Misoprostol Raw Materials Misoprostol Powder

CAS:59122-46-2

MF:C22H38O5

MW:382.54

EINECS:664-288-5

Specification: 99% min Misoprostol Powder

Sample:Misoprostol Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: Yellow Liquid

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Misoprostol Powder Usage and Synthesis.

Misoprostol, also known as Hiker's ulcer, Misoprot, Misoprostol, first marketed in the United States in 1985, is a synthetic prostaglandin E1 analogue, with the appearance of a yellowish viscous liquid, extremely difficult to dissolve in water, and can be mixed with ethanol, ether, and chloroform. Unstable at room temperature. It is a new type of anti-progestational hormone, a derivative of synthetic prostaglandin E1, which has the effect of stimulating mucus and bicarbonate secretion, promoting mucosal blood flow, and thus has a protective effect on gastric and duodenal mucosa, which is conducive to the healing of ulcers.

Uses and functions of Misoprostol.

The first chemically synthesised prostaglandin E1 antiulcer drug, has a powerful inhibitory effect on gastric acid secretion and prevents ulcer formation. The gastric acid that can be inhibited includes basal gastric acid secretion and gastric acid secretion due to histamine pentapeptide gastrin, food or coffee stimulation, and it also reduces gastric acid secretion at night.

It is the earliest anti-peptic ulcer drug applied in the clinic. It is superior to violaceous receptor antagonists for prolonging ulcer recurrence, but less effective than islet receptor antagonists for relieving peptic ulcer pain.

Used for gastric and duodenal ulcers, especially in cases with low prostaglandin levels.

Pharmacological Effect of Misoprostol.

Misoprostol is well absorbed orally, F about 70% to 80%, and is quickly de-esterified into pharmacologically active misoprostic acid. After a single oral dose, Tmax is 0.5-10 h. PPB is 80%-90%. Rapid clearance, T1/2 is 1.5～1.7h.

Distribution in the body is mainly in the liver, kidney, stomach and large intestine. 75% of the administered dose is excreted by urine, 15% by faeces, and about 56% is excreted in urine within 8 h. It does not affect hepatic drug enzyme activity, and no interaction with other drugs has been found.

Clinically used for the treatment of k treatment of duodenal ulcer and gastric ulcer, can also be used for acute gastric mucosal injury and bleeding, stress ulcers, especially suitable for the treatment and prevention of ulcers due to oral non-steroidal anti-inflammatory drugs. The mechanism of action of this product in inhibiting gastric acid secretion has not been elucidated.

It is more effective than cimetidine in protecting the gastric mucosa from damage. The main adverse reactions to misoprostol are loose stools or diarrhoea with an incidence of 8%, others may include mild transient nausea, headache, dizziness and abdominal discomfort. Misoprostol is contraindicated in pregnant women and in those with prostaglandin analogue hypersensitivity.

Caution should be exercised in patients with cerebrovascular or coronary artery disease.

Product Method of Bulk Misoprostol Powder.

Azelaic acid as raw material, and diimidazole sulfoxide reaction, to generate imidazole acylation product, the product has a strong acylation activity, and malonic acid monomethyl ester reaction, and then acidification and decarboxylation to generate 2-[8-(methoxycarbonyl)octanoyl]acetic acid methyl ester, and then hydrolysis and decarboxylation to generate 8-oxo-decanoic acid, and oxalic acid dimethyl ester cyclic and then decarboxylation to generate 3-position-substituted cyclopentanetrone, selective hydrogenation of which one of the carbonyl group for the Hydroxyl, and acetone acetal reaction and then reduced to generate 4-hydroxy-2-(heptanoic acid methyl ester-7-yl)-2,3-cyclopentenone, and finally and organo-aluminium reagent reaction to obtain misoprostol.

The route is complex and some of the products need to be purified by chromatography, with an overall yield of less than 1%.