Abstract

STUDIES ON THE DESIGN OF ORAL CONTROLLED RELEASE DRUG DELIVERY SYSTEMS OF WATER SOLUBLE AMBROXOL HYDROCHLORIDE EMPLOYING GELUCIRES

Sambasivarao A.*

ABSTRACT

Ambroxol Hcl is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. The objective of the present research work was to develop controlled release matrix tablets of Ambroxol by melt granulation technique using different grades and at different concentration of meltable polmers such as gelicuire 54/02,50/13 and 43/01 and semi hydroxyl propyl methyl cellulose (HPMC-K100M). The prepared formulations were evaluated for physical characterization, hardness, friability, weight variation, drug content uniformity, dissolution studies. The results indicated that the controlled release tablets formulation (F16) with Drug: gelicuire 54/02) at a ratio of 1: 3 and lactose as diluent could be suitable for extending the drug release up to 12 hrs. In-vitro drug release kinetics evaluated using the linear regression method was found to follow the zero order release, Higuchi, Korsemeyer and Peppas model. The stability studies has carried on optimized formulation F16 in 40ºc/75% RH for 6 months,and the stability data is found to be similar with initial data. The drug and excipient interaction was studied by using FTIR and DSC.In vivo studies is conducted for optimized formulation and pjarmacokinetic parameters was found to be Tmax - 3.0hrs ,Cmax - 45ng/ml, T1/2- 12 hrs ,AUC – 95.86ng.h\ml and it has proven that controlled release formulation is able to maintain drug concentration for 24 hrs

Keywords: Ambroxol, HPMC, Matrix, Controlled release, Gelucire, Zero order, Higuchi, Peppas plot.