title: [Pharmacokinetics of mestinon-phospholipid complex in rats].
abstract: OBJECTIVE
  To determine the pharmacokinetics characteristics of mestinon-phospholipid complex (PBPLC) in rats.
  
  
  METHODS
  This study adopted a single-dose, randomized, open-label, two-period crossover trial design. Twelve healthy rats were randomly divided into two groups. One group was orally administered with mestinon-phospholipid complex, and the other group was orally administered with reference mestinon solution (1.5 mg/kg of mestinon). The plasma concentrations of the drugs in ophthalmic vein bloods were determined using HPLC. The pharmacokinetic parameters were calculated with the aid of DAS2.1.1 software.
  
  
  RESULTS
  Pharmacokinetic parameters of mestinon-phospholipid complex were Tmax 2 h, Cmax 22.79 microg x min/mL and AUC(0-infinity) 7128.21 microg x min/mL, which were different from those of free mestinon--Tmax, 2 h, Cmax 6.00 microg/mL and AUC(0-infinity) 1772.36 microg x min/mL. The relative bioavailability of mestinon-phospholipid complex was 410.98% of free mestinon.
  
  
  CONCLUSIONS
  The oral bioavailability of mestinon increases remarkably when administered as mestinon-phospholipid complex.
authors: Medicine Engineering Research Center in University, Chongqing Key Laboratory of Biochemical & Molecular Pharmacology, Chongqing Medical University, Chongqing 400016, China.
authors: Ni-Ni
authors: NN
authors: Hu
authors: Qun-You
authors: QY
authors: Tan
authors: Li
authors: L
authors: Zhang
authors: Hua-Feng
authors: HF
authors: Yin
authors: Jing-Qing
authors: JQ
authors: Zhang
mesh_terms: D000818:Animals; D001682:Biological Availability; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics*; D004338:Drug Combinations; D008297:Male; D010743:Phospholipids / Q000493:pharmacokinetics*; D011729:Pyridostigmine Bromide / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D002800:Cholinesterase Inhibitors; D004338:Drug Combinations; D010743:Phospholipids; D011729:Pyridostigmine Bromide