Etodolac

ABSTRACTEtodolac is used for the management of rheumatoid osteoarthritis. The site of absorption of Etodolac is in the whole GI tract and has a long half-life of 7± 4 hrs. The aim of the study was to develop colon targeted compression coated tablets of Etodolac using HPMC as swellable, time-controlled polymer, Eudragit S 100 as a coating polymer guar gum and chitosan as carriers in the treatment of Osteoarthritis. All the formulations (F1 to F5) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Etodolac released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F3 released 95.24% of Etodolac. The results of the study showed that formulation F3 is most likely to provide targeting of Etodolac for local action in the colon owing to its minimal release of the drug in the first 5 h. The most satisfactory formulation was stable during stability studies conducted for 60 days as per ICH guidelines. It showed no significant changes in the physicochemical parameters, in vitro release pattern. The studies confirmed that, the designed formulation could be used potentially for colon delivery by controlling drug release in stomach and the small intestine.Keywords: Etodolac, rheumatoid osteoarthritis, HPMC and colon targeted.    

The development of an immediate release (IR) dosage form can minimize the problems associated with controlled release systems of etodolac tablets with its higher ability to release drug into blood circulation, increased bioavailability and patient acceptability. In the present study, an effort has made to formulate and evaluate an immediate release etodolac tablet works against the rheumatoid arthritis and human prostate cancer. These immediate release etodolac tablets were prepared by wet granulation process. Eighteen formulation trials were taken to optimize the final formula. From these, formulation F18 have been optimized as a final formulation. Pre-formulation studies were evaluated to measure the flow properties of pre-compressed powder blend of formulations. Then, post-compression studies include weight variation, thickness, hardness were conducted to evaluate the physical parameters of the final formulation. In vitro drug release studies were conducted to know the intrinsic drug releasing ability of etodolac tablets in dissolution medium. In addition, IR etodolac tablets shown a good stability profile. All results from pre and post-formulation studies were within the acceptable limits which are prescribed by USP. These results suggesting that optimized F18 was a stable formulation, suitable for preparation of immediate release etodolac tablet and also has good dissolution profile with that of innovator product.

The objective of the current study was to design and optimize Etodolac loaded Eudragit RS 100 microcapsules using solvent evaporation method. Quality by design approach was implemented for development of Etodolac microcapsules using I-Optimal RSM design. Based on initial risk assessment and preliminary study, two independent variables, Drug: Eudragit RS 100 ratio and stirring speed were selected for Design of Experimentation (DoE) to see effect on critical quality attributes (CQAs); entrapment efficiency and particle size. The prepared Etodolac loaded Eudragit RS 100 microcapsules were characterized for particle size, entrapment efficiency, in-vitro dissolution study, DSC, XRD and SEM. Acceptance criteria for CQAs were considered as particle size in the range of 22-200 µm and entrapment efficiency in the range of 72.86-97.25 %, which generated the design space with combination of selected critical parameters leading to the acceptable operating ranges for formulating microcapsules with respect to desired Target Quality Product Profile (TQPP). The obtained Etodolac loaded Eudragit RS 100 microcapsules were spherical in shape, having better entrapment efficiency and sustained drug release profile. Validation of model was carried out by comparing experimental values with predicted value of optimized formulation. Optimized formulations within design space were capable of sustaining drug release for about 22 hours and were expected to reduce dosing frequency thus reducing side effects associated with therapy.

Etodolac is a non steroidal anti-inflammatory drug. it is an inhibitor of cycloxygenase which belongs to the pyranocarboxylic acid group. Which is effective in treating fever, pain, and inflammation in the body. which is degraded in stomach .Thus, the purpose of the study is to formulate a dosage form which is coated by coating polymer(s) which passed the acidic medium and exhibit significant effect in intestine. An attempt was made to formulate microspheres with two coating polymers: HPMC & Ethyl Cellulose as well as using of floating properties of polymers will release drug in controlled manner. Thus, these different type of microspheres was characterized in terms of Particles size, buoyancy study, Entrapment efficiency and In-vitro studies.