trait | White or milky white powder. |
Use | as a special polymer, polycarbopol non-calcium has the dual function of treating constipation and Diarrhea. And because the Poly carbopol calcium is a prodrug, the active ingredient is the Poly carbopol, under the action of gastric acid, the Poly carbopol calcium occurs decalcification ion exchange reaction, calcium is produced as a by-product, and therefore, polycarbopol calcium has the unique advantage of calcium supplementation while being treated. calcium polycarbophil was first developed by Abbott, USA, and has been widely used in Europe, America and Japan to relieve symptoms of IBS and constipation due to various causes. |
pharmacological action | polycarbopol non-calcium has very unique biochemical properties, which can rapidly decalcify in acidic environment, poly-carbopol was formed. However, Poly-carbomer can absorb 10 times its own weight of water in an acidic environment, and the expansion rate increases significantly at pH> 4, in the neutral or weak alkaline environment can reach 60~100 times of their own weight. Animal experimental study showed that the calcium detachment rate in the stomach was more than 70% in 30min when the rats were given Poly-carbopol non-calcium, which was basically consistent with the calcium detachment curve of the in vitro experiment. It is proved that the water absorption of poly-Kappa non-calcium is affected by pH value, and the higher the pH value, the greater the water absorption. |
mechanism of action | 1. The main mechanism of action of Poly carbopol calcium in the intestine is:(1) water retention in the digestive tract. In the rat experiment, there was no effect on the water metabolism of the intestinal tube, and the water was maintained in the intestinal tube. (2) the regulation of the transport of the contents of the digestive tract. In experiments in mice and rats, in an animal model of enhanced intestinal delivery, administration of polycarbopol calcium found that gastrointestinal content delivery was inhibited. In an animal model of delayed intestinal delivery, administration of polycarbopol calcium was found to improve gastrointestinal content delivery. 2. Diarrhea inhibition and improvement of constipation effect: the Diarrhea model of mice, rats and dogs showed a Diarrhea reduction in the number of times and did not induce constipation. The constipation model in rats showed an ameliorative effect of increasing the amount of defecation, and Diarrhea was not induced. Pharmacokinetics in rats and dogs after oral administration of 14c-polycarbopol calcium or 14c-polycarbopol, blood radiomarker concentration determination test, urine/fecal excretion test, the results of whole body autoradiography, bile excretion test and in situ digestive tract absorption test in rats showed that the two compounds were not absorbed in the stomach, duodenum, jejunum, ileum and colorectal. In addition, there was no radioactive damage to any tissues when 14c-polycarbopol calcium was orally administered to rats, and no radioactivity was found in urine when 14c-polycarbopol calcium was orally administered to rats and dogs, the radioactivity of the drug is also almost completely absorbed by the feces. The above results show that the polycarbopol calcium is not absorbed by the digestive tract and is not metabolized by intestinal bacteria when it is orally administered, and is finally excreted out of the body through feces. |
synthesis method | ① firstly, magnesium sulfate and divinyl glycol were fully dissolved in water in a stirred reactor, stirring and heating to 76°C, to fully dissolve; ② Then add the mixture of acrylic acid and azobisisobutyronitrile Dropwise, stir evenly, heat preservation reaction for 3 hours; ③ clean with water at 76°C, get poly-carbopol; ④ fully stir the aqueous solution of poly-carbopol and calcium carbonate in the reaction kettle, and at the same time raise the temperature to 100°C for 6.5 hours; ④ put down the centrifugal dehydration, dry, pulverize, poly-carbo-non-calcium can be packaged if it is qualified by inspection. The yield of poly (carbo-non-calcium) synthesized by the above method is close to 100%, and the calcium content in the product quality item reaches 22%. Compared with the conventional synthesis method, significantly improve the yield and quality of the product. |