Amoxicillin Solubility and Supercritical Carbon Dioxide

Abstract

During the past 20 years, an increase through measuring, correlating, and calculating solid solubilities especially pharmaceuticals in supercritical fluids for processes such as purification, extraction, and size reduction processes have been observed. In this direction, the solubility of amoxicillin with the International Union of Pure and Applied Chemistry (IUPAC) name of (2S,5R,6R)-6-{[(2R)-2-amino-2-(4-hydroxyphenyl)-acetyl]amino}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0] heptane-2-carboxylic acid in the pressure and temperature ranges of 16 MPa to 40 MPa and 308.15 K to 338.15 K, respectively, has been measured. For this purpose, a simple gravimetric-based method was utilized to obtain the amoxicillin solubility in supercritical carbon dioxide. During the measurements it was found that the amoxicillin solubility was in the range of 1.08·10–5 and 7.23·10–3 based on the mole fraction. Besides, due to a vast number of efforts have been performed on the solubility correlation by several researchers, four semiempirical density-based correlations including Mendez-Santiago and Teja (MST), Bartle et al., Chrastil, and Kumar and Johnston (K-J) models were used to correlate the measured solubility data. The obtained results revealed the capability of the used correlation through the solubility correlation with an acceptable level of accuracy.

Solubility of Solids in Sub- and Supercritical Fluids: A Review 2010–2017

“…Precise experimental determination of a solid drug's solubility in supercritical fluids and its correlation is extremely important to the development of high pressure technologies for the pharmaceutical industry. 23 Phase equilibrium data are significant for the design of separation or formulation processes. Micronization techniques with supercritical fluids have been used in the polymer industry, in pharmaceuticals, cosmetics, and the food industry to produce ultrafine particles.…”

“…In the past few decades, many approaches to predicting, correlating, and estimating the solubility of solids have been studied. 23 Generally, equations of state (EOSs) are the first option for estimating the solubility of compounds in supercritical fluids. Unfortunately, the application of the EOSs is usually very limited for pharmaceuticals.…”

“…Therefore, more recently, densitybased semiempirical correlations such as the Chrastil, Mendez-Santiago and Teja (M-S-T), Bartle et al, and Kumar and Johnston (K-J) models have been used to predict the solubility of solids. 23 Among the nonsteroidal anti-inflammatory drugs for relieving pain, fever, swelling, and stiffness, naproxen has attracted considerable attention. The solubility of naproxen and nicotinamide and their mixture in acetone + SC CO 2 systems was measured as functions of composition and temperature.…”

“…Precise experimental determination of a solid drug’s solubility in supercritical fluids and its correlation is extremely important to the development of high pressure technologies for the pharmaceutical industry . Phase equilibrium data are significant for the design of separation or formulation processes.…”

“…It is not always possible to determine solubility experimentally. In the past few decades, many approaches to predicting, correlating, and estimating the solubility of solids have been studied …”