Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 1.130
Filter
1.
Braz. dent. j ; 32(4): 45-54, July-Aug. 2021. tab, graf
Article in English | LILACS, BBO | ID: biblio-1345520

ABSTRACT

Abstract The ability of mouth rinses, available in the international market, to form reaction products on demineralized enamel (bioavailability test) was evaluated in vitro. Nine mouth rinses purchased in Chile were evaluated; eight formulated with NaF (one containing 100 µg F/mL and seven containing 226) and one with Na2FPO3 (226 µg F/mL as ion F). Demineralized enamel slabs (n=15 per mouth rinse) were sectioned; one half was subjected to the assigned mouth rinse treatment for 10 min and the other half was used to obtain baseline data. Loosely bound and firmly bound fluoride formed on enamel were determined with an ion-specific electrode and the values were expressed in µg F/cm2. The concentration of fluoride and the pH of the mouth rinses were previously determined. Concentrations of loosely bound and firmly bound fluoride formed on enamel were independently analyzed by ANOVA and Tukey's test (α=5%). The loosely bound and firmly bound fluoride concentrations (µg F/cm2) formed ranged from 3.2 to 36.2 and 0.4 to 1.7, respectively. Loosely bound fluoride formed on enamel was significantly more effective in discriminating the effect of different commercial mouth rinses than firmly bound fluoride. Mouth rinses with 226 ppm F as NaF and low pH presented significantly greater bioavailability of fluoride on enamel than those with higher pH or lower NaF concentration. The mouth rinse with Na2FPO3 showed low reactivity. Although further studies are necessary, the findings showed that commercial fluoride-containing mouth rinses have important variations in enamel fluoride bioavailability, which may result in differences on anticaries efficacy.


Resumo Os enxaguatórios bucais comerciais fluoretados diferem na concentração e tipo de sal de fluoreto, no pH e têm alguns ingredientes que podem interferir na reatividade do fluoreto com o esmalte desmineralizado. A capacidade de enxaguatórios bucais comerciais de formar produtos de reação em esmalte desmineralizado (teste de biodisponibilidade) foi avaliada in vitro. Nove enxaguatórios bucais adquiridos no Chile foram avaliados, oito formulados com NaF (um contendo 100 µg F/mL e sete contendo 226) e um com Na2FPO3 (226 µg F/mL como íon F). Os blocos de esmalte desmineralizados (n=15 por grupo) foram seccionados, uma metade foi submetida ao tratamento com o enxaguatório designado por 10 min e a outra metade foi usada para dados baseline. Fluoreto fracamente e firmemente ligados formados no esmalte foram determinados com um eletrodo íon-específico e os valores foram expressos em µg F /cm2. A concentração de fluoreto e o pH dos enxaguatórios foi previamente determinada. As concentrações de fluoreto tipo fluoreto fracamente ligado e fortemente ligado formadas no esmalte foram analisadas independentemente por ANOVA e teste de Tukey (α=5%). As concentrações de fluoreto fracamente ligado e fortemente ligado formados variaram de 3,2 a 36,2 e 0,4 a 1,7, respectivamente. O fluoreto fracamente ligado formado no esmalte foi significativamente mais eficaz para discriminar o efeito dos diferentes enxaguatórios bucais comerciais do que o fluoreto firmemente ligado. Enxaguatórios bucais com 226 ppm F na forma de NaF e baixo pH apresentaram significativamente maior biodisponibilidade de fluoreto no esmalte do que aqueles com maior pH ou menor concentração de NaF. O enxaguatório com Na2FPO3 apresentou reatividade muito baixa. Embora mais estudos sejam necessários, os resultados mostraram que os enxaguatórios bucais comerciais contendo fluoreto apresentam variações importantes na biodisponibilidade do fluoreto, o que poderia resultar em diferenças na eficácia anticárie.


Subject(s)
Fluorides , Mouthwashes , Sodium Fluoride , Biological Availability , Dental Enamel
2.
Braz. dent. j ; 32(2): 90-99, Mar.-Apr. 2021. tab, graf
Article in English | LILACS, BBO | ID: biblio-1339331

ABSTRACT

Abstract The ability of mouthrinses, available in the international market, to form reaction products on demineralized enamel (bioavailability test) was evaluated in vitro. Nine mouthrinses purchased in Chile were evaluated; eight formulated with NaF (one containing 100 µg F/mL and seven containing 226) and one with Na2FPO3 (226 µg F/mL as ion FPO3 ). Demineralized enamel slabs (n=15 per mouthrinse) were sectioned; one half was subjected to the assigned mouthrinse treatment for 10 min and the other half was used to obtain baseline data. Loosely bound and firmly bound fluoride formed on enamel were determined with an ion-specific electrode and the values were expressed in µg F/cm2. The concentration of fluoride and the pH of the mouthrinses were previously determined. Concentrations of loosely bound and firmly bound fluoride formed on enamel were independently analyzed by ANOVA and Tukey's test (α=5%). The loosely bound and firmly bound fluoride concentrations formed ranged from 3.2 to 36.2 and 0.4 to 1.7, respectively. Loosely bound fluoride formed on enamel was significantly more effective in discriminating the effect of different commercial mouthrinses than firmly bound fluoride. Mouthrinses with 226 ppm F as NaF and low pH presented significantly greater bioavailability of fluoride on enamel than those with higher pH or lower NaF concentration. The mouthrinse with Na2FPO3 showed low reactivity. Although further studies are necessary, the findings showed that commercial fluoride-containing mouthrinses have important variations in enamel fluoride bioavailability, which may result in differences on anticaries efficacy.


