Abstract

FORMULATION AND EVALUATION OF FLOATING MICROSPHERE OF BERBERINE HYDROCHLORIDE FOR THE TREATMENT OF RHEUMATOID ARTHRITIS

*Namrata Singh

Abstract

Arthritis a chronic progressive disease characterized by synovial inflammation, autoantibody production, bone and cartilages destruction. In addition to the local lesion occurring in the joints systemic symptoms including cardiovascular, pulmonary, psychological and skeletal disorders are also common in patients with RA. Berberine is considered to be a predominantly selective Jak3 antagonist. Data from kinase assays and protein-compound docking simulation show that berberine blocked Jak3 catalytic activity after binding to the kinase domain of Jak3. Floating microspheres are gastro-retentive drug delivery system based on non-effervescent approach. The floating microsphere alters the absorption of the drug thus enhancing the bioavailability. They prolong the dosing intervals which will allow developing once a day formulation and thereby increasing patient compliance beyond the level of existing dosage form by achieving control over gastric residence time. Berberine with wide range of biological activity possesses low absorption. This was selected for the studies as it is poorly absorbed in the lower GIT and have short elimination half life. The floating microsphere beneficially alters the absorption of the drug and enhancing bioavailability. They prolong the dosing interval which will allow to develop once a day formulation and thereby enhance patient compliance beyond the level of existing dosage forms by achieving the control over gastric residence time. Floating microsphere are gastro retentive drug delivery system based on non effervescent approach. They floats over gastric content for long period of time. As the system floats over the gastric content the drug is released slowly at desired rate resulting in increased gastric retention with reduced fluctuations in plasma drug concentration.

Keywords: Berberine hydrochloride, Floating Microsphere, Rheumatoid Arthritis, HPMC, Tween 80 Etc.