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1.
Medicine (Baltimore) ; 98(39): e17239, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31574836

RESUMO

BACKGROUND: This study aims to evaluate the efficacy and safety of montelukast for the treatment of patients with pediatric allergic purpura (PAP). METHODS: We will retrieve the following electronic databases from inception to the present: MEDILINE, Embase, CENTRAL, CINAHL, AMED, Chinese Biomedical Literature Database, China National Knowledge Infrastructure Database, Wanfang, and VIP database without language limitation. Two authors will carry out study selection, data extraction, and quality evaluation independently. RevMan V5.3 software will be used for statistical software. RESULTS: This study will summarize high-quality evidence-based medicine to evaluate the efficacy and safety of montelukast for the treatment of PAP. CONCLUSION: This study will provide strong evidence to determine whether montelukast is an effective and safety treatment for PAP. SYSTEMATIC REVIEW REGISTRATION: PROSPERO CRD42019145472.


Assuntos
Acetatos/uso terapêutico , Púrpura de Schoenlein-Henoch/tratamento farmacológico , Quinolinas/uso terapêutico , Criança , Feminino , Humanos , Masculino , Projetos de Pesquisa , Revisão Sistemática como Assunto , Resultado do Tratamento
2.
Eur J Med Chem ; 182: 111645, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31494472

RESUMO

As our research focus on anticancer drugs, two series of novel derivatives of Flexicaulin A (FA), an ent-kaurene diterpene, condensation with amino acid trifluoroacetate were synthesized, and their anti-proliferative activity against four human cancer cell lines (TE-1, MCF-7, A549 and MGC-803) were evaluated. Compared with FA, the anticancer activity and solubility of most derivatives were significantly improved. Among them, compound 6d had the best activity, and its IC50 value against Esophageal cancer cells (TE-1) was up to 0.75 µM. Subsequent cellular mechanism studies showed that compound 6d could inhibit the proliferation of cancer cells, the formation of cell colonies, and increase the level of ROS on TE-1 cells. In addition, 6d could up-regulate the expressions of SAPK/JNK pathway-associated proteins (p-ASK1, p-MKK4 and p-JNK) and pro-apoptotic proteins (Bak, Bad and Noxa), remarkably increase the ratio of Bax to Bcl-2 and activate Cleaved Caspase-3/9/PARP. These results indicate that compound 6d induces apoptosis through the ROS/JNK/Bcl-2 pathway and holds promising potential as an anti-proliferative agent.

3.
Biomed Res Int ; 2019: 1238581, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31275960

RESUMO

Beta-1,3-glucanosyltransferase (Gas1p) plays important roles in cell wall biosynthesis and morphogenesis and has been implicated in DNA damage responses and cell cycle regulation in fungi. Yeast Gas1p has also been reported to participate in endoplasmic reticulum (ER) stress responses. However, the precise roles and molecular mechanisms through which Gas1p affects these responses have yet to be elucidated. In this study, we constructed GAS1-deficient (gas1Δ) and GAS1-overexpressing (GAS1 OE) yeast strains and observed that the gas1Δ strain exhibited a decreased proliferation ability and a shorter replicative lifespan (RLS), as well as enhanced activity of the unfolded protein response (UPR) in the absence of stress. However, under the high-tunicamycin-concentration (an ER stress-inducing agent; 1.0 µg/mL) stress, the gas1Δ yeast cells exhibited an increased proliferation ability compared with the wild-type yeast strain. In addition, our findings demonstrated that IRE1 and HAC1 (two upstream modulators of the UPR) are required for the survival of gas1Δ yeast cells under the tunicamycin stress. On the other hand, we provided evidence that the GAS1 overexpression caused an obvious sensitivity to the low-tunicamycin-concentration (0.25 µg/mL). Collectively, our results indicate that Gas1p plays an important role in the ageing and ER stress responses in yeast.

