Diclofenac potassium delayed-sustained release pellets were prepared by double-layer coating method with ethylcellulose aqueous dispersion.The effects of release condition and pellet compositions on the in vitro drug release were evaluated.The formulation was optimized by the central composite design-response surface methodology.It was shown that the pH of the media greatly affected the in vitro drug release of the pellets while the viscosity of the media had little influence.Drug release from the pellets was related to the proportion of the inner coat to the outer coat and the amount of pore forming agent in the outer coat.The optimization of the formulation could be achieved by the central composite design-response surface methodology.

OBJECTIVE:To provide reference for medical costs control in China. METHODS:Based on main characteristics of the United States health service system,information asymmetry,principal-agent theory and Freedman’s consumption theory were used to analyze the advantages of restrictive relationship among doctors,hospitals and health insurance institutions in control-ling medical costs and improving the quality of diagnosis and treatment. The growth rate of medical cost,the percentage of drug ex-penditure and other aspects were compared between China and the United States;the effect of restrictive relationship on medical cost control was demonstrated. RESULTS & CONCLUSIONS:In the United States,there are hierarchical medical system and two-way referral system;for-profit hospitals and non-profit hospitals are mutually complementary;different natures of health insur-ance system,different payment methods and strict“commercial bribe”monitoring system are carried out;doctors,hospitals and health insurance restrict each other. Not only there are many advantages in theory,but also in practice the growth rate of medical cost and the percentage of drug expenditure are superior to our country. Finally it controls the rapid growth of medical cost to a cer-tain extent. Combined with our national conditions,learning from the United States experience,restrictive relationship among doc-tors,hospitals and health insurance institutions is established to control the increase of medical cost in China through reducing infor-mation asymmetry and standardizing payment audit;establishing a scientific pattern of mixed payment;strengthening the indirect impact of the health insurance institutions on doctors and hospitals,etc.

Both sides of the picornavirus genome have 5'-untranslated region (5'UTR) and 3'- untranslated region (3'UTR). This study demontrated that both the 5'-and 3'-UTR can form complex structures, such as stem-loop, clover and pseudoknot structure, These structures play an important role in the regulaton of the replication and translation of the viruses. This article reviewed the progress of research on the structure and function of picornavirus' 3'-UTR over recent years.
3' Untranslated Regions ; Animals ; Humans ; Nucleic Acid Conformation ; Picornaviridae ; chemistry ; genetics ; metabolism ; Picornaviridae Infections ; virology ; RNA, Viral ; chemistry ; genetics ; metabolism

Objective To observe the therapeutic effect of microencapsulated human retinal pigment epithelial (RPE) cell transplantation into the striatum in a rat model of Parkinson' disease (PD). Methods Cultured RPE cells were microencapsulated by alginate-polylysine-alginate (APA) using a high voltage electrostatic system. The Parkinsonian rats were divided into 4 groups, namely the model group, RPE group, APA group and RPE-APA group, and in the latter 3 groups, RPE cells, empty APA microcapsules and APA-capsulated RPE cells, respectively, were transplanted into the right striatum of the rats via stereotactic surgery. After the transplantation, the changes in apomorphine-induced rotation of the rats were investigated and the striatum DA contents were measured with high-performance liquid chromatography with electrochemical detection. Results TThe rotation of the rats in RPE-APA group was reduced by 51.48%, showing significant difference from that in the model control group 4 weeks after the transplantation (P<0.05). At 8 weeks after the transplantation, apomorphine-induced rotation in the RPE-APA group showed further significant reduction by 54.43% (P<0.05). The changes of DA contents in the striatum after transplantation were consistent with the changes in the rotation behavior of the rats. Conclusions Microencapsulated human RPE cell transplantation is a promising approach for the treatment of PD.

OBJECTIVETo determine the molecular basis of late onset ornithine transcarbamylase (OTC) deficiency in a Chinese family of Han nationality and the exon sequences of OTC gene of this patient.

METHODSPolymerase chain reaction-single strand conformation polymorphism and direct sequencing were used to identify the mutation type.

RESULTSA missense mutation E122G in the conserved residue of exon 4 was identified which is unreported before.

CONCLUSIONThe E122G mutation in human OTC gene may cause late onset OTC deficiency.

