What is Ursodeoxycholic acid?
Ursodeoxycholic acid powder is white powder; odorless, bitter. MP: 203-204℃. It is easily soluble in ethanol and glacial acetic acid, soluble in sodium hydroxide test solution, and insoluble in chloroform and chloroform. UDCA is an isomer of CDCA, and its litholytic effect is stronger than CDCA, without diarrhea and liver toxicity. UDCA can reduce the absorption of cholesterol, and can reduce the synthesis of cholesterol and the cholesterol content in bile. In addition, UDCA can also reduce the concanavalin A binding fragment, which can promote the formation of bile crystals, thereby inhibiting the formation of stones. The combined use of UDCA and CDCA can enhance the litholytic effect of each alone, while reducing side effects. The combination of the two is mainly used to treat gallbladder cholesterol stones. When the patient's gallstones are of equal density to bile or the CT value of the gallstones is less than 75 units, the stone dissolving speed of UDCA is the fastest. After using this product, patients with cholelithiasis can increase the number of peripheral platelets.
Ursodeoxycholic acid is a unique component in bear bile. The biological half-life is 3.5 to 3.8 days. UDCA rapidly combines with glycine or taurine in the liver, and is discharged from the bile into the small intestine to participate in the enterohepatic circulation. Part of the UDCA bound in the small intestine is hydrolyzed back to the free form; the other part is converted into LCA under the action of bacteria, and the latter is then sulfated, thereby reducing its potential liver toxicity. It has the effects of dissolving gallstones, inhibiting cholesterol deposition in the blood, calming the liver, promoting bile secretion, and detoxifying. Its sodium salt has a stronger effect than other bile acids in promoting liver glycogen storage, fatty acid hydrolysis, and lowering blood sugar.
| Product name | Ursodeoxycholic acid |
| CAS | 128-13-2 |
| Molecular formula | C24H40O4 |
| Molecular weight | 392.57 |
| EINECS Number | 204-879-3 |
| Storage condition | 2-8°C |
| Melting point | 203-204 °C (lit.) |
| Solubility | Ethanol: 50 mg/mL, clarified. |
| Appearance | White powder |
| Boiling point | 437.26°C (rough estimate) |
| Density | 0.9985 (rough estimate) |
What is the pharmacological mechanism of Ursodeoxycholic acid?
Ursodeoxycholic acid is the 7β-hydroxy diastereomer of chenodeoxycholic acid. It is this slight difference in structure that makes ursodeoxycholic acid powder hydrophilic. Ursodeoxycholic acid can reduce the activity of β-hydroxy-β-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme for cholesterol synthesis in the liver, thereby inhibiting cholesterol synthesis; and it forms a stable liquid crystalline suspension with cholesterol, making the cholesterol in the bile unsaturated, thereby promoting the precipitation and dissolution of cholesterol in the stones. Ursodeoxycholic acid can also inhibit the intestinal absorption of cholesterol. Ursodeoxycholic acid can also antagonize the cytotoxic effect of endogenous hydrophobic bile acids and protect liver cell membranes. Ursodeoxycholic acid exerts an immunomodulatory effect by reducing the overexpression of the major histocompatibility antigen MHC-1 on the liver cell membrane; inhibiting the production of interleukins-2, 4, tumor necrosis factor and interferon α; increasing the levels of interleukins-10 and 12 in the body; and directly binding to glucocorticoid receptors. In addition, ursodeoxycholic acid also has the effects of inhibiting cell apoptosis, inhibiting inflammation, scavenging free radicals and anti-oxidation.
Product Specification
| Item | Specification | Results |
| Appearance | White powder | Complies |
| Identification | Meets the requirements | Complies |
| Heavy Metals | ≤10ppm | 5ppm |
| Iron | ≤10ppm | 3ppm |
| Chloride | ≤0.05% | 0.01% |
| Arsenic | ≤2ppm | 0.5ppm |
| Loss on Drying | ≤1.0% | 0.3% |
| Redidue on Ignition | ≤0.1% | 0.06% |
| Assay | ≥98.0% | 99.37% |
| Conclusion: | Conform with enterprise specification. | |
What are the effects of ursodeoxycholic acid?
Ursodeoxycholic acid powder usually has the effects of promoting bile secretion, regulating bile secretion, improving liver function, protecting liver cells, and relieving bile stasis.