4.
Chin Med J (Engl) ; 132(14): 1689-1699, 2019 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-31268909

RESUMO

BACKGROUND: Depression affects approximately 5% of elderly people and its etiology might be related to chronic stress exposure during neurodevelopmental periods. In this study, we examined the effects of adolescent chronic social stress in aged mice on depressive behaviors and the excitatory-inhibitory (E/I) balance in stress-sensitive regions of the brain. METHODS: Sixty-four adolescent, male C57BL/6 mice were randomly assigned to either the 7-week (from post-natal days 29 to 77) social instability stress (stress group, n = 32) or normal housing conditions (control group, n = 32). At 15 months of age, 16 mice were randomly selected from each group for a series of behavioral tests, including two depression-related tasks (the sucrose preference test and the tail suspension test). Three days following the last behavioral test, eight mice were randomly selected from each group for immunohistochemical analyses to measure the cell density of parvalbumin (PV)- and calretinin (CR)-positive gamma-aminobutyric-acid (GABA)ergic inhibitory inter-neurons, and the expression levels of vesicular transporters of glutamate-1 (VGluT1) and vesicular GABA transporter (VGAT) in three stress-sensitive regions of the brain (the medial pre-frontal cortex [mPFC], hippocampus, and amygdala). RESULTS: Behaviorally, compared with the control group, adolescent chronic stress increased depression-like behaviors as shown in decreased sucrose preference (54.96 ±â€Š1.97% vs. 43.11 ±â€Š2.85%, t(22) = 3.417, P = 0.003) and reduced latency to immobility in the tail suspension test (92.77 ±â€Š25.08 s vs. 33.14 ±â€Š5.95 s, t(25) = 2.394, P = 0.025), but did not affect anxiety-like behaviors and pre-pulse inhibition. At the neurobiologic level, adolescent stress down-regulated PV, not CR, inter-neuron density in the mPFC (F(1, 39) = 19.30, P < 0.001), and hippocampus (F(1, 42) = 5.823, P = 0.020) and altered the CR, not PV, inter-neuron density in the amygdala (F(1, 28) = 23.16, P < 0.001). The VGluT1/VGAT ratio was decreased in all three regions (all F > 10.09, all P < 0.004), which suggests stress-induced hypoexcitability in these regions. CONCLUSIONS: Chronic stress during adolescence increased depression-like behaviors in aged mice, which may be associated with the E/I imbalance in stress-sensitive brain regions.

5.
Hippocampus ; 29(11): 1063-1074, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31066147

RESUMO

The early postnatal stage is a critical period of hippocampal neurodevelopment and also a period of high vulnerability to adverse life experiences. Recent evidence suggests that nectin-3, a cell adhesion molecule, mediates memory dysfunction and dendritic alterations in the adult hippocampus induced by postnatal stress. But it is unknown whether postnatal nectin-3 reduction alone is sufficient to alter hippocampal structure and function in adulthood. Here, we down regulated hippocampal expression of nectin-3 and its heterophilic adhesion partner nectin-1, respectively, from early postnatal stage by injecting adeno-associated virus (AAV) into the cerebral lateral ventricles of neonatal mice (postnatal day 2). We found that suppression of nectin-3, but not nectin-1, expression from the early postnatal stage impaired hippocampus-dependent novel object recognition and spatial object recognition in adult mice. Moreover, AAV-mediated nectin-3 knockdown significantly reduced dendritic complexity and spine density of pyramidal neurons throughout the hippocampus, whereas nectin-1 knockdown only induced the loss of stubby spines in CA3. Our data provide direct evidence that nectins, especially nectin-3, are necessary for postnatal hippocampal development of memory functions and structural integrity.

