ABSTRACT
Objective The article was to speed up the dissolution rate of poorly soluble drugs, reduce the configuration time and improve the allocative efficiency by analysis on factors influencing dissolution and adoption of proper allocative approaches accord-ing to different characteristics of insaluble drugs. Methods 5 insaluable drugs were chosen for the study, which were ornithine as-partate, mezlocillin sodium and sulbactam sodium, teicoplanin, omeprazole sodium injection and imipenem and cilastatin sodium.The control group were allocated by routine configuration approach, while the experiment group were improved by increasing the amount of solvent, loosing the powder inside the bottle before configuration, reducing the bubble, adopting special solvent and increasing the dis-solution temperature.Observation and comparative experiment were made on two groups along with the timing from configuration to com-plete dissolution into clear transparent liquid. Results As to the average complete dissolution time of 5 drugs, significant difference was found between two groups([42±5]s vs [246±35]s, [3±1]min vs [30±3]min, [5±1]min vs [10±3]min, [5±3]min vs [10± 5]min, [2±1]min vs [10±1]min, P<0.05).Compared with the control group, the dissolution time of 5 drugs was cut down by 83%, 90%, 50%, 50%, 80%in experiment group. Conclusion Appropriate increase of solvent, loose powder, bubble reduction, special solvent and increased solution temperature contribute to shortening the dissolution time of insoluble drugs and improving the configura-tion efficiency of pharmacy intravenous admixture.
ABSTRACT
The present study has investigated various ways to formulate a bi-layer tablet dosage form containing an immediate release and a sustained release portion of a neuroprotective compound named vinpocetine. The bi-layer matrix tablet was prepared by simple compression of the SR granules and IR granules of vinpocetine. The sustained release effect of vinpocetine was achieved with polymers methocel K15M CR, kollidon SR and carbomer 934P. Physical properties of powders, granules and the finished tablets were evaluated. The drug release study of the tablets was studied for 2 hours in 0.1N HCl followed by 8 hours in pH 6.8 phosphate buffer as media using United States Pharmacopoea (USP) XXII paddle type dissolution apparatus. The effect of above mentioned polymers on vinpocetine release profile was investigated. The MDT values of all the formulations were calculated and correlated with the rate retardation capacity of drug release of the polymers used. The release rate of vinpocetine immediate release layer was found to be influenced little by kollidon CL and direct compressible grade lactose. The release rate, extent and mechanisms of sustained release layers were found to be governed by the nature and the extent of the polymer used in the formulation. Kinetic modeling of dissolution profiles reveled that vinpocetine release mechanism ranges from the anomalous / non – fickian transport to super case II transport in the given situations. These studies indicated that the proper balance between a matrix forming agent and a channeling agent can produce a drug dissolution profile similar to a theoretical dissolution profile will overcome the disadvantages of conventional tablets of vinpocetine.