With the development of natural products, the research activities on the solubilization methods of water-insoluble natural products have been carried out worldwide. Big molecular weight and poor solubility of most natural active ingredients lead to a very poor oral absorption and low bioavailability, which has extremely limited their development in pharmaceutical fields and clinical application. As a result, it is necessary to find out a suitable technique to improve the solubility and enhance the oral bioavailability of insoluble natural drugs. Based on the related references published in these years, this review introduced some new techniques to improve the solubility and bioavailability of natural drugs, including prodrugs, inclusion complex, solid dispersion, cocrystals, osmotic pump, liquisolid compacts, micronization, self-microemulsifying, nanosuspensions, lipsomes, polymeric micelles and so on, and summarized the theory, characteristics, application range, application examples, problems and development direction of each technique.
Administration, Oral ; Biological Availability ; Biological Products ; administration & dosage ; chemistry ; pharmacokinetics ; Chemistry, Pharmaceutical ; methods ; trends ; Solubility ; Technology, Pharmaceutical ; methods ; trends ; Water

Objective This study was to observe the biological effects of eprenone on proliferation ,migration and apoptosis in human gastric epithelial cell line .Methods Human gastric epithelial cells GES‐1 were cultured in vitro .MTT assay were used to e‐valuate the proliferation of GES‐1 cells in different concentrations of teprenone and ensure the appropriate drug concentration .T ran‐swell test and scratch test were used to detect the migration ability of GES‐1 cells treated with appropriate concentration of eprenone .Flow cytometry analysis were used to detect the apoptosis of GES‐1 cells treated by the appropriate concentration of eprenone .Results Treated with eprenone for 24 h ,the proliferation of GES‐1 cells were increased as the concentration of teprenone from 10 to 80 μmol/L ,but from 80 to 320 μmol/L ,the promoting effect showed no staticall significant changes .So the appropriate drug concentration was determined to be 80 μmol/L .Treated with teprenone (80 μmol/L) for 24 h ,the transwell test showed that the migration rate of the teprenone group was 3 .338 ± 0 .293 and the control group was 1 .328 ± 0 .208 .So the number of staining blue cells in eprenone group were more than in control group obviously under membrane of transwell chambers (P<0 .01) .Scratch test showed that the migration rate of the eprenone group was 1 .00 ± 0 .18 and the control group was 0 .72 ± 0 .08 .Similarly ,the migration rate of eprenone group was higher than the control group(P<0 .05) .Treated with teprenone (80 μmol/L) for 48 h ,the apoptosis rate of the teprenone group was (11 .90 ± 1 .53)% and the control group was (25 .61 ± 0 .15)% ,the cellular apoptosis of eprenone group was lower than the control group (P<0 .01) .Conclusion Teprenone can promote the proliferation and migration , inhibit the apoptosis of GES‐1 cells .

Objective To study the clinical significance of P - selection expression in children with viral encephalitis and the correlation between this expression and the cerebral infarction with critical viral encephalitis. Methods Flow cytometric was employed to detect the expression of P- selection on the surface of platelet membrane in 44 children with viral encephalitis(20 light patients and 24 critical patients) and 20 healthy control children. The area of the cerebral infarction was determined by computed tomographic scan in 20 patients with critical viral encephalitis. The correlation between the two variables was analyzed. Results The expressions of P - selection on the surface of platelet membrane on less than 5 days and on 2 weeks after the onset of viral encephalitis were significantly higher in critical patients than those in normal control children and light patients( P

Aged ; Angina Pectoris, Variant ; physiopathology ; Coronary Vasospasm ; physiopathology ; Coronary Vessels ; physiopathology ; Humans ; Male

Humans ; Hypertension, Pulmonary ; etiology ; Male ; Middle Aged ; POEMS Syndrome ; complications

Cerebrospinal Fluid Rhinorrhea ; surgery ; Craniotomy ; methods ; Endoscopy ; Frontal Sinus ; surgery ; Humans ; Male ; Nose ; surgery ; Reconstructive Surgical Procedures ; methods ; Young Adult

Objective To reproduce a scratch-wound model in cultured rat astrocytes (AST).Methods The secondary cultured AST prepared from newborn Wistar rat cerebral cortex were scratched with plastic pipette tips. The morphologic change of AST was observed through microscope at 10 min before and 1, 3, 6, 12, and 24 h after injury, meanwhile the lactate dehydrogenase (LDH) leakages in the cultured medium were determined.Results Immediately after injury the edge of the scratch was lined with irregularly shaped cell. 6 h after injury the AST processes began extending to cell-free area, and elongated further at 12 and 24 h after injury, with presented of new generated cells in the denuded area. At different times after injury, the LDH leakages of the experiment group were higher than that before injury ( P<0.05), and were higher than that of the control group ( P<0.05).Conclusion According to observed AST morphologic changes and determined LDH leakages in culture medium, the scratch-wound model in cultured rat AST is successfully reproduced.

