Intra-ocular distribution and pharmacokinetics of musk eye drops in the rabbits / 中成药

ABSTRACT

AIM: To study intra-ocular distribution and pharmacokinetics of musk eye drops in the rabbit eyes.METHODS: After administration,twenty seven rabbits were euthanatized and taken eye in 0.083 h,0.167 h,0.5 h,1 h,2.0 h,4.0 h,8.0 h and 12 h,and then isolated aqueous humor,vitreous body,further cornea and ciliary margin of iris from rabbits’eyes.The intraocular concentrations of muscone were measured by GC after topical instillation with 10% musk solution in rabbits.The pharmacokinetic parameters were calculated with 3p97 program.RESULTS: Results showed that the peak concentrations(max) of muscone in various ocular tissues were (107.52 ?67.07),(2.15 ?1.49),(0.034 ?0.007 6),(2.87 ?1.50) and(0.013 ?0.004 5)?g/g or ?g/mLin lacrimal fluid,cornea,aqueous humor,iris and vitreous body;Its half-Life(T1/2) was(8.08 ? 3.08),(2.87? 2.24),(3.37 ? 0.68),(4.69 ? 1.32) and(8.37 ? 2.70) h,respectively.AUC(0→T) of various tissues was (114.57 ?37.41),(11.57 ?7.16),(0.18 ?0.056),(2.86 ?0.42) and(0.079 ?0.017)?g/(h.g) or(?g/h.mL),respectively.CONCLUSION: The results indicate that musk in eye drop has a good permeability and high concentration in various intraocular tissues of rabbit after ocular instillation.