ABSTRACT
<p><b>OBJECTIVE</b>To prepare paeonol-beta-cyclodextrin inclusion complex (Pae-beta-CYD) loaded colon-specific release tablets.</p><p><b>METHOD</b>The 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.</p><p><b>RESULT</b>About 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.</p><p><b>CONCLUSION</b>Pae-beta-CYD loaded colon-specific release tablets showed pH environment and enzyme dependant release properties.</p>
Subject(s)
Animals , Humans , Rats , Acetophenones , Pharmacokinetics , Therapeutic Uses , Colitis, Ulcerative , Drug Therapy , Colon , Drug Delivery Systems , Methods , Excipients , Chemistry , Hydrogen-Ion Concentration , Rats, Sprague-Dawley , Tablets, Enteric-Coated , Chemistry , beta-Cyclodextrins , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To study the stability and degradation kinetics of Ketoprofen-Paeonol conjugate (Ket-Pae).</p><p><b>METHOD</b>RP-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.</p><p><b>RESULT</b>Ket-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.</p><p><b>CONCLUSION</b>The lipophilicity of Ket-Pae is increased, its stability is affected by temperature and pH value.</p>
Subject(s)
Acetophenones , Chemistry , Drug Stability , Drugs, Chinese Herbal , Chemistry , Hydrogen-Ion Concentration , Ketoprofen , Chemistry , Kinetics , SolubilityABSTRACT
<p><b>OBJECTIVE</b>To prepare the diammonium glycyrrhizinate-loaded chitosan nanoparticles (DG-CS NPs), and evaluate its pharmaceutical properties and pharmacodynamic effects on ulcerative colitis (UC).</p><p><b>METHOD</b>DG-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.</p><p><b>RESULT</b>The 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.</p><p><b>CONCLUSION</b>DG-CS NPs prepared by spray drying method showed efficacy on UC mice.</p>
Subject(s)
Animals , Female , Male , Mice , Chitosan , Chemistry , Colitis, Ulcerative , Drug Therapy , Dextran Sulfate , Toxicity , Disease Models, Animal , Glycyrrhizic Acid , Chemistry , Therapeutic Uses , Nanoparticles , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To prepare ginkgo biloba extract (GBE) sustained-release tablets and observe its in vitro release profile.</p><p><b>METHOD</b>GBE sustained-release tablets were prepared by direct compression method using sodium carboxymethylcellulose (CMC-Na) and hydroxypropyl methylcellulose HPMC) as matrix excipients. Based on the result of single-factor selecting experiment, the formulations and preparation process were optimized through orthogonal design, and release difference of tablets was evaluated with similarity factor (f2).</p><p><b>RESULT</b>The ratio of HPMC and CMC-Na, the viscosity of HPMC and the different types of the diluents had pronounced effect on the release of GBE sustained release tablets, although the hardness and weight difference of tablets did not show notable influences.</p><p><b>CONCLUSION</b>GBE sustained-release tablets that prepared by using the mixture of HPMC and CMC-Na display constant release profile in 12 h.</p>
Subject(s)
Delayed-Action Preparations , Chemistry , Drug Compounding , Methods , Drug Stability , Ginkgo biloba , Chemistry , Plant Extracts , Chemistry , Tablets , ChemistryABSTRACT
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.