S rozvojom civilizačných chorôb, ako je diabetes mellitus, metabolický syndróm, prípadne obezita, rastie aj úsilie nachádzať nové liečivá predovšetkým z prírodných zdrojov. Patria medzi ne aj inhibítory α-amylázy, enzýmu, ktorý v tele zdravého človeka štiepi polysacharidy na jednoduchšie cukry. Vzhľadom k tomu, že toto štiepenie ovplyvňuje glykémiu, ktorú je snaha terapeuticky meniť, vzrastá aj záujem o tieto látky. Tento prehľadový článok mapuje druhy inhibítorov amylázy vrátane ich prírodných zdrojov.
Development of civilization diseases such as diabetes mellitus, metabolic syndrome or obesity, enforces the increasing effort to find new drugs, especially from natural sources. These include α-amylase inhibitors, which break down polysacharides into simple sugars in the body of a healthy person. As this cleavage affects the level of blood sugar, which is sought to be therapeutically influenced, there is a growing interest in these substances. This review maps the types of amylase inhibitors, including their natural resources.
- Klíčová slova
- rostlinné inhibítory, štěpení škrobu,
- MeSH
- alfa-amylasy antagonisté a inhibitory terapeutické užití MeSH
- amylasy * antagonisté a inhibitory terapeutické užití MeSH
- lidé MeSH
- škrob metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- přehledy MeSH
Warfarin is intensively discussed in terms of generic substitution due to particular cases of bleeding, which are attributable to fluctuations in API content or the substitution of crystalline (WSC) for amorphous (WSA) warfarin. The aim of this study was to assess to what extent the in vitro release was affected by the form of API depending on the composition and technology. Bioequivalent tablets containing 5 mg of WSA or WSC prepared by wet granulation or direct compression were used. Furthermore, tablets of the same composition with WSC or WSA prepared by direct compression were evaluated. Raman spectroscopy was used to confirm the presence of WSA or WSC. The dissolution was more influenced by the technology than by the form of API but even tablets with dissimilar profiles were bioequivalent. This is probably due to the precipitation of WSA and WSC in the stomach on a poorly soluble acidic form, which subsequently dissolves in the neutral environment of the small intestine. Recrystallization was demonstrated in the in vitro assay at a pH of 1.2 and 4.5 using Raman spectroscopy and X-ray diffraction. In summary, the content uniformity appears to be the main factor affecting the safety of the treatment.