Abstract��
OBJECTIVE: To develop less kidney distributed and less toxic alternatives for Sandimmun Neoral?(Neoral),Cyclosporine A (CyA) loaded polylacticacid Nanospheres Colloid (NSC),with diameters of (58.8��
11.3)nm,and Nanocapsules Colloid (NCC),with diameters of (81.7��
36.7)nm,were prepared.The pharmacokinetic characteristics and oral absorption of NSC,NCC were compared with Neoral. METHODS: NSC,NCC and aqueous dilution of Neoral were po administrated to 8 rats respectively in a dosage of 10 mg��kg-1.The CyA concentration in whole blood samples were determined by HPLC.Pharmacokinetic parameters were calculated by 3P87 and ANOVA were done by EXCEL. RESULTS: The concentrationtime data of the 3 preparations were best fit to 2 compartments open model with a weight of 1/C2,Comparing to Neoral,NSC and NCC had smaller Cmax values (P<0.05),smaller distribution rates (P<0.05),and smaller elimination rates (P<0.05).The relative bioavailabilities of NSC ansd NCC were 112.9% and 100.35% comparing to Neoral. CONCLUSION: Comparing to Neoral,NCC and NSC may change the tissue distribution of CyA,lower its elimination and improve bioavailabilities after oral administration.The two colloid preparations were suitable for further studies.
Li Hongshan,
Li Hongshan
.Preparation of cyclosporine a loaded polylacticacid nanoparticle colloids and their oral bioavailabilities on rats[J] Chinese Pharmaceutical Journal, 1999,V34(08): 532-536
1999, Vol. 34 
