OBJECTIVE: To prepare starch microspheres of diclofenac sodium by inverse crosslink emulsification method. METHODS: Mean particle size and encapsulation efficiency of starch microspheres were used as indicators, single factor and orthogonal design methods were performed for optimizing preparation process and formulations of starch microspheres. The appearance and structure of the microspheres were researched by optical microscope, transmission electron microscope, infrared spectroscopy and differential thermal analyzer. In vitro drug release behavior was investigated by dialysis method. RESULTS The preparation conditions optimized by orthogonal design; the concentration of starch 10%, crosslinking temperature 55℃, dosage of cross-linking agent 0.2 g, the volume ratio of oil phase and water 5:1, amount of emulsifier 5 mL, cross-linking time 60 min. Starch microsphere obtained by above condition has an average particle size of 9 μm, appearance is irregular spherical shape, and encapsulation efficiency was 67.52%. Results of IR spectra and DTA curves showed that starch cross-links have happened. CONCLUSION In vitro releasing curve showed that the diclofenac sodium starch microspheres have good sustain release effect, drug release complies with the Weibull equation.

OBJECTIVE: To prepare coenzyme Q10-γ-cyclodextrin nano-crystal suspension using high pressure homogeneous combining freeze-drying method, optimize the preparation technology, and evaluate the quality of the product. METHODS: Encapsulation efficiency and mean particle size of inclusion complex were used as indicators, and response surface method was performed for optimizing preparation process and formulations. The stability and transdermal performance in vitro of the inclusion complexes were investigated. RESULTS: The optimal technical parameters were as follows; the mass ratio of γ-cyclodextrin and drug, 7.76:1; ultrasonic temperature, 40℃; ultrasonic time, 28.33 min; homogeneous pressure, 40 MPa. Under such conditons, an average encapsulation efficiency of 48.39% and average particle size of 324 nm were obtained for the nano-crystal suspension. The transdermal experiment in vitro showed that the infiltration rate of inclusion was 5.68 μg·cm-2·h-1. CONCLUSION: The preparation method is simple and feasible. The product quality is stable. Moreover, it is easy to manufacture.

OBJECTIVE: To investigate the O/W submicron emulsion injection formulation, and investigate its pharmacokinetics in the rat. METHODS: Pseudo-ternary phase diagrams were established using the water titration method. The effects of different surfactants, cosurfactants and Km values on the phase diagram were investigated, and the prescription of submicron emulsion formulation was optimized. Stability of coenzyme Q10 submicron emulsion was evaluated, and the pharmacokinetics in the rat after intravenous injection was study. RESULTS: Coenzyme Q10 submicron emulsion consisting of Poloxamer188/Lipoid S100/ethanol/PEG400/water has the lower viscosity, the smaller size and the higher encapsulation efficiency. An obvious sustained-release effect of coenzyme Q10 submicron emulsion was observed after iv injection in the pharmacokinetics experiment, and mean residence time is 6. 55 h. CONCLUSION: The optimized coenzyme Q10 submicron emulsion consumes smaller quantities of auxiliary materials and shows good stability. Moreover, it is easy to manufacture and convenient for clinical use. Copyright 2012 by the Chinese Pharmaceutical Association.

Objective To evaluate the radioprotective effect of vanillin derivative VND3207 on DNA damage induced by different LET ionizing radiation.Methods The plasmid DNA in liquid was irradiated by 60Co γ-rays, proton or 7Li heavy ion with or without VND3207.The conformation changes of plasmid DNA were assessed by agarose gel electrophoresis and the quantification was done using gel imaging system.Results The DNA damage induced by proton and 7Li heavy ion was much more serious as compared with that by 60Co γ-rays, and the vanillin derivative VND3207 could efficiently decrease the DNA damage induced by all three types of irradiation sources, which was expressed as a significantly reduced ratio of open circular form (OC) of plasmid DNA.The radioprotective effect of VND3207 increased with the increasing of drug concentration.The protective efficiencies of 200 μmol/L VND3207 were 85.3% (t =3.70,P =0.033), 73.3% (t = 10.58, P =0.017)and 80.4% (t =8.57,P =0.008)on DNA damage induction by 50 Gy of γ-rays, proton and 7Li heavy ion, respectively.It seemed that the radioprotection of VND3207 was more effective on DNA damage induced by high LET heavy ion than that by proton.Conclusions VND3207 has a protective effect against the genotoxicity of different LET ionizing radiation, especially for γ-rays and 7 Li heavy ion.

