What Is Ursodeoxycholic Acid?

Ursodeoxycholic acid, whose main component is 3a, 7-dihydroxy-5-cholestane-24-acid, is an organic compound, odorless and bitter. This product is soluble in ethanol and insoluble in chloroform; soluble in glacial acetic acid and soluble in sodium hydroxide test solution. It is used in medicine to increase the secretion of bile acids, change the composition of bile, reduce the cholesterol and cholesterol in bile, and help the cholesterol in gallstones to gradually dissolve.

Ursodeoxycholic acid, whose main component is 3a, 7-dihydroxy-5-cholestane-24-acid, is an organic compound, odorless and bitter. This product is soluble in ethanol and insoluble in chloroform; soluble in glacial acetic acid and soluble in sodium hydroxide test solution. It is used in medicine to increase the secretion of bile acids, change the composition of bile, reduce the cholesterol and cholesterol in bile, and help the cholesterol in gallstones to gradually dissolve.

Chinese name

Ursodeoxycholic acid

Foreign name

Ursodeoxycholic Acid

Main traits

White powder; odorless, bitter

Safety term

Avoid contact with skin and eyes

CAS number

128-13-2

EINECS number

201-483-2

Melting point

200-201

Boiling point

547.148 at 760 mmHg

Flash point

298.768

PSA

77.76000

LogP

4.47790

Brief introduction of ursodeoxycholic acid compounds

Ursodeoxycholic acid Basic information

Chinese name: Ursodeoxycholic acid

Chinese alias: 3, 7-dihydroxy-5-cholestane-24-acid; pig deoxycholic acid; isodeoxycholic acid; dihydroxycholic acid; 3, 6-dihydroxycholic acid; dihydroxychol Alkanoic acid; heparin; deoxyursolic acid; ursodeoxycholic acid; ursodeoxycholic acid;

Phonetic name: Xiongquyangdansuan

English name: Ursodeoxycholic Acid

English alias: 3alpha, 6alpha-Dihydroxy-5beta-cholan-24-oic acid; Pig Hyodeoxycholic acid; 3,6-dihydroxycholan-24-oic acid; (3alpha, 5beta, 6alpha, 8xi, 9xi, 14xi) -3,6 -dihydroxycholan-24-oic acid; (3alpha, 5beta, 6alpha) -3,6-dihydroxycholan-24-oic acid; 4-[(3R, 5R, 6S, 10R, 13R, 17R) -3,6-dihydroxy- 10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta [a] phenanthren-17-yl] pentanoic acid (3alpha, 6alpha) -3,6-dihydroxycholan-24-oic acid; (3alpha, 5beta, 6alpha) -3,6-dihydroxycholan-24-oate; Acidum Ursodesoxycholicum; Actigall; Chenodiol; CholitUrsan; Delursan; Destolit; UDCA ; Ursacol; URSO; Ursochol; Ursodiol; Ursofalk; Ursolvan; Usochol

CAS number: 128-13-2

EINE number: 204-879-3

Molecular formula: C ₂₄ H ₄₀ O ₄

Molecular weight: 392.57200

Exact mass: 392.29300

PSA: 77.76000

LogP: 4.47790

Physiochemical properties of ursodeoxycholic acid

Appearance and properties: white crystalline powder, odorless, bitter. The product is easily soluble in ethanol and insoluble in chloroform; soluble in glacial acetic acid and soluble in sodium hydroxide test solution.

Density: 1.128 g / cm ³

Melting point: 203-206ºC

Boiling point: 547.1ºC at 760mmHg

Flash point: 298.8ºC

Stability: stable under normal temperature and pressure

Storage conditions: sealed

Vapor pressure: 0mmHg at 25 ° C ^[1]

Ursodeoxycholic Acid Safety Information

Customs code: 2918199090

WGK Germany: 2

Danger category code: R36 / 37/38

Safety instructions: S24 / 25

RTECS number: FZ2000000

Dangerous goods mark: Xi ^[1]

Safety term

S24 / 25Avoid contact with skin and eyes.

