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Feasibility studies of utilizing disk intrinsic dissolution rate to classify drugs
Lawrence X Yu1, Alan S Carlin, Gordon L Amidon
1Food and Drug Administration, Office of Pharmaceutical Science, Center for Drug Evaluation and Research, 5600 Fishers Lane, Rockville, MD 20857, USA. yul@cder.fda.gov
International Journal of Pharmaceutics
|January 17, 2004
Summary
Disk intrinsic dissolution rate (DIDR) shows promise for determining drug solubility class membership. This method offers a reliable approach for classifying drug solubility, though further research is needed for regulatory use.
Area of Science:
- Pharmaceutical Sciences
- Drug Development
- Physical Chemistry
Background:
- Accurate drug solubility classification is crucial for predicting in vivo performance.
- The Biopharmaceutics Classification System (BCS) is widely used but relies on solubility data that can be variable.
- Intrinsic dissolution rate (IDR) offers a more intrinsic measure of a drug's dissolution properties.
Purpose of the Study:
- To evaluate the feasibility of using disk intrinsic dissolution rate (DIDR) for Biopharmaceutics Classification System (BCS) solubility class determination.
- To establish optimal parameters for the DIDR method using a model system.
- To compare DIDR-based classification with established BCS solubility classes for various model drugs.
Main Methods:
- Utilized a VanKel dissolution apparatus with a Wood's intrinsic dissolution die.
- Investigated the influence of compression force, dissolution volume, die position, and rotation speed on DIDR using furosemide and metoprolol.
- Determined DIDR for 15 model drugs across different pH values (1.2, 4.5, 6.8) and compared with BCS classification.
Main Results:
- Compression force, dissolution volume, and die position did not significantly impact DIDR.
- Proposed optimal parameters: 2000 psi compression force, 900 ml volume, 0.5 in. die position, and 100 rpm rotation speed.
- A strong correlation was observed between DIDR and BCS solubility class for 15 model drugs, with a proposed boundary of 0.1 mg/min/cm(2).
Conclusions:
- DIDR is a feasible method for assessing drug solubility class membership.
- The proposed DIDR method demonstrates good agreement with BCS classification, particularly for drugs with typical dose ranges.
- Further research and discussion are warranted before regulatory adoption of the DIDR method for solubility classification.