What are the guidelines for preparing Ursodiol (ursodeoxycholic acid) tablets?

Ursodiol Tablet Preparation Guidelines

Direct Answer

There are no specific guidelines for "preparing" ursodiol tablets themselves, as they are commercially available in ready-to-use tablet and capsule formulations; however, if you need to create a liquid suspension from tablets or capsules for patients who cannot swallow solid dosage forms, extemporaneous compounding protocols exist with documented stability data.

Commercial Formulations Available

• Ursodiol is commercially available as 300-mg capsules and 250-mg tablets 1
• No commercial liquid dosage form exists, necessitating extemporaneous compounding when liquid formulations are required 1

Extemporaneous Liquid Suspension Preparation

When Liquid Formulation is Needed

For patients unable to swallow tablets/capsules (pediatric patients, those with dysphagia), pharmacists can prepare stable liquid suspensions using validated compounding protocols.

Validated Preparation Method #1: Sweetened Suspension

• Formulation: Combine contents of 300-mg ursodiol capsules with glycerin, Ora-Plus, and orange syrup to achieve final concentration of 25 mg/mL 2
• Stability: Stable for 60 days when stored in amber plastic bottles at both room temperature (22-23°C) and refrigerated (2-6°C) 2
• Storage: Protect from light in amber plastic prescription bottles 2

Validated Preparation Method #2: Sugar-Free Base

• Formulation: Prepare suspensions at 50 mg/mL or 100 mg/mL concentrations using PCCA base SuspendIt (a sugar-free, paraben-free, dye-free, gluten-free thixotropic vehicle) 1
• Stability: Physically and chemically stable for 181 days (6 months) at both refrigerated (5°C) and room temperature (25°C) 1
• Advantages: The thixotropic vehicle thickens upon standing to minimize settling and becomes fluid upon shaking for convenient administration 1
• Drug retention: Maintains >97% of initial drug concentration throughout 181-day period 1

Critical Compounding Pitfall to Avoid

Do not prepare ursodiol in water alone without a suspending agent - this results in rapid settling and high variability in content uniformity, making dosing unreliable and potentially dangerous 2

Clinical Dosing Context (Not Preparation, But Relevant)

Standard Therapeutic Doses by Indication

• Primary biliary cirrhosis: 13-15 mg/kg/day is the optimal dose 3, 4
• Intrahepatic cholestasis of pregnancy: 10-15 mg/kg/day total daily dose, given in divided doses 5
• Gallstone prevention post-bariatric surgery: 500-600 mg daily 5

Dose-Response Evidence

• Doses of 13-15 mg/kg/day provide optimal biochemical improvement without additional benefit from higher doses (23-25 mg/kg/day) in primary biliary cirrhosis 4
• Lower doses (5-7 mg/kg/day) are significantly less effective 4