Metabolism / Metabolites
The known human metabolites of isursodeoxycholic acid include 4-(7-hydroxy-10,13-dimethyl-3-oxo-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecylhydrocyclopenta[a]phenanthrene-17-yl)valerate and 3,6,7-trihydroxycholan-24-acid.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Ursodeoxycholic acid (UCCA) is naturally present in breast milk. Due to the low levels of UCCA in breast milk after exogenous administration, and the minimal intake by the infant, no adverse effects are expected on breastfed infants. Usodeoxycholic acid has been used directly in newborns, safely and effectively treating neonatal jaundice. No special precautions are required.
◉ Effects on Breastfed Infants
One breastfed infant (feeding extent not specified) developed normally in the first 6 months after birth, with the mother taking 750 to 1000 mg of UCCA daily.
Seven women took 14 mg/kg of UCCA daily near delivery and postpartum. They reported no adverse reactions in breastfed infants in the early postpartum period.
A mother with primary biliary cirrhosis reportedly took 250 mg of ursodeoxycholic acid three times daily and breastfed her infant normally, but the extent and duration of breastfeeding were not specified.
A woman with primary biliary cirrhosis developed severe itching and elevated serum bile acids three weeks postpartum. She started taking ursodeoxycholic acid at a dose of 500 mg (7.5 mg/kg) daily, increasing to 1500 mg (25 mg/kg) daily over the next eight weeks. Her breastfed infant (feeding extent not specified) showed normal psychomotor development, and no significant side effects were observed.
A retrospective analysis of medical records of pregnant women diagnosed with primary biliary cirrhosis at a hospital in Ankara, Turkey, found that eight patients took ursodeoxycholic acid postpartum at a dose of 13-15 mg/kg daily. "Most" of these patients breastfed their infants (feeding extent not specified). No side effects were reported in the infants.
A woman breastfed her 8-day-old premature infant 10 times a day, each time for about 15 minutes. The infant was delivered by cesarean section at 34 weeks of gestation, weighing 3600 grams. She was diagnosed with cholestasis, type 1 diabetes, and hypothyroidism. She received ursodeoxycholic acid 500 mg/day, insulin Lantus and aspart, and levothyroxine. She also took cefuroxime, flurbiprofen, and a combination of acetaminophen, disopyrfenone, and caffeine. The mother took ursodeoxycholic acid for 12 days, cefuroxime and the above-mentioned combination analgesics for 10 days, and flurbiprofen for 15 days. No adverse reactions were observed during ursodeoxycholic acid treatment.
Twenty lactating women with cholestasis received ursodeoxycholic acid at a daily dose of 500 to 1500 mg or 13 to 15 mg/kg, depending on their condition. Ursodeoxycholic acid was discontinued 3 days postpartum. Based on standard clinical examinations of newborns in the early postnatal period, no significant side effects were observed in any newborns; no postnatal developmental deterioration was also observed during a one-year follow-up period following routine pediatric examinations.
◉ Effects on breastfeeding and lactation
As of the revision date, no relevant published information was found.

[1]. Study of human isoursodeoxycholic acid metabolism.Journal of Hepatology.Volume 26, Issue 4, April 1997, Pages 863-870.

[2]. Metabolism and effects on cholestasis of isoursodeoxycholic and ursodeoxycholic acids in bile duct ligated rats. Biochim Biophys Acta. 2001 Apr 3;1526(1):44-52.

Isursodeoxycholic acid is a dihydroxy-5β-cholanic acid, formed by replacing the β-hydroxy groups at the 3 and 7 positions of (5β)-cholan-24-acid. It is a human metabolite and the conjugate acid of isursodeoxycholic acid salt.

C₂₄H₄₀O₄

392.57

392.293

78919-26-3

Ursodeoxycholic acid-2,2,4,4-d4;347841-46-7

127601

White to off-white solid powder

1.128g/cm3

547.1ºC at 760 mmHg

298.8ºC

1.543

4.477

3

4

4

28

605

10

C[C@@]12[C@@H]([C@H](C)CCC(=O)O)CC[C@H]1[C@@H]1[C@@H](O)C[C@@H]3C[C@H](CC[C@]3(C)[C@H]1CC2)O

RUDATBOHQWOJDD-DNMBCGTGSA-N

InChI=1S/C24H40O4/c1-14(4-7-21(27)28)17-5-6-18-22-19(9-11-24(17,18)3)23(2)10-8-16(25)12-15(23)13-20(22)26/h14-20,22,25-26H,4-13H2,1-3H3,(H,27,28)/t14-,15+,16+,17-,18+,19+,20+,22+,23+,24-/m1/s1

(4R)-4-[(3S,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-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

Isoursodeoxycholic acid 3βUrsodeoxycholic acid 3β Ursodeoxycholic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~254.73 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)