Avoid contact with skin and eyes

Ursodeoxycholic acid uses

For the treatment of gallstones, cholestatic liver disease, fatty liver, various types of hepatitis, toxic liver disorders, cholecystitis, cholangitis and bile indigestion, bile reflux gastritis, eye diseases, etc. ^[1] .

Ursodeoxycholic acid pharmacopoeia standard

Ursodeoxycholic acid source (name), content (potency)

This product is 3, 7-dihydroxy-5-cholestane-24-acid. Calculated on dry basis, containing C ₂₄ H ₄₀ O ₄ shall not be less than 98.5%.

Ursodeoxycholic acid

This product is white powder; odorless and bitter.

This product is soluble in ethanol and insoluble in chloroform; soluble in glacial acetic acid and soluble in sodium hydroxide test solution.

Melting point

The melting point of this product (Appendix VIC of Part Two of the 2010 Pharmacopoeia) is 200-204 ° C.

Specific rotation

Take this product, weigh it accurately, add absolute ethanol to dissolve and quantitatively dilute it to make a solution containing 40mg per 1ml, and measure it according to the law (Appendix VI E of the second edition of the Pharmacopoeia, 2010 edition). The specific rotation is + 59.0 ° to + 62.0 ° .

Identification of ursodeoxycholic acid

(1) Take 10mg of this product, add 1ml of sulfuric acid and 1 drop of formaldehyde to dissolve, leave it for 5 minutes, and then add 5ml of water to form a blue-green suspension.

(2) The infrared light absorption spectrum of this product should be the same as that of the control ("Drug Infrared Spectra Collection" 534).

Ursodeoxycholic acid test

Foul smell

Take 2.0g of this product, add 100ml of water, and boil for 2 minutes, it should be odorless.

chloride

Take 1.0g of this product, add 10ml of glacial acetic acid, shake to dissolve, dilute to 100ml with water, shake well, let stand for 10 minutes, filter, and take 25ml of the filtrate, check it according to law (Appendix A of Part Two of the 2010 Pharmacopoeia), and the standard The control solution made from 5.0ml of sodium chloride solution must not be more concentrated (0.02%).

Sulfate

Take 40ml of the remaining filtrate under the above chloride and check it according to law (Appendix B of Part II of the Pharmacopoeia 2010), compared with the control solution made of 2.0ml of standard potassium sulfate solution, it must not be more concentrated (0.05%).

relative substance

Take this product, use acetone-water (9: 1) to make a solution containing 10mg per Im1 as the test solution; take the ursodeoxycholic acid reference substance and chenodeoxycholic acid reference substance, and use acetone-water (9: 1) Prepare a mixed solution containing 0.4mg per 1ml as the reference solution (1); take another chenodeoxycholic acid reference and use acetone-water (9: 1) to make each A solution containing 0.1mg was used as the reference solution (2); a bilestone reference was taken and a solution containing 0.01mg per 1ml was prepared with acetone-water (9: 1) as the reference solution (3); Acid reference substance, made with acetone-water (9: 1) containing a solution containing 0.05mg per 1ml, as the reference solution (4); accurately measure the test solution, quantify with acetone-water (9: 1) Dilute to make a solution containing 0.01, 0.02, and 0.05 mg per 1 ml, and use them as control solutions (1), (2), and (3), respectively. According to the thin-layer chromatography (2010 Appendix B Pharmacopoeia Part II) test, draw 5 l of each of the above eight solutions, point them on the same silica gel G thin-layer plate, and use dichloromethane-acetone-glacial acetic acid (60: 30: 3) ) As a developing agent, unfolded, air-dried, dried at 120 ° C for 10 minutes, sprayed with a 4.5% solution of phosphomolybdic acid in sulfuric acid-glacial acetic acid (1:20), and then heated at 120 ° C for 3 to 5 minutes, and inspected immediately. The reference solution (1) should show two spots; if the test solution shows impurity spots in the same position as the reference solution (2), its color must be darker than the main spot of the reference solution (2) (1.0%) ; If the spots of impurities that are the same as the reference solution (3), the color must not be darker than the main spots of the reference solution (3) (0.1%); if the spots are the same as the reference solution (4) The color of the spots must be darker than the main spots of the reference solution (4) and must not be darker (0.5%). The color of other spots must be the same as that of the main spots of the control solutions (1), (2), and (3). The amount must not exceed 0.5%.

