Formulation Development of an Immediate Release Tablet for Oral Suspension of an Antineoplastic Drug

Abstract

The present experimental work was carried out to formulate and develop a generic formulation for the US market. The formulation entails an immediate release dosage form for a BCS class IV anti-neoplastic agent. The major challenges for formulating this formulation is the low solubility of the drug substance and minimising the oxidative degradation of the drug substance. The first issue of low solubility was addressed by incorporating the drug into an amorphous solid dispersion with a hydrophilic hypromellose. The second issue was addressed by buying a preprocessed drug substance with 2% BHT, for reduction of oxidation. Preliminary studies on the drug product were started with literature search to understand the intricacies of the formulation and the method of analysis. The next step in the process was to characterize the RLD product. Similar excipients as the RLD product were used in the generic drug product development. Preformulation studies were carried out to check the compatibility of the excipients with the drug substance. After obtaining satisfactory preformulation results, development batch trials were conducted. Varied IPQC tests were conducted to obtain an optimized formulation similar to the RLD product. F1 and F2 similarity was done to check the percentage of similarity between the RLD product and the developed product. The drug product successfully passed the accelerated stability studies. The developed drug product is found to be scalable and marketable in the near future.