[Pharmacokinetics of puerarin in the aqueous humor and vitreous of rabbit eye following systemic administration].
OBJECTIVE
To study dynamic changes of puerarin in aqueous humor and vitreous humor of rabbit eye following a single dose intraperitoneal injection.


METHODS
Rabbits were randomly divided into 11 groups. Puerarin (80 mg/kg) was given by a single dose intraperitoneal injection. After the administration, the aqueous humor, vitreous were harvested at different time points and the concentration of puerarin was determined by reversed phase high performance liquid chromatography (RP-HPLC).


RESULTS
The concentration-time data of puerarin in aqueous humor, vitreous was subject to two-compartment open model. The pharmacokinetic parameters were separately as following. Cmax = 1.61, 0.09 microg/ml. tmax = 1.68, 1.81 h. t1/2alpha = 1.36, 1.05 h. t1/2beta = 19.72, 15.18 h. CL = 2.17, 12.43 L/h. The practical data of the concentration of puerarin in aqueous humor and vitreous humor that were detected was (0.78 +/- 0.29) microg/ml, (0.06 +/- 0.02) microg/ml at 30 min respectively and reach maximum concentration was (2.32 +/- 0.15) microg/ml, (0.12 +/- 0.04) microg/ml at 2 h. Then the concentration of puerarin in aqueous humor and vitreous humor was gradually decreased. The concentration of puerarin was 0.57 microg/ml in the aqueous humor, 0.05 microg/ml in the vitreous humor at 6 h. The concentration of puerarin declined to a lower point 0.03 microg/ml or below in aqueous humor and vitreous humor after 16 h.


CONCLUSIONS
Using HPLC method to detect puerarin in the aqueous humor and vitreous humor was particular, accurate and sensitive. The puerarin can penetrate blood-ocular barrier to enter aqueous humor and vitreous humor. The concentration of puerarin in the aqueous humor was obviously more than that in the vitreous humor. The quantitation of puerarin entering vitreous humor was limited. The clearance of the compound were slower and half-life were longer in aqueous humor and vitreous, that can provide principle basis for treating eye diseases with puerarin by systemic administration.
Deng
Xinguo
X
State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat-sen University, Guangzhou 510060, China.
Zhang
Qingjiong
Q
Hu
Shixing
S
Gao
Yang
Y
Yan
Liu
L
D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism*; D005260:Female; D006207:Half-Life; D007529:Isoflavones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D011817:Rabbits; D014822:Vitreous Body / Q000378:metabolism*
D007529:Isoflavones; C033607:puerarin