Loss on drying

Take this product and dry it at 105 for 2 hours, and the weight loss shall not exceed 1.0% (Appendix L of Part Two of the Pharmacopoeia, 2010 Edition).

Residue on ignition

Take 1.0g of this product and check it according to law (Appendix N of Part Two of the 2010 Pharmacopoeia). The residual residue shall not exceed 0.2%.

Barium salt

Take the solution under the foul smell, add 2ml of hydrochloric acid, boil for 2 minutes, let cool, filter, and wash with water. Combine the washing solution with the filtrate to make 100ml, shake well; take 10ml, add 1ml of dilute sulfuric acid, no turbidity should occur.

Heavy metal

Take the residue left under the item of burning residue and check it according to law (Appendix H of the second edition of the Pharmacopoeia of 2010 Edition, the second method H), the content of heavy metals must not exceed 20 parts per million.

Arsenic salt

Take 1.0g of this product, add 10ml of 2% magnesium nitrate ethanol solution, ignite the ethanol, and slowly heat to ashing. If there is still carbonization, add a small amount of nitric acid to humidify, and continue heating (500 600 ) until the ashing is complete. Cold, add 21ml of water to dissolve, add 5ml of hydrochloric acid, check according to law (Appendix J of the second edition of the Pharmacopoeia of 2010 Edition J first method), should meet the requirements (0.0002%).

Determination of ursodeoxycholic acid

Take about 0.5g of this product, accurately weigh, add 40ml of neutral ethanol (Phenolphthalein indicator solution is neutral) and 20ml of freshly boiling and cold water. After dissolving, add 2 drops of phenolphthalein indicator solution and titrate with sodium hydroxide Liquid (0.1mol / L) titration, near the end point, add 100ml of freshly boiled cold water, continue to titrate to the end point. Each 1ml of sodium hydroxide titration solution (0.1mol / L) is equivalent to 39.26mg of C ₂₄ H ₄₀ O _{4 ^[2]} .

Ursodeoxycholic acid category

Gallstone dissolving medicine.

Ursodeoxycholic acid storage

Shaded and sealed.

Ursodeoxycholic acid preparation

Ursodeoxycholic acid tablets

Ursodeoxycholic acid version

Pharmacopoeia of the People's Republic of China 2010

Determination of ursodeoxycholic acid

Method name: Ursodeoxycholic Acid-Determination of Ursodeoxycholic Acid-Neutralization Titration

Scope of application: This method uses neutralization titration to determine the content of ursodeoxycholic acid (C ₂₄ H ₄₀ O ₄ ).

This method is suitable for the determination of ursodeoxycholic acid.

Principle of the method: Take an appropriate amount of the test product, add neutral ethanol (which is neutral to the phenolphthalein indicator solution) and freshly boiled cold water, add phenolphthalein indicator solution, and titrate with sodium hydroxide titration solution (0.1mol / L). 1mL sodium hydroxide titration solution (0.1mol / L) is equivalent to 39.26mg of C ₂₄ H ₄₀ O ₄ .

Reagent: 1. Water (new boiling to room temperature)

Neutral ethanol

3. Sodium hydroxide titration solution (0.1mol / L)

4. Phenolphthalein indicator liquid

5. Reference potassium phthalate

equipment:

Sample preparation: 1. Sodium hydroxide titration solution (0.1mol / L)

Preparation: Take an appropriate amount of sodium hydroxide, add water and shake to dissolve it into a saturated solution. After cooling, place it in a polyethylene plastic bottle and let it stand for several days. Take 5.6mL of a clear saturated sodium hydroxide solution, add freshly boiled cold water to 1000mL, and shake well.