Resumo Os enxaguatórios bucais comerciais fluoretados diferem na concentração e tipo de sal de fluoreto, no pH e têm alguns ingredientes que podem interferir na reatividade do fluoreto com o esmalte desmineralizado. A capacidade de enxaguatórios bucais comerciais de formar produtos de reação em esmalte desmineralizado (teste de biodisponibilidade) foi avaliada in vitro. Nove enxaguatórios bucais adquiridos no Chile foram avaliados, oito formulados com NaF (um contendo 100 µg F/mL e sete contendo 226) e um com Na2FPO3 (226 µg F/mL como íon F). Os blocos de esmalte desmineralizados (n=15 por grupo) foram seccionados, uma metade foi submetida ao tratamento com o enxaguatório designado por 10 min e a outra metade foi usada para dados baseline. Fluoreto fracamente e firmemente ligados formados no esmalte foram determinados com um eletrodo íonespecífico e os valores foram expressos em µg F /cm2. A concentração de fluoreto e o pH dos enxaguatórios foi previamente determinada. As concentrações de fluoreto tipo fluoreto fracamente ligado e fortemente ligado formadas no esmalte foram analisadas independentemente por ANOVA e teste de Tukey (α=5%). As concentrações de fluoreto fracamente ligado e fortemente ligado formados variaram de 3,2 a 36,2 e 0,4 a 1,7, respectivamente. O fluoreto fracamente ligado formado no esmalte foi significativamente mais eficaz para discriminar o efeito dos diferentes enxaguatórios bucais comerciais do que o fluoreto firmemente ligado. Enxaguatórios bucais com 226 ppm F na forma de NaF e baixo pH apresentaram significativamente maior biodisponibilidade de fluoreto no esmalte do que aqueles com maior pH ou menor concentração de NaF. O enxaguatório com Na2FPO3 apresentou reatividade muito baixa. Embora mais estudos sejam necessários, os resultados mostraram que os enxaguatórios bucais comerciais contendo fluoreto apresentam variações importantes na biodisponibilidade do fluoreto, o que poderia resultar em diferenças na eficácia anticárie


Subject(s)
Dental Enamel , Fluorides , Biological Availability
3.
Article in Chinese | WPRIM | ID: wpr-879012

ABSTRACT

To evaluate the effects of Hydroxypropyl methylcellulose acetate succinate(HPMCAS MF) on absorption of silybin(SLB) from supersaturable self-nanoemulsifying drug delivery system which was pre-prepared at the early stage experiment. The cell toxicity of self-emulsifying preparation was evaluated by the MTT method, and the in vitro membrane permeability and absorption promoting effect of the self-emulsifying preparation were evaluated by establishing a Caco-2 cell monolayer model. The in vivo and in vitro supersaturation correlation was evaluated via the blood concentration of SLB. The results of MTT showed that the concentration of the preparation below 2 mg·mL~(-1)(C_(SLB) 100 μg·mL~(-1)) was not toxic to Caco-2 cells, and the addition of polymer had no significant effect on Caco-2 cells viability. As compared with the solution group, the transport results showed that the P_(app)(AP→BL) of the self-emulsifying preparation had a very significant increase; the transport rate of silybin can be reduced by polymer in 0-30 min; however, there was no difference in supersaturated transport between supersaturated SLB self-nanoemulsion drug delivery system(SLB-SSNEDDS) and SLB self-nanoemulsion drug delivery system(SLB-SNEDDS) within 2 hours. As compared with SLB suspension, pharmacokinetic parameters showed that the blood concentration of both SLB-SNEDDS and SLB-SSNEDDS groups were significantly increased, and C_(max) was 5.25 times and 9.69 times respectively of that in SLB suspension group, with a relative bioavailability of 578.45% and 1 139.44% respectively. C_(max) and relative bioavailability of SLB-SSNEDDS were 1.85 times and 197% of those of SLB-SNEDDS, respectively. Therefore, on the one hand, SSNEDDS can increase the solubility of SLB in gastrointestinal tract by maintaining stability of SLB supersaturation state; on the other hand, the osmotic transport process of SLB was regulated through the composition of its preparations, and both of them could jointly promote the transport and absorption of SLB to improve the oral bioavailability of SLB.


