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 To observe the preventive effect of salmeterol xinafoate and fluticasone propionate aerosol on radiation pneumonia in patients with local advanced non-small cell lung cancer (NSCLC) after radiotherapy.Methods Sixty-four patients with local advanced NSCLC were randomly divided into the study group and the control group.Both groups were treated with intensity modulated radiation therapy treatment and routine interventions.Salmeterol xinafoate and fluticasone propionate aerosol were given to the study group from the first day of radiation therapy at both the morning and evening time.Clinical symptoms,chest CT,Karnofsky score and tumor necrosis factor-α (TNF-α) levels in the two groups were analyzed at the time before radiotherapy and three months after radiotherapy.Results The radiation pneumonia incidence of the study group was lower than that of the control group [21.9 ％(7/32) vs 46.9 ％(15/32)].The plasma TNF-α content after radiotherapy of the study group was lower than that of the control group [(9.18±3.45) ng/ml vs (13.38 ± 2.75) ng/ml].Moreover,the Karnofsky score of the study group was higher than that of the control group [(81.67 ± 7.18) scores vs (75.00+ 6.74) scores].The differences between the two groups were statistically significant (all P＜ 0.05).Conclusion Salmeterol xinafoate and fluticasone propionate aerosol can reduce the radiation incidence of the patients with local advanced NSCLC,improve patients' quality of life after radiotherapy and prevent the radiation pneumonia.

Peroxisome proliferator-activated receptors (PPARs) are nuclear transcriptional factors closely related to glucose and lipid metabolism, insulin sensitivity. Activation of PPARs targets treated type 2 diabetes, obesity, hypertension and other metabolic diseases by insulin resistance. Recently, a variety of active ingredients of traditional Chinese medicines (TCMs) have been proved to activate PPARs targets for improving insulin resistance, which has attracted widespread attention at home and abroad. In this paper, we reviewed the pathological mechanisms between insulin resistance and PPARs, and summarized the active ingredients of TCMs improved insulin resistance based on PPARs targets. This paper may provide some theoretical guidance for the development of new drugs and TCMs.
Animals ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Insulin Resistance ; Metabolic Diseases ; drug therapy ; genetics ; metabolism ; Peroxisome Proliferator-Activated Receptors ; antagonists & inhibitors ; genetics ; metabolism

Objective To evaluate the feasibility and clinical value of combined clonidine and sleep-deprivation induced seizures for ictal brain SPECT imaging in patients with epilepsy. Methods Fiftytwo epilepsy patients were given oral clonidine plus sleep-deprivation to induce seizures with video-electroencephalogram (VEEG) monitoring. Forty-seven patients were selected as control group, whose seizures were induced by sleep-deprivation only. 99Tcm-ethylcysteinate dimer (ECD) was injected within 30 s since a clinical sign and/or a typical EEG discharge of epilepsy was recognized. Brain SPECT was performed 30 min after 99TcmECD injection. X2-test was performed by using software SPSS 10. 0. Results One to two hrs after oral intake of clonidine plus sleep-deprivation, 75% (39/52) patients were induced seizures, including 92.3% (36/39) with subclinical seizures and 7.7% (3/39) with clinical seizures. Ictal brain SPECT localized the lesions with high uptake of 99Tcm-ECD in 37 (94.9%) patients. In control group, 38.3% ( 18/47) were induced epileptic seizures, including 77.8% (14/18) with subclinical seizures and 22.2% (4/18) with clinical seizures. The induction rate of epileptic seizures in clonidine plus sleep-deprivation group was significantly higher than that of control group (X2 = 13.614, P ＜ 0.01 ). However, there was no significant difference in clinical seizures between the two groups (X2 = 1.253, P ＞ 0.05 ). Conclusions The combination of oral intake of clonidine and sleep-deprivation could increase the induction rate of epileptic seizures and it is effective for epilepsy SPECT imaging.

