[Preparation of enteric nanoparticles of Schisandra total lignanoids and preliminary study on its pharmacokinetics].
To study the preparation method of Schisandra total lignanoids enteric (SLE) nanoparticles and evaluate its pharmacokinetics in rats, SLE nanoparticles were prepared by modified emulsion solvent diffusion method. The properties of SLE nanoparticles were evaluated of morphology, mean diameter and entrapment efficiency. An HPLC method was employed to determine the concentration of deoxyschisandrin (QS) and schisantherin A (SA) in plasma, which were used as an index of Schisandra total lignanoids, and the bioavailability of the nanoparticles was compared with the reference group by oral administration using SD rats. The nanoparticles observed by transmission electronmicroscopy were round, and the mean particle sizes of SLE were (36.7 +/- 4.4) nm. Entrapment efficiency of QS and SA were (97.5 +/- 0.7)% and (91.3 +/- 0.8)%, respectively. Its pharmacokinetic process calculated with 3p97 software was fitted to a one-compartment model. The pharmacokinetic parameters showed sustained-release property. Compared with reference formulation, the AUCs of SLE nanoparticles were 2.3 and 5.8 times separately. These results suggested that the incorporation into Eudragit S100 of Schisandra total lignanoids can improve the bioavailability.
Huang
Ya-Jie
YJ
China Military Institute of Chinese Materia Medica, 302 Military Hospital of China, Beijing 100039, China.
Li
Ya-Bin
YB
Yuan
Hai-Long
HL
Huang
Xue
X
Wang
Qi
Q
Xiao
Xiao-He
XH
D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D034242:Cyclooctanes / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D005260:Female; D017705:Lignans / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D011083:Polycyclic Compounds / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D032141:Schisandra
D034242:Cyclooctanes; D017705:Lignans; D011083:Polycyclic Compounds; C011105:schizandrin