Subject(s)
Administration, Oral , Biological Availability , Caco-2 Cells , Drug Delivery Systems , Emulsions , Humans , Methylcellulose/analogs & derivatives , Nanoparticles , Particle Size , Silymarin , Solubility
4.
Braz. j. med. biol. res ; 54(8): e11073, 2021. tab, graf
Article in English | LILACS | ID: biblio-1249327

ABSTRACT

The study evaluated the effect of the supernatant of placental explants from preeclamptic (PE) and normotensive (NT) pregnant women after tissue treatment with or without vitamin D (VD) on oxidative stress and nitric oxide (NO) bioavailability in human umbilical vein endothelial cells (HUVEC). Placental explants were prepared from eight NT and eight PE women, and supernatants were obtained after incubation with or without hydrogen peroxide (H2O2) and/or VD. HUVEC were cultured for 24 h with supernatants, and the following parameters were analyzed in HUVEC cultures: NO, nitrate (NO3-), and nitrite (NO2-) levels, lipid peroxidation, and intracellular reactive oxygen species (ROS). Results showed that the production of NO3-, NO2-, malondialdehyde (MDA), and ROS were significantly higher in HUVEC treated with explant supernatant from PE compared to NT pregnant women, while the supernatant of PE explants treated with VD led to a decrease in these parameters. A significantly high production of NO was detected in HUVEC cultured with control supernatant of NT group, and in cultures treated with supernatant of PE explants treated with VD. Taken together, these results demonstrated that cultures of placental explants from PE women with VD treatment generated a supernatant that decreased oxidative stress and increased the bioavailability of NO in endothelial cells.


Subject(s)
Humans , Female , Pregnancy , Pre-Eclampsia/metabolism , Nitric Oxide/metabolism , Placenta/metabolism , Vitamin D/metabolism , Biological Availability , Cells, Cultured , Oxidative Stress , Human Umbilical Vein Endothelial Cells , Hydrogen Peroxide
5.
Braz. dent. j ; 31(3): 257-263, May-June 2020. tab, graf
Article in English | LILACS, BBO | ID: biblio-1132306

ABSTRACT

Abstract The aim of this in vitro study was to determine the fluoride concentration in silver diamine fluoride (SDF) products and their bioavailability with demineralized dentine. The products evaluated (expected fluoride concentrations) were: I: Saforide 38% (45,283 ppm F); II: Advantage Arrest 38.3 to 43.2% (45,283 to 51,013 ppm F); III: Ancárie 12% (14,100 ppm F); IV: Ancárie 30% (35,400 ppm F), V: Cariestop 12% (14,100 ppm F) and VI: Cariestop 30% (35,400 ppm F). The fluoride concentration was evaluated using an ion-specific electrode (ISE) by direct technique, which was confirmed after microdiffusion. The pH of the products was determined with a pH test strip. For the bioavailability test, demineralized dentine slabs were treated with one of the products for 1 min. Loosely (CaF2-like) and firmly-bound fluoride (FAp) were determined. The fluoride concentration found in the products (mean±SD; ppm F) by the ISE direct technique was: I:53,491±554; II:57,249±1,851; III:4,814±268; IV:5,726±43; V:10,145±468; VI:11,858±575; these values were confirmed after microdiffusion (t-test; p>0.05) and disagree with the declared by the manufacturers. The pH of Ancárie 12 and 30% was 6.0 and 4.5, respectively, in disagreement with the alkaline pH expected for SDF solution and found in the other products evaluated. There was no correlation between either CaF2-like (r=0.221; p=0.337) or FAp (r=-0.144; p=0.830) formed in demineralized dentine and fluoride concentration found in the products. The problems of pH and fluoride concentration found in available professional commercial SDF products suggest that they are not under sanitary surveillance.


Resumo O objetivo deste estudo in vitro foi determinar a concentração de fluoreto nos produtos de diamino fluoreto de prata (DFP) e sua biodisponibilidade com dentina desmineralizada. Os produtos avaliados (concentrações esperadas de flúor) foram: I: Saforide 38% (45.283 ppm F); II: Advantage Arrest 38,3 a 43,2% (45.283 a 51.013 ppm F); III: Ancárie 12% (14.100 ppm F); IV: Ancárie 30% (35.400 ppm F), V: Cariestop 12% (14.100 ppm F) e VI: Cariestop 30% (35.400 ppm F). A concentração de fluoreto foi avaliada utilizando um eletrodo íon-específico (EIE) por técnica direta, que foi confirmada após microdifusão. O pH dos produtos foi determinado com uma tira de teste de pH. Para o teste de biodisponibilidade, blocos de dentina desmineralizada foram tratados com um dos produtos por 1 min. Fluoreto fracamente (tipo CaF2) e firmemente ligado (FAp) foram determinados. A concentração de fluoreto encontrada nos produtos (média±DP; ppm F) pela técnica direta com EIE foi: I: 53.491±554; II: 57.249±1.851; III: 4.814±268; IV: 5.726±43; V: 10.145±468; VI: 11.858±575; esses valores foram confirmados após microdifusão (teste t; p>0,05) e discordam dos declarados pelos fabricantes. O pH do Ancárie 12 e 30% foi de 6,0 e 4,5, respectivamente, em desacordo com o pH alcalino esperado para a solução de DFP e encontrado nos demais produtos avaliados. Não houve correlação entre CaF2 (r=0,221; p=0,337) ou FAp (r=-0,144; p=0,830) formados na dentina desmineralizada e concentração de fluoreto encontrada nos produtos. Os problemas de pH e concentração de fluoreto encontrados nos produtos comerciais profissionais disponíveis de DFP sugerem que eles não estão sob vigilância sanitária.


