This invention relates to the production of saccharase inhibitors in which a polysaccharidic or oligosaccharidic amylase inhibitor is hydrolytically degraded either enzymatically or by acid hydrolysis. The invention also relates to the use of said saccharase inhibitors in pharmaceutically acceptable therapeutic compositions in the treatment of conditions indicating adiposity, hyperlipaemia (atherosclerosis), diabetes, pre-diabetes, caries and the like.
The invention relates to a saccharase inhibitor derived from Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, means for the production of said saccharase inhibitors comprising cultivation of Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, in appropriate nutrient solutions which are characterized by being starch free under conditions most favorable to growth and production of said saccharase inhibitor and recovering a saccharase inhibitor from culture broths of said nutrient solutions, as well as the use of said inhibitor in pharmaceutically acceptable therapeutic compositions suitable for use in the treatment and relief of conditions indicative of adiposity, diabetes, pre-diabetes, hyperlipaemia (atherosclerosis), caries and the like.
A new amylase inhibitor, called Amylostatin-A, which can be distinguished from those disclosed heretofore on the basis of its constitution, molecular weight, specificity for certain types of amylase and adsorbability, is obtained by cultivating a strain of actinomycetes belonging to Streptomyces diastaticus var. amylostaticus FERM P-2499 in a medium containing starch, preferably amylopectin, as the sole source of carbon; the conditions of cultivation, methods of isolation and purification and therapeutical application thereof are disclosed.
Disclosed herein is a process for preparing highly pure acarbose of formula (I) useful as medicine for the treatment of diabetes. The disclosed process comprises prepurifying an acarbose-containing solution using a synthetic adsorbent to produce a prepurified acarbose having an acarbose content of a predetermined level or more; and contacting the prepurified acarbose with a monodispersed, strongly acid cation exchanger, in one step, to absorb acarbose.
An improved process for the purification of crude aqueous solutions of acarbose by passing such solutions through a strong acid cation-exchange resin, saturating such resin and recovering as an eluate a substantially pure acarbose solution. Purities of more than 98%, and preferably about 99% or higher, are thus obtained.