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Chronic diabetic wound remains a critical challenge suffering from the complicated negative microenvironments, such as high-glucose, excessive reactive oxygen species (ROS), hypoxia and malnutrition. Unfortunately, few strategies have been developed to ameliorate the multiple microenvironments simultaneously. In this study, Chlorella sp. (Chlorella) hydrogels were prepared against diabetic wounds. In vitro experiments demonstrated that living Chlorella could produce dissolved oxygen by photosynthesis, actively consume glucose and deplete ROS with the inherent antioxidants, during the daytime. At night, Chlorella was inactivated in situ by chlorine dioxide with human-body harmless concentration to utilize its abundant contents. It was verified in vitro that the inactivated-Chlorella could supply nutrition, relieve inflammation and terminate the oxygen-consumption of Chlorella-respiration. The advantages of living Chlorella and its contents were integrated ingeniously. The abovementioned functions were proven to accelerate cell proliferation, migration and angiogenesis in vitro. Then, streptozotocin-induced diabetic mice were employed for further validation. The in vivo outcomes confirmed that Chlorella could ameliorate the undesirable microenvironments, including hypoxia, high-glucose, excessive-ROS and chronic inflammation, thereby synergistically promoting tissue regeneration. Given the results above, Chlorella is considered as a tailor-made therapeutic strategy for diabetic wound healing.
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Objective:To explore the effect of music relaxation training combined with Huangqi Jianzhong Decoction oral administration and foot bath on fatigue status and quality of life in patients with cancer related fatigue.Methods:A total of 90 patients with cancer related fatigue in our hospital from January 2019 to October 2020 were selected. The patients were divided into 2 groups by random number table method, with 45 in each group. Both groups were given health and diet education. The control group was given music relaxation training, and the observation group took Huangqi Jianzhong Decoction oral administration and foot bathing on the basis of the control group. Both groups have a course of treatment of 4 weeks, a total of 3 courses. The TCM syndrome scores were observed before and after treatment, and the Piper Fatigue Score (PFS) was used to evaluate fatigue status, and the Karnofsky functional state score was used to evaluate the quality of life of patients, evaluation of clinical efficacy.Results:After treatment, 43 patients in the observation group and 42 patients in the control group were analyzed. The total effective rate of the observation group was 83.72% (36/43), which was significantly higher than 64.29% (27/42) of the control group ( χ2=4.18, P=0.041). After treatment, the TCM syndrome scores in the observation group was significantly lower than that of the control group ( t=2.48, P=0.015). After treatment, the Karnofsky functional state score in the observation group was significantly higher than that of the control group ( t=2.83, P=0.006). After treatment, the emotion score (4.35±1.02 vs. 5.03±1.01, t=3.09), feeling score (4.31±1.06 vs. 5.00±1.02, t=3.06) and total score (4.23±1.07 vs. 4.87±1.10, t=2.72) in the observation group were significantly lower than those in the control group ( P<0.01). Conclusion:Music relaxation training combined with Huangqi Jianzhong Decoction oral administration and foot bathing can alleviate the fatigue state of CRF patients and improve the quality of life.
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Metabolic regulation has been proven to play a critical role in T cell antitumor immunity. However, cholesterol metabolism as a key component of this regulation remains largely unexplored. Herein, we found that the low-density lipoprotein receptor (LDLR), which has been previously identified as a transporter for cholesterol, plays a pivotal role in regulating CD8
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@#PLZ-NPs (PNS-lipid-zein nanoparticles) prepared by co-assembly of Panax notoginseng saponins, lecithin, β-sitosterol and zein were applied for in vitro cell experiment and oral gavage to study the protective effect of cerebral ischemia-reperfusion rats.PLZ-NPs were characterized by Malvin-particle size analyzer and transmission electron microscope (TEM), respectively. The toxicity of PLZ-NPs and free carrier were evaluated by MTT, and the uptake of nanoparticles in Caco-2 cells was analyzed by laser confocal and flow cytometry. The cerebral ischemia reperfusion rat model was established by MCAO method and then be given samples by gavage for 3 days. The brain tissues were taken to stain by 2, 3, 5-triphenyltetrazole chloride (TTC) and the biochemical indicators of MDA, inflammatory cytokines IL-1β and TNF-α, apoptosis-related proteins Bax and Bcl-2 from the harvested brain tissues were detected to evaluate the protective effect of PNS in PLZ-NPs on cerebral ischemia reperfusion. The particle size, PDI, and zeta potential of formed PLZ-NPs were (116.4 ± 0.81) nm, 0.048 and -(31.5 ± 0.31) mV, respectively. The results of MTT showed that the zein lipoprotein carrier was non-toxic to Caco-2 cells. The results of laser confocal and flow cytometry showed that FITC uptake of nanoparticles could be significantly improved in Caco-2 cells.The uptake from the nanoparticles at 4h was 1.76 times of that of the free FITC group.Compared with the model group, the TTC staining images of free drug PNS group and PLZ-NPs group showed certain reduction in the white infarct area.The contents of MDA, IL-1β, TNF-α and Bax were significantly decreased, while the content of Bcl-2 was significantly increased. Furthermore, all parameters of PLZ-NPs group showed better results than those of PNS group, and there was a significant difference (P < 0.05). All results indicated that the prepared PLZ-NPs had good stability and biological safety, and could significantly increase the uptake in intestinal epithelial cells, and effectively protect against the damage caused by cerebral ischemia reperfusion in rats.
