[Optimization of the preparation and the properties of conjugate of 5-Fluorouracil and peanut agglutinin].
OBJECTIVE
This study was aimed at optimizing the preparation of 5-Fluorouracil and peanut agglutinin conjugates so as to obtain a conjugate with high activity and high drug ratio, and to choose suitable dosage form in the light of its properties.


METHODS
Every single factor was tested. The drug ratio and activity were chosen according to the criteria for judgement. The stability of the conjugate was tested after treatment.


RESULTS
A conjugate with high activity and drug ratio was obtained under the condition of 5-Fu : EDC : NHS= 1:5:2 for 12 h with the protection of D-galactose (D-galactose : PNA(w/w) = 2.5:1).


CONCLUSIONS
The addition of D-galactose could protect the activity of PNA. The conjugate is stable.
Qin
Cai
C
Department of Pharmaceutical Sciences, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Zhang
Zhi-rong
ZR
D000964:Antimetabolites, Antineoplastic / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D005472:Fluorouracil / Q000737:chemistry*; D005690:Galactose / Q000737:chemistry; D006801:Humans; D037102:Lectins; D019887:Peanut Agglutinin / Q000737:chemistry*
D000964:Antimetabolites, Antineoplastic; D037102:Lectins; D019887:Peanut Agglutinin; D005472:Fluorouracil; D005690:Galactose