Abstract

FORMULATION, DEVELOPMENT AND OPTIMIZATION OF CAPECITABINE TABLET DOSAGE FORM AND IN VITRO EVALUATION OF PHYSICOCHEMICAL PROPERTIES

Jafrin Jobayer Sonju*, Sultana Razia Shikha and Md. Fokhrul Islam

Abstract

Background: Capecitabine is an antimetabolite type analogue utilized as an antineoplastic agent to treat metastatic and highly developed manifestations of breast and colon cancer, frequently in blend with different other options.[1] Capecitabine is a tumor-enacted antineoplastic operator that fits the novel fluoropyrimidine carbamate class. It was soundly outlined as an orally managed forerunner of 5'- deoxy-5-fluorouridine (5'-DFUR).[2] The present study was carried out to develop and optimize various formulations of Capecitabine tablet dosage forms and characterize the drug's physical, chemical, and mechanical characteristics keeping in mind the end goal to pick what different items (Known as excipients) ought to be utilized as a part of the experiment. Methods: Development of Capecitabine oral tablet dosage form was done using suitable excipients like Ludipress Ph. Grade, Microcrystalline Cellulose USP (Avicel PH 102), Pregelatinized Starch USP, Sodium Starch Glycolate USP, Lactose Spray Dried, Crospovidone USP, Magnesium Stearate USP, Colloidal Anhydrous Silica BP (Aerosil-200), Purified Talc BP. Four different formulations F-1, F-2, F-3, and F-4 were developed among which F-4 showed acceptable results and showed good comparison with reference and marketed products. Results: It was observed that F-4 creates stable tablets with good characteristics. Different parameters of tablet dosage forms like weight variation test, hardness, weight variation test, friability test, disintegration, thickness, and dissolution showed acceptable results. The average hardness of F-4 was 12.7 kp, the average thickness was 5.41 mm, the friability was 0.02%, the disintegration time was 4 minutes 25 seconds and the average dissolution was 93.16%. Reference standard, RS, and market sample, MS showed drug content 505.32 mg and 494.22 mg whereas F-4 showed 501.82 mg. Conclusion: Parameters like thickness, friability, disintegration, and average dissolution showed good results of F-4 compared with the reference standard market sample. Six months of stability studies of F-4 revealed that there was no significant alteration in physical parameters, drug content, and other profiles.

Keywords: Antineoplastic agent, Capecitabine, Breast and colon cancer, Orally administered.