Micronization of Organic Drugs and Discussion of Shape Changes by Microemulsion and Antisolvent System
Date Issued
2009
Date
2009
Author(s)
Lin, Yu-Hsin
Abstract
For poor solubility in water or lower bioavailability organic drugs, micronization is one of the most direct and safe way to increase the surface area in order to enhance the dissolution rate and bioavailability of the drugs in body. So in this research, we want to us microemulsion system－temperature changing process and solvent diffusion process to micronize organic drugs of mitotane、Glybenclamide (GBM) and warfarin. Further, we want to research the effects of recrystalized drugs’ shape and size by changing system composition, operating conditions and adding extra addition. or mitotane, we can get 1*0.4-3*2micrometer products by water / butyl lactate / lecithin-ethanol / taurodeoxycholic acid sodium salt hydrate (TDC), oil in water (O/W) microemulsion－solvent diffusion process (original drug：50*30-200*80 micrometer). By dissolution rate test, we find the dissolution rate of products increase 4.81 times at 5 mins and the dissolution rate coefficient (kW) increase 7.54 times. In addition, we finish the phase diagram of water / benzyl alcohol / sodium dodecyl sulfate (SDS) system at 10oC-60oC. And we find that when we use this (O/W) microemulsion－temperature changing process or solvent diffusion process to recrystalize the drugs, we can make the products’ shape change from needlelike to lump by changing system composition－increasing the concentration of surfactant SDS.or Glybenclamide (GBM), we can get 0.3*0.2-1*1 micrometer products (mostly in 300-500nm) by cyclohexane / dimethyl sulfoxide (DMSO) / dioctyl sulfosuccinate sodium salt (AOT), water in oil (W/O) microemulsion－temperature changing process(original drug：15*10-100*70 micrometer). By dissolution rate test, we find the dissolution rate of products increase 6.51 times at 5 mins and the dissolution rate coefficient (kW) increase 10.01 times. Furthermore, we find that in antisolvent process we can effectively decrease the particle size by adding extra material－Tw80. or warfarin, we can get mostly 0.8*0.7-4*3 micrometer products by water / benzyl alcohol / sodium dodecyl sulfate (SDS), (O/W) microemulsion－temperature changing process (original drug：20*5-100*30 micrometer). By dissolution rate test, we find the dissolution rate of products increase 1.78 times at 5 mins and the dissolution rate coefficient (kW) increase 13.29 times.
Subjects
micronization
microemulsion
antisolvent
Type
thesis
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