Manufacturing Lipstatin&Orlistat Technology
Lipstatin is a potent, irreversible inhibitor of pancreatic lipase. It is a natural product, and was first isolated from the Actinobacterium Streptomyces toxytricini. The popular antiobesity drug orlistat (trade names Xenical and alli) is a saturated derivative of lipstatin.
Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. Orlistat is a single diastereomeric molecule that contains four chiral centers, with a negative optical rotation in ethanol at 529 nm.
Orlistat works by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested. Only trace amounts of orlistat are absorbed systemically; the primary effect is local lipase inhibition within the GI tract after an oral dose. The primary route of elimination is through the feces.
Orlistat is a white to off-white crystalline powder. Orlistat is practically insoluble in water, freely soluble in chloroform, and very soluble in methanol and ethanol. Orlistat has no pKa within the physiological pH
Technology Data:
Strain and technological know-how is available
Final titre: 10+1.0 g/L
Fermentation time 168 hrs
Recovery yield: 75 %
Hydrogenation Yield: 80%
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