ENHANCED AQUEOUS SOLUBILITY AND IN VITRO DISSOLUTION OF THE ANTI-HYPERLIPIDEMIC AGENT USING SYNTHESIZED SOLID DISPERSION CARRIER

DARSHAN R. TELANGE; SURENDRA S. AGRAWAL; ANIL M. PETHE; ANKITA V. HADKE

doi:10.22159/ijap.2023v15i1.46657

Authors

DARSHAN R. TELANGE Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education and Research (Deemed to be University), Sawangi (Meghe) Wardha. 442001, Maharashtra, India https://orcid.org/0000-0003-3016-8237
SURENDRA S. AGRAWAL Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education and Research (Deemed to be University), Sawangi (Meghe) Wardha. 442001, Maharashtra, India https://orcid.org/0000-0002-1149-5307
ANIL M. PETHE Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education and Research (Deemed to be University), Sawangi (Meghe) Wardha. 442001, Maharashtra, India https://orcid.org/0000-0002-6380-1847
ANKITA V. HADKE Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education and Research (Deemed to be University), Sawangi (Meghe) Wardha. 442001, Maharashtra, India https://orcid.org/0000-0001-7163-0307

DOI:

https://doi.org/10.22159/ijap.2023v15i1.46657

Keywords:

Atorvastatin, Co-processed excipients, Eudragit®RS100, Pentaerythritol, Solid dispersion

Abstract

Objective: To improve ATN's solubility, permeability, and dissolution rate of pentaerythritol-eudragit^®RS100 co-processed excipients (CE) and their potential as a solid dispersion carrier (ATN-CE-SD).

Methods: The ATN-CE-SD was prepared using the solvent evaporation technique. The pure ATN, physical mixture, CE carrier, and optimized ATN-CE-SD was physicochemically characterized using Scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, solubility, and in vitro dissolution was used to evaluate solid dispersions.

Results: Physical and chemical analysis showed that ATN-CE-SD formed via the involvement of weak intermolecular forces of attraction between CE carrier and ATN. The prepared solid dispersion showed the drug content around ~ 96.94 % w/w, indicating that the solvent evaporation method improved the encapsulation of ATN and, thus, enhanced its drug content. Compared to pure ATN (~ 0.11 mg/ml), ATN-CE-SD (1:2) significantly increased the aqueous solubility by around ~ 25-fold (~ 2.78 mg/ml), indicating solid dispersion improves the solubility of ATN. ATN-CE-SD enhanced the rate of dissolution of ATV (~ 65 %) compared to pure ATN (~ 25 %) and PM (~ 34 %). Likewise, ATN-CE-SD (1:2) improved the rate and extent of ATN (~ 60 %) across the biological membrane compared to pure ATN (~ 22 %) and PM (~ 32 %). The ATN-CE-SD (1:2) improved the dissolution efficiency by around ~ (57.31%) compared to pure ATN (~ 7.02%) and PM (~ 20.43%). According to the study, co-processed excipients could serve as a promising solid dispersion carrier and improve ATN's water solubility, permeability, and dissolution rate.

Conclusion: Based on the results, it is possible to use synthetic solid dispersion carriers as alternatives to improve the low water solubility and permeability of ATN.

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