AIM: To establish the preparative method of dispersible tablet of total notoginseng saponin (DTTNS) by powder direct compression,and to evaluate it pharmaceutical characteristics. METHODS: The effect of factors on the disintegration of DT-TNS was investigated by single factor method,and the formulation was optimized through orthogonal design. RESULTS: The disintegration time of DT-TNS containing 40% total notoginseng saponin was within 1 min while the formulation mainly consisted of 49% MCC as filler,12% of PVPP mixed with 3% L-HPC as disintegrating agent. In addition,the dissolution of DT-TNS was almost finished in 10-15 min. CONCLUSION: The preparative method of DT-TNS by powder direct compression is simple,with short disintegration time and high dissolution rate.

OBJECTIVETo prepare the diammonium glycyrrhizinate-loaded chitosan nanoparticles (DG-CS NPs), and evaluate its pharmaceutical properties and pharmacodynamic effects on ulcerative colitis (UC).

METHODDG-CS NPs were prepared by spray drying method and optimized by orthogonal design. The morphology, size and in vitro release of DG-CS NPs were investigated. The therapeutic effects of DG-CS NPs on UC mice induced by dextran sulfate were evaluated preliminarily through disease active index method.

RESULTThe size of DG-CS NPs with loading capacity about (51.25 +/- 1.75)% was in the range of 300-600 nm. The release of DG-CS NPs was associated with environmental pH value and displayed significant therapeutic and preventive effects on UC.

CONCLUSIONDG-CS NPs prepared by spray drying method showed efficacy on UC mice.

Animals ; Chitosan ; chemistry ; Colitis, Ulcerative ; chemically induced ; drug therapy ; Dextran Sulfate ; toxicity ; Disease Models, Animal ; Female ; Glycyrrhizic Acid ; chemistry ; therapeutic use ; Male ; Mice ; Nanoparticles ; chemistry

OBJECTIVETo prepare paeonol-beta-cyclodextrin inclusion complex (Pae-beta-CYD) loaded colon-specific release tablets.

METHODThe core tablets were prepared with the mixture of Pae-beta-CYD inclusion complex, peotin and calcium acetate, and coated with ethanolic solution of Eudragit S100. The effects of coating weight, amount of plasticizer, curing time and temperature on the release of drug from tablets were investigated in vitro.

RESULTAbout 5-6 h retarded release of paeonol in the dissolution media of pectinase or rats colon contents were obtained by 12% coating weight gain and 20% Dibutyl phthalate (DBP) was used as plasticizer, and subsequently curing the tablets at 45 degrees C for 12 h.

CONCLUSIONPae-beta-CYD loaded colon-specific release tablets showed pH environment and enzyme dependant release properties.

Acetophenones ; pharmacokinetics ; therapeutic use ; Animals ; Colitis, Ulcerative ; drug therapy ; Colon ; drug effects ; Drug Delivery Systems ; methods ; Excipients ; chemistry ; Humans ; Hydrogen-Ion Concentration ; Rats ; Rats, Sprague-Dawley ; Tablets, Enteric-Coated ; chemistry ; beta-Cyclodextrins ; chemistry

OBJECTIVETo study the stability and degradation kinetics of Ketoprofen-Paeonol conjugate (Ket-Pae).

METHODRP-HPLC method was used to determine the solubility and partition coefficient of Ket-Pae. Stability test was carried out to investigate the factors affecting Ket-Pae. The kinetic studies of Ket-Pae degradation were conducted in different pH buffer solutions and 80% rat plasma at 37 degrees C.

RESULTKet-Pae showed significant degradation phenomenon at high temperature. The solubility of Ket-Pae was decreased about 200 to 300 times compared with parent drugs in water while the lnP increased about 4 times. The degradation curve displayed a V-shape, and kept maximum stability at week acidic (pH 5.0, t(1/2) = 11.4 d). Ket-Pae degraded quickly with very short half life of 1.3 min in plasma, therefore easily released ketoprofen and paeonol.

CONCLUSIONThe lipophilicity of Ket-Pae is increased, its stability is affected by temperature and pH value.

Acetophenones ; chemistry ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Hydrogen-Ion Concentration ; Ketoprofen ; chemistry ; Kinetics ; Solubility