Subject(s)
Cariostatic Agents , Fluorides , Sodium Fluoride , Biological Availability , Fluorides, Topical , Silver Compounds , Dentin , Quaternary Ammonium Compounds , Hydrogen-Ion Concentration
6.
Rev. cuba. invest. bioméd ; 39(1): e260, ene.-mar. 2020. graf
Article in Spanish | LILACS, CUMED | ID: biblio-1126582

ABSTRACT

Introducción: los ácidos biliares no solo tienen como actividad biológica regular la absorción de vitaminas liposolubles, colesterol y lípidos, sino actúan también como moléculas de señalización, moduladores de la proliferación celular intestinal, de la expresión de genes y del metabolismo energético según estudios in vitro e in vivo; en condiciones fisiológicas mantienen su homeostasis, que al ser interrumpida promueve suacción toxicológica. Objetivo: describir la actualidad de los nuevos conocimientos sobre la actividad biológica y toxicológica de los ácidos biliares en el aparato digestivo, dirigido a cirujanos generales, gastroenterólogos, clínicos y fisiólogos que les permitan contextualizar el proceso inflamación-carcinogénesis relacionado con los efectos toxicológicos de los ácidos biliares. Método: se realizó una revisión sistemática de la actividad biológica y toxicológica de los ácidos biliares para los cirujanos generales, gastroenterólogos, clínicos y fisiólogos, como herramienta útil en la compresión fisiopatológico del metabolismo de los ácidos biliares. Conclusión: los ácidos biliares desempeñan una función clave como moléculas de señalización en la modulación de la proliferación de células epiteliales, la expresión de genes y el metabolismo energético, que cuando se interrumpe su homeostasis se promueve la acción tóxica de estos, lo que se traduce en el proceso inflamación-carcinogénesis digestiva(AU)


Introduction: bile acids not only have as a regular biological activity the absorption of fat-soluble vitamins, cholesterol and lipids, but also act as signaling molecules, modulators of intestinal cell proliferation, gene expression and energy metabolism according to in vitro studies and in vivo; under physiological conditions they maintain their homeostasis, which when interrupted promotes their toxicological action. Objective: to describe the news of the new knowledge about the biological and toxicological activity of bile acids in the digestive system, aimed at general surgeons, gastroenterologists, clinicians and physiologists that allow them to contextualize the inflammation-carcinogenesis process related to the toxicological effects of bile acids. Method: A systematic review of the biological and toxicological activity of bile acids was performed for general surgeons, gastroenterologists, clinicians and physiologists, as a useful tool in the pathophysiological compression of bile acid metabolism. Conclusion: bile acids play a key role as signaling molecules in the modulation of epithelial cell proliferation, gene expression and energy metabolism, which when their homeostasis is interrupted, their toxic action is promoted, which translates in the inflammation-digestive carcinogenesis process(AU)


Subject(s)
Humans , Bile Acids and Salts/analysis , Bile Acids and Salts/toxicity , Biological Availability , Digestive System/metabolism
7.
Article in Chinese | WPRIM | ID: wpr-828411

ABSTRACT

Quercetin is a kind of typical flavonoid, mainly found in various vegetables, fruits and Chinese herbs that are consumed daily, with the functions of anti-oxidation, anti-tumor, prevention and treatment of cardiovascular and cerebrovascular diseases. Quercetin is a natural compound with defined anti-tumor activity. Due to its low bioavailability and poor water solubility, quercetin has limitations in clinical application. The quercetin derivatives with good solubility, high bioavailability, metabolic stability, and low toxicity have been obtained through modification of quercetin structure. In recent years, a large number of quercetin ethers, esters, complexes, C-4 carbonyloxy substituted derivatives, A,B-ring modified compounds and other derivatives have been synthesized and tested for in vitro anticancer activity. The quercetin derivatives with anti-tumor activity synthesized in the last 5 years were reviewed in this paper.


