Abstract:
OBJECTIVE To evaluate the characteristic of the dosage form of the new Mu-an in-situ forming eye gel by compare the effect of the drug transit pharmacokinetics character in rabbit aqueous humor of the phase transition process with common gel.
METHODS Taken New Zealand rabbits as research objects, after giving new Mu-an in-situ forming eye gel(had phase transition process) and common gel in ocular, obtained aqueous humor in different time points, detected the content of ganciclovir, established the transit pharmacokinetics equations of drug in aqueous humor, calculated the transit pharmacokinetics parameters of drugs
in vivo, made a comparison between the new Mu-an in-situ forming eye gel and the common gel.
RESULTS The transit pharmacokinetics equations of ganciclovir in aqueous humor of new Mu-an in-situ forming eye gel was
C=18.94×
e-0.015 4 t-18.94×
e-0.079 85 t, the transit pharmacokinetics equations of ganciclovir in aqueous humor of common gel was
C=15.42×
e-0.015 3 t-15.42×
e-0.048 8 t. It could explain that both two gel had the same transit mechanism in aqueous humor of rabbits. Through the comparative analysis of different pharmacokinetic parameters, it showed that time to peak of new Mu-an in-situ forming eye gel was 25.51 min, the concentration to peak was 10.31 μg·mL
-1,
t1/2 was 8.679 min and the AUC was 992.4 μg·mL
-1·min, while for common gel, the time to peak was 34.63 min, the concentration to peak was 6.232 μg·mL
-1,
t1/2 was 14.20 min and the AUC was 691.4 μg·mL
-1·min.
CONCLUSION Phase transition energy(△
H) turns into kinetic energy of drug permeate cornea in the phase transition process of in-situ gel, which can take pesticide effect for it to be as effective as possible.