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Absorption kinetics of sublingually administered propranolol.

Journal of Medicine

|January 1, 1977

Summary

Buccal absorption of propranolol is incomplete, with only about 40% absorbed. Drug appearance in plasma is a separate, rate-limiting step from oral cavity uptake.

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Area of Science:

Pharmacokinetics
Drug Delivery Systems
Oral Mucosal Absorption

Background:

Buccal drug administration offers potential for rapid systemic drug delivery.
Understanding the kinetics of propranolol absorption from the buccal cavity is crucial for optimizing its use.

Purpose of the Study:

To investigate the absorption kinetics of propranolol administered via the buccal route.
To differentiate between drug disappearance from the oral cavity and systemic absorption.

Main Methods:

Healthy male volunteers received 10 mg propranolol retained in the mouth for varying durations.
Analysis of both plasma and oral cavity drug concentrations.
Kinetic modeling of drug absorption and appearance in plasma.

Main Results:

Propranolol exhibited incomplete buccal absorption, with approximately 40% absorbed.
Disappearance from the oral cavity did not directly correlate with systemic absorption.
Buccal mucosal absorption followed first-order kinetics (half-life: 1-17 min).
Plasma appearance also followed first-order kinetics (half-life: 20-25 min).

Conclusions:

Buccal uptake and plasma appearance of propranolol are distinct processes.
Transport into the plasma represents the rate-limiting step in buccal absorption.
Findings provide insights into buccal absorption models for propranolol.

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