[Preparation of rivastigmine liposome and its pharmacokinetics in rats after intranasal administration].
To prepare rivastigmine liposome, rivastigmine was loaded into liposome via ammonium sulfate gradient method. Its pharmacokinetic profile in rats was evaluated after intranasal administration. The size, zeta potential, entrapped efficiency and release of rivastigmine from the liposome in vitro were determined. Plasma concentration of rivastigmine was determined by high performance liquid chromatography-tandem mass spectrometry (HPLC/MS) using antipyrine as internal standard. The pharmacokinetic parameters were calculated by DAS 2.0. The entrapped efficiency of rivastigmine liposome was (33.41 +/- 6.58) %, with the mean diameter of 154-236 nm and zeta potential of (-10.47 +/- 2.41) mV. The release behavior of rivastigmine was fitting the first order equation in vitro. The pharmacokinetic studies indicated that the C(max), T(max) and AUC(0-infinity), of rivastigmine liposome were (1.50 +/- 0.15) mg x L(-1), 15 min and (89.06 +/- 8.30) mg x L(-') x min, respectively. Rivastimine liposome was absorbed rapidly, and could reach a certain concentration in rat plasma after intranasal delivery.
School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Zhen-Zhen
ZZ
Yang
Zhan-Zhang
ZZ
Wang
Kai
K
Wu
Xian-Rong
XR
Qi
D000281:Administration, Intranasal; D000818:Animals; D019540:Area Under Curve; D002853:Chromatography, Liquid; D004337:Drug Carriers; D004339:Drug Compounding; D008081:Liposomes; D008297:Male; D018696:Neuroprotective Agents / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D010316:Particle Size; D048448:Phenylcarbamates / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000068836:Rivastigmine; D053719:Tandem Mass Spectrometry
D004337:Drug Carriers; D008081:Liposomes; D018696:Neuroprotective Agents; D048448:Phenylcarbamates; D000068836:Rivastigmine