Desenvolvimento e caracterização de comprimidos de liberação prolongada contendo cloridrato de atenolol.

Abstract

Systemic arterial hypertension (SAH) is notable as a pathology responsible for premature death. Atenolol is a specific antagonist for beta-1 receptors, widely used for patients with concomitant illnesses such as arterial hypertension associated with one or more of the following pathologies: arrhythmia, angina pectoris, and coronary heart disease. Although the possibility of dose dumping of the drug as well as the gastrointestinal effects by oral immediate release administration reduces obligingness of patients, the current thesis intends to provide an alternative to the immediate release of atenolol, drug delivery systems (DDS) are well established as a way in literature to do a controlled release of drugs reducing side effects, in these system polymers derived from cellulose can be employed to control drug release. Our research group has been developing tablets for different types of releases. Thus, to reduce the side effects of high drug doses, inserting a new form of administration for this more selective and specific drug, maintaining plasma levels of the drug closer to desirable levels and increasing patient adherence to treatment due to the smaller number of drug administrations, this work developed a type of prolonged-release tablet using the cellulose derivatives hydroxypropylmethylcellulose and ethylcellulose in variable ratio between 3:1; 1:1 and 1:3, respectively and the obtained tablets were characterized physicochemically and by pharmacopeial tests. Tablets have undergone physicochemical and pharmacopeial tests that showed a 35%, 14% and 12% water absorption index. The pharmacopeial tests demonstrated compliance of tablets to required legislative characteristics for all the following tests: weight determination, content uniformity, dosage, and in vitro release pallets showed they could release between 87% and 95% of the drug in 24 hours, infrared demonstrated the absence of incompatibilities between the polymers and atenolol, due to specific bands of all of the constituents were present. Thus, the data obtained infers that the developed system using polymers may have potential applications along with use for therapy with reduced dosage and also side effects arising from the conventional formulation, although increase patient adherence to treatment.