Age of Onset ; Base Sequence ; Child, Preschool ; DNA ; chemistry ; genetics ; DNA Mutational Analysis ; Family Health ; Fatal Outcome ; Female ; Humans ; Male ; Models, Molecular ; Mutation, Missense ; Ornithine Carbamoyltransferase ; chemistry ; genetics ; Ornithine Carbamoyltransferase Deficiency Disease ; enzymology ; genetics ; pathology ; Pedigree ; Polymorphism, Single-Stranded Conformational ; Protein Structure, Secondary

OBJECTIVETo establish fluorescence resonance energy transfer (FRET) assay method of detecting proteolytic activity of non-structural protein 3-4A (NS3-4A) serine protease of hepatitis C virus (HCV) for high throughput screening inhibitors against HCV in vitro.

METHODSHCV recombinant plasmid pMAL~c2/NS3-4A was transformed into the E.coli strain K12TB1. Maltose-binding-protein (MBP) NS3-4A fusion protein expression was induced by adding isopropyl-β-D-thiogalacto-pyranoside (IPTG) and purified by affinity chromatography. The proteolytic activity of MBP-NS3-4A protease was analyzed by FRET with the special protease substrate. The reaction system in this model was optimized, and the reliability of the model was evaluated.

RESULTSHigh throughput screening model for HCV NS3-4A protease inhibitors was established, and the best concentrations of enzyme and substrate were optimized. In the model, the Km value of protease was 4.74 μmol/L, Z factor was up to 0.80, and coefficient of variation (CV) was 1.91%. BILN 2061, one of the known HCV protease inhibitors, was measured with the Ki of 0.30 nmol/L.

CONCLUSIONThe assay model using FRET method for HCV NS3 4A serine protease is stable and reliable, and the model is suitable for high throughput screening for HCV NS3 4A protease inhibitors.

Antiviral Agents ; pharmacology ; Drug Evaluation, Preclinical ; Fluorescence Resonance Energy Transfer ; Hepacivirus ; enzymology ; High-Throughput Screening Assays ; methods ; Protease Inhibitors ; pharmacology ; Viral Nonstructural Proteins ; antagonists & inhibitors ; genetics

Animals ; Binding Sites ; Blood Glucose ; metabolism ; Diabetes Mellitus, Type 2 ; blood ; Enzyme Activation ; drug effects ; Enzyme Activators ; chemistry ; pharmacology ; Glucokinase ; chemistry ; metabolism ; Humans ; Hypoglycemic Agents ; chemistry ; pharmacology ; Molecular Conformation ; Phosphorylation ; drug effects ; Sulfones ; pharmacology ; Thiazoles ; pharmacology

BACKGROUNDIt is generally accepted that spleen plays a complex role in the tumor immunity, which would change in the different periods of cancer. In this study, we investigated the changes in the function of splenic macrophage (Mphi) in different stages of liver cancer induced by diethylnitrosamine (DEN) in rats. The aim was to support the characteristics of "two-way" and "phase" of spleen in tumor immunity.

METHODSThe model of pulmonary metastasis of liver cancer was established in forty male SD rats by DEN. In the 8th, 13th and 16th week, 10 rats were randomly chosen and sacrificed, and divided into cirrhosis, liver cancer and pulmonary metastasis groups depending on the pathological result, respectively. The other 10 rats were taken as control group. The Mphi was isolated by anchoring cultivation. The changes in ultrastructure, phagocytosis, cytokine secretion, antigen processing and presenting, and viability of splenic Mphi were detected by transmission electron microscopy, Vybrant(TM) Phagocytosis Assay, DQ(TM) Ovalbumin, and rat TNF-alpha ELISpot kits.

RESULTSUnder the electron microscope, the Mphi in the control group had some pseudopodium-like prominences, and mitochondria, ribosome, rough endoplasmic reticulum, lysosome can be found in the cytoplasm, and phagocytized RBC. In the liver cirrhosis and liver cancer group, Mphi had more prominences, meanwhile much more mitochondria, ribosome, rough endoplasmic reticulum, lysosome can be found in the cytoplasm, especially in the liver cancer group. In the pulmonary metastasis group, the Mphi was swelling, with few organelle. As compared to the control group, the function of splenic Mphi increased in cirrhosis and cancer groups, but decreased in metastasis group (phagocytosis rate: (84.7 +/- 1.9)%, (89.5 +/- 3.1)%, and (36.0 +/- 2.6)% vs (75.6 +/- 1.7)%, P < 0.05, P < 0.01; viability: (1.53 +/- 0.15)%, (1. +/- 0.14)%, and (1.12 +/- 0.29)% vs (1.48 +/- 0.17)%, P < 0.05, P < 0.01; TNF-alpha secretion: (741.0 +/- 52.9)%, (1126.2 +/- 174.5)%, and (313.8 +/- 50.8)% vs (626.6 +/- 24.6)%, P < 0.05, P < 0.01; positive cell rate of antigen processing and presenting: (24.03 +/- 1.87)%, (27.95 +/- 2.63)%, and (10.46 +/- 2.16)% vs (16.45 +/- 1.86)%, P < 0.01).