Subject(s)
Biological Availability , Humans , Neoplasms , Oxidation-Reduction , Quercetin , Solubility
8.
Article in Chinese | WPRIM | ID: wpr-828399

ABSTRACT

In order to improve the supersaturation and maintenance time of drug dispersion in curcumin self-nanoemulsion(CUR-SNEDDS), precipitation inhibitors(PPIs) were introduced to prepare curcumin supersaturated self-emulsion(CUR-SSNEDDS). The composition of CUR-SNEDDS prescriptions was selected through the solubility test, the compatibility of oil phase and surfactant, the investigation of the emulsifying ability of the surfactant and the drawing of the pseudo-ternary phase diagram. Analytic hierarchy process was used in combination with central composite design-response surface method to optimize the prescription. The type and dosage of precipitation inhibitors(PPIs) were selected to maintain the supersaturated concentration and duration of CUR in artificial gastrointestinal fluids. At the same time, polarizing microscope was used to evaluate the crystallization inhibition effect and the quality and in vitro release behavior of CUR-SSNEDDS. The prepared CUR-SSNEDDS prescription was capryol 90-kolliphor RH40-transcutol HP-Soluplus(7.93∶66.71∶25.36∶5), with the drug loading of(65.12±1.25) mg·g~(-1). CUR-SSNEDDS was transparent yellow, and the nanoemulsion droplets were spherical with uniform distribution. The emulsification time was(21.02±0.13) s, the average particle size was(57.03±0.35) nm, the polydispersity index(PDI) was(0.23 ± 0.01), and the Zeta potential was(-18.10±1.30) mV. CUR-SSNEDDS significantly inhibited the generation and growth of crystals after in vitro dilution. The supersaturation could be maintained above 10 within 2 h, and the dissolution rate and degree of CUR in artificial gastrointestinal fluid were significantly increased. Soluplus could effectively maintain the supersaturated state of CUR and enhance CUR dissolution in vitro.


Subject(s)
Biological Availability , Curcumin , Emulsions , Nanoparticles , Particle Size , Solubility , Surface-Active Agents
9.
Article in Chinese | WPRIM | ID: wpr-878861

ABSTRACT

To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.


Subject(s)
Anisoles , Biological Availability , Diterpenes, Kaurane , Drug Delivery Systems , Emulsions , Particle Size , Solubility , Surface-Active Agents
10.
Article in Chinese | WPRIM | ID: wpr-878840

ABSTRACT

Trace metals deficiency or excess are associated with the etiology and pathogenesis of rheumatoid arthritis(RA). Aconiti Radix Cocta(A) and Paeoniae Radix Alba(B) are commonly used together for the treatment of RA. In this study, we aim to determine anti-arthritic-related metal bioavailability in the compatibility of herb A and B for avoiding metal deficiency or excess, and optimize the combination ratio of herb A and B, accordingly. Anti-arthritic-related metal bioaccessibility were evaluated by in vitro simulator of all gastrointestinal tract(including mouth, stomach, small and large intestines), and the roles of gastrointestinal digestive enzymes and intestinal microflora were investigated. Anti-arthritic-related metal bioavailability was assessed by the affinity adsorption with liposomes. The results indicated that compatibility proportion of corresponding herbal plants, gastrointestinal digestion and microbial metabolic, which could affect metal digestion and absorption. The optimal compatibility proportion of 1 A∶1 B is recommended, according to the dose of anti-arthritic-related metal bioavailability, which is often chosen for clinical practice of RA therapy. Thus, anti-arthritic-related metal bioavailability might be the key active substances for RA treatment.


Subject(s)
Aconitum , Biological Availability , Drugs, Chinese Herbal , Paeonia
12.
Article in English | WPRIM | ID: wpr-881040

ABSTRACT

As a representative drug for the treatment of severe community-acquired pneumonia and sepsis, Xuebijing (XBJ) injection is also one of the recommended drugs for the prevention and treatment of coronavirus disease 2019 (COVID-19), but its treatment mechanism for COVID-19 is still unclear. Therefore, this study aims to explore the potential mechanism of XBJ injection in the treatment of COVID-19 employing network pharmacology and molecular docking methods. The corresponding target genes of 45 main active ingredients in XBJ injection and COVID-19 were obtained by using multiple database retrieval and literature mining. 102 overlapping targets of them were screened as the core targets for analysis. Then built the PPI network, TCM-compound-target-disease, and disease-target-pathway networks with the help of Cytoscape 3.6.1 software. After that, utilized DAVID to perform gene ontology (GO) function enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis to predict the action mechanism of overlapping targets. Finally, by applying molecular docking technology, all compounds were docked with COVID-19 3 CL protease(3CLpro), spike protein (S protein), and angiotensin-converting enzyme II (ACE2). The results indicated that quercetin, luteolin, apigenin and other compounds in XBJ injection could affect TNF, MAPK1, IL6 and other overlapping targets. Meanwhile, anhydrosafflor yellow B (AHSYB), salvianolic acid B (SAB), and rutin could combine with COVID-19 crucial proteins, and then played the role of anti-inflammatory, antiviral and immune response to treat COVID-19. This study revealed the multiple active components, multiple targets, and multiple pathways of XBJ injection in the treatment of COVID-19, which provided a new perspective for the study of the mechanism of traditional Chinese medicine (TCM) in the treatment of COVID-19.