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Antibody repertoire refers to the totality of the superbly diversified antibodies within an individual to cope with the vast array of possible pathogens. Despite this extreme diversity, antibodies of the same clonotype, namely public clones, have been discovered among individuals. Although some public clones could be explained by antibody convergence, public clones in naive repertoire or virus-neutralizing clones from not infected people were also discovered. All these findings indicated that public clones might not occur by random and they might exert essential functions. However, the frequencies and functions of public clones in a population have never been studied. Here, we integrated 2,449 Rep-seq datasets from 767 donors and discovered 5.07 million public clones - ~10% of the repertoire are public in population. We found 38 therapeutic clones out of 3,390 annotated public clones including anti-PD1 clones in healthy people. Moreover, we also revealed clones neutralizing SARS-CoV-2, Ebola, and HIV-1 viruses in healthy individuals. Our result demonstrated that these clones are predisposed in the human antibody repertoire and may exert critical functions during particular immunological stimuli and consequently benefit the donors. We also implemented RAPID - a Rep-seq Analysis Platform with Integrated Databases, which may serve as a useful tool for others in the field.
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Objective To explore the association,consistency and complications prognostic value of thromboelastography and conventional coagulation tests in detecting coagulation function of antiplatelet after endovascular treatments in patients with acute ischemic stroke.Methods A retrospective cohort survey of 240 patients,admitted to our hospital from September 2012 to December 2017,was performed.All acute ischemic stroke patients accepted coagulation function monitoring 5 d after aspirin and clopidogrel and endovascular treatments by thromboelastography (R time,K time,α angle,maximum amplitude [MA]) and routine coagulation tests (prothrombin time [PT],activated partial thromboplastin time [APTT],fibrinogen [FIB],international normalized ratio [INR],blood platelet count).The association,consistency,and sensitivity,specificity,positive predictive value,negative predictive value of complications prognostic value of thromboelastography and conventional coagulation tests were analyzed.Results (1) R time and APTT,K time and APTT,α angle and FIB,and α angle and PLT were positively correlated;K time and FIB,R time and PLT,and α angle and APTT were negatively correlated.(2) R time and APTT (κ=0.266,P=0.000),K time and APTT (κ=0.134,P=0.024),and α angle and FIB (κ=0.162,P=0.007) had agreement in identifying hypercoagulability;R time and APTT (κ=0.211,P=0.001),K time and APTT (κ=0.198,P=0.002),and blood platelet count and K (κ=0.388,P=0.000),and α angle and PLT (κ=0.099,P=0.041) had agreement in identifying hypocoagulability.(3) The sensitivity of thromboelastography and routine coagulation tests in identifying early neurological deterioration was 17.65% and 58.82%,and the sensitivity in identifying symptomatic hemorrhages by thromboelastography and routine coagulation tests was 73.68% and 47.39%.Conclusions Some parameters has correlations in peroperative period,and has agreement in identifying hypercoagulability and hypocoagulability.Accordingly,routine coagulation tests might be superior in evaluating early neurological deterioration,and thromboelastography might be superior in evaluating symptomatic hemorrhages in patients with acute ischemic stroke.
