[Studies on diclofenac sodium pulsatile release pellets].
OBJECTIVE
To investigate the preparation of diclofenac sodium pulsatile release pellets (DS-PRP), the release in vitro and the pharmacokinetics of the drug.


METHODS
Diclofenac sodium (DS) core pellets prepared by extrusion-spheronization technology were coated in a mini-fluidized bed spray coater with swelling material as the inner coating swelling layer and ethylcellulose aqueous dispersion as the outer coating controlled layer. The effects of formulation and medium on pulsatile release of DS were investigated under release rate test. Pharmacokinetic and bioavailability study in eight human subjects were performed by HPLC method.


RESULTS
The delayed-release time and release rate of DS from DS-PRP were influenced obviously by the swelling material, the concentration of SDS in medium, the coating level of the inner swelling layer and the outer controlled layer. In vitro, the delayed-release time T0.1 was 3.1 h, and the pulsed-release time T0.1-0.2 was 1.2 h. In vivo, the delayed-release time Tlag was 2.8 h, and the bioavailability was (91 +/- 12)%.


CONCLUSIONS
The release of drug from DS-PRP was shown to be in pulsed way both in vitro and in vivo.
Guo
Tao
T
Department of Pharmacy, General Hospital of Shenyang Military Region, Shenyang 110016, China. guotao@mail.sy.ln.cn
Zheng
Chun-li
CL
Song
Hong-tao
HT
Sui
Yin
Y
Dang
Da-sheng
DS
Sun
Xue-hui
XH
D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D011897:Random Allocation; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004008:Diclofenac; D012967:Sodium Dodecyl Sulfate; C013517:ethyl cellulose; D002482:Cellulose