| Abstrakt: |
Purpose: The aim of the study was to improve bioavailability of paliperidone, a class II drug, via cocrystallization with a peep to the effect of HPMC as a precipitation inhibitor (PPI). An attempt was made to prepare paliperidone cocrystals with benzamide, boric acid, nicotinamide, and PHBA as coformers after the prediction of cocrystal formation using Hansen solubility parameter (HSP) as a prediction tool. Method: The cocrystals were prepared, with a 1:1 M ratio of drug and coformer, by the solvent evaporation method. The prepared cocrystals were characterized by melting point, saturation solubility and in vitro drug release along with instrumental analytical techniques such as FTIR, DSC, PXRD, and SEM. Results: The formation of paliperidone cocrystals using benzamide, nicotinamide, and PHBA was confirmed, as predicted by HSP, by collective assessment of the results. On the other hand, the formation of paliperidone cocrystals by boric acid could not be proved. These findings revealed the suitability of HSP as a cocrystal formation prediction tool. In spite of this, the successfully prepared paliperidone-PHBA (PAL-PHBA) cocrystals had shown a tremendous increase in their solubility (0.115 mg/ml to 16.29 mg/ml, 141.6 fold) and dissolution (49% in 60 min to100 % release in 30 min) when compared to the pure drug. Therefore, these cocrystals further studied for paliperidone bioavailability in albino rabbits, in the presence and absence of HPMC as a PPI. The results showed an improvement in the bioavailability of paliperidone in the presence of precipitation inhibitor. Conclusion: Thus cocrystallization and precipitation inhibition technique increases the bioavailability of the drug. [ABSTRACT FROM AUTHOR] |
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