| Autor: |
Swati C. Jagdale, Ajay S. Bhadoriya, Aniruddha R. Chabukswar |
| Jazyk: |
angličtina |
| Rok vydání: |
2012 |
| Předmět: |
|
| Zdroj: |
Revista de Ciências Farmacêuticas Básica e Aplicada, Vol 33, Iss 1, Pp 83-94 (2012) |
| Druh dokumentu: |
article |
| ISSN: |
1808-4532 |
| Popis: |
Clonazepam (CLZ) is an anticonvulsant benzodiazepine widely used in the treatment of epilepsy. CLZ is a BCS Class II drug and its bioavailability is thus dissolution limited. The objective of the present study was to prepare solid dispersions (SDs) of CLZ by various techniques, using the amphiphilic carrier Gelucire 50/13 in various proportions, to increase its water solubility. Drug-polymer interactions were investigated by Fourier-transform infrared (FTIR) and UltraViolet (UV) spectroscopy. The SDs were characterized physically by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). A phase solubility study was performed and the stability constant (Ks) was found to be 275.27, while the negative Gibbs free energy (ΔGo tr) indicated spontaneous solubilization of the drug. The dissolution study showed that the SDs considerably enhanced the dissolution rate of the drug. The FTIR and UV spectra revealed no chemical incompatibility between the drug and Gelucire 50/13. XRD patterns and the DSC profiles indicated the CLZ was in the amorphous form, which explains the improved dissolution rate of the drug from its SDs. Finally, mouth dissolving tablets (MDTs) were prepared from the optimized batches (kneading method) of solid dispersion, using crospovidone and Doshion P544 resin as superdisintegrants. The tablets were characterized by in-vitro disintegration and dissolution tests. The study of the MDTs showed disintegration times in the range 32.0±0.85 to 20.0±1.30 sec and dissolution was faster than for the commercial preparation. In conclusion, this investigation demonstrated the potential of solid dispersions of a drug with Gelucire 50/13 for promoting the dissolution of the drug and contributed to the understanding of the effect of a superdisintegrant on mouth dissolving tablets containing a solid dispersion of a hydrophobic drug. |
| Databáze: |
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