Calibration: Take about 0.6g of standard potassium hydrogen phthalate dried to constant weight at 105 ° C, weigh it accurately, add 50mL of freshly boiled cold water, shake it to dissolve it as much as possible, add 2 drops of phenolphthalein indicator solution, When this solution is titrated, when the end point is reached, potassium hydrogen phthalate should be completely dissolved and titrated until the solution becomes pink. Each 1mL of sodium hydroxide titration solution (0.1mol / L) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of this solution based on the consumption of this solution and the amount of potassium hydrogen phthalate taken.

Storage: Put it in a polyethylene plastic bottle and keep it in a sealed container. There are 2 holes in the plug. One glass tube is inserted into the hole. One tube is connected to the soda lime tube. One tube is used to suck out the liquid.

Phenolphthalein indicator

Take 1 g of phenolphthalein and add 100 mL of ethanol to dissolve.

Operation steps: take 0.5g of this product, weigh it accurately, add 40mL of neutral ethanol (p-phenolphthalein indicator solution is neutral) and 20mL of freshly boiled cold water, after dissolving, add 2 drops of phenolphthalein indicator solution, titrate with sodium hydroxide (0.1mol / L) titration, near the end point, add 100mL of freshly boiled cold water, continue to titrate to the end point, each 1mL sodium hydroxide titration solution (0.1mol / L) is equivalent to 39.26mg of C ₂₄ H ₄₀ O ₄ .

Note 1: "Precise weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision weighing" means that the accuracy of the measured volume should conform to the national standard for the volume of the pipette. Precision requirements.

Note 2: "Determination of moisture" uses the drying method, taking 2 to 5 g of the test sample, and spreading it in a flat weighing bottle that is dry to constant weight, the thickness is not more than 5 mm, and the loose test sample is not more than 10 mm. Open the bottle cap and dry it at 100 105 for 5 hours. Place the cap on the dryer, cool it for 30 minutes, and weigh it precisely. Then dry it at the above temperature for 1 hour, cool it, and weigh it twice. The difference in weighing does not exceed 5 mg. Calculate the moisture content (%) in the test product based on the weight lost.

Ursodeoxycholic acid drug description

Ursodeoxycholic acid classification

Digestive System Drugs> Cholesterol Drugs

Ursodeoxycholic acid dosage form

1. Tablet: 50mg, 150mg;

2. Capsule: 250mg.

Pharmacological effects of ursodeoxycholic acid

1. Increase the secretion of bile acids, leading to changes in the composition of bile acids, increasing their content in the bile, which is beneficial to the bile effect. The average bile acid secretion of patients increased from 1.8mmol to 2.24mmol per hour. Long-term use can increase the content of UDCA in bile without increasing the content of bile acid.

2. Can inhibit the synthesis of cholesterol in the liver, significantly reduce the amount of cholesterol and cholesterol ester in bile and the saturation index of cholesterol, which is conducive to the gradual dissolution of cholesterol in stones. In addition, UDCA can promote the formation of liquid cholesterol crystal complexes, which can accelerate the excretion of cholesterol from the gallbladder to the intestine.

3. Relaxing Oddi sphincter, which has a beneficial effect on bile.

4. Reduce liver fat, increase liver catalase activity, promote the accumulation of liver glycogen, and improve the liver's ability to resist and detoxify.

5. Can reduce the concentration of triacylglycerol in liver and serum.

6. Inhibit the secretion of digestive enzymes and digestive juices.

7. Foreign studies have also shown that ursodeoxycholic bile cholic acid has an immunoregulatory effect in chronic liver diseases, which can significantly reduce the expression of HLAI-like antigens in liver cells and reduce the number of activated T cells. Ursodeoxycholic acid dissolves cholesterol stones in the body better than chenodeoxycholic acid (CDCA) ^[3] .

