Search for technological reasons to develop a capsule or a tablet formulation with respect to wettability and dissolution.
Proquazone, a poorly wettable compound, was used as a model drug in the search for reasons to develop a capsule or tablet formulation. The capsules were filled with proquazone as active ingredient, with lactose monohydrate (200 mesh) as filler and with magnesium stearate as lubricant. The tablet was made out of a granulate as internal phase which consisted of proquazone as active ingredient, lactose as filler, corn starch as disintegrant and PVP as a binding agent. The external phase consisted of magnesium stearate and corn starch. The concentration of proquazone in the capsule and in the tablet formulation was varied. The capsule formulations showed a significantly slower dissolution of the drug substance than the tablet formulations especially for a high-drug load. Independently of the drug load, only the tablet formulation showed a high-dissolution rate. Thus, concerning drug load, only the tablet formulations showed to be robust. It became clear that proquazone needs to be formulated as a granulate or a tablet to achieve a fast dissolution rate. Thus, a poorly wettable drug, especially when it is found in high concentrations, can have direct impact on the decision to develop a tablet or a capsule formulation.
von Orelli
Johannes
J
Institute of Pharmaceutical Technology, Pharmacenter, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.
Leuenberger
Hans
H
D002214:Capsules; D002626:Chemistry, Pharmaceutical; D011799:Quinazolines / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical; D017155:Wettability
D002214:Capsules; D011799:Quinazolines; D013607:Tablets; C011385:proquazone