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<p><b>OBJECTIVE</b>To evaluate the efficacy and safety of mechanical thrombectomy with the Solitaire AB device in recanalization of patients with acute ischemic stroke of posterior circulation.</p><p><b>METHODS</b>The clinical data of 17 consecutive patients with acute ischemic stroke of posterior circulation, treated with the Solitaire AB device from August 2011 to August 2015 in Department of Neurosurgery, the Military General Hospital of Beijing People's Liberation Army, were extracted and then retrospectively analyzed. There were 12 male and 5 female patients with a median age of 60 years (ranging from 44 to 75 years). Among them, 8 cases occluded in basilar artery, 4 cases occluded in vertebral artery and 5 cases occluded in vertebral plus basilar artery. Recanalization rate as well as complications after treatment were analysized. Also, neurological functions of the patients before and after treatment, measured by National Institute of Health stroke scale (NIHSS) score, were compared via t test and the clinical outcomes were assessed by modified Rankin score (mRS) at 90 days after treatment.</p><p><b>RESULTS</b>Fifteen patients resulted in successfully recanalization, and 2 cases failed both of whose onset to sheath time were above 7.5 hours. The NIHSS score at 7 days was 11±10, which was significantly decreased compared to the admission NIHSS score 17±5 (t=2.949, P=0.009). No symptomatic intracranial hemorrhage case was found after thrombectomy. At 90 days, one patient died(mRS 6), one patient seriously disabled (mRS 5), two patients moderately seriously disabled (mRS 4), four patients resulted in moderate outcome (mRS 3) and the other 9 patients achieved good outcome (mRS 0 to 2). The dead and seriously disabled cases were both due to failure in recanalization. Two moderately seriously disabled cases were probably attributed to their severe admission condition (NIHSS >20) and prolonged time (onset to sheath time >6 hours).</p><p><b>CONCLUSION</b>Mechanical thrombectomy with the Solitaire AB device contributes to a high rate of recanalization with a low probability of complication and improves functional outcome in patients with acute ischemic stroke of posterior circulation.</p>
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Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estudios Retrospectivos , Stents , Accidente Cerebrovascular , Cirugía General , Trombectomía , Resultado del TratamientoRESUMEN
Objective To observe the influence of carotid endarterectomy in cognitive functions of patients with symptomatic carotid stenosis.Methods Forty-three patients admitted to our hospital and performed carotid endarterectomy from February 2013 to August 2014, were enrolled in the study.Cognitive functions of the patients were evaluated by Montreal cognitive function assessment (MoCA) and cerebral blood flow (CBF) by cerebral perfusion CT scan three days before and three months after operation, respectively.According to the MoCA scores after operation, the patients were divided into significant improvement group and non-significant improvement group, and their cerebral hemodynamics indexes were compared.Results (1) As compared with those before operation (24.1±2.2, 0.97±0.08), the MoCA scores (26.02±2.9) and relative cerebral blood volumes (rCBV, 1.00±0.08) three months after operation were significantly different (P<0.05).(2) The postoperative relative CBF, rCBV and relative mean transmit time in the significant improvement group were significantly improved as compared with those preoperative indexes (P<0.05);whereas, these values in the non-significant improvement group didn't show significant difference between preoperative and postoperative indexes(P>0.05).Conclusion Carotid endarterectomy may help to improve the cognitive function in those patients with symtompatic carotid stenosis, and the effect might be associated with the improvement of cerebral perfusion.
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Lactoferrin (Lf) is one of the food protein belonged to the innate immune system. Apart from its main biological function of binding and transport of iron ions, lactoferrin also has many other functions and properties such as antibacterial, antiviral, antiparasitic, catalytic, anti-cancer, anti-allergic and radioprotecting. Lf is usually used as additives of food and cosmetics. The research of lactoferrin has been increasingly reported, and the application of lactoferrin as a drug carrier has drawn extensive attention over the recent year. In this paper, researches of lactoferrin as drug carriers are classified and summarized in brain targeting, liver tumor targeting, lung tumor targeting and oral delivery systems according to their different characteristics.
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Objective To investigate the role of motility of Oddi's sphincter in pigment gallbladder stone formation in the model of guinea pigs.Methods Thirty-four general adult male Hartley guinea pigs were divided randomly into two groups.Control group (10 guinea pigs)and pigment stone groups (24 guinea pigs,which were divided into 4 subgroups with 6 guinea pigs each according to the time they were sacrificed),fed with pigment lithogenic diet.After 3,6,9 and 12 weeks later,Oddi's sphincter manometry and myoelectric activity record were obtained by multifunctional physiograph at each stage.Results The incidence of pigment gallstone formation was 0,0,16.7% and 66.7% in 3w,6w,9w and 12w group,respectively.The frequency of myoelectric activity decreased apparently in the 3w group(P < 0.05).The amplitude of myoelectric activity had the tendency of decreasing but not statistically significant.The motility frequency of Oddi's sphincter decreased greatly in the 9w group (P < 0.05).The basal pressure of Oddi's sphincter and common bile duct increased markedly in the 12w group [from (25 ± 8) mmHg (1 mmHg =0.133 kPa) to (41 ± 12) mmHg and from (22 ± 8) mmHg to (39 ± 12) mmHg,P < 0.05)].Conclusions Pigment lithogenic diet may induce dysfunction of Oddi's sphincter.The disturbance of Oddi's sphincter motility may play a role in pigment gallstone formation.
