Ursodeoxycholic acid

METHOD OF PREPARATION

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Empty the ursodiol capsules and pulverize the powder thoroughly.

4. Add the glycerin and mix until smooth.

5. Add the Ora-Plus and mix well.

6. Add the orange syrup, then the syrup to volume, and mix well.

7. Package and label.

PACKAGING

Package in tight, light-resistant containers.

LABELING

Keep out of reach of children. Use only as directed. Shake well before taking.

STABILITY

A beyond-use date of 60 days can be used for this preparation.1,2

USE

Ursodiol oral liquid is used as an anticholelithogenic agent.

QUALITY CONTROL

Quality-control assessment can include weight/volume, pH (3.2 to 4.0), specific gravity, active drug assay, color, rheological properties/ pourability, physical observation, and physical stability (discoloration, foreign materials, gas formation, mold growth).3

DISCUSSION

Ursodiol is a naturally occurring bile acid that is present in small quantities in human bile. It suppresses the synthesis and secretion of cholesterol by the liver and inhibits intestinal absorption of cholesterol. It has been used for the dissolution of cholesterol-rich gallstones and in the treatment of chronic liver disease.4

Ursodiol USP (C^sub 24^H^sub 40^O^sub 4^, MW 392.57, ursodeoxycholic acid, Actigall) occurs as a white or almost white, crystalline powder. It is practically insoluble in water, and freely soluble in alcohol and in glacial acetic acid.2 Ursodiol capsules (Actigall) also contain colloidal silicon dioxide, ferric oxide, gelatin, magnesium stearate, cornstarch, and titanium dioxide. Ursodiol tablets (URSO 250) also contain microcrystalline cellulose, povidone, sodium starch glycolate, magnesium stearate, ethylcellulose, dibutyl sebacate, carnauba wax, hydroxypropyl methylcellulose, polyethylene glycol 3350, polyethylene glycol 8000, cetyl alcohol, sodium lauryl sulfate, and hydrogen peroxide.5

Glycerin (C^sub 3^H^sub 8^O^sub 3^, MW 92.1, glycerol, 1,2,3-propane triol) occurs as a clear, colorless, odorless, viscous, hygroscopic liquid with a sweet taste about two thirds as sweet as sucrose. It has a specific gravity of about 1.25 and a melting point of 17.8°C. It is miscible with water and 95% ethanol. It is hygroscopic and should be stored in airtight containers in a cool place.6

Ora-Plus is an oral suspending vehicle with a pH of approximately 4.2 and an osmolality of about 230 mOsm/kg. It contains purified water, microcrystalline cellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, sodium phosphate and citric acid as buffering agents, simethicone as an antifoaming agent, and potassium sorbate and methylparaben as preservatives.7

Orange Syrup NF contains not less than 450 mg and not more than 550 mg of citric acid in each 100 mL. It is prepared from sweet orange peel tincture (50 mL), citric acid anhydrous (5 g), talc (15 g), sucrose (820 g), and sufficient purified water to make 1000 mL. It is prepared using the technique of clarification by filtration. It should be preserved in tight containers and stored in a cold place.2

Syrup NF (simple syrup) is a clear, sweet vehicle used as a sweetening agent and the base for many flavored and medicated syrups. It contains 85% w/v sucrose in water and has a specific gravity of not less than 1.30. It should be stored in tight containers, preferably in a cool place.2

References

1. Mallett MS, Hagan RL, Peters DA. Stability of ursodiol 25 mg/mL in an extemporaneously prepared oral liquid. Am J Health Syst Pharm 1337; 54(12):1401-1404.

2. US Pharmacopeial Convention, Inc. USP-Pharmacists' Pharmacopeia. Rockville, MD: US Pharmacopeial Convention, Inc.; 2005: 377, 388, 408-431, 716.

3. Allen LV Jr. Standard operating procedure for quality assessment of oral and topical liquids. IJPC 1999; 3(2): 146-147.

4. Sweetman SC. MARTINDALE: The Complete Drug Reference. 33rd ed. London: Pharmaceutical Press; 2002:1677-1678.

5. [No author listed.] Physicians' Desk Reference. 58th ed. Montvale, NJ: Thomson PDR; 2004; 802-803, 3298-3299.

6. Price JC. Glycerin. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 257-259.

7. Ora-Plus [product information]. Minneapolis, MN: Paddock Laboratories, Inc.

Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2005
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