[Pharmacodynamics of compound danshen pH-dependent delayed release pellets in dogs].
OBJECTIVE
To prepare the compound danshen pH-dependent delayed release pellets and filled them in capsules and then study thier pharmacodynamics.


METHODS
The pH-dependent delayed release pellets were prepared by coating with HPMC, Eudragit L-30D-55 and Eudragit L100-Eudragit S100 (1:6), separately, and mixed in proper proportion to prepare the two pH-dependent delayed release systems T1 and T2. The release of delayed release pellets was determined according to the method of China Pharmacopoeia (2000) in the simulated gastrointestinal pH conditions. The pharmacodynamic,parameters were evaluated by serum pharmacology method.


RESULTS
The compound danshen pH-dependent delayed release pellets were prepared with the characteristics of pH dependent delayed release profile in vitro. In single oral dose, the pharmacodynamic parameters of rapid release tablets R Emax (%) and Tmax (h) were 34.63% and 0.58 h, respectively. Tmax S of delayed-release pellets T1 and T2 were extended to 2.42, 3.17 h and Emax S (%) were declined to 13.57%, 14.52%. The relative bioavailabilities of T1 and T2 were 99.3%, 133.6% , respectively. In multiple oral doses of R the pharmacodynamic parameter of DF was 7.32 and those T1, T2 DF were 3.40, 3.03, respectively.


CONCLUSIONS
The compound danshen pH-dependent delayed release capsules have characteristics of pH dependent releasing in vitro and characteristics of delayed release in vivo. In multiple oral (loses the DF of delayed release capsules was lower than that of rapid release tablet at steady state.
Yang
Dong-li
DL
School of Pharmacy ,Shenyang Pharmaceutical University, Shenyang 110016, China.
Yu
Ye-ling
YL
Tang
Xing
X
Wan
Hui-jie
HJ
Song
Hong-tao
HT
D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D029745:Codonopsis / Q000737:chemistry; D003692:Delayed-Action Preparations; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives; D010946:Plants, Medicinal / Q000737:chemistry; D011109:Polymethacrylic Acids; D011897:Random Allocation
D003692:Delayed-Action Preparations; D004338:Drug Combinations; D004365:Drugs, Chinese Herbal; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D065347:Hypromellose Derivatives; D008747:Methylcellulose