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The purpose of this study is to investigate the penetration effects and mechanism of N-arginine chitosan (ACS). This novel transdermal enhancer with a mimetic structure of cell-penetration peptides was synthesized by introducing hydrophilic arginine groups to the amino-group on chitosan's side chain. The structure of ACS was confirmed by FT-IR, 1H NMR and element analysis. In addition, attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) was used to study the protein conformation and the water content of stratum corneum, and the result suggested that ACS can change the orderly arrangement of the molecules in the stratum corneum, making the stack structure of keratin become loose. And ACS can increase the water content of the stratum corneurn. Inverted fluorescence microscope and flow cytometry were used to examine penetration effect of ACS on Hacat cell. The result confirmed that the uptake of ACS was enhanced with increased substitution degree of arginine by 4-8 folds compared to chitosan. In vitro penetration studies on three electrical types of drugs were carried out using three model drugs of negatively charged aspirin, positively charged terazosin and neutral drug isosorbide mononitrate by the method of Franz diffusion cells. The results showed that ACS has obviously penetration of the negatively charged drug aspirin, and certain penetration of neutral drug issorbide mononitrate, but inhibition of positively charged terazosin. In vivo imaging technology research results show that the ACS can significantly enhance the fluorescence intensity of morin, which is the auto-fluorescence anionic drug. These obtained results suggested that ACS, as a promising transdermal enhancer, can change the structure of the keratinocytes and analog penetrating peptides promote absorption, but have certain selectivity for the drug.
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The compound excipient containing sodium stearyl fumarate and plasdone S-630 was prepared by applying spray drying method. The basic physical properties of compound excipient were studied by solubility test, scanning electron microscope, differential scanning calorimeter, X-ray diffraction and Fourier transform infra-red spectroscopy. The effect of compound excipient on moisture absorption and ferulic acid in vitro dissolution of spray drying power of angelica were investigated. The results showed that the chemical constituents of compound excipient did not change before and after spray drying. The water soluble compound excipient can improve significantly moisture absorption and has application prospect.
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To investigate the rat intestinal absorption of stearic acid-octaarginine (SA-R8) modified solid lipid nanoparticles containing paclitaxel (SA-R8-PTX-SLN), compared with the commercially available preparation of PTX (Taxol) and PTX-loaded solid lipid nanoparticles (PTX-SLN), the in situ intestinal absorption of SA-R8-PTX-SLN was investigated by means of single-pass rat intestinal perfusion technique. The absorptions of the preparations were investigated at different intestinal segments, different drug concentrations and in the presence of P-glycoprotein inhibitor (verapamil). The results showed that PTX could be absorbed at each intestinal segment and the three preparations all showed maximum absorptions at the duodenum. The cumulative absorptions of three preparations at each intestinal segment appeared SA-R8-PTX-SLN > PTX-SLN > Taxol (P 0.05). SA-R8 and SLN might both effectively improve the oral absorption of PTX in the intestinal tract.
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Because of the changed metabolic behaviors of cancer cells, tumor cells uptake a corresponding larger amount of glucose in physiological condition when compared with normal cells. And they were prone to metabolize glucose for generating energy in anaerobic glycolysis ways in order to grow quickly. Anaerobic glycolysis consumes more glucose than aerobic way when the same amount of energy is obtained, which also results in large demand of glucose in tumor cells. This review briefly describes therapy methods related to characteristic mentioned above, and summarizes the research progress of drugs, diagnostic reagents and carriers conjugated with glucose, glucose derivatives or other kinds of sugars for cancer targeting. Furthermore, typically relative research reports from 2012 till now were listed and analyzed.
