Preparation Of Levodopa CMS-Na Microspheres Used In Nasal

OBJECTIVE Levodopa (L-DOPA) has a better treatment effect in the treat of Parkinson's disease, and the effect is higher than the other types of anti-Parkinson drugs. Oral tablet is the most familiar dosage form of L-dopa but the amount absorbed into the brain is less-than 1%. The bioavailability is low and the side effects to peripheral nervous system is high. In the paper we researched the L-DOPA CMS-Na microspheres used in nasal and we discovered it can improve bioavailability and reduce side effects. METHODS microspheres were produced by emulsion chemical-crossline technique. CMS-Na was used as the carrier, Castor Oil as the oil phase, Towen-80 as the emulsifier,1,4-benzenedicarbonyl chloride as the chemical-crossline agent.The orthogonal design method was applied to optimize the preparation technology. HPLC method was used for the determination of L-DOPA in CMS-Na microspheres. And some characters about of L-DOPA CMS-Na microspheres were researched in this paper.RESULTS The CMS-Na microspheres had a good shape. Its diameter was in the range of 32-55μm, and the average particle diameter was 41.2μm. The percentage of the microspheres between 40-50 u m is 67.5%. The average drug loading and rate of entrapment of L-DOPA in the microspheres were 9.26% and 39.72%CONCLUSION The product of L-DOPA CMS-Na microspheres is easy.Its quality level comply with the drug standers and the stability of L-DOPA is improved in the CMS-Na microspheres. L-DOPA CMS-Na microspheres used in nasal declined the bad effects of L-DOPA and can go directly into the brain.