Study on solubility enhancement of etravirine by crystal engineering method
By: Bhattacharyya, Sayani
.
Contributor(s): Adhikari, H.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2022Edition: Vol.84(3), May-Jun.Description: 575-585p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: Etravirine, an antiretroviral agent, used in the treatment of human immunodeficiency virus belongs to
biopharmaceutical classification system classification IV. The reported solubility of the drug is 0.0169 mg/
ml. In the present study, an attempt was made to enhance the solubility of etravirine by crystal engineering
technique. The cocrystallization method was carried out using 12 different coformers and each coformer
was studied in two different stoichiometric ratios. A preliminary screening of all the cocrystals was done
by determination of melting point and solubility. A statistical evaluation of all the cocrystals on solubility
was carried out at a significance level of p<0.05. The best cocrystals were subjected to drug content, in vitro
drug release, solid-state study (fourier transform infrared spectroscopy, differential scanning calorimetry,
powder x-ray diffraction) and stability study for 3 mo. Coformer benzoic acid showed a significant
improvement in etravirine solubility in the drug:coformer ratio of 1:1 and 1:2. The drug:benzoic acid
ratio of 1:2 was found to have more solubility and showed enhanced dissolution compared to pure drug.
The in vitro dissolution rate of the drug:benzoic acid ratio of 1:2 was found to be more than 90 % in 60
min. Therefore, it can be concluded that the cocrystallization method with benzoic acid as coformer can be
a promising approach for solubility improvement of etravirine.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
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Articles Abstract Database
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School of Pharmacy Archieval Section | Not for loan | 2023-0419 |
Etravirine, an antiretroviral agent, used in the treatment of human immunodeficiency virus belongs to
biopharmaceutical classification system classification IV. The reported solubility of the drug is 0.0169 mg/
ml. In the present study, an attempt was made to enhance the solubility of etravirine by crystal engineering
technique. The cocrystallization method was carried out using 12 different coformers and each coformer
was studied in two different stoichiometric ratios. A preliminary screening of all the cocrystals was done
by determination of melting point and solubility. A statistical evaluation of all the cocrystals on solubility
was carried out at a significance level of p<0.05. The best cocrystals were subjected to drug content, in vitro
drug release, solid-state study (fourier transform infrared spectroscopy, differential scanning calorimetry,
powder x-ray diffraction) and stability study for 3 mo. Coformer benzoic acid showed a significant
improvement in etravirine solubility in the drug:coformer ratio of 1:1 and 1:2. The drug:benzoic acid
ratio of 1:2 was found to have more solubility and showed enhanced dissolution compared to pure drug.
The in vitro dissolution rate of the drug:benzoic acid ratio of 1:2 was found to be more than 90 % in 60
min. Therefore, it can be concluded that the cocrystallization method with benzoic acid as coformer can be
a promising approach for solubility improvement of etravirine.
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