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With the development of the modernization drive of traditional Chinese medicine (TCM) preparations, new-type TCM dosage forms research have become a hot spot in the field. Because of complexity of TCM components as well as uncertainty of material base, there is still not a scientific system for modern TCM dosage forms so far. Modern TCM preparations inevitably take the nature of the multi-component and the general function characteristics of multi-link and multi-target into account. The author suggests building a multiple drug release system for TCM using diverse preparation techniques and drug release methods at levels on the basis the nature and function characteristics of TCM components. This essay expounds elaborates the ideas to build the multiple traditional Chinese medicine release system, theoretical basis, preparation techniques and assessment system, current problems and solutions, in order to build a multiple TCM release system with a view of enhancing the bioavailability of TCM components and provide a new form for TCM preparations.
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Animales , Humanos , Disponibilidad Biológica , Química Farmacéutica , Métodos , Formas de Dosificación , Sistemas de Liberación de Medicamentos , Métodos , Medicamentos Herbarios Chinos , Química , Farmacocinética , Medicina Tradicional ChinaRESUMEN
<p><b>OBJECTIVE</b>To determine the major factors affecting the conversion efficiency of naringin-HP-beta-CD that was enzymed to prepare naringenin were determined and select the process condition with high conversion efficiency, stable and suitable for industrial production.</p><p><b>METHOD</b>The dropping method was used to prepare naringin-HP-beta-CD, which was hydrolyzed by snailase to obtain naringenin. With the bioconversion rate as the index, the effects of pH value, temperature, reaction time, dosage of enzyme and concentration of naringin-HP-beta-CD on conversion rate of naringenin were detected for the purpose of optimizing the preparation condition. the conversion efficiency of naringin-HP-beta-CD was verified by scanning calorimetry, and the Hydrolysis product was identified by H-NMR, and 13C-NMR.</p><p><b>RESULT</b>The optimum enzymolysis of naringin-HP-beta-CD with snailase was 98.4% under the conditions of 37 degrees C, a pH 5.0 acetic acid- sodium acetate buffer solution for 12 hours. The substrate concentration was 30 g x L(-1) and the weight ratio of enzyme and substrate was 3: 5. Under the optimum enzymolysis condition, the conversion rate of naringin-HP-beta-CD was higher than naringin that was not entrapped with HP-beta-CD, with 272.25 reaction product relative molecules. The structure of naringenin was confirmed by the analysis of 1H-NMR and 13C-NMR.</p><p><b>CONCLUSION</b>Naringin which is entrapped with HP-beta-CD to prepare naringenin can significantly improve the conversion efficiency by shortening the reaction time, increasing the concentration of the substrate and reducing the amount of enzyme. Therefore, the process is stable and it was suitable for industrialization.</p>
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2-Hidroxipropil-beta-Ciclodextrina , Flavanonas , Química , Hidrólisis , Solubilidad , beta-Ciclodextrinas , QuímicaRESUMEN
ObjectiveTo induce human peripheral blood mononuclear cells differentiate into hepatocyte-like cells by hepatocyte growth factor (HGF) and fibroblast growth factor-4 (FGF-4) in vitro and determine whether PKH26 could be used to serve as an effective tracer for the cells,and observe the ability of transplanted hepatocyte-like cells differentiate into hepatic cells in nude mice.MethodsGroup A and B were set up respectively.In Group A,mononuclear cells were cultivated without hepatocyte growth factor (HGF) and fibroblast growth factor-4 (FGF-4) in cell culture.They were used as negative control group.In Group B,mononuclear cells were cultured with the administration of both HGF and FGF-4 to induce the differentiation into liver hepatocyte-like cells.The changes in cell morphology were observed and the expressions of AFP and CK 19 were detected by immunocytochemical staining in two groups at different times after induction.The hepatocyte-like cells differentiated from human peripheral blood mononuclear cells labeled by the fluorescent dye PKH26 injected into caudal vein in nude mice is experimental group.The nude mice injected with equal amount of normal saline in control group.The migration of the labeled cells into the liver are observed by the fluorescence microscope in the hepatic tissue sections of nude mice and the expressions of ALB were detected by immunocytochemical staining two weeks after the cells transplantation.ResultsCells in group B have a strong proliferative activity.It becomes large and oval,grows in colonies following induction.Cells in group A that showed spherical shape when peripheral blood mononuclear cells were just isolated are gradually becoming inconformity in morphology,spindle or fibroid,and a few cells are round:cells developed apoptosis and cracked following incubation.The expressions of AFP and CK19 were positive after induction in group B as detected by immunocytochemicat staining.Inversely,the expressions of AFP and CK19 were negative in group A after incubation.The experimental group showed numerous PKH26 labeled cells in the hepatic tissue sections of nude mice.But the control group did not show PKH26 labeled cells.The expressions of ALB were positive in the experimental group as detected by immunocytochemical staining after two weeks of the cells transplantation.ConclusionHuman peripheral blood mononuclear cells have the potential to differentiate into hepatocyte-like cells under the induction of HGF and FGF-4.Additionally,PKH26 is an effective tracer in hepatocyte-like cell transplantation.The hepatocyte-like cells settled in hepatic tissue begin to differentiate into mature hepatocyte after two weeks of the cells transplantation.It plays hepatic cells function and expresses alhnmin.
