Acupuncture Therapy ; Adult ; Combined Modality Therapy ; Female ; Humans ; Male ; Musculoskeletal Manipulations ; Osteitis ; pathology ; therapy ; Sacroiliac Joint ; pathology ; Sclerosis ; therapy ; Young Adult

OBJECTIVE: To explore the characteristics of crystallization inhibition by cellulose polymers against supersaturated drugs. METHODS: The biopharmaceutics classification system(BCS) II class drug indometacin was selected as the model drug.Supersaturated amorphous drug solid was prepared and the solubility of indometacin was measured. The types, added amounts, ionic intensity and viscosity of cellulose polymers were employed as influential factors to assess the crystallization inhibition effect of polymers against indometacin. RESULTS: HPMC E15 displayed the strongest crystallization inhibition effect. The crystallization inhibition was enhanced by adding larger amount of polymers, decreasing the viscosity of polymers and increasing the ionic intensity. CONCLUSION: The study is helpful to clarify the profiles that cellulose polymers inhibit the crystallization of drugs in supersaturated states. This research may provide scientific guide for the practical application of cellulose polymers for drug crystallization.

OBJECTIVE: To prepare curcumin solid dispersions by different preparation technologies and compare their properties. METHODS: Curcumin/poloxamer 407 solid dispersions were prepared by freeze-drying, co-precipitation and microwave/quench cooling methods, respectively. Internal properties of obtained solid dispersion were analyzed by SEM, DSC, XRD and FT-IR. The improvement effect on the insolubility of curcumin by making it into solid dispersions by different technologies was characterized by dissolution and solubility experiments. RESULTS: Curcumin was dispersed in solid dispersions in micro-crystal form. Compared with other technologies, microwave/quench cooling method could significantly improve the solubility and dissolution of insoluble curcumin. CONCLUSION: The study provides reference for choice of applicable production technology for solid dispersions of insoluble Chinese traditional medicine curcumin.

Animals ; Binding Sites ; drug effects ; Brain ; metabolism ; Calcium ; metabolism ; Cerebral Cortex ; metabolism ; Cyclic AMP ; metabolism ; Hippocampus ; metabolism ; Insecticides ; toxicity ; Male ; Organothiophosphorus Compounds ; toxicity ; Phosphoramides ; Rats ; Rats, Sprague-Dawley

Animals ; Cells, Cultured ; Interleukin-1beta ; pharmacology ; Male ; Neurons ; drug effects ; metabolism ; Nitric Oxide ; metabolism ; Nitriles ; toxicity ; Pyrethrins ; toxicity ; Rats ; Rats, Sprague-Dawley ; Sodium-Potassium-Exchanging ATPase ; metabolism

A lipopeptide compound was isolated from the culture of Bacillus subtilis HSO121 by methods of acidic precipitation, solvent extract, fractional precipitation, adsorption and prepared thin-layer chromatography; and its molecular structure was determined by by ninhydrin assay and IR methods following the Amino analysis, MS-MS and ESI-MS. It shows that the isolated lipopeptide consists of two homologues with molecular mass 1,022D and 1,036D and bearing a cyclic structure with the amino acid sequence Leu-Leu-Asp-Val-Leu-Leu-Glu in the peptide chain, which indicates that the isolated lipopeptide falls into the analogs of surfactin.

Adenocarcinoma ; pathology ; surgery ; Aged ; Carcinoma, Signet Ring Cell ; pathology ; surgery ; Cell Differentiation ; Female ; Follow-Up Studies ; Gastrectomy ; methods ; Humans ; Male ; Middle Aged ; Paneth Cells ; pathology ; Stomach Neoplasms ; pathology ; surgery

OBJECTIVEChinese herbal medicine has been extensively used in the treatment of vascular dementia (VaD), but lacked systematic review on its efficacy and safety. So we conducted a systematic review to assess the efficacy and safety of Chinese herbal medicine in treating VaD.

METHODSCNKI, CBM, PubMed, and Wiley Online Library were retrieved for randomized trials (RCTs) on Chinese herbal medicine treating VaD patients. Randomized parallel control trials by taking Chinese herbal medicine as one treatment method and placebos/cholinesterase inhibitors/Memantine hydrochloride as the control were included. Quality rating and data extraction were performed. RevMan5.2.0 Software was used for meta-analysis. Standardized mean difference (SMD) at 95% confidence interval (CI) was used to indicate effect indicators of results.

