[A applicability of sugar esters in hot-melt technology].
One of the most important tasks in pharmaceutical technology is the optimization of drug release. The hot-melt technology is an important method with which to modify the bioavailability. Sugar esters (SEs) have a wide range of HLB values (1-16). Due to their low melting points, they are promising carriers for the melting method. The aims of the present work were to study the thermal properties (DSC) and the structures (XRPD) of SEs with low, medium or high HLB values, and to evaluate their applicability in the hot-melt technology. Relationships were found between the HLB value, the structure and the thermal behaviour. After melting and solidification, the SEs have partially amorphous layered structures which slowly crystallize in time; the original structure does not return for SEs with high, moderate, or low HLB values. These results demonstrate that changes in morphology must be considered during research and development. During the examination of meloxicam-SE melted products the SEs influenced the drug release, depending on their HLB values. In the cases of ibuprofen-SE melted products, the SEs did not influence the drug release. Here, a change in the drug distribution was the predominant effect, which was accompanied by movement in the SE structure.
Szuts
Angéla
A
Szegedi Tudományegyetem, Gyógyszertechnológiai Intézet, Szeged, Eötvös u 6 -- 6720.
Laczkovich
Orsolya
O
Nassab
Parya Reisi
PR
Aigner
Zoltán
Z
Szabone Révész
Piroska
P
D001682:Biological Availability; D002241:Carbohydrates / Q000737:chemistry* / Q000493:pharmacokinetics*; D004952:Esters / Q000737:chemistry* / Q000493:pharmacokinetics*; D013329:Structure-Activity Relationship; D013816:Thermodynamics
D002241:Carbohydrates; D004952:Esters