6.
Chin Med J (Engl) ; 132(13): 1582-1590, 2019 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-31045908

RESUMO

BACKGROUND: Exposure to adverse experiences in early life may profoundly reshape the neurodevelopmental trajectories of the brain and lead to long-lasting behavioral and neural alterations. One deleterious effect of early-life stress that manifests in later life is sleep disturbance, but this has not been examined in aged mice and the underlying neural mechanisms remain unknown. Considering the important role of the nucleus accumbens (NAc) in the sleep-wake regulation, this study aimed to assess the effects of early-life stress on the sleep behaviors in aged mice and the potential involvement of the NAc in stress-induced sleep abnormalities. METHODS: Twenty aged male C57BL/6 mice (>16 months, n = 10 per group) were used in this study. During post-natal days 2 to 9, dams were provided with either sufficient (control) or a limited nesting and bedding materials (stressed). When the mice were 16 to 17 months old, their sleep-wake behaviors were recorded over 24 h using electroencephalogram and electromyelogram. The amount of each sleep-wake stage, mean duration, and stage transition was analyzed. Then, five animals were randomly chosen from each group and were used to measure the expression levels of vesicular glutamate transporter-1 (VGluT1) and vesicular transporters of γ-aminobutyric acid (VGAT) in the NAc using immunohistochemistry. Group comparisons were carried out using Student t test or analysis of variances when appropriate. RESULTS: Compared with the control mice, the early-life stressed aged mice spent less time awake over 24 h (697.97 ±â€Š77.47 min vs. 631.33 ±â€Š34.73 min, t17 = 2.376, P = 0.030), accordingly, non-rapid eye movement sleep time was increased (667.37 ±â€Š62.07 min vs. 723.54 ±â€Š39.21 min, t17 = 2.326, P = 0.033) and mean duration of rapid eye movement sleep was prolonged (73.00 ±â€Š8.98 min vs. 89.39 ±â€Š12.69 min, t17 = 3.277, P = 0.004). Meanwhile, we observed decreased VGluT1/VGAT ratios in the NAc in the stressed group (F(1, 16) = 81.04, P < 0.001). CONCLUSION: Early adverse experiences disrupt sleep behaviors in aged mice, which might be associated with the excitatory-inhibitory imbalance in the NAc.

7.
Cell Rep ; 21(4): 891-900, 2017 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-29069596

RESUMO

Calbindin modulates intracellular Ca2+ dynamics and synaptic plasticity. Reduction of hippocampal calbindin levels has been implicated in early-life stress-related cognitive disorders, but it remains unclear how calbindin in distinct populations of hippocampal neurons contributes to stress-induced memory loss. Here we report that early-life stress suppressed calbindin levels in CA1 and dentate gyrus (DG) neurons, and calbindin knockdown in adult CA1 or DG excitatory neurons mimicked early-life stress-induced memory loss. In contrast, calbindin knockdown in CA1 interneurons preserved long-term memory even after an acute stress challenge. These results indicate that the dysregulation of calbindin in hippocampal excitatory, but not inhibitory, neurons conveys susceptibility to stress-induced memory deficits. Moreover, calbindin levels were downregulated by early-life stress through the corticotropin-releasing hormone receptor 1-nectin3 pathway, which in turn reduced inositol monophosphatase levels. Our findings highlight calbindin as a molecular target of early-life stress and an essential substrate for memory.


Assuntos
Região CA1 Hipocampal/metabolismo , Calbindinas/metabolismo , Interneurônios/metabolismo , Transtornos da Memória/metabolismo , Estresse Psicológico/metabolismo , Animais , Região CA1 Hipocampal/citologia , Região CA1 Hipocampal/fisiologia , Calbindinas/genética , Giro Denteado/citologia , Giro Denteado/metabolismo , Giro Denteado/fisiologia , Interneurônios/fisiologia , Masculino , Transtornos da Memória/etiologia , Memória de Longo Prazo , Camundongos , Camundongos Endogâmicos C57BL , Nectinas/metabolismo , Receptores de Hormônio Liberador da Corticotropina/metabolismo , Memória Espacial , Estresse Psicológico/complicações
8.
J Cardiovasc Pharmacol ; 68(5): 383-390, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27557342

RESUMO

The nuclear receptors (NR)-farnesoid X receptor (FXR, NR1H4) and pregnane X receptor (PXR, NR1I2)-have important effects on the expression of genes related to the pharmacokinetics (PKs) of rosuvastatin. This study was designed to investigate whether the genetic variants in drug disposition genes (SLCO1B1 and ABCG2) combined with their upstream regulators (NR1H4 and NR1I2) would affect the PKs of rosuvastatin in a Chinese population. Sixty-one healthy male volunteers were enrolled and the plasma concentrations of rosuvastatin were measured using the liquid chromatographic-tandem mass spectrometry/MS method. All subjects were analyzed and grouped according to the genotypes of NR1H4, NR1I2, SLCO1B1, and ABCG2. The exposure of rosuvastatin was higher in subjects carrying the SLCO1B1 521C or ABCG2 421A allele compared with noncarriers. No association was observed of single-nucleotide polymorphisms in NR1H4 or NR1I2 genes with the PKs of rosuvastatin. After adjusting for the 421C>A and 521T>C variants, the Cmax in subjects with NR1I2 63396TT wild type were about 2-fold of those of NR1I2 mutant type (63396CC and CT) (10.7 vs. 20.4 ng/mL, P = 0.023), whereas no significant differences were observed for other parameters. Polymorphisms investigated in the genes of NR1H4 and NR1I2 seemed to play no significant role in the disposition of rosuvastatin.


