Solubility and Crystal Size of Sirolimus in Different Organic Solvents

Abstract

The solubility of sirolimus drug in different organic solvents, viz., acetone, chloroform, methanol, ethanol, and dichloromethane, has been measured for the temperature range of (295 to 345) K by a gravimetric method. The relation between solubility and crystal size formation has also been studied. It was found that the higher the solubility of material, the larger the crystal size and vice versa. The stability of crystals has been measured, and it was found that smaller crystals have a moderate level of stability when compared with that of larger crystals. From the observations of the present study, it may be suggested that for cardiovascular applications of sirolimus drug one can use ethanol and methanol as a solvent for deriving crystals of less than 400 nm size.

Impact of Artificial Plaque Composition on Drug Transport

“…Based on the estimated k L values and the external solution concentrations, the concentration of drug in the lipid‐rich phases is approximately 0.8 and 30 mg/mL for tetracycline and fluvastatin, respectively. We note that the value for fluvastatin is consistent with previous observations on siroliumus, a common drug used in DES applications with a logP over 5,16 in which lipid solubilities in the range of tens of mg/mL have been reported, in significant excess of its water solubility ( 2–3 μg/mL) 46. The ability of hydrophobic drugs to selectively deposit in vascular tissue and substantially exceed the applied concentration has been attributed to this enhanced drug solubility in fatty regions.…”

“…Thus, it is not clear how physiological differences may impact treatment outcomes. The majority of studies aimed at quantifying these parameters have been conducted on arterial tissue samples ex vivo 13–20. For example, effective diffusivities for arterial tissue segments have been estimated for both paclitaxel and rapamycin (and analogs, e.g., sirolimus), common drugs incorporated into DES platform 17–19.…”

Solubility Measurement and Modeling of Eszopiclone in Four Binary Solvents

“…In the crystallization process, the MSZW (metastable zone width) might change with increasing solubility resulting from adding water, which was the key kinetic parameter, and would affect the nucleation , and growth , step of crystallization. Furthermore, the morphology , and particle properties of the crystal production might be improved. Therefore, the increasing solubility data of eszopiclone would be helpful in the research of the crystallization process.…”

Solubility of Ethyl p-Aminobenzoate in Six Alcohols within (283.15 to 327.15) K

“…The determination of solubility of the solute in the solvent is generally achieved by the gravimetric or dynamic method. − In this study, the last solid disappearance method, as a member of dynamic methods, was applied to measure the solubility of EPAB in six pure alcohols. The detailed apparatus and procedure to measure the solubility of EPAB in our laboratory were described in our previous reported literatures. − A belief summary was presented as follows: A known mass of solvent (about 40g ± 0.001g) was added into a three-necked flask that is equipped with a stirrer, a condenser, and mercury thermometer (standard uncertainty of 0.05 K).…”