Pharmacokinetics of Ursodeoxycholic Acid

Ursodeoxycholic acid is weakly alkaline and is rapidly absorbed by passive diffusion after oral administration. The most effective part of absorption is the ileum in a moderately alkaline environment. The bioavailability is 90% and the total protein binding rate is 70%. Ursodeoxycholic acid is taken up 5% to 60% through the liver, which is significantly lower than chenodeoxycholic acid, only a small amount of the drug enters the systemic circulation, and the blood concentration is very low. Two peak plasma concentrations appeared at 1 h and 3 h after oral administration. When used for dissolving gallstones, it takes effect 3 to 6 months after oral administration. The therapeutic effect of ursodeoxycholic acid does not depend on the blood drug concentration but is related to the drug concentration in the bile. The half-life is 3.5 to 5.8 days. Ursodeoxycholic acid is rapidly combined with glycine or taurine in the liver, is excreted from the bile into the small intestine, and participates in the hepato-intestinal circulation. Part of the ursodeoxycholic bile cholic acid incorporated in the small intestine is hydrolyzed back to the free form, and another part is converted to lithocholic acid by the action of bacteria, which in turn is sulfated to reduce its potential liver toxicity. Ursodeoxycholic acid is mainly excreted with feces and a small amount is excreted by the kidneys. Whether ursodeoxycholic acid is excreted in human milk is unclear. Only a small amount is excreted by the kidneys after oral administration. Whether ursodeoxycholic acid is excreted in human milk is unclear. Since only a small amount of ursodeoxycholic bile acid appears in the serum after oral administration, if it is present in the milk, its amount is also very small ^[3] .

Ursodeoxycholic acid indication

1. Suitable for non-calcified stones with normal gallbladder function, light transmission, and diameter of 10 ~ 15mm.

2. Prevention of gallstone formation: patients who need long-term use of drugs that easily form cholesterol stones (such as estrogen, clobetin and its derivatives, cholestyramine), those who have been on a high cholesterol diet for a long time, or have susceptible inheritance Factors can take ursodeoxycholic acid to prevent gallstone formation.

3. Treatment of cholecystitis, cholangitis, biliary dyspepsia, jaundice, etc.

4. Treatment of fatty diarrhea, hypertriglyceridemia, hepatomegaly, chronic hepatitis after ileal resection, can also be used for bile reflux gastritis.

5. Also used for primary biliary cirrhosis and primary sclerosing cholangitis.

Contraindications to ursodeoxycholic acid

1. Severe hepatitis and severe liver dysfunction.

2. Those with complete biliary obstruction.

3. Stomach, duodenal ulcer and other intestinal diseases.

4. Those who are allergic to bile acids.

5. Patients with indications for cholecystectomy, including persistent acute cholecystitis, cholangitis, gallstone pancreatitis, or biliary gastrointestinal fistula.

6. Banned for pregnant women, children and breastfeeding women.

Ursodeoxycholic acid precautions

Ursodeoxycholic acid cannot dissolve bile pigment stones, calcified cholesterol stones, mixed stones, and radiopaque stones.

Ursodeoxycholic acid adverse reactions

1. Mainly diarrhea, the incidence is about 2%. Occasionally constipation, stomach pain, pancreatitis and so on.

2. Hepatotoxicity: Ursodeoxycholic acid is not toxic to the liver.

3. Respiratory system: Foreign data report that there may be adverse reactions to the respiratory system such as bronchitis, cough, and pharyngitis.

4. Central nervous system: occasional headaches, dizziness, etc.

5. Skin: Itching, hair loss, etc. may occur.

6. Musculoskeletal: joint pain, arthritis, back pain and myalgia can occur.

7. Carcinogenic and mutagenic effects: Animal experiments have not found ursodeoxycholic acid to have mutagenic effects. Observation under light and electron microscopy has not found structural changes in liver cells after incubation with ursodeoxycholic acid. Animal tests (mouse and rat) have shown that ursodeoxycholic acid is not carcinogenic at 5.4 times the maximum dose.

