Study On Formulation Technology Of Celecoxib Capsules

Celecoxib is a COX-2 selective nonsteroidal anti-inflammatory drug developed by companies of Pharmacia and Pfizer,which chemical name is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1-hydro-pyrazole-1-yl] benzenesulfonamide.Celecoxib has a unique mechanism,it is a highly selective reversible inhibitor of the COX-2 isoform of cyclooxygenase,celecoxib inhibits the transformation of arachidonic acid to prostaglandin precursors.Celecoxib is used for osteoarthritis(OA),rheumatoid arthritis(RA),acute pain(AP),musculoskeletal pain,painful menstruation,ankylosing spondylitis,and to reduce the number of colon and rectal polyps in people with familial adenomatous polyposis.Celecoxib is the only oral dosage form selective COX-2 inhibitor in China.It has been widely used since its listing in the United States in February 1999.In September 2000,the State Food and Drug Administration approved Pfizer's Celebrex(Celciclos Capsule)imported and packaged in China with a specification of 0.1 and 0.2 g.According to the information of the original research,we have investigated the dosage and processing condition of the raw materials of Celecoxib Capsule,such as Lactose monohydrate lactose,croscarmellose sodium,povidone K30,sodium lauryl sulfate,stearic acid.We have study on granulation method,mixing time,drying temperature,particle moisture and moisture absorption in the production process.The dissolution rate of celecoxib capsules was taken as the main indicator,and the particle flowability and appearance were used as reference indicators to carry out conduct accelerated tests and long-term tests.By studying the prescription optimization and production process of celecoxib capsule generics,and the final product quality was consistent with the original product.The optimized prescription was composed of celecoxib 200 mg,lactose monohydrate 51.1 mg,sodium dodecyl sulfate 8.1 mg,sodium carboxymethyl cellulose 5.4 mg,povidone K30 2.7 mg,magnesium stearate 2.7 mg.In vitro dissolution of celecoxib capsules prepared by the prescription and the process is well,the quality of the finished product is stable,meeting the standard.Production process of Celecoxib capsules is simple and feasible,and suit for industrialization.