Online ISSN: 2515-8260

Keywords : Poorly water-soluble drug

Impact, Improvement Of Solubility On Drug Belonging To BCS-II And Their Formulation For Oral Delivery

N. Madhavi; V.T. Iswariya

European Journal of Molecular & Clinical Medicine, 2022, Volume 9, Issue 7, Pages 2965-2977

The present study aimed to enhance the dissolution rate of a poorly water-soluble drug, haloperidol by adopting liquisolid compact technique and formulating it into an orodispersible system. Haloperidol is widely used neuroleptic which is a butyrophenone. Though well absorbed after oral dosing, there is a first pass metabolism leading to a reduced bioavailability of the drug (60- 70%). Therefore the present investigation is concerned with development orally disintegrating tablet of haloperidol. Different formulations of liquisolid compacts of drug were formulated by varying the concentration of drug solution from 10- 30%w/v. Avicel 102 and Aerosil 200 was used as carrier and coating material respectively. Crospovidone and SSG in the ratio of 1:1were added to the formulation for faster disintegration. Prior to the compression of orodispersible tablets all batches of liquisolid compacts were subjected to pre-compression evaluations and the results were found   to be satisfactory. Further, the prepared powder blends were directly compressed into  orodispersible liquisolid tablets. These tablets were evaluated for the post-compression parameters. Liquisolid tablet (F2) demonstrated a significantly higher drug release rate than those of marketed tablet, which may be due to enhanced wetting properties and effective surface area of the drug. The results of the kinetic study revealed that the formulation followed first-order kinetics with a dissolution-controlled release pattern. In conclusion the liquisolid compacts technique can be a promising alternative for the formulation of water-insoluble drugs by combining the liquisolid technology and orodispersible system can be used to improve the dissolution rate of poorly water-soluble drugs.