Subject(s)
Angiotensin-Converting Enzyme 2/metabolism , Biological Availability , COVID-19/virology , Coronavirus 3C Proteases/metabolism , Drugs, Chinese Herbal/therapeutic use , Humans , Medicine, Chinese Traditional/methods , Molecular Docking Simulation/methods , Protein Interaction Mapping/methods , SARS-CoV-2/physiology , Signal Transduction/drug effects , Spike Glycoprotein, Coronavirus/metabolism
13.
Article in English | WPRIM | ID: wpr-881037

ABSTRACT

In the present study, liquiritigenin-phospholipid complex (LPC) was developed and evaluated to increase the oral bioavailability of liquiritigenin. A single-factor test methodology was applied to optimize the formulation and process for preparing LPC. The effects of solvent, drug concentration, reaction time, temperature and drug-to-phospholipid ratio on encapsulation efficiency were investigated. LPCs were characterized by UV-visible spectroscopy, differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and powder X-ray diffractometry (PXRD). The apparent solubility and n-octanol/water partition coefficient were tested. The pharmacokinetic characteristics and bioavailability of the LPC were investigated after oral administration in rats in comparison with liquiritigenin alone. An LPC was successfully prepared. The optimum level of various parameters for liquiritigenin-phospholipid complex was obtained at the drug concentration of 8 mg·mL


Subject(s)
Administration, Oral , Animals , Biological Availability , Flavanones/pharmacokinetics , Phospholipids/pharmacokinetics , Rats , Solvents
14.
Biosci. j. (Online) ; 35(3): 818-825, may./jun. 2019. ilus, tab, graf
Article in English | LILACS | ID: biblio-1048687

ABSTRACT

The mangrove forest is an important transitional ecosystem consisted of terrestrial and marine environment located in tropical and subtropical regions with average temperatures above 20 °C. In Alagoas, the mangrove forests are found on the entire coastline from Maragogi to Piaçabuçu. In the last 20 years, due to the pollution of water resources, studies of coastal aquatic ecosystems have been developed. The objective of this study was to analyze the physicochemical properties and determine the levels of heavy metals in mangrove sediments of the Mundaú-Manguaba estuary lagoon complex (MMELC) and Meirim River in Alagoas. Zinc, copper, lead, cadmium and chromium were chosen due to their relationship with sewer, agricultural, and industrial wastes. 22 soil samples were collected in the MMELC and in the Meirim River. The samples were submitted to soil routine analyses of Embrapa. The heavy metals were extracted by the Mehlich-1 method and analyzed by atomic absorption spectrometry. The mean concentrations of these metals in thesediment samples followed the order Mn > Zn >Pb > Cr> Cu >Cd in MMELC and Zn > Mn >Pb > Cr> Cu >Cd in Meirim River. All proposed heavy metals were found in sediments, however, the cadmium levels were above the normal levels proposed by Environment National Council (CONAMA) and Canadian Council of Ministers of the Environment. The study shows that the analysis of sediment can contribute to environmental monitoring actions and development of public policies aimed to controlling the sustainable use of natural resources of the studied areas.


O manguezal é um importante ecossistema de transição entre o ambiente marinho e terrestre, localizado em regiões tropicais e subtropicais com temperaturas médias acima de 20°C. Em Alagoas podemos encontrar florestas de mangue em praticamente todo o litoral desde Maragogi até Piaçabuçu. Nosúltimos 20 anos, a poluição dos recursos hídricos tem levado ao estudo dos ecossistemas aquáticos costeiros, que são importantes para preservação e equilíbrio da vida. O objetivo deste trabalho foi analisar as propriedades físico-químicas e determinar os teores ambientalmente disponíveis de metais nos sedimentos do mangue existente na foz CELMM (e do rio Meirim em Alagoas. Foram escolhidos os metais zinco, cobre, chumbo, cádmio e crômio por estarem ligados aos despejos de esgotos, projetos agropecuários, e fontes industriais. Foram coletadas 22 amostras de solo nos estuários do CELMM e do rio Meirim. As amostras foram submetidas as análises de rotina para solos da Embrapa. As concentrações médias desses metais nas amostras de sedimento seguiram a ordem Mn > Zn >Pb > Cr> Cu >Cd in CELMM e Zn > Mn >Pb > Cr> Cu >Cd no Rio Meirim. Os metais foram extraídos pelo método Mehlich-1 e analisados por meio de espectrometria de absorção atômica. Foram encontrados nos sedimentos todos os metais propostos na pesquisa com destaque para os teores de cádmio detectados em valores absolutos acima de valores considerados normais pelo Conselho Nacional doMeio Ambiente e pelo Canadian Council of Ministers of the Environment em alguns pontos do estuário do rio Meirim. O estudo mostra que a análise dos sedimentos pode, portanto, contribuir para ações de monitoramento ambiental, subsidiando a implantação e desenvolvimento de políticas públicas que visem controlar o usoracional e sustentável dos recursos naturais das áreas do estudas.