8. Others: occasional allergies, bradycardia, tachycardia, etc. ^[3] .

Ursodeoxycholic acid usage dosage

1. Cholesterol: 50mg each time, 150mg per day.

2. Dissolved gallstones: 450 to 600 mg per day, or 8 to 10 mg / kg per day, divided into two servings morning and evening. When gallstones are cleared, 500 mg orally every night to prevent recurrence.

3. Hepatomegaly and chronic hepatitis: 8 to 13 mg / kg per day for 6 to 24 months.

4. Bile reflux gastritis: 1,000 mg per day, divided into 2 doses.

Ursodeoxycholic acid drug interactions

1. The combination of ursodeoxycholic acid and chenodeoxycholic acid, the reduction of cholesterol content and saturation in bile is greater than the two drugs alone, and it is greater than the additive effect of the two drugs. This may be related to the different mechanisms of action of the two drugs on cholesterol synthesis, metabolism, and dissolution kinetics.

2. Oral contraceptives can increase bile saturation and affect the efficacy of ursodeoxycholic acid, so other birth control measures should be taken when treating with ursodeoxycholic acid.

3. Medicinal charcoal can bind bile acids in in vitro tests, so the combination with ursodeoxycholic acid will affect the absorption of the latter.

4. Aluminum-containing antacids can absorb bile acids in in vitro tests, so when combined with ursodeoxycholic acid, it can reduce the absorption of ursodeoxycholic acid.

5. Because cholestyramine and colestipol can bind bile acids in in vitro tests, it can interfere with the absorption of the latter when combined with ursodeoxycholic acid.

Ursodeoxycholic acid expert review

Ursodeoxycholic acid was previously used to treat gallstone disease, which can dissolve cholesterol stones, and is now also used to treat cholestatic diseases. Domestic ursodeoxycholic bile cholic acid is not pure, which contains chenodeoxycholic bile cholic acid, which can dissolve gallstones, but the protective effect on hepatocytes is far less than that of UDCA. It is clinically used for cholestasis of hepatocytes. That's good. It has a higher cure rate for non-calcified floating cholesterol stones.

Ursodeoxycholic acid liver disease treatment

Ursodeoxycholic acid (3, 7-dihydroxy-5-cholic acid, UDCA) is a dihydroxycholic acid that accounts for 3% of human total bile. It was first named after Shoda from Okayama University in Japan was isolated from Chinese bile bile. Leuschner et al. Found a decrease in serum transaminase when they used it to treat gallstones with hepatitis in 1985. Since then, a large number of clinical studies have confirmed that UDCA has exact treatment for some liver diseases effect. Its mechanism of action and efficacy are briefly described below:

Mechanism of ursodeoxycholic acid

Cholestatic liver disease is associated with the accumulation of chenodeoxycholic acid, deoxycholic acid, and lithocholic acid, which cause liver cell damage due to the descaling effect. UDCA is a non-toxic hydrophilic bile acid that competitively inhibits the absorption of toxic endogenous bile acid in the ileum. By activating the signal network composed of calcium ions and protein kinase C, and enhancing the secretory capacity of cholestatic liver cells by activating split active protein kinases, the endogenous concentration of hydrophobic bile acids in blood and liver cells is reduced to achieve anti-cholestasis. effect. UDCA can also competitively replace toxic bile acid molecules on cell membranes and organelles, preventing liver cells and bile duct cells from being damaged by more toxic bile acids. The above effects are specifically manifested in: (1) cytoprotective effects. UDCA conjugates can significantly reduce the lysis of hepatocytes induced by hydrophobic cholic acid and reduce the apoptosis induced by toxic cholic acid in cultured rat and human hepatocytes. (2) Film stabilization. UDCA prevents bile acid-induced changes in mitochondrial membrane permeability, that is, it can prevent toxic bile acid-induced damage to mitochondrial membranes, basement membranes, and small bile duct membranes through membrane stabilization. (3) Antioxidant effect. UDCA can inhibit the activation of Kupffer cells caused by toxic bile acid, and can increase the levels of glutathione and thiol-containing proteins in liver cells, preventing oxidative damage to liver cells. (4) Immune regulation. UDCA inhibits indirectly by reducing the stimulation of hydrophobic cholic acid, and directly inhibits the expression of histocompatibility complex (MHC) class I and II genes by activating the glucocorticoid receptor.

