ABSTRACT
This study aims to explore the characteristics of crystallization inhibition by cellulose polymers at the supersaturated states of drugs. The study was performed by simulating supersaturated process and preparing supersaturated drug solid, and was carried out by measuring the content of drugs at different time points using dissolution apparatus. The types, amounts, ionic intensity and viscosity of cellulose polymers were examined to assess the crystallization inhibition effect on BCS II class drug indomethacin. HPMC E15 exhibited the strongest crystallization inhibition effect. The more added, more obvious crystallization suppression was observed against indomethacin. The decrease in viscosity and increase in ionic intensity led to an enhanced inhibition. The research provides a scientific guide for the crystallization inhibition of supersaturated drug by cellulose polymers.
ABSTRACT
OBJECTIVE: To explore the characteristics of crystallization inhibition by cellulose polymers against supersaturated drugs. METHODS: The biopharmaceutics classification system(BCS) II class drug indometacin was selected as the model drug.Supersaturated amorphous drug solid was prepared and the solubility of indometacin was measured. The types, added amounts, ionic intensity and viscosity of cellulose polymers were employed as influential factors to assess the crystallization inhibition effect of polymers against indometacin. RESULTS: HPMC E15 displayed the strongest crystallization inhibition effect. The crystallization inhibition was enhanced by adding larger amount of polymers, decreasing the viscosity of polymers and increasing the ionic intensity. CONCLUSION: The study is helpful to clarify the profiles that cellulose polymers inhibit the crystallization of drugs in supersaturated states. This research may provide scientific guide for the practical application of cellulose polymers for drug crystallization.