ABSTRACT
A lot of prescription medicines have become switch over-the-counter (OTC) medicines. However, additives in brand-name drugs, generic drugs, and switch OTC drugs differ; therefore, the feelings associated with the use of these medicines vary for patients. The aim of this study was to compare the physicochemical properties and the feeling of use (assuming skin as an index of usability) of acyclovir (ACV) ointments. Five ACV ointments were used: ACV-A, a brand-name drug, ACV-B and ACV-C, generic drugs, and ACV-D and ACV-E, switch OTC drugs. The physicochemical properties were evaluated by determining the content uniformity, water content, flattening, viscosity and viscoelasticity, and near-infrared (NIR) absorption spectroscopy. Skin friction was measured to evaluate the feeling associated with use. Results of the content uniformity test indicated that the ACV content was uniform, and equivalence was observed. Measurement of moisture content indicated that this parameter differed in each ointment preparation. The yield value, which was calculated by measuring flattening, was 4416.7 dyne/cm2 for ACV-A, 1175.7 dyne/cm2 for ACV-B, 2114.9 dyne/cm2 for ACV-C, 4234.5 dyne/cm2 for ACV-D, and 3620.7 dyne/cm2 for ACV-E. Measurement of viscosity and viscoelasticity revealed that viscosity increased with time and the viscoelasticity of each ointment. The second derivative of the NIR spectrum revealed that ACV-B and ACV-C had a wider spectrum of absorption than the other ointments. ACV-B had lesser friction than other ointments. These findings suggest that differences in the type and content of additives (macrogol) result in differences in the physicochemical properties of individual ointments.
ABSTRACT
Miglitol (MT) is an α-glucosidase inhibitor with a postmeal blood glucose level lowering effect that is used to treat type 2 diabetes. In addition, α-cyclodextrin (αCD) has been reported to inhibit increases in postmeal blood glucose. The aim of this study was to prepare a freeze-dried product (FD) composed of MT and αCD or γCD (molar ratio of MT/αCD = 1/1, MT/γCD = 1/1) and to evaluate the physicochemical properties and biological activity of the FD. The PXRD profile of FD exhibited a halo pattern, and characteristic peaks derived from MT, αCD, and γCD were not observed. The TG-DTA results for FD indicated an increased weight loss temperature and the absence of an endothermic peak for MT. The NIR absorption spectrum measurement suggested an intermolecular interaction between MT and αCD or γCD in the FD. 1H-1H NOESY NMR spectroscopy (D2O) revealed an intermolecular interaction in the FD. The results of the α-glucosidase activity inhibition test and the α-amylase activity inhibition test indicated that the FD exhibited the same inhibition rate as MT alone and the effects of MT were not altered by the freeze-drying method.
