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The main formulations of cyclosporine A ( Cyclosporine A , CyA ) is currently listed as soft capsules, oral solution and injection . These absorption of oral dosage forms need to bile salts involved in the self-emulsifying , self bioavailability difference larger excipients polyoxyethylene castor oil used has a series of side effects , the complex process of the preparation of soft capsules , oral poor taste . Due to the low solubility of cyclosporin A problem is not resolved , the most common in the pharmaceutical solid dosage forms on the market has not yet appeared . Lipid material of the subject aimed at developing a process by solid dispersion technology simple CyA quick release tablets, this process will CyA was dissolved in a molten state of polyethylene glycol 1000 Vitamin E succinate (TPGS) , and polyethylene glycol a mixture of fatty acid glycerides ( Gelucire 44 ) , aerosil sufficiently adsorbed , was cooled to room temperature curing , grinding , sieving , obtained CyA solid dispersion , adding microcrystalline cellulose and crosslinked povidone , mixed evenly , the pressure sheet . Optimize the prescription and process of the the CyA active -release tablets ( CyA ART ) was investigated in vitro dissolution of ART , and self- producer ( excluding CyA ART lipid ) , homemade capsules ( CyA - lipid melt filled hard gelatin capsules ) , commercially available soft gelatin capsules were compared. The results show that , within 30 minutes , about 80% of CyA ART dissolution , soft capsules with a commercially available in vitro release profile of a certain comparability . Drug dispersed in microemulsion form in the dissolution medium , the tests show that the particle size distribution and the range of 250nm or less of the laser particle size analyzer (PCS) . A powder X -ray diffraction ( PXRD ) suggest that the drug may be provided to the molecular state exists in ART . The CyA the ART room temperature shield light Store in a dry place 3 months after the determination of tablet content , in vitro dissolution and PXRD testing , its considerable stability . The subject from the perspective of Pharmacy verify the feasibility of active release tablets development , and technology development for the immediate release formulation of insoluble drugs and Inspiration .
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