Pigment epithelium-derived factor (PEDF) is an antiangiogenic factor which is effective in tumour inhibition in a variety of tumours and has not yet been studied in bladder tumour before. In this study the expression of PEDF, interleukin-1α (IL-1α) and -8 (IL-8) in bladder tumours was investigated. Immunohistochemistry was performed on 64 bladder tumour and 23 normal uroepithelium samples. Expression change of the factors was compared with clinicopathological parameters. Correlations between PEDF, IL-1α and IL-8 were analyzed. None of the factors was in relation to gender, tumour occurrence, and size or onset pattern. PEDF (P=0.014) and IL-1α (P=0.049) expression was down-regulated with grade progression. PEDF expression was lower in normal uroepithelium than in papillary urothelial neoplasm of low malignant potential (PUNLMP) (P=0.000) and carcinoma (P=0.009) whilst IL-1α (P=0.000 and P=0.000 respectively) and IL-8 (P=0.000 and P=0.023 respectively) expression was higher in the same grouping. PEDF expression had a negative correlation with IL-8 in PUNLMP (P=0.049, r=-0.578) as well as in tumour grouping (P=0.033, r=-0.276). Deranged expressional change of PEDF, IL-1α and IL-8 could be in relation to loss of differentiation from normal uroepithelium to papillary lesion and eventually to carcinoma.

Objective To investigate the influence of angelica sinenisis injection on bone marrow histology and ultrastructure in immune-induced aplastic anemia(AA) mice.Methods Female Balb/c mice were divided into normal group,model group,therapy group and contrast group.All mice were killed by cutting neck on the 12 th day, ulnas and femur were taken out. The bone marrow histology section and ultrastructure of mice ulnas were observed. The quantities of hematopoietic cells were counted. The number of femur bone marrow mononucleate cells (MNC) were measured.Results The quantities of hematopoietic cells in model group were lower than those in normal group (P

SW872 preadipocytes were cultured and induced to differentiate by oleic acid in vitro.The levels of adiponectin and its receptors (AdipoR1 and AdipoR2) mRNA were measured by semiquantitative RT- PCR.The concentration of adiponectin in the culture medium was assayed by ELISA.The results showed that rhIL- 6 could inhibit adiponectin,AdipoR1 mRNA expressions and adiponectin secretion in SW872 adipocytes in a time- and dose-dependent manner,but did not influence adipoR2 mRNA expression.

Objective: To observe the effect of mFOLFOX7 protocolon advanced gastric cancer. Methods: Forty-eight patients with advanced gastric cancer were randomly divided into two groups: conventional treatment group (24 cases, surgery-adjuvant chemotherapy)and synthesized treatment group (24 cases, mFOLFOX7 neoadjuvant chemotherapy-surgery-adjuvant). The effect and toxic reaction of mFOLFOX7 on the patients with advanced gastric cancer were observed, and the R0 resection rate, complications incidence, survival rate were compared between two groups. Results: In synthesized treatment group, total effective rate was 58.3% . Fourteen patients (58.3%)achieved R0resection in synthesized group were compared with 7 patients (29.2%)achieved R0 resection in conventional group (P0.05).Conclusion: mFOLFOX7 neoadjuvant chemotherapy protocol is low toxic reaction. It can improve R0 resection rate of advanced gastric cancer, complications correlated with surgery are not increased. But it can’t improve the survivalrate.

Total RNA was extracted from leaf of Suaeda hetroptera kitag, then the CMO ( choline monooxygenase) cDNA was amplified using the reverse transcriptase polymerase chain reaction ( RT-PCR) method and cloned into pMD-T-simple vector. The positive clones from the Blue/White Screen were sequenced. After confirming its validity, the CMO gene fragment was cloned into pBI121 vector. Double enzyme restriction and PCR analysis indicated that the pBI121/CMO recombinant plasmid was successfully constructed.

Objective To compare the effects of vitrification with slow-freezing on the developmental ability of day 3 cleavage stage embryos.Methods Patients who had no less than 4 high quality embryos were included in this study.These embryos were cryopreserved using the methods of vitrification or slow-freezing.In the eryopreserved embryo transfer cycles,the embryos which were cryopreserved using one of the methods were chosen randomly.The developmental ability of embryos was compared between these two groups.Results A total of 80 patients were included in this study with 160 embryos.In the group of slow-freezing,73(91%)embryos were survived and achieved 15(38%)clinical pregnancies.Among these,3 were twins and the implantation rate was 25%(18/73).In the group of vitrification,71(89%)embryos were survived and achieved 19(48%)clinical pregnancies.Among these, 9 were twins and the implantation rate was 39%(28/71),which was significantly higher than the slow- freezing group(P