Objective: To study the protective effects of Panax quinquefolium 20s-protopanaxdiolsaponins extracted from leaves of P.quinquefolium（PQDS）on acute myocardial infarction（AMI）in dogs. Method：The parameters of myocardial infart size , the serum CK and LDH activity, myocardial metabolism,free radicals and coronary circulation etc were determined by using the model of ligation of LAD in the anaesthetized open-chest dogs. Result：In dogs treated with PQDS（in a dosage of 10 and 20 mg*kg-1 iv infusion），the myocardial infarct size, the activity of serum CK ,LDH and the contents of serum FFA and LPO were decreased，whereas the activity of serum SOD and GSH-Px increased markedly.At the same time, myocardial blood flow was increased and coronary vascular resistance decreasedsignificantly. Conclusion：PQDS has protective effect on myocardial ischemia by modifying metabolic dysfunction of FFA, inhibiting oxygen free radicalmediated peroxidation of membrane lipids ， enhancing endogenous antioxidase activity and increasing myocardial blood supply.

OBJECTIVETo observe effects of ginsenoside-Rb (G-Rb) on total cholesterol, lipoprotein cholesterol metabolism and anti-oxidation in experimental hyperlipidemia rats.

METHODHyperlipidemia rats were respectively given G-Rb 50, 100, 200 mg x kg(-1) x d(-1) ig for twelve days. Total cholesterol, lipoprotein cholesterol and lipid peroxidation (LPO) contents, prostacycline (PGI2), thromboxane (TXA2), superoxide dismutase (SOD) and blood viscosity were measured. Fat accumulation in liver was also observed.

RESULTTriglyceride (TG), total cholesterol (TC), low density lipoprotein cholesterol (LDL-c) in serum, TXA2 in plasma, LPO in serum and liver, and blood viscosity were decreased significantly. High density lipoprotein cholesterol (HDLc) in serum, PGI2 in plasma and SOD in serum and liver were significantly increased by G-Rb (100, 200 mg x kg(-1)) in experimental hyperlipidemia rats. In addition, G-Rb could decrease TC/HDL-c, LDLc/HDL-c ratio, increase PGI2/TXA2 ratio and inhibit fat accumulation in liver.

CONCLUSIONG-Rb could have anti-arteriosclerosis effect by improving cholesterol and lipoprotein-cholesterol metabolism, suppressing lipid peroxidation, increasing anti-oxidase activity and PGI2/TXA2 ratio.

Animals ; Antioxidants ; pharmacology ; Female ; Ginsenosides ; pharmacology ; Hyperlipidemias ; metabolism ; Lipid Peroxides ; metabolism ; Liver ; metabolism ; Male ; Rats ; Rats, Wistar

This study was aimed to investigate the expression and clinical significance of IL-18, IL-18 binding protein (IL-18BP), IFN-γ and IL-4 secreted from splenocytes of patients with idiopathic thrombocytopenic purpura (ITP) in vitro. Spleen mononuclear cells (MNC) were prepared by using routine sterile method, and were cultured in RPMI 1640 complete medium containing 10 µg/ml PHA, 10% fetal calf serum at 37°C and 5% CO2. The levels of IFN-γ, IL-4, IL-18 and IL-18BP secreted from MNC of ITP patients and normal controls were determined after culture for 48 hours. The results showed that after culture of spleen MNC for 48 hours, the levels of IL-18 and IFN-γ were significantly higher in patients with ITP than that in controls, but the levels of IL-18BP was not significantly elevated in ITP patients. The level of IL-4 was below the detectable limit of the assay used. It is concluded that imbalance between IL-18 and IL-18BP may play an important role in pathogenesis of ITP, and regulation of balance between IL-18 and IL-18BP may be a therapeutic approach against ITP.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Cells, Cultured ; Female ; Humans ; Intercellular Signaling Peptides and Proteins ; secretion ; Interferon-gamma ; secretion ; Interleukin-18 ; secretion ; Interleukin-4 ; secretion ; Lymphocytes ; cytology ; metabolism ; Male ; Middle Aged ; Purpura, Thrombocytopenic, Idiopathic ; metabolism ; Spleen ; cytology ; metabolism ; Young Adult

OBJECTIVETo observe the time course of proliferation and differentiation of neural stem cells (NSCs) in the subventricular zone (SVZ) of rats following traumatic craniocerebral injury (TBI).

METHODSForty-eight SD rats were randomized into 3 groups, namely the control group without any treatment, the sham-operated group with scalp incision and preparation of a cranial window, and TBI group with craniocerebral injury induced by Feeney's method. With nestin and BrdU as two cell markers, NSE as the neuron-specific marker and GFAP as the glial cell marker, immunofluorescence assay with double labeled antibodies was performed to examine the proliferation and differentiation of endogenous NSCs in the SVZ at different time points after TBI.

