Pharmacokinetics and in vitro and in vivo correlation of huperzine A loaded poly(lactic-co-glycolic acid) microspheres in dogs.
The purpose of this study was to investigate the pharmacokinetics and in vitro/in vivo correlation (IVIVC) of huperzine A loaded poly(lactic-co-glycolic acid) (PLGA) microspheres in dogs. Several huperzine A loaded PLGA microspheres were prepared by an O/W method and three of them (single dose) were injected intramuscularly (i.m.) or subcutaneously (s.c.) to five beagle dogs, respectively. With the increase of the molecular weight of PLGA and the particle size of microspheres, the in vitro and in vivo release periods of huperzine A were prolonged. After s.c. injection, the release of huperzine A from microspheres was faster than that after i.m. injection. The IVIVC models of huperzine A loaded PLGA microspheres were established successfully and after i.m. administration the linear relationship between the in vitro and the in vivo releases was better than that after s.c. administration. It was also found when the particle size of the microspheres was smaller; the values of correlation coefficient were higher.
Chu
Da-Feng
DF
School of Pharmacy, Yantai University, No. 32 Qingquan Road, 264005 Yantai, Shandong Province, PR China.
Fu
Xue-Qi
XQ
Liu
Wan-Hui
WH
Liu
Ke
K
Li
You-Xin
YX
D000470:Alkaloids; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002853:Chromatography, Liquid / Q000379:methods; D004285:Dogs; D004339:Drug Compounding / Q000379:methods; D005260:Female; D007273:Injections, Intramuscular; D007279:Injections, Subcutaneous; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D013058:Mass Spectrometry / Q000379:methods; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D011108:Polymers; D012717:Sesquiterpenes; C050426:huperzine A; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid