K21. The mean t1/2(?) was (2.7?0.4) h, Vd was about 11.18 L?kg-1.The C-T profile conformed to two compartment open model. The plasma Dau concentration-time curves showed a double-peak phenomenon in all dosages of all dogswhen dauricine was given by intragastric was.The tpeak(1) was (0.8?0.6) ～(1.2?0.5) h,tpeak(2) was (5.2?3.2) ～(6.5?1.9)h,Cmax(2) 0.05) and the AUC was increased in proportion.The drug is eliminated non-linearly when the dosage is above 50 mg?kg-1, the parameters t1/2(el),CL, AUC/X0 shows great difference (P

Aim The relative bioavailability of domestic ibudilast sustained release capsules in healthy volunteers was observed.Methods A single oral dose of 20 mg of imported and domestic ibudilast sustained release capsules and 10 mg of ibudilast raw material was separately given to 12 healthy volunteers in a randomized crossover study. Ibudilast concentration in plasma was determined by HPLC method.Results The Cmax were (54.9?9.7),(60.7?9.1) and (62.2?11.5) ?g?L-1; the tmax were (3.8?0.8),(3.9?0.8) and (1.8?0.3) h;the t1/2(ke) were (1.5?1.4),(12.1?1.0) and (3.5?0.5) h,and the AUC(0～t) were (618.1?57.7),(588.1?66.6) and (233.0?46.4) ?g?h?L-1 in imported capsule group, domestic capsule group and raw material group respectively. The relative bioavailability of domestic sustained release capsules of ibudilast is (95.6?11.0)%. Conclusion The results of statistical analysis demonstrate that the imported and domestic sustained capsules have significant character of significantly sustained release and are bioequivalent.

BACKGROUND:Erythromycin spreads widely in the body with a short period of effective concentrations and has a lot of adverse effects.Therefore,it is necessary to make erythromycin as targeted medicine.OBJECTIVE:To optimize the preparation conditions of erythromycin gelatin microspheres.DESIGN,TIME AND SETTING:An orthogonal controlled test was performed in the Department of Pharmacy,Guangdong Pharmaceutical University from June to December in 2005.MATERIALS:Erythromycin and gelatin.METHODS:According to the emulsion principle,erythromycin dispersed in the gelatin solution.In the process of preparing microspheres,the gelatin solution and oil should form W/O emulsion and then it turned into spheres by solidification.The formation and quality of microspheres were influenced by four factors,namely the concentration of gelatin,dosage of emulsifier,the solidification time and the speed of mixing.The arithmetic mean diameter of microspheres,the drug loading efficiency and the encapsulation efficiency were targets for the survey in this study on the basis of pretests.The best preparation conditions were optimized in accordance with the results of L9 (34) orthogonal tests.The optimized preparation conditions were obtained according to the results of orthogonal tests.MAIN OUTCOME MEASURES:The mean diameter of microspheres,the drug loading efficiency,the encapsulation efficiency,and the orthogonal tests were examined.RESULTS:The optimized preparation conditions of erythromycin gelatin microspheres included 15% gelatin,3.0 mL emulsifier,0.5 hour solidification and mixing at 1 000 r/rain.The erythromycin gelatin microspheres were regular in their morphology.Drug was enveloped in microspheres.The average particle size was (14.15±0.20) μm;the drug loading efficiency and the encapsulation efficiency were (5.83±0.38)% and (65.70±0.56)%,respectively.Over 90.16% of the microspheres was in the range of 7-25 μm;The reappearance of pharmaceutical technology was good.CONCLUSION:The optimized preparation conditions of erythromycin gelatin microspheres are obtained using L9 (34)orthogonal tests.The microspheres prepared meet the requirement of the size for lung targeting.

In recent years, clear aligner technology has been maturing and is rapidly gaining popularity in the orthodontic market for its aesthetic and removable properties. However, despite the background of its large-scale clinical application, mechanical properties of clear aligners need to be studied in depth. This paper reviews the factors influencing mechanical properties of clear aligners and the current status of research to provide evidence-based guidance for clinical application.

AIMTo establish a solid phase extraction-high performance liquid chromatographic (SPE-HPLC) method for determining plasma scutellarin concentration, and study its pharmacokinetics after i.v. breviscapine in rabbits.

METHODSMethanol-water-phosphoric acid (50:50:0.5) mixture was used as mobile phase, Nucleosil C18 column (250 mm x 4.6 mm ID) was selected. The wavelength of UV detection was 335 nm. Fifteen rabbits, randomized into 3 groups, were given breviscapine i.v. at the dose of 10, 20 and 40 mg.kg-1. Scutellarin in plasma was determined by SPE-HPLC method.

RESULTSLinearity was obtained over the range of 0.02-10.0 mg.L-1 of scutellarin. The method recovery was 96.15%-99.31%; the within-day and between-day RSDs were all below 10%. After i.v. 10, 20 and 40 mg.kg-1 of breviscapine to rabbits, the concentration-time curve of scutellarin fitted to a three compartment model. The main pharmacokinetic parameters showed no significant difference between low and medium doses, but the difference was significant between high dose and other doses.

CONCLUSIONThis assay method was accurate, sensitive, simple and suitable for the measurement of plasma scutellarin concentration. The pharmacokinetic characteristics were found to fit a three-compartment model following i.v. injection of breviscapine to rabbits. The changes of drug concentration in vivo exhibited linear kinetics ove the dosage range of 10-20 mg.kg-1, but when the dosage was 40 mg.kg-1, the linear kinetic properties disappeared.

Animals ; Apigenin ; Area Under Curve ; Chromatography, High Pressure Liquid ; methods ; Flavonoids ; blood ; pharmacokinetics ; Male ; Rabbits

OBJECTIVETo discuss the anti-inflammatory mechanism of sinomenine on inflammatory media in joint of adjuvant arthritis rats.

METHODRats were randomly divided into the normal group and the model group, the prednisone group, the small, medium, large of sinomenine group (30, 60, 120 mg x kg(-1)). Except for the rats in the normal group, animals were modeled to adjuvant arthritiswith freund's complete adjuvant. The arthritis index (AI) and the swelling degree of paws were recorded, and the activity of IL-1, TNF and the levels of NO, PGE2 in joint fluids of secondary arthritis were determined.

RESULTCompared with the normal group, the activity of IL-1, TNF and the levels of NO, PGE2 in joint fluids of secondary arthritis were increased significantly in the model group (P < 0.05). Compared with the model group, it was shown to exert a dramatic inhibitory effect on secondary reaction of freund's adjuvant arthritis of rats, and the activity of IL-1, TNF and the levels of NO, PGE2 in joint fluids of secondary arthritis were significantly decreased in the sinomenine group (P < 0.05).

CONCLUSIONSinomenine has a remarkable treatment effect on RA. It is via NO to inhibit the activity of cytokines and decrease the level of inflammation mediators, which may be one of its curing RA mechanism.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; therapeutic use ; Arthritis, Experimental ; drug therapy ; Dinoprostone ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Interleukin-1 ; metabolism ; Male ; Morphinans ; therapeutic use ; Nitric Oxide ; metabolism ; Phytotherapy ; Random Allocation ; Rats ; Rats, Wistar ; Sinomenium ; chemistry ; Synovial Fluid ; metabolism

OBJECTIVETo explore the effect of Chinese herbs (CH) for cool-moistening and freeing collaterals on gastro-dynamic disturbance in patients of diabetes mellitus type 2 with gastroparesis (DM-GP).

METHODSFifty-three patients of DM-GP were enrolled and treated with CH (n = 28) and Cisapride (n = 25) respectively for 4 weeks, the changes of gastrin and electro-gastrogram (EGG) before and after treatment were observed.

RESULTSAfter treatment, the EGG improved significantly, showing the rhythm significantly improved, and level of serum gastrin lowered significantly, as compared with those before treatment, the difference was significant (P<0.01), but insignificant difference was found between the two groups. Fifteen patients in each group were followed-up afar stopping medication for 3 months, recurrence occurred in 1 patient of CH treated group, and 2 patients of Cisapride treated group. No adverse reaction was found in the rest patients.

CONCLUSIONCH could obviously improve the gastro-intestinal motility and hormones abnormality.

Adult ; Aged ; Diabetes Mellitus, Type 2 ; blood ; complications ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Electromyography ; Electrophysiology ; Female ; Gastric Emptying ; drug effects ; Gastrins ; blood ; Gastrointestinal Agents ; therapeutic use ; Gastrointestinal Motility ; drug effects ; Gastroparesis ; drug therapy ; etiology ; physiopathology ; Humans ; Male ; Middle Aged ; Phytotherapy

Adolescent ; Adult ; Aged ; Child ; Decision Trees ; Female ; Hepatitis B, Chronic ; diagnosis ; Humans ; Male ; Middle Aged ; Young Adult

AIMTo investigate the protective effects of sodium beta-aescin on cerebral ischemia-reperfusion injury in rats.

METHODSRats were pretreated with sodium beta-aesein for 7 d and then subjected to cerebral ischemia-reperfusion injury induced by a middle cerebral artery occlusion (MCAO). The neurological outcome was evaluated by the Longa's method; The infarct volume was assessed by hemmatoxylin-Eosin staining and the cerebral water content was measured by dry weight method. The activities of SOD, GSH-Px, CAT, Na+ -K+ -ATPase and the MDA content were measured in the cortex and hippocampus of ischemic and non-ischemic hemisphere.

RESULTSSodium beta-aescin significantly reduced the volume of cerebral infarct and water content, and ameliorated the neurological deficit (P < 0.05). In vehicle-treated rats, the activities of SOD, GSH-Px and Na+ -K+ -ATPase in the cortex and hippocampus of ischemic hemisphere were all decreased (P < 0.01) , while the CAT activity was slightly elevated and the MDA of content was significantly increased (P < 0.01) compared with the sham-operated group. After treated with sodium beta-aescin, the effects on recovery of SOD, GSH-Px, Na+ -K+ -ATPase activities were observed (P < 0.05), and the MDA content was reduced (P < 0.05).

CONCLUSIONThese results showed that pretreatment with sodium beta-aescin can attenuate brain injury and its antioxidant activity on rats which encountered cerebral ischemia-reperfusion.

Animals ; Brain ; metabolism ; Brain Ischemia ; metabolism ; pathology ; Catalase ; metabolism ; Escin ; pharmacology ; Glutathione Peroxidase ; metabolism ; Male ; Malondialdehyde ; metabolism ; Neuroprotective Agents ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; metabolism ; pathology ; Sodium-Potassium-Exchanging ATPase ; metabolism ; Superoxide Dismutase ; metabolism

OBJECTIVETo review the effects of the active components of Chinese herbs on drug metabolizing-enzymes.

METHODRelevant research papers reported in recent years were consulted and studied.

RESULTThe drug metabolizing-enzymes cytochrome P450 and UDP-glucuronosyl transferase and glutathione S-transferase were inhibited or induced by the flavonoids, furocoumarins, and the active components extracted from salvia miltiorrhiza and hypericum perforatum, and so on, which therefore slowed or sped metabolism of other drugs in vivo and in vitro.

CONCLUSIONMuch attention should be paid to the metabolic interaction of the Chinese herbs when coadministered with other drugs.

Animals ; Cytochrome P-450 Enzyme System ; metabolism ; Flavonoids ; isolation & purification ; pharmacology ; Furocoumarins ; isolation & purification ; pharmacology ; Glucuronosyltransferase ; metabolism ; Glutathione Transferase ; metabolism ; Humans ; Plants, Medicinal ; chemistry ; Salvia miltiorrhiza ; chemistry