Preparation And Quality Study Of Poor Soluble Celecoxib Capsule

Celecoxib is a kind of non-steroidal anti-inflammatory drugs(NSAIDs),and also is a kind of selective cycloxygenase-2(cox-2)inhibitor.In clinical,it is mainly used for osteoarthritis and rheumatoid arthritis,and also be used for the peripheral and central analgesia. Compared with the traditional non-steroidal anti-inflammatory drugs,the gastrointestinal adverse reactions of celecoxib is lighter.But celecoxib has low solubility,which can affect its absorption in body. To increase the absorption of celecoxib in the human body, this paper carried out the study of improving the solubility of celecoxib. Established the mature prescription and processes of celecoxib capsule that are safe,effective and stable.Objective:To obtain the prescription and processes which can product celecoxib capsule smoothly by experiments. The prescription and processes of celecoxib capsule should be stable and controllable,and can product the same qualitied celecoxib capsule with reference preparations.Method:To improve the solubility of celecoxib,the grinding process is used to reducing the particle size.In order to select the amount of excipients and process parameters,processes and quality of reference preparations were analyzed and the dissolution profiles of reference preparations were used as indicators. In the experiment, select the same kind of excipients with reference preparations and do compatibility tests of celecoxib and excipients. Then ultimately determine the amount of each excipients in the formulation by dissolution test at 45 min in p H1.0 dissolution medium. Based on the imported drug registration standard of celecoxib capsule(Celebrex) and the preparation,establish a quality standard of celecoxib capsules. Related method validations were carried out respectively.In the processes study,parameters of wet mixing granulator speed, premixed time, screen aperture, drying temperature,mixing speed,mixing time and capsule filling speed were investigated.Then Set the final preparation.Make three batches of amplification test by using the final preparation.Finally,compare the quality and dissolution profiles of reference preparations with the samples. Study stability of the samples.Result:The quality standard of celecoxib capsule was established. The method validation of contents,impurity species and dissolution were carried out,and the results were in line with provisions.The process of amplification testes is smooth,stable,controlled and easy to operate and the samples are consistent with the quality standards of celecoxib capsules.The test results show that the contents,impurity species and dissolution of homemade samples are similar to the reference preparations.And homemade samples have the similar dissolution profiles with reference preparations in all of the dissolution medium including the p H1.0 hydrochloric acid solution with 1% SLS,the p H4.5 acetate buffer solution with 1% SLS,the p H6.8 phosphate buffer solution with 1% SLS,the water with 1% SLS and the p H12 phosphate buffer solution with 1% SLS. All of f2 values are greater than 50.Stress testing results show that the quality of product has no significant change in the condition of strong light and high temperature. But in the condition of high humidity, the dissolution decreased slightly. Place the product under accelerated test conditions for 6 months,in addition to a slight dissolution decrease,other inspection items are not changed significantly. Place the product under long-term test conditions for 9 months,in addition to a slight dissolution decrease,other inspection items are not changed significantly.Conclusion:With this prescription and processes,we can product qualified celecoxib capsule with good stability. The preparation is practical,simple,and easy to control.