc, due to gastrointestinal pH. This leads poor bioavailability of drugs, which are not stable in G.I pH. To overcome this problem, increase the bioiavailibility, reduce the dose and dose dumping Transdermal delivery system is better option as novel drug delivery system, which bypass the hepatic first pass metabolism, and avoid drug degradation due to systemic absorption of the drug. Minimize plasma level fluctuations and extend the drug activity besides improving patient compliance. Sumatriptan succinate is a selective 5hydroxytryptamine receptor subtype agonist. Sumatriptan succinate is chemically designated as 3-[2-(dimethylamino)ethyl]-N-methyl-indole-5methanesulfonamide succinate. Sumatriptan succinate is a white to off-white powder that is readily soluble in water. Oral administration of Sumatriptan succinate suffers from poorbioavailability, partly due to presystemic metabolismsome of it gets broken down in the stomach and bloodstream before it reaches the target arteries. Sumatriptan is metabolized primarily by monoamine oxidase A into an indole acetic acid analogue, part of which is further conjugated with glucuronic acid. These metabolites excreted in the urine and bile. Only about 3% of the active drug may be recovered unchanged. Because of this the bioavailability is only 15% with half life is 2.5 hrs. In this work, the effort has done to improve bioavailability of the sumatriptan succinate by transdermal patches dosage form by using polymers HPMCK4M, carbopol934 and Dibutylpthalate as used as plasticizers. INTRODUCTION: Transdermal drug delivery systems (TDDS), also known as “patches,” are dosage forms designed to deliver a therapeutically effective amount of drug across a patient’s skin. In order to deliver therapeutic agents through the human skin for systemic effects, the comprehensive morphological, biophysical and physicochemical properties of the skin are to be considered. Transdermal delivery provides a leading edge over injectables and oral routes by increasing patient compliance and avoiding first pass metabolism respectively . Transdermal delivery not only provides controlled, constant administration of the drug, but also allows continuous input of drugs with short biological half-lives and eliminates pulsed entry into

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تاریخ انتشار 2012