Hrk supply Misoprostol Raw materials powder

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Misoprostol powder of Usage and Synthesis.

Misoprostol can be administered orally, vaginally, sublingual, or orally. It is suggested that vaginal administration and sublingual administration can avoid liver metabolic pathway, and the clinical effect is better than oral administration. Sublingual administration is directly absorbed by the oral mucosa, which makes the drug produce short time and the blood drug concentration rise quickly, but the drug related side effects are obvious. However, oral and sublingual administration reduces gynecological operation costs and has better compliance.

Although misoprostol is the most common gastrointestinal reaction, do not ignore the very serious allergic reaction. There have been reports of anaphylactic shock after oral administration in China, so patients should be asked about their previous drug allergy history before medication. Although misoprostol has many advantages in clinical application, there are also drug contraindication, which is prohibited for patients with cardiac, liver and renal dysfunction, and prohibited for patients with glaucoma, asthma and prostaglandin drug allergy.

Uses of Misoprostol.

The first chemically synthesized prostaglandin E1 anti-ulcer drug has a powerful effect on inhibiting gastric acid secretion and preventing ulcer formation. The gastric acid that can be inhibited includes basic gastric acid secretion and gastric acid secretion caused by histamine pentaglacin, food or coffee stimulation, and can also reduce gastric acid secretion at night. It is the first anti-peptic ulcer drug used in clinic. It is better than antireceptor antagonists for prolongation of ulcer recurrence, but less effective than island receptor antagonists for relieving peptic ulcer pain. For gastric and duodenal ulcers, especially in cases with low prostaglandin levels.

It is used for gastric and duodenal ulcer, hemorrhagic gastritis, acute gastric mucosal lesions and other diseases.

Pharmacological action of Misoprostol.

Misoprostol is well absorbed orally, F is about 70% ~ 80%, and it is quickly absorbed to esterify Misoprost acid with pharmacological activity. After a single oral dose, Tmax was 0.5-10h. The PPB is 80% to 90%. The value of T1/2 is 1.5 to 1.7 hours. It is mainly distributed in the liver, kidney, stomach and large intestine. 75% of the dose was excreted in the urine, 15% in the stool, and about 56% in the urine within 8h, which did not affect the activity of liver drug enzymes, and no interaction with other drugs was found.

Clinical for the treatment of duodenal ulcer and gastric ulcer, can also be used for acute gastric mucosal injury and bleeding, stress ulcer, especially suitable for the treatment and prevention of oral non-steroidal anti-inflammatory drugs caused by ulcers. The mechanism of inhibiting gastric acid secretion has not been elucidated. It is more effective than cimetidine in protecting the gastric mucosa from damage. The main adverse effects of misoprostol were loose stools or diarrhea (8%), while others included mild and transient nausea, headache, dizziness, and abdominal discomfort. Pregnant women and people with prostaglandin allergies are prohibited. It should be used with caution in patients with cerebrovascular or coronary artery disease.

Product Methods of Bulk Misoprostol powder.

Azelaic acid is used as raw material to react with diimidazole sulfoxide to produce imidazole acylation product, which has strong acylation activity. After reacting with monomethyl malonate, the product is acidified and decarboxylated to produce 2-[8-(methoxycarbonyl) octyl] acetate methyl ester, and then carboxylic acid is produced by water decarboxylation, and dimethyl oxalate is cyclized and decarboxylated to produce 3-substituted cyclopentatrione. One of the carbonyl groups is selectively hydrogenated to a hydroxyl group, which is then reduced to 4-hydroxy-2 -(methyl enanthate - 7-yl)-2, 3-cyclopentenone after reaction with acetone acetal. Finally, Misoprostol is obtained by reaction with organoaluminum reagent. The route is complex, some products need to be purified by chromatography, and the total yield is less than 1%.

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