Assuntos
Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/genética , Grupo com Ancestrais do Continente Asiático/genética , Transportador 1 de Ânion Orgânico Específico do Fígado/genética , Proteínas de Neoplasias/genética , Receptores Citoplasmáticos e Nucleares/genética , Receptores de Esteroides/genética , Rosuvastatina Cálcica/farmacocinética , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Adulto , Voluntários Saudáveis , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacocinética , Transportador 1 de Ânion Orgânico Específico do Fígado/metabolismo , Masculino , Proteínas de Neoplasias/metabolismo , Polimorfismo de Nucleotídeo Único/efeitos dos fármacos , Polimorfismo de Nucleotídeo Único/genética , Receptor de Pregnano X , Receptores Citoplasmáticos e Nucleares/metabolismo , Receptores de Esteroides/metabolismo , Adulto Jovem
9.
Pharmacol Rep ; 63(3): 815-25, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21857093

RESUMO

The aim of this study was to retrospectively evaluate the effect of polymorphisms in the CYP3A4, CYP3A5 and ABCB1 genes on the dose-adjusted concentration and dose requirement of cyclosporine A(CsA) in Chinese recipients during the early period after bone marrow or hematopoietic stem cell transplantation. Ninety-one bone marrow transplant recipients were genotyped by the polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) assay or by direct sequencing for the C1236T, G2677T/A and C3435T polymorphisms in CYP3A4*18B, CYP3A5*3, and ABCB1, respectively. The concentration at zero before administration (C0) and concentration at 2 h after administration (C2) of whole blood CsA were measured by fluorescence polarization immunoassay. Dose-adjusted C0 and C2 were determined and compared among groups with different genotypes. Compared with CYP3A5*3/*3 individuals, CYP3A5*1/*1 subjects have a significantly lower dose-adjusted C0 and C2 at days 1-10 and a higher dose requirement for CsA at days 16-30 (p < 0.05). In addition, homozygotes for the ABCB1 3435T mutant have a significantly higher dose-adjusted C0 and C2 and a lower dose requirement compared with wildtype (p < 0.05). Similar results were also derived for carriers of the T-G-C haplotype in CYP3A5 producers compared with non-carriers (p < 0.05 and p < 0.01, respectively). In summary, the ABCB1 3435T SNP, T-G-C haplotype in CYP3A5 producers, and CYP3A5*3 SNP are all associated with differences in CsA pharmacokinetics and dose requirements during the first month after bone marrow or hematopoietic stem cell transplantation. Genetic testing can therefore help to determine initial dosage and individualize immunosuppressive therapy.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Ciclosporina/farmacocinética , Citocromo P-450 CYP3A/genética , Subfamília B de Transportador de Cassetes de Ligação de ATP , Adolescente , Adulto , Transplante de Medula Óssea/métodos , Criança , Pré-Escolar , China , Ciclosporina/administração & dosagem , Relação Dose-Resposta a Droga , Feminino , Imunoensaio de Fluorescência por Polarização , Genótipo , Haplótipos , Transplante de Células-Tronco Hematopoéticas/métodos , Humanos , Imunossupressores/administração & dosagem , Imunossupressores/farmacocinética , Masculino , Polimorfismo de Fragmento de Restrição , Polimorfismo de Nucleotídeo Único , Estudos Retrospectivos , Adulto Jovem
10.
Pharmacol Rep ; 61(5): 843-50, 2009 Sep-Oct.
Artigo em Inglês | MEDLINE | ID: mdl-19904007

