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Development of midazolam sublingual tablets: in vitro study
P Odou1, C Barthelemy, H Robert
1Department of Clinical Pharmacy, Faculty of Pharmaceutical and Biological Sciences, Lille, France.
European Journal of Drug Metabolism and Pharmacokinetics
|September 2, 1998
Summary
This study developed 5 mg midazolam sublingual tablets for anesthesia, optimizing citric acid content for better drug absorption. The chosen formulation balances dissolution and membrane diffusion for effective sublingual delivery.
Area of Science:
- Pharmaceutical Sciences
- Pharmacology
Background:
- Midazolam, a short-acting benzodiazepine, is primarily used for general anesthesia.
- Currently, only injectable midazolam formulations are available in French hospital pharmacies.
Purpose of the Study:
- To develop 5 mg midazolam sublingual tablets for achieving short general anesthesia without injections.
- To optimize the formulation for enhanced sublingual drug delivery.
Main Methods:
- Investigated the effect of citric acid on midazolam dissolution and lipid membrane diffusion using Dibbern's Resomat apparatus.
- Analyzed midazolam ionization and precipitation in relation to pH and citric acid concentration.
Main Results:
- Incorporating citric acid increased midazolam dissolution rates.
- Higher citric acid concentrations (10 mg) decreased lipid membrane diffusion due to midazolam ionization.
- Midazolam precipitation at higher pH further reduced diffusion.
Conclusions:
- A sublingual formulation containing 5 mg of citric acid per tablet was selected as a compromise between dissolution and diffusion.
- This formulation offers a non-injectable alternative for midazolam administration.
- Optimized citric acid levels are crucial for effective sublingual midazolam delivery.