The Study On Preparation Of Cerdinir Capsules And Improvement Of Its Dissolution

Cefdinir, a third generation of semi-synthetic broad-spectrum oral antibiotics, which was developed by fujisawa strain. It has not only kept a high stability toβ-lactamase,but also compensated the third generation of cephalosporins'weak fuction to the Gram-positive bacterial. It has a strong role of killing both gram negative and gram positive bacterium. Especially for the most stableβ-lactamases, the clinical effect is remarkable. Cefdinir is widely used in surgery, dermatology, obstetrics and gynecology, urology and other infections caused by sensitive bacteria. A large number of clinical trials showed that Cefdinir is an efficient, safe and convenient oral third-generation cephalosporins antibiotics.Three kinds of fomulations were approved by State Food and Drug Administration (SFDA), such as granules, capsules and dispersible tablets. Only capsules was collected by the 2010 edition of Chinese Pharmacopoeia(ChP) So this study is to prepare to meet standards of cefdinir capsules and compare with the quality of commercial reference preparations. In addition, analysising of the factors that affect the dissolution of pharmaceutical and selecting sutible materials from the point of prescription to improve the solid preparation of insoluble drug dissolution were studied.The study before prescriptions were mainly refered the powder properties of raw matierial. And a high performance liquid chromatography(HPLC) method for the determination of cefdinir capsules and related substances was established. UV spectrophotometry can determin the dissolution of Cefdinir capsules. Testing the drugs according such methods, the content and ralad substances of Cefdinir raw materials can meet ChP2010, so as the dissolution of commercial reference preparation.The prescription was based on the information of original comapany of Japan. We set the appearance of contents, liquitity and dissolution as the main indexes to evaluate the prescription and technology. The results showed that prscription and technology were reasonable,and different batches of raw material and excipents wre not the same. So their source should be consistened with the original research.The request of Cefinir capsules which recorded by ChP2010 was referd. We made a comparative study of quality between testing product and refered product, and selected the f2 factor method for its dissolution profile similarity assessment. It showed that both are qualified.The factors which affect the dissolution of insoluble drug were analysised. And selecting sutible materials to improve the solid preparation of insoluble drug dissolution were studied. Other common pharmaceutical exipients were tested to improve the dissolution of cefinir. Carboxymethylstarch sodium(CMS-Na) and cross-linked polyvinylpyrrolidone and dry starch could not replace low-substituted hydroxypropyl cellulose(L-HPC), sodium dodecyl sulfate(SDS) is equal with polyoxyl (40) stearate(S-40), and magnesium stearate could be replaced by silicon dioxide.In addition, study found that silicon dioxide was used as flow agent in a low dose, and it had the effect of dispersion and adorption in a large dosage to improve the dissolution of cefdinir. However, when the silicon dioxide with excessive liquidity, the liquidity was reduced. Cefdinir capsules with different size of crude drug, micronized drugs hindered the dissolution, but in the granules it showed a trend that the smaller particle size, the faster it dissoluted.