TAILORING OF SOLUBILITY OF IBUPROFEN IN THE PRESENCE OF HYDROPHILIC EXCIPIENTS IN WATER-ETHANOL MIXTURES BY CRYSTALLIZATION METHOD

AFRINA AFROSE; EDWARD T. WHITE; MD ABDUR RASHID; TONY HOWES; YAHYA ALHAMHOOM

doi:10.22159/ijap.2022v14i2.43871

Authors

AFRINA AFROSE Queensland University of Technology, Pharmacy Discipline, Faculty of Health, Institute of Health and Biomedical Innovation, Brisbane, QLD, Australia
EDWARD T. WHITE School of Chemical Engineering, The University of Queensland, Brisbane, QLD, Australia
MD ABDUR RASHID Department of Pharmaceutics, College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Kingdom of Saudi Arabia https://orcid.org/0000-0001-9404-5186
TONY HOWES School of Chemical Engineering, The University of Queensland, Brisbane, QLD, Australia
YAHYA ALHAMHOOM Department of Pharmaceutics, College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Kingdom of Saudi Arabia https://orcid.org/0000-0002-8368-9047

DOI:

https://doi.org/10.22159/ijap.2022v14i2.43871

Keywords:

Ibuprofen, Solubility, Aqueous ethanol, Crystallization, Excipients, UV spectrophotometry

Abstract

Objective: The objective of this study was to determine the effect of some commonly used pharmaceutical excipients on the solubility of Ibuprofen (Ibu) in a co-solvent consisting of water (W) and ethanol (E).

Methods: The Ibu solubility studies were carried out by dissolving the drug to equilibrium into aqueous ethanol solvents at a fixed temperature. The temperature of the water bath was kept constant (±0.1 °C of the desired temperatures 10, 25 and 40 °C). The solubility of Ibu was measured by using UV spectrophotometry.

Results: The low solubility (~ 50 ppm) of Ibu without excipients in water (zero ethanol) was observed. However, Ibu solubility was increased near exponentially with excipient containing co-solvent system. The maximum solubility of Ibu (1726 ppm) was occurred in a co-solvent containing 1.52% leucine, 5.22% mannitol, 0.25% HPMC, 1.55% Pl F127 and 10.75% w/w ethanol. The phase separation between 34% and 63% w/w E/(E+W) was observed at 40 °C. The individual effect of Pl F127 on enhancing the Ibu solubility was significant.

Conclusion: The individual addition of leucine, mannitol and HPMC has limited impact on the solubility of Ibu. However, the effect of combining these excipients together on Ibu solubility is significantly high.

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