Clinical application of ursodeoxycholic acid

Primary biliary cirrhosis (PBC). PBC is a chronic progressive cholestatic liver disease that mainly occurs in middle-aged women and may be related to immune factors. Pares et al. Conducted a trial with an average biopsy interval of 4.5 years. It was found that UDCA did prevent the progression of histological stages of PBC. In 1999, Angulo et al reported that in a long-term treatment trial of UDCA in non-cirrhotic PBC patients (average 6.6 years), the time to cirrhosis in the treatment group was delayed compared with patients receiving the ineffective treatment group. In most UDCA treatment trials, a dose of 13 to 15 mg / kg per day is used. Two recent studies aimed at exploring the appropriate dose of UDCA found that the daily doses of 13 to 15 mg / kg and 20 to 25 mg / kg were better than 10 to 15 mg / kg or less. The efficacy of UDCA combined with methotrexate or colchicine in the treatment of PBC is not better than that of UDCA alone; but in combination with prednisone or prednisone plus azathioprine, its efficacy in improving inflammation is significantly better than that of UDCA alone.

Primary sclerosing cholangitis (PSC). PSC is a rare cholestatic disease that manifests as narrow and dilated bile ducts inside and outside the liver. A recent prospective randomized placebo-controlled trial consisting of 105 patients with an average treatment time of 2.2 years (UDCA 13-15 mg / kg daily) showed significant improvement in patients' biochemical indicators, clinical symptoms, and liver histology There were no significant changes. However, for obvious bile duct strictures, UDCA combined with endoscopic treatment can improve the prognosis of patients.

Intrahepatic cholestasis of pregnancy (ICP). ICP often occurs in late pregnancy. The main symptoms are pruritus and jaundice in pregnant women, which can cause complications such as premature delivery, stillbirth and stillbirth. It is believed to be genetically related to elevated estrogen in the body. A randomized, double-blind, placebo-controlled trial of UDCA in the treatment of IPC included 15 patients with improvement in pruritus and liver biochemical parameters in the treatment group. Eight pregnant women (receiving UDCA 1.0 g / day) delivered at or near the due date; placebo Five of the seven pregnant women who were treated gave birth at 36 weeks of gestation, and one of them was stillborn. No maternal and infant side effects occurred during treatment. Therefore, UDCA seems to be effective and safe in the treatment of ICP.

Gallbladder fibrosis liver disease (CF). In a follow-up double-blind placebo-controlled trial involving 55 patients, Colom bo et al compared UDCA treatment (15 mg / kg daily) to placebo after 1 year. It was found that symptoms, nutritional status, and biochemical indicators in the treatment group were significantly improved. VandeMeeberg and SulliVan et al. Reported that higher doses of UDCA (20 mg / kg daily) are more effective than lower doses (5 to 15 mg / kg daily).

Chronic hepatitis C. In 2001, several randomized placebo-controlled trials of UDCA combined with -interferon in the treatment of chronic hepatitis C reported that biochemical indicators improved after treatment, but they were not effective in clearing hepatitis C virus (HCV) -RNA and did not change liver histological characteristics .

other. Studies have shown that UDCA combined with cyclosporine A and methotrexate for heterotopic bone marrow transplantation can prevent venous occlusion and acute graft-versus-host disease. UDCA at 15 mg / kg daily can improve the symptoms and biochemical indicators of cholestasis of progressive familial intrahepatic cholestasis, bile duct atresia, and total parenteral nutrition-related liver disease. UDCA has also been used to treat other liver diseases, such as alcoholic liver disease, non-alcoholic fatty liver, benign recurrent intrahepatic cholestasis, congenital intrahepatic bile duct cystic dilatation, autoimmune hepatitis and acute hepatitis The efficacy needs to be further evaluated ^[4] .