3.Advanced in solubilization methods of water-insoluble natural drugs.
Hui ZHONG ; Yuan ZHU ; Jiang-nan YU ; Xi-ming XU
China Journal of Chinese Materia Medica 2014;39(17):3226-3231
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
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Biological Availability
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Biological Products
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administration & dosage
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chemistry
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pharmacokinetics
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Chemistry, Pharmaceutical
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methods
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trends
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Solubility
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Technology, Pharmaceutical
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methods
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trends
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Water
5.Significance of the neutrophil-lymphocyte ratio in elderly type 2 diabetic patients with coronary heart disease
Xi HE ; Hongwen TAN ; Ruiping YU ; Jianhua LUO ; Shujing XU
Chinese Journal of Geriatrics 2016;35(3):252-255
Objective To evaluate the value of the neutrophil-lymphocyte ratio (NLR) in elderly type 2 diabetic patients (T2DM) with coronary heart disease (CHD).Methods We performed a retrospective observational study on 228 patients undergoing coronary angiography in Guizhou Provincial People's Hospital from April 2014 to July 2015.Patients were divided into three groups:the simple T2DM group (n=77),simple CHD group (n=72),and T2DM complicated with CHD group (n=79).Meanwhile,70 healthy elderly subjects served as the control group.The white blood cell count,high-sensitivity C-reactive protein (hs-CRP) and other clinical and laboratory parameters were collected,and NLR was calculated.Risk factors for CHD in T2DM patients were determined by logistic regression analysis.Multiple stepwise regression analysis was adopted to identify factors influencing NLR.Results The white blood cell count,neutrophil count,NLR and hs-CRP level in the simple T2DM,CHD,and T2DM+CHD groups were higher than in the control group [(7.48 1.81) 109/L,(7.72± 1.89) 109/L,(7.98±2.12) 109/L vs.(6.22± 1.61) 109/L;(4.49±1.38) 109/L,(4.88±1.56) 109/L,(5.35±1.40) 109/L vs.(3.52±0.84) 109/L;(2.84± 0.77),(3.07±0.79),(3.34±0.83) vs.(1.58±0.42);(2.92±0.65) mg/L,(3.20±0.86) mg/ L,(4.98±1.10) mg/L vs.(1.105±0.23) mg/L;respectively,P<0.05 or P<0.01].The lymphocyte count in the simple T2DM,CHD,and T2DM+CHD groups were lower than in the control group [(1.57±0.41) × 109/L,(1.58±0.40) × 109/L,(1.61±0.48) × 109/L vs.(2.22± 0.51) × 109/L,P<0.05].NLR and hs-CRP levels in the T2DM+CHD group were higher than in the former two groups (all P<0.05).Pearson correlation analysis showed that NLR was positively correlated with the Gensini score and hs-CRP level (r=0.7455 and 0.7792,both P<0.01).Logistic regression analysis showed that NLR,hs-CRP levels and glycosylated hemoglobin A1c (HbA1c) were the risk factors for CHD in T2DM patients (OR=4.331,3.997 and 2.928,all P<0.05).Multiple stepwise regression analysis showed that NLR was positively correlated with fasting plasma glucose,HbA1 c levels and systolic blood pressure (β' =0.3133,0.4720 and 0.3069,all P<0.05).Conclusions NLR may be a valuable predictive factor for CHD in elderly T2DM patients.
