Asian Journal of Pharmaceutical and Clinical Research Vol.2 Issue 3, July-September 2009
DISSOLUTION ENHANCEMENT OF CARVEDILOL BY USING SURFACTANT AS A COATING MATERIAL
VINAYAK D. KADAM, SURENDRA G.GATTANI, Department of Pharmaceutics, R.C. Patel Institute of Ph’ Education and Research. Shirpur, District Dhule, Maharashtra, India, firstname.lastname@example.org SAGAR D. KADAM, H.K.E’s College of pharmacy, Sedam Road, Gulbarga, Karnataka. India
Carvedilol is a poorly water-soluble oral antihypertensive agent, with problems of variable bioavailability and bio-in equivalence. This work was investigated to develop the carvedilol tablets, allowing fast, reproducible and complete drug dissolution, by using surfactant. The tablets were prepared by wet granulation technique. The prepared tablets were evaluated for thickness, uniformity of weight, hardness, friability, in-vitro disintegration time and in-vitro drug release. The tablets apart from fulfilling all official and other specifications, the Carvedilol dissolution profile from the newly developed tablets was clearly better than those batches without surfactants in the coating. The stability studies conducted as per ICH guidelines at 40°±2° and 75%±5% RH showed insignificant loss in drug content and on physical evaluations at the end of three months. So many techniques are available for the solubility enhancement such as micronization, spray drying, and complex formation. Some drugs such as carvedilol, zolpidem tartarate may show change in polymorphism by using above techniques. The purpose of the research was to increase the solubility of carvedilol by adding the surfactants in coating without changing its polymorph so as to develop an immediate release formulation. The study shows that the use of 3 % surfactant increases the dissolution rate up to 12 % in first 20 minutes in pH 6.8 Phosphate buffer, USP II, 50 rpm. Thus by incorporating the surfactants like tween 80, we can enhance the solubility of low solubility drugs.
KEY WORDS Antihypertensive, surfactant, tablet coating.
Carvedilol is an alpha and a beta adrenoreceptor-blocking agent used in the treatment of various cardiovascular disorders such as angina pectoris, cardiac arrhythmia and hypertension1. Carvedilol is indicated for the treatment of mild to severe chronic heart failure, Left ventricular dysfunction following myocardial infraction in clinically stable patients and hypertension. Carvedilol is a poorly water-soluble oral antihypertensive agent, with problems of variable bioavailability and bio-inequivalence related to its poor water-solubility. Its biological half-life (2.2 hours) is very short and it is 90% absorbed from GIT. Earlier
In this work an attempt has been made to increase the dissolution of the carvedilol
tablets which ultimately increases the bioavailability, also to give the benefits in terms of patient compliance, rapid onset of action, low side effect and good stability which make these tablets popular as a dosage form for the treatment of hypertension.
MATERIAL AND METHODS
Carvedilol was procured from Zentiva; (Germany), povidone is taken as a gift sample from Cipla ltd. (kurkumbh), lactose
collidal silicon dioxide from Degussa (Bombay), polyplasdone INF 10 and magnesium stearate from Mallinckrodt and tween 80 were obtained as gift samples from Wockhardt R & D (Aurangabad). The rest of the chemical of analytical grade were supplied by S. D. fine