Subject(s)
Metals, Heavy , Environmental Pollution , Wetlands , Biological Availability
15.
S. Afr. fam. pract. (2004, Online) ; 61(1): 30­38-2019. ilus
Article in English | AIM | ID: biblio-1270082

ABSTRACT

Background: This study analysed the views of a stratified sample of 444 older adult women from selected health districts in Botswana on their family planning (FP) use, knowledge, accessibility and availability.Methods: Four health districts (two rural and two urban) were purposively selected. The sample of 444 older adults was proportionally allocated to the districts. The snowball technique was used in identifying older adults from each district. Results: Contraceptive prevalence among the older adults is low (25. 2%); ever used rate was 23.6%, with unmet need as high as 75.2%. The traditional methods are mainly used. Knowledge, availability and accessibility of the natural methods are high. The likelihood ratio test shows that age, educational status, marital status and employment jointly significantly predicts (p < 0.05) the use of FP.Conclusion: Family planning programme developers and policy-makers should develop educational interventions that will be age specific and relevant to older adults


Subject(s)
Biological Availability , Botswana , Family Planning Services , Frail Elderly
16.
Article in Chinese | WPRIM | ID: wpr-773251

ABSTRACT

Curcumin( Cur) is a natural active substance extracted from the roots or tubers of traditional Chinese medicinal materials. It has anti-inflammatory and anti-tumor activities on brain diseases. Due to the poor stability,low solubility,poor absorption and low bioavailability of curcumin,N-acetyl-L-cysteine( NAC) was used as an absorption enhancer and mixed with curcumin to improve the absorption of curcumin in the body. In this paper,curcumin was smashed by airflow pulverization,and Cur-NAC mixtures were prepared by being grinded with liquid. Then,the raw material and the product were analyzed by differential scanning calorimetry( DSC),X-ray diffraction( XRD) for structural characterization. The dissolution was determined by high performance liquid chromatography( HPLC) analysis. The characteristic peaks of the samples prepared by grinding method were similar to those of the raw materials,while the melting temperature and the accumulated dissolution degree were not significantly changed. The crystal forms of the products were not changed,and no new crystal form was formed after grinding. After the administration of intranasal powder,blood samples were collected from the orbit,while the whole brain tissues were removed from the skull and dissected into 10 anatomical regions. The concentrations of curcumin in these samples were determined by UPLC-MS/MS. The concentrations of curcumin in plasma and brain were compared at different time points. After intranasal administration of two drugs,it was found that the concentration of curcumin after sniffing up the mixtures in plasma was high,and the concentration of the drug in the olfactory bulb,hippocampus,and pons was increased significantly. Within 0. 083-0. 5 h,the olfactory bulb,piriform lobe and hippocampus remained high concentrations,the endodermis,striatum,hypothalamus and midbrain reached high concentrations within 1-3 h; and the cerebellum,pons and brain extension maintained relatively high concentrations within 3-7 h. The experiment showed that nasal administration of Cur-NAC mixtures can significantly improve the bioavailability of curcumin,and lead to significant differences in brain tissue distribution.


Subject(s)
Acetylcysteine , Pharmacology , Administration, Intranasal , Animals , Biological Availability , Brain , Brain Chemistry , Chromatography, Liquid , Curcumin , Pharmacokinetics , Rats , Tandem Mass Spectrometry , Tissue Distribution
17.
Article in English | WPRIM | ID: wpr-763392

ABSTRACT

During the clinical trial development of directly acting antivirals (DAAs), evidence regarding the treatment efficacy in chronic hepatitis C patients with hepatocellular carcinoma (HCC) was scarce because these patients have always been excluded. Apart from the clinical trials, more HCC patients are currently being treated in daily practice, given that these treatments are highly effective and involve well-tolerated regimens. Large scale, real-world studies have demonstrated potentially suboptimal antiviral treatment efficacy in HCC patients who received DAAs. It is postulated that the impairment of the bioavailability of DAAs may account for the inferior treatment response. However, the results could not be generalized across all studies. The differing results were attributed to diverse patient characteristics, suboptimal regimens or imprecise definitions of active cancer statuses at the time of treatment initiation. Additional large-scale studies that utilize the treatment of choice in clearly defined HCC patients with different disease severities are warranted to clarify the issue.