7.Different doses ofearly enteral nutrition for patients with ac ute gastrointestinal dysfunction
Yanxi KONG ; Xingwei XU ; Fengchan XI ; Wenkui YU
Journal of Medical Postgraduates 2015;(4):373-376
Objective Acute gastrointestinal dysfunction (AGD) is a common problem in critically ill patients, for whomearly enteral nutrition ( EN) is widely used, but its application dosage remains controversial.This study aimed to observe the influence of dif-ferent doses of early EN on acute gastrointestinal tolerance, new infections and other complications, inflammation indexes, and prognosis in AGD patients. Methods We selected 120 critically ill patients that met thecriteria of class-ⅡAGD and needed EN support andequal-ly randomized them intoa standard-dose and a low-dose ENgroup.The former group received EN at 20 mL/h, with an addition of 10 mL/h every 12 hours according to the tolerance and supplemented byparenteral nutrition (PN) to achieve the target calories(60%) on the 3 rd day, while the latterat 20 mL/h for 7 days, supplemented by PN to achieve the target calories on the 3 rd day and from the 7 th day gradu-ally increased to the full volume.We recorded the patients′ICUdays, hospitaldays, mortality rate, organ function support days, incidence of feeding intolerance within 7 days, incidence of new infections within 7 and 28 days, and levels of C-reactive protein (CRP), procalci-tonin (PCT), tumor necrosis factor-α(TNF-α) and interleukin-6 (IL-6) and compared these indexes between the two groups. Resulst There were no statistically significant differences between the low -and standardd-ose EN groups in the patients′ICU days, hospital days, mortality rate,organ function support days, or incidence of new infections within 7 and 28 days ( P>0.05) .The incidence of feeding intol-erance on the 7 th day was significantly lower in the low-dose than in the standard-dose EN group ( 13.3 vs 36.7%, P<0.05).On the 1st, 3rd, and 7 th day, the level of CRP was (5.90±0.72), (16.52± 3.09) , and ( 32.11 ±4.33 ) ng/L, respectively, in the low-dose groupversus(5.83±0.59), (15.83±1.19), and (33.16±4.51)ng/L in the standard-dose group, while that of PCTwas (4.71±1.25), (10.63± 2.21), and ( 16.89±3.39) ng/mL, respectively, in the former versus (4.55±0.67), (10.41±1.99), and (17.49±3.87)ng/mL in the latter, both increased in a time-dependent manner and with significant differ-ences among the three time points within the same group ( P<0.05) .The levels of TNF-αand IL-6 were elevated in the same manner and also with significant differences among the three time points within the same group ( P<0 .05) . Conc lusion Lowdose of early enteral nutrition can improve the feeding tolerance of AGDpatients, but does not influence the incidence of new infections and prognosis.
8.The cytotoxicity of IL-24 gene-modified CIK cells to HL-60 cells
Wei XIA ; Xin YU ; Punan WANG ; Hongwei XU ; Yu CHEN ; Huaxin XI ; Jicheng YANG ; Jingcheng MIAO
Chinese Journal of Immunology 2009;25(12):1080-1084
Objective:To study the antitumor effect and mechanism of cocultured CIK cells modified with IL-24 gene and autologous DCs on HL-60 cells in vitro.Methods:DCs and CIK cells were prepared routinely from human peripheral blood mononuclear cells ( PBMC).IL-24 gene was transferred into CIK cells via electroporation.The cells obtained were named CIK-IL24.RT-PCR and ELISA were used to evaluate expression of IL-24 gene in transfected CIK cells.The phenotypic changes of CIK cells were identified by flowcytometry analysis.The concentration of IFN-γ and TNF-α in supernatant of CIK was determined by ELISA.FCM was used to determine the cytotoxicity of cocultured CIK cells modified with IL-24 gene and autologous DCs against HL-60 cells.Results:Eukaryotic expressing plasmid pcDNA3.0-IL24 was transferred into CIK cells successfully via electroporation.The expressing rate of CD3~+、CD3~+CD56~+ cells had no significant change in CIK cells.However,the rate of CD4~+CD25~+ cells was significantly decreased compared with that of the control group.Expression of adhesion molecules CD54,CXCR4 were significantly increased on CD3+CD56+ cells.CIK-IL24 cells produced markedly higher levels of IFN-γ and TNF-α as compared with the CIK cells.By comparison with non-transfected CIK cells co-cultured with DCs,transfected CIK cells co-cultured with DCs had a significantly higher lytic activity against HL-60 cells.Conclusion:IL-24 gene modification can enhance the anti-tumoral immunity of CIK cells,the mechanism of which might be related to the increased secretion of IFN-γ,TNF-α,up-regulation of adhesion molecule expression,and reduction of the rate of CD4~+CD25~+ cells in CIK cells.