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<p><b>OBJECTIVE</b>To prepare the solid dispersion of tanshinone II A (TS II A) by the combined application of nano-silica and poloxamer 188 (F68), in order to observe its dissolution and stability.</p><p><b>METHOD</b>Tanshinone II A solid dispersion was prepared by the solvent method with nano-silica and poloxamer 188 as binary vectors. Its physical characteristics, in vitro dissolution and stability were further assessed.</p><p><b>RESULT</b>The tanshinone II solid dispersion was prepared with the weight ratio of nano-silica and poloxamer 188 of 1: 3. The differential scanning calorimetry (DSC) demonstrated that Tanshinone II A existed in vectors as amorphous state. The in vitro dissolution of tanshinone II A solid dispersion is up to 90% at 60 min. Accelerating experiment showed that content and in vitro dissolution of tanshinone II A solid dispersion did not change after storage over 3 months.</p><p><b>CONCLUSION</b>Solid dispersion of binary vector of tanshinone II A can obviously improve the dissolution and stability of tanshinone II in practice.</p>
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Rastreo Diferencial de Calorimetría , Abietanos , Química , Estabilidad de Medicamentos , Medicamentos Herbarios Chinos , Química , SolubilidadRESUMEN
<p><b>OBJECTIVE</b>To prepare ursolic acid ethosomes and investigate the penetration characteristics of ursolic ethosomes as a transdermal vehicle.</p><p><b>METHOD</b>Ursolic acid ethosomes were prepared by injection method, and the shape and particle size of the ethosomes were analyzed. Ursolic acid permeation tests in vitro through the skin of rats were performed in TP-3 diffusion cell. The accumulated permeation amounts of ursolic acid 10% isopropanol solution, ursolic acid liposomes, ursolic acid ethosomes were compared.</p><p><b>RESULT</b>The average encapsulation percentage, particle size, and Zeta potential of the ethosomes were (95.83 +/- 0.86)%, (87.5 +/- 7.5) nm and - (38.4 +/- 3.6) mV, respectively. The accumulated permeation amount of the ethosomes in 12 h was 146.49 microg x cm(-2), and its transdermal permeability in 12 h was 12.17 microg x cm(-2) x h(-1).</p><p><b>CONCLUSION</b>The encapsulation percentage of the ethosomes is good, and the stability of the ursolic acid ethosomes is fine. Ethosomes can significantly enhance the diffusion rate of ursolic acid through the skin of rats.</p>
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Animales , Ratas , Administración Cutánea , Cromatografía Líquida de Alta Presión , Métodos , Portadores de Fármacos , Química , Farmacocinética , Etanol , Química , Farmacocinética , Liposomas , Química , Farmacocinética , Tamaño de la Partícula , Permeabilidad , Piel , Metabolismo , Absorción Cutánea , Solubilidad , Triterpenos , Química , FarmacocinéticaRESUMEN
<p><b>OBJECTIVE</b>To optimize the conditions for enzymolysis of Icariin by snail hydrolase.</p><p><b>METHOD</b>Take conversion rate as index, the effects of pH, temperature, reaction time, dosage of enzyme, concentration of Icariin and metal ion on hydrolysis were studied by single-factor designs and a L9 (3(4)) orthogonal design. The product was characterized through MS, 1H-NMR and 13C-NMR methods.</p><p><b>RESULT</b>The optimum enzymolysis conversion rate was achieved at 37 degrees C, pH 6.0 acetic acid-sodium acetate buffer solution and 48 h. The Ca2+, Mg2+ and Zn2+ had activation on helicase slightly but the Fe2+ inhibited enzymolysis significantly. The production was presumed as icaritin on the basis of spectral evidences.</p><p><b>CONCLUSION</b>Snail hydrolase can be used for preparing of icaritin. The condition is mildness and suitable for industrialization.</p>