FORMULATION AND EVALUATION OF NAPROXEN AND L-TRYPTOPHAN COCRYSTAL
The poor solubility and low oral bioavailability of active pharmaceutical ingredients (APIs) pose significant challenges in product development, particularly for drugs classified as Biopharmaceutic Classification System (BCS) Class II. Various strategies have been explored to improve the physicochem...
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| Format: | Final Project |
| Language: | Indonesia |
| Online Access: | https://digilib.itb.ac.id/gdl/view/82660 |
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| Institution: | Institut Teknologi Bandung |
| Language: | Indonesia |
| Summary: | The poor solubility and low oral bioavailability of active pharmaceutical ingredients (APIs) pose significant challenges in product development, particularly for drugs classified as Biopharmaceutic Classification System (BCS) Class II. Various strategies have been explored to improve the physicochemical properties of APIs, one of which is cocrystal formation. Cocrystallization offers a promising approach to enhance the physicochemical properties of drug products, including bioavailability, compactibility, and stability, without altering the pharmacological profile of the API. Naproxen, a nonsteroidal anti-inflammatory drug (NSAID) belonging to BCS Class II, exhibits poor compactibility. This study aims to investigate the formation of naproxen (NPX) cocrystals with L-tryptophan (TRY) and to evaluate their physicochemical properties. NPX-TRY cocrystals were prepared using the slurry method with a 1:1 molar ratio in two different solvents: ethanol and water. Cocrystals were characterized using Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), Fourier Transform Infrared (FTIR), and Differential Scanning Calorimetry (DSC). The solubility, dissolution rate, and compactibility profiles of the cocrystals were evaluated and compared to pure naproxen. PXRD results of cocrystals demonstrated distinct diffraction patterns from its components. DSC thermogram revealed the melting point of NPX-TRY water slurry to be 204,96°C, while the NPX-TRY ethanol slurry exhibited a melting point of 201,99°C. Notably, the solubility of the NPX-TRY ethanol and water slurry increased by 9,52 and 3,06 times, respectively. The intrinsic dissolution test conducted in a pH 7,4 phosphate buffer medium demonstrated a dissolution rate of 0,77 mg cm-2min-1 for NPX-TRY water slurry and 0,59 mg cm-2 min-1 for NPX-TRY ethanol slurry after 45 minutes. However, the compactibility profiles of both cocrystals were improved compared to pure naproxen.
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