Abstract
The aim of the present study was to develop an olanzapine freeze-dried tablet (FDT). The solubility and dissolution rate of poorly water-soluble olanzapine was improved by preparing a freeze-dried tablet of olanzapine using the freeze-drying technique . The FDT was prepared by dispersing the drug in an aqueous solution of highly water-soluble carrier materials consisting of gelatin, glycine, and sorbitol. The mixture was poured in to the pockets of blister packs and then was subjected to freezing and lyophilisation. The FDT was characterised by DSC, XRD and SEM and was evaluated for saturation solubility and dissolution. The samples were stored in a stability chamber to investigate their physical stability. Results obtained by DSC and X-ray were analysed and showed the crystalline state of olanzapine in FDT transformation to the amorphous state during the formation of FDT. Scanning electron microscope (SEM) results suggest reduction in olanzapine particle size. The solubility of olanzapine from the FDT was observed to be nearly four and a half times greater than the pure drug. Results obtained from dissolution studies showed that olanzapine FDT significantly improved the dissolution rate of the drug compared with the physical mixture (PM) and the pure drug. More than 90% of olanzapine in FDT dissolved within 5 minutes, compared to only 19.78% of olanzapine pure drug dissolved over the course of 60 minutes. In a stability test, the release profile of the FDT was unchanged, as compared to the freshly prepared FDT after 90 days of storing.
Highlights
Olanzapine, 2-methyl-4-(4-methyl1-piperazinyl)-10H-thieno-[2, 3b], [1, 5] benzodiazepine is a potent antipsychotic agent
Olanzapine belong to class II category under the biopharmaceutical classification system (BCS), i.e., it is inherently highly permeable through biological membranes, but exhibits low aqueous solubility
The matrix of the freeze-drying rapid dissolving tablets (RDT) consists of two components that work together to ensure the development of a successful formulation
Summary
Olanzapine, 2-methyl-4-(4-methyl1-piperazinyl)-10H-thieno-[2, 3b], [1, 5] benzodiazepine is a potent antipsychotic agent. There is wide availability of literature describing the preparation of RDT by freeze-drying, the number of matrix-supporting/disintegration-enhancing agents used has been limited to saccharides and polyols, with the majority of the work dedicated to the inclusion of mannitol (Segar, 1998; Corveleyn et al, 1998; Farhan et al, 2010). This is primarily because the incorporation of these matrix-forming agents requires fulfillment of stringent characteristics, such as reasonable drying time and stability during freeze-drying process, as well as formation of elegant tablets with short disintegration time and adequate mechanical properties. The present study aims to develop novel excipients by investigating the feasibility of using amino acids as matrix-supporting agents (second component) for the fabrication of RDT prepared by freeze-drying, in order to produce tablets with enhanced properties and wider application to the pediatric and geriatric patient population
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