Dissolution Kinetics of Single Crystals of α-Lactose Monohydrate

Abstract The dissolution kinetics of α‐lactose monohydrate (αLM) single crystals were studied by a flow‐cell method at different undersaturations. Linear dissolution profiles were obtained as a function of time for all the faces except the (010) face. The dissolution rates, obtained from these profiles, were anisotropic and varied considerably with undersaturation. At low undersaturations (0–2%), the order of dissolution rate was (110) > (100) > (011) = (110) > (010). This order changed with increasing undersaturation (>5%) to (011) >> (100) > (110) > (110) > (010). In αLM crystals in which lattice strain was induced by synchrotron X‐irradiation, the rates of dissolution of all faces increased with increasing strain. The increase was less significant for the (011) faces than for the remainder. Under this constraint, the (010) face became the fastest dissolving one and the {011}face became the slowest one. The results of all experiments are explained on the basis that although dislocations may act as initiating dissolution centers at very low undersaturations, these sources rapidly give way to two‐dimensional nucleation of randomly distributed dissolution sites as the undersaturation is increased. Under these conditions, which better reflect the normal dissolution processes of materials, bulk lattice strain plays the most significant role in defining the dissolution rate. The results show a potential route to the controlled engineering of the dissolution behavior of crystalline materials. © 2002 Wiley‐Liss Inc. and the American Pharmaceutical Association J Pharm Sci 91:2166–2174, 2002