Correlation between dissolution characteristics and absorption of methaqualone from solid dosage forms.
A methaqualone tablet in two strengths, 150 and 300 mg, was developed. The dissolution rate of an experimental formulation in pH 7.0 phosphate buffer, measured by the resin flask method, was shown to correlate with bioavailability in humans. The dissolution rate criterion was used to develop the final tablet formulation. Bioavailability of this formulation in two strengths was compared with a commercial capsule formulation and a slowly dissolving tablet formulation. Correlation between dissolution rate and bioavailability was shown in freshly prepared methaqualone tablet formulations. Bioavailability of tablets under accelerated stability testing conditions remained unaltered, whereas the dissolution rates in pH 7 phosphate buffer decreased, using the resin flask method. A rotating-flask method was developed, and dissolution in 0.1 N HCl at 2 rpm correlated with the bioavailability of both new and aged tablet formulations.
D000042:Absorption; D001682:Biological Availability; D002214:Capsules; D004355:Drug Stability; D008702:Methaqualone; D012995:Solubility; D013607:Tablets; D013997:Time Factors
D002214:Capsules; D013607:Tablets; D008702:Methaqualone