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Acta pharmaceutica Hungarica

[The applicability of sucrose laurate in hot-melt technology].


PMID 21595305

Abstract

Nowadays, one of the most important task of the pharmaceutical technology is to optimize the dissolution of active ingredients, because most of the drug candidates have a poorly water solubility and hence a slow absorption. According to the latest examinations, the bioavailability of poorly water soluble drugs can be increased significantly by using surfactants or the mixture of surfactants and polymers. Nowadays, surfactants (like polysorbates) are generally used in the production of solid dispersions, so the use of surface-active sucrose esters can be resulted an innovative solution in the pharmaceutical technology. The aim of our investigation was to examine the applicability of sucrose laurate in hot-melt technology in order to influence the crystalline structure and dissolution rate of a poorly water soluble drug (gemfibrosil) having low-melting point. The results of the X-ray powder diffractometry have showed that the sucrose laurate had no significant effect on the crystallization degree of the drug which is important in case of the stability. On the bases of the results of in-vitro dissolution studies, it can be concluded that the sucrose laurate (using minimum 5%) can be well applied in hot-melt technology with carriers having characteristic melting point (e.g. Macrogol) to increase the dissolution rate of poorly soluble drugs.

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84110
Sucrose monolaurate, BioXtra, ≥97.0% (TLC)
C24H44O12