STUDY OF EXCIPIENTS AND TEMPERATURE EFFECT ON THE STABILITY OF ARIPIPRAZOLE

• Main Author: Hashina Mailawani, Lani
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/45692
• Institution: Institut Teknologi Bandung

Aripiprazole is an atypical antipsychotic drug that has high polymorphism properties and may develop into some form of crystals with different stability properties. In this study, the effect of excipients addition and temperatures on the stability of aripiprazole will be examined. Stability test was conducted on physical mixtures of aripiprazole:excipients (1:1), stability test utilizing the fractional order randomized block design for mixtures of aripiprazole with all excipients, and stability test of physical mixtures of aripiprazole:excipients (1:1) after heated at 60°C for 24 hours. In the physical mixtures of 1:1, aripiprazole was mixed together with lactose monohydrate (APZ-LM), microcrystalline cellulose (APZ- MS), corn starch (APZ-A), hydroxypropylcellulose (APZ-HS), and magnesium stearate (APZ-M). Stability test was conducted in climatic chambers at 40 o C±2 o C, RH 75%±5% within a specific time period. The aripiprazole concentration remaining in the physical mixture was determined by using high performance liquid chromatography. Identification of crystal thermal profile and changes in crystal internal structure were observed by using a Differential Scanning Calorimeter (DSC) and Powder X-ray Diffractometer (PXRD). The results showed that there were no significance difference between the remaining concentration of pure aripiprazole with its physical mixtures 1:1, except in APZ- HS mixture after 35 days of storage. While the result of the stability test from the mixture of aripiprazole with all excipients using fractional order randomized block experimental design showed that the best formula was mixture of X with the remaining concentration of aripiprazole was 90.84%. This result has no significance different with pure aripiprazole. Furthermore, heating of aripiprazole and its mixtures with excipients 1:1 at 60°C for 24 hours can improved the stability of aripiprazole. During the stability study of 35 days, aripiprazole had been degraded only about 2.20% in comparison with aripiprazole without heating process of 8.30%. Based on examination using DSC, its was found that aripiprazole using in this study was a metastable form with three endothermic peaks at 93.90 o C, 143.73 o C, and 151.83 o C. However, based on examination using PXRD, the result had similarities pattern with aripiprazole form III.