Comparative dose study of a theophylline sustained-release tablet formulation after repeated administrations

Area of Science:

• Pharmacology
• Pulmonology
• Drug Formulation

Background:

• Chronic obstructive pulmonary disease (COPD) management often involves bronchodilators like theophylline.
• Sustained-release formulations aim to improve patient compliance and maintain therapeutic drug levels.
• Understanding the pharmacokinetics of theophylline is crucial for optimizing COPD treatment.

Purpose of the Study:

• To evaluate the pharmacokinetic parameters of a sustained-release theophylline formulation in COPD patients.
• To determine the optimal dosage regimen for once-daily administration of theophylline.
• To assess theophylline plasma levels over time following single and multiple doses.

Main Methods:

• Two groups of COPD patients received different doses of sustained-release theophylline.
• Pharmacokinetic parameters were assessed after single drug administration.
• Theophylline plasma concentrations were measured at various time points (1, 2, 4, 8, 12, 24 hours).
• In a separate experiment, patients received once-daily dosing for nine days, with plasma levels monitored on specific days.

Main Results:

• Patients receiving 700 mg/day of theophylline showed plasma levels ranging from 8.49 to 20.99 µg/mL.
• Theophylline concentrations remained above 10 µg/mL at 24 hours post-administration in the 700 mg/day group.
• Single daily administration of sustained-release theophylline at a high dosage is required to maintain therapeutic concentrations.

Conclusions:

• High-dose, once-daily administration of sustained-release theophylline is effective in maintaining therapeutic drug levels in COPD patients.
• The study highlights the importance of dosage adjustment for sustained-release theophylline in COPD management.
• Optimizing theophylline dosing can lead to improved therapeutic outcomes for COPD patients.