9.Enhancing effect of IL-24 gene modified dendritic cells co-cultured with CIK cells on cytotoxicity against A549 cells
Xin YU ; Wei XIA ; Punan WANG ; Hongwei XU ; Yu CHEN ; Huaxin XI ; Jicheng YANG ; Jingcheng MIAO
Chinese Journal of Microbiology and Immunology 2009;29(9):841-846
Objective To study the antitumor effect and mechanism of co-cultured cytokine-induced killer(CIK) cells and autologous DC modified with IL-24 gene on A549 cells in vitro. Methods DC and CIK cells were prepared routinely from human peripheral blood mononuclear cells(PBMC). Recombinant adenovirus vector pAdEasy-1-pTrack-CMV-IL-24 was extracted from DH5α, it was lineared with Pac I and transfected into A293 cells, and then the IL-24 recombined adenovirus(Ad-IL-24) was obtained. Ad-IL-24 was used to infect DC. The cells obtained were named DC-IL-24. RT-PCR and ELISA were used to evaluate the expression of IL-24 gene in transfected DC. The phenotypes change of DC were identified by flow cytometry analysis, the concen-tration of IL-12 and TNF-α in supernatant of DC were determined by EIJSA. The ability of CIK producing per-forin was measured by homolysis method. FCM was used to determine the cytotoxicity of cocultured CIK cells and autologous DC modified with IL-24 gene to A549 cells. Results We obtained the high titre of Ad-IL-24.IL-24 gene was transfered into DC successfully via Ad-IL-24. The green fluorescence was observed on DC by fluorescence microscope. The expression rate of CD80, CD83, HI.A-DR, CD40, CXCR4 on DC-IL-24 was sig-nificantly increased compared with that of the control group. DC-IL-24 produced markedly higher levels of IL-12 and TNF-α as compared with DC. DC-IL-24 can enhance the ability of CIK cells producing perforin. On com-parison with non-transfected DC co-cultured with CIK cells, transfected DC co-cultured with CIK cells had a sig-nificantly higher lytic activity against A549 cells. Conclusion IL-24 gene modification can enhance the anti-tu-moral immunity of DC. The mechanism of which might be related to the increased secretion of IL-12 and TNF-α, up-regulation expression of co-stimulatory molecules and MHC Ⅱ class molecules on DC, promoting the acti-vation and maturation of DC, and then enhancing CIK cells to generate specific anti-tumoral immunity.
10.Efficacy observation of chiropractic plus foot bath with Chinese medicine for transient synovitis of the hip in children
Zhi-Xing LI ; Bao-Hua PAN ; Rui-Xi ZHANG ; Yu-Yu XU ; Xiao-Zhuan CHEN
Journal of Acupuncture and Tuina Science 2021;19(1):37-42
Objective: To compare the efficacy of different treatment protocols in treating transient synovitis of the hip (TSH) in children and to optimize the clinical treatment strategy for this condition. Methods: Ninety kids with TSH were divided into a control group, a chiropractic group and a chiropractic plus foot bath group using the random number table method, with 30 cases in each group. The control group was treated with conventional traction; the chiropractic group was given chiropractic treatment based on the control group; the chiropractic plus foot bath group was given Chinese medicine foot bath based on the chiropractic group. Traction and foot bath were conducted once daily while chiropractic was done once every other day, all with 14 d as a treatment course for a total of two courses. Changes in the visual analog scale (VAS) score and range of motion (ROM) of the hip joint in the three groups were observed, and the efficacy was compared. Results: The total effective rate was 93.3% in the chiropractic plus foot bath group, versus 76.7% in the chiropractic group and 66.7% in the control group, and the total effective rate was notably higher in the chiropractic plus foot bath group than in the other two groups (both P<0.05). Respectively after the first and second treatment course, the VAS score decreased significantly in each of the three groups compared with that before treatment (all P<0.01), and the ROM of the hip joint in flexion increased significantly (all P<0.01). After two treatment courses, the VAS score was lower in the chiropractic plus foot bath group than in the other two groups (both P<0.05), and its ROM of the hip joint in flexion was larger than that in the other two groups (both P<0.05). Conclusion: Based on traction, chiropractic plus Chinese medicine foot bath can effectively reduce pain and improve motor function of the hip joint in treating TSH.