The Study And Evaluation On Formulation And Technique Of Gefitinib Tablets

Gefitinib is a targeting anticancer drug which was developed by Astra Zeneca. It can be dosed to cure advanced or metastatic non small cell lung cancer(NSCLC) which had been treated by chemotherapy. Gefitinib is effective in curing NSCLC. However, it is expensive. Hence, this study is to develop a mimic preparation of gefitinib tablets for those in need. The main contents and results of the study are as follows:1. The quality control of gefitinib tablets. The degradation products of gefitinib were traced by stressing test. Then the oxidative impurity was synthetised, its qualitatively and quantitatively determination were carried out. The detecting method of impurities in gefitinib tablets was established by investgating the proportion of mobile phase and the p H of aqueous phase.2. The formulation and technique of gefitinib tablets. Excipients were selected by excipients compatibility experiment, and the methods of determining the content and dissolution of gefitinib tablets were established. According to the dissolution curves, the property of drug and dosage of excipients were investigated to determine the formulation as follows: 250 mg of gefitinib, 106 mg of diluents, 100 mg of diluents, 30 mg of disintegrants, 9mg of binders, 5mg of lubricants, and the coating weight of 3%. The dissolution profiles of magnifying samples were in consistent with that of the original preparation under four dissolution media.3. The stability of gefitinib tablets. According to the draft of quality standard, the stability of mimic preparation was investigated under stress testing, accelareted test and long-term test. The results showed that the mimic preparation was of good stability, and corresponded to the original preparation.Above all, the formulation and technique of gefitinib tablets was stable and reliable so that it could be a basic for the commercial process of mimic preparation of gefinib tablets.