CONCLUSIONSIn the stage of cirrhosis and early cancer, the immune functions of splenic Mphi were reinforced. It may promote the non-specificity tumor immunity. On opposite, in the stage of pulmonary metastasis, the immune functions of splenic Mphi were impaired. It may lead to the decrease of tumor immunity.

Animals ; Cells, Cultured ; Diethylnitrosamine ; toxicity ; Disease Models, Animal ; Liver Cirrhosis ; immunology ; pathology ; Liver Neoplasms, Experimental ; chemically induced ; complications ; immunology ; ultrastructure ; Lung Neoplasms ; immunology ; secondary ; ultrastructure ; Macrophages ; pathology ; ultrastructure ; Male ; Microscopy, Electron, Transmission ; Rats ; Rats, Sprague-Dawley ; Spleen ; pathology ; ultrastructure

It review the structure-function relationship of natural anthraquinone derivatives from Radix et Rhizoma Rhei. The anthraquinone derivatives had many identical activities because they have the identical mother nucleus; but the strength of their activities were different, because they have different substitution groups. The anthraquinone derivatives shown the obvious structure-function relationship in many respects, such as antioxygenation, antibiosis, anticancer, the influence of immunity and so on.
Anthraquinones ; chemistry ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Molecular Structure ; Rheum ; chemistry ; Structure-Activity Relationship

OBJECTIVETo observe clinical results of Chinese herbs promoting blood circulation and removing blood stasis on the treatment of reflex sympathetic dystrophy (RSD) with type of stagnation of vital energy and blood stasis.

METHODSRSD with type of stagnation of vital energy and blood stasis was distinguished as erubescence, high temperature, perspiration, damp and acro-edema, with middle level pain. From 2006 to 2008, 58 patients with RSD of stagnation of vital energy and blood stasis were randomly divided into the treatment group (30 cases) and the control group (28 cases). The former were treated with Chinese medicine to activate blood circulation and improve bone and muscle nourishment. Chinese medicine includes: Caesalpinia Sappan 10 g, Ligusticum Chuanxiong 6 g, Frankincense 6 g, Angelica 10 g, Safflower 6 g, Myrrh 6 g, Ground Beetle 10 g, Araliaceae 3 g, Radix Paeoniae Rubra 10 g, Pericarpium Citri Reticulatae 5 g, Lawn Pennywort Herb 15 g, Manis Pentadactyla 10 g, Corydalis Yanhusuo 10 g, Rhizoma Drynariae 15 g, which were boiled into decoction and the patients were take orally everyday with a course of treatment for 10 days, together with the boiled Chinese traditional medicine of stretching muscle and activating blood circulation to fume and wash the limbs twice everyday. The compatibility of medicines in prescription includes: Lycopodium Japanicum Grass 10 g, Gentiana Macrophylla Pall 10 g, Radix Angelicae Pubescentis 10 g, Angelica 10 g, Uncaria 10 g, Frankincense 6 g, Myrrh 6 g, Safflower 6 g. Control group were treated with a placebo of the same color for oral use and external application. The delivery times, method and the time of therapy were all the same as the treatment group. After 30 days' treatment, the effective indexes of VAS pain score and swelling condition were observed in both groups.

RESULTSVAS pain score: the treatment group decreased (3.8 +/- 0.8) points and the control group decreased (1.0 +/- 0.3) points, the difference between the two groups was significantly (P < 0.01). There was significantly difference in volume decrease of the swelling limb between treatment group (21.8 +/- 2.5) ml and the control group (10.3 +/- 2.1) ml (P < 0.01). The efficiency difference between treatment group and control group was significantly(P<0.01).

CONCLUSIONWith the different treatment based on different syndrome and emphasis on the nourishment of bone and soft tissue, treated by Chinese medicine to promote blood circulation and remove blood stasis in stagnation of vital energy and blood stasis, RSD get a favorable result.

Adult ; Aged ; Blood Circulation ; drug effects ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Reflex Sympathetic Dystrophy ; drug therapy ; Treatment Outcome