[Aqueous humor penetration of ligustrazine hydrochloride eye drops after topical administration in rabbit eyes].
OBJECTIVE
To study the aqueous humor penetration of ligustrazine hydrochloride after ocular administration in rabbits.


METHODS
Eighteen rabbits were randomly divided into 6 groups. The aqueous humor was collected at 5, 15, 30, 60, 120 and 180 minutes following topical administration of ligustrazine hydrochloride eye drops and the concentration of ligustrazine hydrochloride was determined by HPLC. Analytical column was Diamonsil C18 stainless steel column (250 mm x 4.6 mm, 5 microm); The mobile phase was methanol: water(62:38); Flow rate was 0.9 ml/min; The detection wavelength was 280 nm.


RESULTS
The concentrations of ligustrazine hydrochloride in aqueous humor were (15.785 +/- 2.988) microg/mL, (11.900 +/- 1.743) microg/mL, (8.286 +/- 1.182) microg/mL, (2.745 +/- 0.807) microg/mL, (0.379 +/- 0.091) microg/mL, (0.049 +/- 0.038) microg/mL, respectively, after a time interval of 5 min, 15 min, 30 min, 60 min, 120 min, 180 min. The maximum concentration was 15.785 microg/mL at 5 min, and then the concentration of ligustrazine hydrochloride gradually decreased and declined to a lower point at 180 min.


CONCLUSIONS
The penetration of ligustrazine hydrochloride in aqueous humor after ocular administration was good. The results provided experimental data for the management of eye diseases with ligustrazine hydrochloride by topical administration.
State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat-sen University, Guangzhou 510060, China.
Meifeng
M
He
Xinguo
X
Deng
Wei
W
Wu
Yandong
Y
Wang
D060433:Administration, Ophthalmic; D000818:Animals; D000867:Anterior Chamber / Q000378:metabolism*; D001082:Aqueous Humor; D009883:Ophthalmic Solutions; D011719:Pyrazines / Q000493:pharmacokinetics*; D011817:Rabbits
D009883:Ophthalmic Solutions; D011719:Pyrazines; C017953:tetramethylpyrazine