1. Promoting bile
Ursodeoxycholic acid can increase the secretion of bile acid, and can also inhibit the absorption of cholesterol in bile, thereby increasing the excretion of cholesterol in bile, playing a role in promoting bile secretion.
2. Regulating bile secretion
Ursodeoxycholic acid can increase the bile acid content in bile, thereby improving bile secretion and helping to relieve the discomfort caused by reduced bile secretion.
3. Improving liver function
Ursodeoxycholic acid can improve liver function, mainly by promoting the regeneration of liver cells, thereby achieving the effect of improving liver function.
4. Protecting liver cells
Ursodeoxycholic acid can protect liver cells, mainly by inhibiting the cholesterol content in the liver, thereby achieving the effect of protecting liver cells.
5. Relieving bile stasis
Ursodeoxycholic acid can relieve bile stasis, mainly by promoting the excretion of bile, thereby achieving the effect of relieving bile stasis.
HTML5 atlas of Ursodeoxycholic acid
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IR1 of Ursodeoxycholic acid
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What are the main effects of Ursodeoxycholic acid?
1. Cytoprotective effect. UDCA conjugates can significantly reduce the cell lysis of hepatocytes induced by hydrophobic bile acid and reduce the apoptosis of cultured rat and human hepatocytes induced by toxic bile acid.
2. Membrane stabilizing effect. UDCA can prevent the changes in the permeability of mitochondrial membranes induced by bile acid, that is, it can prevent the damage of mitochondrial membranes, basement membranes and small bile duct membranes induced by toxic bile acid through membrane stabilization.
3. Antioxidant effect. UDCA can inhibit the activation of Kupffer cells caused by toxic bile acid, and can also increase the levels of glutathione and thiol-containing proteins in hepatocytes to prevent oxidative damage to hepatocytes.
4. Immunomodulatory effect. UDCA indirectly inhibits by reducing the stimulation of hydrophobic bile acid, and directly inhibits the expression of class I and class II genes of the histocompatibility complex (MHC) by activating glucocorticoid receptors.
What is the difference between ursodeoxycholic acid, hyodeoxycholic acid and chenodeoxycholic acid?
Chenodeoxycholic acid
Effects of chenodeoxycholic acid: This product is one of the most widely used drugs for the treatment of gallstones in the world, and it is also the raw material for the synthesis of ursodeoxycholic acid (UDCA) and other steroid compounds.
The main function of chenodeoxycholic acid (CDCA) is to reduce the saturation of cholesterol in bile, and cholesterol is in an unsaturated state, so that the cholesterol in the stones dissolves and falls off. Large doses of CDCA can inhibit the synthesis of cholesterol and increase the secretion of bile in patients with cholelithiasis, but the secretion of bile salts and phospholipids remains unchanged.
Hyodeoxycholic acid
Effects of hyodeoxycholic acid: This product is a bile acid extracted from pig bile. It can inhibit the formation of bile acid and dissolve fat, reduce blood cholesterol and triglycerides, and is suitable for type ⅰa or ⅰb hyperlipidemia and atherosclerosis. It has a certain antibacterial effect on Bordetella pertussis, Bordetella diphtheria, Staphylococcus aureus, etc. It can be used as an anti-inflammatory drug to treat chronic bronchitis, viral upper respiratory tract inflammation in children, etc. This product can stimulate bile secretion, making bile thinner without increasing the amount of solids; it can also accelerate the excretion of cholecystography contrast agent from the liver and help with imaging. It can also promote intestinal fat decomposition and fat-soluble vitamin absorption, and can be used for indigestion caused by hepatobiliary diseases.
Ursodeoxycholic acid
Ursodeoxycholic acid effects: cholesterol gallstones. Primary cholestatic cirrhosis, primary sclerosing cholangitis. Bile reflux gastritis. This product is used for cholesterol gallstone formation and bile deficiency steatorrhea, and can also be used to prevent drug-induced stone formation and treat steatorrhea.
What are the precautions for using Ursodeoxycholic Acid powder?
1. Long-term use of Ursodeoxycholic Acid Powder can increase the number of peripheral platelets.
2. If there are repeated episodes of biliary colic in the treatment of cholesterol stones, the symptoms are not improved or even aggravated, or obvious calcification of stones occurs, the treatment should be stopped.
3. Ursodeoxycholic Acid can't dissolve bile pigment stones, mixed stones and X-ray opaque stones.
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