Announcing a new article publication for BIO Integration journal. Nitrofurantoin is a BCS II drug with a low solubility and dissolution rate. Therefore, the pharmaceutical applications of nitrofurantoin are limited. The purpose of this study was to enhance the solubility, dissolution, and bioavailability of nitrofurantoin by formulating a solid dispersion (SD).
The SD was developed using 32 factorial designs considering poloxamer 188 and the trituration time as independent variables, and solubility and drug release as dependent variables. The developed SD was characterized for solubility, FTIR, DSC, XRD, in vitro dissolution, and pharmacokinetic studies in rats.
Nitrofurantoin:poloxamer 188 at a 1:1 ratio had higher solubility than nitrofurantoin. The solubility of nitrofurantoin was directly related to the amount of poloxamer 188 and trituration time. In addition, poloxamer 188 concentration was directly related to the DR45 (%), while the rate of stirring was inversely related to the DR45 (%). An FTIR study revealed excellent drug excipient compatibility. The crystallinity of the drug was decreased, which indicated a more amorphous nature of the drug in XRD and DSC studies. Compared to pure drug dispersion, the optimized formulation exhibited a 3.88-fold improvement in the bioavailability of nitrofurantoin, whereas compared to the marketed formulation, a 1.77-fold enhancement in bioavailability was noted.
This study indicates that SD could be a potential carrier system to enhance the solubility, dissolution, and bioavailability of nitrofurantoin.
Source:
Journal reference:
Bhosale, D. S., & Kalshetti, M. S. (2024). Enhanced Drug Dissolution of Nitrofurantoin Using a Solid Dispersion Technique. BIO Integration. doi.org/10.15212/bioi-2024-0025.
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