RESULTSSeven RCTs met the inclusive criteria. Totally 677 VaD patients were randomly assigned to the treatment group and the control group. Descriptive analyses were performed in inclusive trials. The cognitive function was assessed in all trials. Results showed Mini-Mental state examination (MMSE) score was better in the Chinese herbal medicine group than in the placebo group, but with no significant difference when compared with the donepezil group (P > 0.05). Adverse reactions were mainly manifested as gastrointestinal symptoms such as abdominal pain in the Chinese herbal medicine group. But they occurred more in the donepezil group than in the Chinese herbal medicine group.

CONCLUSIONSThe methodological quality of included trials was poor with less samples. Results of different trials were lack of consistency. Present evidence is not sufficient to prove or disapprove the role of Chinese herbal medicine in improving clinical symptoms and outcome indicators of VaD patients. Their clinical efficacy and safety need to be supported by more higher quality RCTs.

Complementary Therapies ; Dementia, Vascular ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Indans ; therapeutic use ; Piperidines ; therapeutic use ; Randomized Controlled Trials as Topic

OBJECTIVETo study the toxicity of methomyl to acetylcholinesterase (AChE) in different regions.

METHODSThe optimal temperature and time for measurement of AChE activity were determined in vitro. The dose- and time-response relationships of methomyl with AChE activity in human erythrocyte membrane, rat erythrocyte membrane, cortical synapses, cerebellar synapses, hippocampal synapses, and striatal synapses were evaluated. The half maximal inhibitory concentration (IC50) and bimolecular rate constant (K) of methomyl for AChE activity in different regions were calculated, and the type of inhibition of AChE activity by methomyl was determined.

RESULTSAChE achieved the maximum activity at 370 °C, and the optimal time to determine initial reaction velocity was 0-17 min. There were dose- and time-response relationships between methomyl and AChE activity in the erythrocyte membrane and various brain areas. The IC50 value of methomyl for AChE activity in human erythrocyte membrane was higher than that in rat erythrocyte membrane, while the Ki value of methomyl for AChE activity in rat erythrocyte membrane was higher than that in human erythrocyte membrane. Among synapses in various brain areas, the striatum had the highest IC50 value, followed by the cerebellum, cerebral cortex, and hippocampus, while the cerebral cortex had the highest Ki value, followed by the hippocampus, striatum, and cerebellum. Lineweaver-Burk diagram demonstrated that with increasing concentration of methomyl, the maximum reaction velocity (Vmax) of AChE decreased, and the Michaelis constant (Km) remained the same.

CONCLUSIONMethomyl is a reversible non-competitive inhibitor of AChE. AChE of rat erythrocyte membrane is more sensitive to methomyl than that of human erythrocyte membrane; the cerebral cortical synapses have the most sensitive AChE to methomyl among synapses in various brain areas.

Acetylcholinesterase ; metabolism ; Animals ; Cerebellum ; drug effects ; Cerebral Cortex ; drug effects ; Erythrocyte Membrane ; drug effects ; enzymology ; Hippocampus ; drug effects ; Humans ; Inhibitory Concentration 50 ; Methomyl ; toxicity ; Rats ; Synapses ; drug effects ; Toxicity Tests

Converting two poorly water-soluble crystalline drugs to co-amorphous drug systems by ball milling, quench-cooling, or cryo-milling method can improve stability of the drug, enhance dissolution rates, and reduce adverse reactions of the single drug. Co-amorphous system has been used to solve problems of co-administration of medicines. Formation and intermolecular interactions of co-amorphous drug systems may be verified by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Raman spectroscopy (RS) and Fourier transform infrared spectroscopy (FT-IR). Stability of co-amorphous drug systems is influenced by their glass transition temperature (Tg) and intermolecular interactions. The theoretical Tg values and the interaction parameter x are calculated by Gordon-Taylor equation and the Flory-Huggins equation, respectively. Thus, co-amorphous drug systems are analyzed theoretically at molecular level. Co-amorphous drug systems provide a new sight for the co-administration of medicines.
Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; methods ; Cimetidine ; chemistry ; Drug Combinations ; Drug Compounding ; Drug Stability ; Glipizide ; chemistry ; Indomethacin ; chemistry ; Naproxen ; chemistry ; Ranitidine ; chemistry ; Simvastatin ; chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Spectrum Analysis, Raman ; Technology, Pharmaceutical ; methods ; Temperature ; X-Ray Diffraction