[In vivo distribution of a novel proliposomal preparation of tegafur following intragastric gavage to rats].
OBJECTIVE
To evaluate in vivo distribution characteristics of a novel proliposomal preparation of tegafur in rats.


METHODS
Concentrations of tegafur in tissues and plasma were measured by HPLC following intragastric gavage of the proliposomal preparation of tegafur (PL-FT207) or aqueous suspension of tegafur tablet (T-FT207) to rats. And the pharmacokinetic parameters including the area under the concentration-time curve (AUC), relative tissue efficiency and the maximum drug concentration were calculated.


RESULTS
Following intragastric gavage of PL-FT207 or T-FT207 to rats, AUC was significantly increased in plasma, liver, kidney, colon and lung (P < 0.01) of PL-FT207 group in contrast to that of T-FT207 group, the relative tissue efficiencies of these tissues were 1.36-1.57, the maximum drug concentrations of brain and lung of PL-FT207 group were significantly declined (P < 0.005).


CONCLUSIONS
The novel proliposomal preparation of tegafur is able to promote drug absorption in gastro-intestine, increase drug distribution in kidney, liver, colon and lung, and decrease the maximum drug concentration in brain and heart, thus providing scientific basis for further studies on this preparation.
Department of Pharmaceutics, Xinjiang Medical University, Urumqi 830054, China. gxli@tefeng.com
Xiao-li
XL
Gao
Murat
M
Kzybek
Hao
H
Wen
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D004337:Drug Carriers; D004355:Drug Stability; D005260:Female; D008081:Liposomes; D008297:Male; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D005641:Tegafur / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D008081:Liposomes; D005641:Tegafur