Melatonin has been reported to inhibit hepatic fibrosis and the mechanism may be correlated to its anti-oxidant effect.Nevertheless,the mechanism is not completely identified.This study was conducted to investigate the effects of melatonin on TGF-β1/Smad signaling pathway in liver fibrosis in rats.The liver fibrosis model was made by the subcutaneous injection of CCl4.The liver pathology changes were detected using hematoxylin and eosin (H&E) staining and Van Gieson (VG) staining.Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities were measured with an autoanalyzer.Glutathione peroxidase (GPx) activities and levels of malondialdehyde (MDA) and hydroxyproline (Hyp) in liver were evaluated by spectrophotometry.Expression levels of TGF-β1,Smad2/3,phosphorylated Smad2/3 (p-Smad2/3) and Smad7 in liver were detected by immunohistochemistry and Western blot analysis.Results showed that melatonin suppressed CC14-induced liver fibrosis,along with an improvement in histological changes,significant decreases in pathologic grading sores and obvious decreases in Hyp levels in liver.Melatonin improved liver function indicated by decreased serum ALT and AST activities.In addition,melatonin exerted its anti-oxidant effects,as supported by decreased MDA levels and increased GPx activities in liver.Furthermore,melatonin inhibited TGF-β1/Smad pathway,as evidenced by decreased TGF-β1,Smad2/3 and p-Smad2/3 expression and increased Smad7 expression in liver.In conclusion,melatonin may suppress CCl4-induced hepatic fibrosis in rats via inhibiting TGF-β1/Smad pathway.It is possible for melatonin to be a potential reagent to treat and cure liver fibrosis.

Objective To investigate the effect of recipient's pre-transplant triglyceride (TG) abnormalities on early graft function (EGF) after kidney transplantation.Methods According to the inclusion and exclusion criteria,154 identified living-kidney transplant recipients in the 309 Hospital of Chinese PLA from Jan.2011 to Dec.2014 were enrolled in present study,including 124 males and 30 females,and aged of 31.9 ± 8.4 years.The cohort was divided into two groups:TG normal group (0.40＜TG≤1.70mmol/L,n=107) and TG abnormalities group (TG＞l.70mmol/L or require lipid lowering therapy,n=47).The incidences of poor early graft renal function (PEGF),slow graft function (SGF) and delayed graft function (DGF) were compared between the two groups,and then the serum creatinine (Scr) levels were compared among the patients showing immediate graft function (IGF) at 3rd,7th and 30th day after transplantation.The ROC curve was drawn up taking TG as diagnosis index to explore the optimal cut-offvalue for predicting PEGF,SGF and DGF after transplantation.Results Compared with the TG normal group,the TG abnormalities group showed significantly higher incidence of PEGF and DGF (P＜0.05).Among the IGF patients,the TG abnormalities group showed higher Scr level at the 7th and 30th day after transplantation (P＜0.05).The area under ROC curve (AUC) reflected TG levels for PEGF,SGF and DGF were 0.774,0.704 and 0.818,respectively (P＜0.05).The optimal cut-offvalues were all 1.37mmol/L.Conclusions Recipients with abnormal pre-transplant TG level may have worse EGF after renal transplantation.The risk of developing PEGF,S GF and D GF tends to emerge when pre-transplant TG level is higher than 1.37mmol/L.

The method of quantitative nuclear magnetic resonance spectroscopy (qNMR) for determination of epigoitrin in Radix Isatidis was established based on solid phase extraction (SPE).The twice ultrasonic extraction method using pure water was used for fully extracting epigoitrin in sample, and then the extraction was enriched and concentrated by poly-Sery MCX SPE cartridge.The effect of sample pretreatment and qNMR experimental conditions was investigated.The qNMR experiment conditions were selected using DMSO as solvent, calibrated 2,3,5-triiodobenzoate as internal standard, and P1(pulse width)=14.1 μs, d1(pulse delay time)=5 s, NS(number of scan)=256.The .1H-NMR peaks of δ 5.365-5.399 (H-7b, d, 1H) of epigoitrin were chosen as the quantitative peaks.Method validation was performed including precision (intra-day precision RSD was 0.5%, and the inter-day precision was 0.8%), linearity (correlation coefficient r>0.9991), LOD (0.05 mg/g, standard curve method) and LOQ (0.19 mg/g, S/N≥150).The recoveries of the SPE-qNMR were 97.4%-101.7%.The result showed that the method was stable, accurate and reliable.With this method the epigoitrin in a real Radix Isatidis was determined to be <0.19-1.26 mg/g.SPE combining with qNMR could extend the application field of qNMR, especially in the detection of low-content component in complex samples.