RESULTSs The numbers of cells positive for nestin/NSE, nestin/GFAP, BrdU/NSE, and BrdU/GFAP in the SVZ of the rats increased significantly after TBI. The positive cells began to increase at 1 day after TBI, reached the peak level at day 3 and became normal at day 14, showing significant differences between the time points of measurement following TBI and from the cell numbers in the control group measured at the same time points. The cells positive for nestin/ GFAP showed the most distinct increase in the SVZ of the rats with TBI.

CONCLUSIONTBI results in mobilization of the NSCs in the SVZ on the injured side to cause the proliferation and differentiation of the endogenous NSCs. The SVZ is one of the most important germinal centers of NSC proliferation and differentiation.

Animals ; Bromodeoxyuridine ; metabolism ; Cell Differentiation ; Cell Proliferation ; Craniocerebral Trauma ; pathology ; Glial Fibrillary Acidic Protein ; metabolism ; Lateral Ventricles ; cytology ; Nestin ; metabolism ; Neural Stem Cells ; cytology ; Neuroglia ; cytology ; Neurons ; cytology ; Phosphopyruvate Hydratase ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo observe the protective effect of Acanthopanax senticosus saponins (ASS) on myocardial ischemia-reperfusion injury in rats.

METHODThe myocardial ischemia-reperfusion model was induced by 30 min left anterior descending coronary occlusion and 120 min reperfusion in rats. The changes of myocardial infarct size (MIS), the serum creatine phosphokinase (CK) and lactate dehydrogenase (LDH) activity, the serum lipid peroxidation (LPO) content and superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activity and plasma endothelin (ET), angiotensin II (Ang II), prostacycline (PGI2) and thromboxane A2 (TXA2) levels and myocardial free fatty acid (FFA) content of infarct and noninfarct area were determined.

RESULTIn rats treated by ASS (in a dosage of 25, 50 and 100 mg x kg(-1) i.v. at 30 min after coronary occulusion), the MIS was significantly reduced, the serum CK and LDH activity, the plasma ET, Ang II and TXA2 level and myocardial FFA content declined, while plasma PGI2 level and PGI2/TXA2 was increased signficantly. In addition, serum LPO content declined, SOD and GSH-Px activity were increased markedly.

CONCLUSIONASS has protective effect on myocardial ischemia-reperfusion injury, which may be due to its function of improving free radicals and myocardial metabolism, decreasing plasma ET, Ang II and TXA2 levels and increasing plasma PGI2 level and PGI2/TXA2 ratio etc.

Animals ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Eleutherococcus ; chemistry ; Female ; Male ; Myocardial Reperfusion Injury ; metabolism ; pathology ; Myocardium ; metabolism ; pathology ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar ; Saponins ; isolation & purification ; pharmacology

OBJECTIVETo observe the protective effect of compound acanthopanax senticosus injection (CASI) on myocardial ischemia-reperfusion arrhythmia in rats.

METHODThe myocardial ischemia-reperfusion model was induced by 30 min coronary occulusion and 60 min reperfusion in openchest anesthetized rats. The changes of arrhythmia with electrocardiogram lead II, the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), the contents of malondialdehyde (MDA) and Ca2+ in myocardium were determined.

RESULTIn rats treated by CASI (in a dosage of 25, 50 and 100 mg x kg(-1) femoral vein infusion at 30 min after coronary occulusion), the incidence of myocardial ischemia-reperfusion ventricular arrhythmias, for instance the ventricular tachycardia (VT) and ventricular fibrillation (Vf), was effectively prevented, the appearing time of arrhythmia was delayed and the duration of arrhythmia was shortened, while the elevated ST segment lowered as well. At the same time, the contents of myocardial Ca2+ and MDA were decreased significantly as well as the activities of myocardial SOD and GSH-Px increased markedly.

CONCLUSIONCASI is of protective effect on myocardial ischemia-reperfusion arrhythmia, which may be related to scavenging the oxygen free radicals and Ca2+ overload formed during reperfusion.

Animals ; Anti-Arrhythmia Agents ; isolation & purification ; pharmacology ; Arrhythmias, Cardiac ; drug therapy ; etiology ; physiopathology ; Calcium ; metabolism ; Drug Combinations ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Electrocardiography ; Eleutherococcus ; chemistry ; Female ; Ginsenosides ; isolation & purification ; pharmacology ; Glutathione Peroxidase ; metabolism ; Male ; Malondialdehyde ; metabolism ; Myocardial Reperfusion Injury ; complications ; Myocardium ; metabolism ; pathology ; Panax ; chemistry ; Phytotherapy ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar ; Saponins ; isolation & purification ; pharmacology ; Superoxide Dismutase ; metabolism