Subject(s)
Antiviral Agents , Biological Availability , Carcinoma, Hepatocellular , Hepatitis C, Chronic , Humans , Treatment Outcome
18.
Article in English | WPRIM | ID: wpr-758893

ABSTRACT

It is crucial to optimize the dose of fluoroquinolones to avoid antibiotic resistance and to attain clinical success. We undertook this study to optimize the dose of enrofloxacin against Salmonella enterica subsp. enterica serovar Enteritidis (S. Enteritidis) in chicken by assessing its pharmacokinetic/pharmacodynamic (PK/PD) indices. The antibacterial activities of enrofloxacin against S. Enteritidis were evaluated. After administering 10 mg/kg body weight (b.w.) of enrofloxacin to broiler chickens of both sexes by intravenous (IV) and peroral (PO) routes, blood samples were drawn at different intervals and enrofloxacin concentrations in plasma were determined. PK/PD indices were calculated by integrating the PK and PD data. The elimination half-lives (T(1/2)), time required to reach peak concentration (T(max)), peak concentration (C(max)), and area under curve (AUC) after administering enrofloxacin by PO and IV routes were 25.84 ± 1.40 h, 0.65 ± 0.12 h, 3.82 ± 0.59 µg/mL, and 20.84 ± 5.0 µg·h/mL, and 12.84 ± 1.4 h, 0.22 ± 0.1 h, 6.74 ± 0.03 µg/mL, and 21.13 ± 0.9 µg.h/mL, respectively. The bioavailability of enrofloxacin was 98.6% ± 8.9% after PO administration. The MICs of enrofloxacin were 0.0625–1 µg/mL against S. Enteritidis strains, and the MIC₅₀ was 0.50 µg/mL. The C(max)/MIC₅₀ were 7.64 ± 0.2 and 13.48 ± 0.7 and the 24 h AUC/MIC₅₀ were 41.68 ± 0.1 and 42.26 ± 0.3 after administering the drug through PO and IV routes, respectively. The data in this study indicate that the application of 50 mg/kg b.w. of enrofloxacin to chicken through PO and IV routes with a dosing interval of 24 h can effectively cure S. Enteritidis infection, indicating the need for a 5-fold increase in the recommended dosage of enrofloxacin in chicken.


Subject(s)
Area Under Curve , Biological Availability , Body Weight , Chickens , Drug Resistance, Microbial , Fluoroquinolones , Pharmacokinetics , Plasma , Salmonella enterica , Salmonella enteritidis , Salmonella , Serogroup
19.
Article in Chinese | WPRIM | ID: wpr-772094

ABSTRACT

OBJECTIVE@#To identify the main active components in Ⅲ and their targets and explore the mechanism by which Ⅲ alleviates proteinuria in chronic kidney disease (CKD) based on network pharmacology.@*METHODS@#The active components of Ⅲ and their potential targets, along with the oral bioavailability and drug-like properties of each component were searched in the TCMSP database. The proteinuria-related targets were searched in the GeneCards database. The active component-target network was constructed using Cytoscape software, and the acquired information of the targets from ClueGO was used for enrichment analysis of the gene pathways.@*RESULTS@#A total of 102 active components were identified from Ⅲ. These active components acted on 126 targets, among which 69 were related to proteinuria. Enrichment analysis revealed fluid shear stress- and atherosclerosisrelated pathways as the highly significant pathways in proteinuria associated with CKD.@*CONCLUSIONS@#We preliminarily validated the prescription of Ⅲ and obtained scientific evidence that supported its use for treatment of proteinuria in CKD. The findings in this study provide a theoretical basis for further study of the mechanism of Ⅲ in the treatment of proteinuria in CKD.


Subject(s)
Biological Availability , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Therapeutic Uses , Humans , Proteinuria , Drug Therapy , Metabolism , Renal Insufficiency, Chronic , Metabolism
20.
Article in Chinese | WPRIM | ID: wpr-773998

ABSTRACT

Objective To explore the pharmacokinetics of nimodipine in plasma of rats after intraocular administration.Methods Totally 135 SD rats were randomly divided into three groups according to drug administration routes:intraocular(io group),intravenous (iv group),and intragastric (ig group). The doses were 5.0 mg/kg for IO and IV groups and 10.0 mg/kg for IG group. The serum nimodipine level was analyzed by high performance liquid chromatography. The main pharmacokinetic parameters were calculated and compared.Results The pharmacokinetic parameters in io group were as follows:C:0.52 mg/ml;t:5.0 min;and AUC:21.10 mg/(ml·min). The main pharmacokinetic parameters in iv group were as follows:C:3.62 mg/ml;and AUC:52.58 mg/(ml·min). The main pharmacokinetic parameters in ig group were as follows:C:0.20 mg/ml;t:5.0 min;and AUC:5.98 mg/(ml·min).Conclusions Nimodipine is rapidly absorbed after io administration,and the ophthalmic formulation has a higher bioavailability than the oral solution. Therefore,the io route may help to improve the treatment effectiveness of cardiovascular diseases.


Subject(s)
Administration, Intravenous , Administration, Oral , Animals , Area Under Curve , Biological Availability , Chromatography, High Pressure Liquid , Nimodipine , Pharmacokinetics , Rats , Rats, Sprague-Dawley
SELECTION OF CITATIONS
SEARCH DETAIL