Formulation and evaluation of orodispersible tablet of dolutegravir -methionine cocrystal

Dolutegravir, a newly approved anti-HIV medication is insoluble in the normal gastric pH range and that results in slow onset of action. The research proposes cocrystallization process to increase the solubility of the drug and hence dissolution. The cocrystals of dolutegravir were formulated using methionine as coformers by solvent evaporation method. The cocrystals were evaluated for solubility, in vitro drug release, and solid-state characterization, study. The orodispersible tablets of dolutegravir cocrystal were successfully prepared by direct compression method. The solid-state characterization study showed the compatibility and amorphization of the drug in the cocrystal form. The cocrystal of drug: methionine (1:2) was found to enhance dissolution by 1.88 times compared to the pure drug. The orodispersible tablets disintegrated at 10.05 secs and 90% drug was released in 20 min. Hence, it can be concluded that the methionine-dolutegravir cocrystal can be a promising means to improve the solubility of the drug

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Publication Details

Journal
Fabad Journal of Pharmaceutical Sciences
Published
2025-03-25
DOI
https://doi.org/10.55262/fabadeczacilik.1516443
Primary Topic
Crystallography and molecular interactions
Type
article
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article

Formulation and evaluation of orodispersible tablet of dolutegravir -methionine cocrystal

Sayani Bhattacharyya, Tamang Rejoys, Ammon Tamang
Fabad Journal of Pharmaceutical Sciences
Crystallography and molecular interactions
article

Formulation and evaluation of orodispersible tablet of dolutegravir -methionine cocrystal

Sayani Bhattacharyya, Tamang Rejoys, Ammon Tamang
article en

Abstract

Dolutegravir, a newly approved anti-HIV medication is insoluble in the normal gastric pH range and that results in slow onset of action. The research proposes cocrystallization process to increase the solubility of the drug and hence dissolution. The cocrystals of dolutegravir were formulated using methionine as coformers by solvent evaporation method. The cocrystals were evaluated for solubility, in vitro drug release, and solid-state characterization, study. The orodispersible tablets of dolutegravir cocrystal were successfully prepared by direct compression method. The solid-state characterization study showed the compatibility and amorphization of the drug in the cocrystal form. The cocrystal of drug: methionine (1:2) was found to enhance dissolution by 1.88 times compared to the pure drug. The orodispersible tablets disintegrated at 10.05 secs and 90% drug was released in 20 min. Hence, it can be concluded that the methionine-dolutegravir cocrystal can be a promising means to improve the solubility of the drug

Fabad Journal of Pharmaceutical SciencesVol. 50(1)
Openalex Percentile: Top 93%
Crystallography and molecular interactions
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Formulation and evaluation of orodispersible tablet of dolutegravir -methionine cocrystal — Sayani Bhattacharyya, Tamang Rejoys, et al. · Fabad Journal of Pharmaceutical Sciences (2025) | TGRS Research Map | TGRS