RESUMO

The aim of this study was to evaluate the effects of ABCB1 gene polymorphisms on azithromycin pharmacokinetics in Chinese Han ethnic subjects. In total, 20 healthy volunteers with various ABCB1 genotypes (6 with 2677GG/3435CC, 8 with 2677GT/3435CT, 6 with 2677TT/3435TT) were enrolled. Each was given a single oral dose of 500 mg azithromycin. Plasma concentration was measured for up to 96 h by LC/MS/MS. As shown, C(max) was significantly lower among individuals with 2677TT/3435TT genotype (468.0 +/- 173.4 ng x h/ml) than those with 2677GG/3435CC (911.2 +/- 396.4 ng x h/ml, p = 0.013). However, the t(max) value was higher among subjects with 2677TT/3435TT (2.0 +/- 0.5 h) than those with 2677GT/3435CT (1.6 +/- 0.3 h) or 2677GG/3435CC (1.4 +/- 0.4 h) genotypes (p = 0.068 and p = 0.026, respectively). Furthermore, the AUC(last) tended to be higher among subjects with 2677GG/3435CC than those with 2677GT/3435CT or 2677TT/3435TT genotypes (5000.2 +/- 1610.0 vs. 4558.0 +/- 805.0 vs. 4131.0 +/- 995.1 ng/ml). Our results showed for the first time that azithromycin pharmacokinetics may be influenced by particular polymorphisms of the ABCB1 gene. Individualized dosage regimen design incorporating such information may improve the efficacy of the drug while reducing adverse reactions.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Antibacterianos/farmacocinética , Azitromicina/farmacocinética , Polimorfismo de Nucleotídeo Único , Subfamília B de Transportador de Cassetes de Ligação de ATP , Área Sob a Curva , Grupo com Ancestrais do Continente Asiático , China , Cromatografia Líquida , Genótipo , Humanos , Masculino , Espectrometria de Massas em Tandem
11.
Br J Clin Pharmacol ; 68(3): 395-401, 2009 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19740397

RESUMO

AIMS: To assess the association between polymorphisms of the ABCB1 gene and the pharmacokinetics of verapamil among healthy Chinese Han ethnic subjects. METHODS: Based on polymorphisms of the ABCB1 gene at positions 2677 and 3435, 24 healthy male participants were divided into three groups: 2677GG/3435CC (n = 6), 2677GT/3435CT (n = 12) and 2677TT/3435TT (n = 6). Each subject had received a single oral dose of verapamil (80 mg) under fasting conditions. Multiple blood samples were collected over 24 h, and plasma concentrations of verapamil were determined by HPLC. Pharmacokinetic characteristics were compared between the different genotypic groups. RESULTS: The pharmacokinetics parameters of verapamil differed significantly among the three genotypic groups. AUC(last) was significantly lower among individuals with the 2677TT/3435TT (159.5 +/- 79.0 ng ml(-1) h) and 2677GT/3435CT (189.3 +/- 73.1 ng ml(-1) h) genotypes than those with the 2677GG/3435CC genotype (303.1 +/- 83.7 ng ml(-1) h) (P= 0.004 and P= 0.008, respectively). However, the CL/F value was higher among subjects with the 2677TT/3435TT (523.0 +/- 173.7 l h(-1)) genotype than those with the 2677GT/3435CT (452.2 +/- 188.6 l h(-1)) or 2677GG/3435CC (265.4 +/- 72.8 l h(-1)) genotypes. A significant difference was also found between the latter two groups (P= 0.034). In addition, the C(max) tended to be higher among subjects with the 2677GG/3435CC genotype than those with the 2677GT/3435CT or 2677TT/3435TT genotypes (42.2 +/- 3.9 vs 32.2 +/- 16.2 vs 38.1 +/- 13.7 ng ml(-1)). CONCLUSIONS: Our study showed for the first time that verapamil pharmacokinetics may be influenced by particular genetic polymorphisms of the ABCB1 gene among healthy Chinese Han ethnic subjects. An individualized dosage regimen design incorporating such information may improve the efficacy of the drug whilst reducing adverse reactions.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Grupo com Ancestrais do Continente Asiático/genética , Bloqueadores dos Canais de Cálcio/farmacocinética , Polimorfismo de Nucleotídeo Único/genética , Verapamil/farmacocinética , Subfamília B de Transportador de Cassetes de Ligação de ATP , Administração Oral , Adulto , Área Sob a Curva , Cromatografia Líquida de Alta Pressão , Genótipo , Meia-Vida , Humanos , Masculino , Fenótipo , Adulto Jovem
12.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 8): o2050, 2009 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-21583712

RESUMO

In the title Schiff base compound, C(14)H(11)N(3)O(5), the dihedral angle between the two benzene rings is 1.6 (1)°. The mol-ecule displays an E configuration about the C=N bond. An intra-molecular O-H⋯O hydrogen bond is observed. In the crystal, mol-ecules are linked into layers parallel to (101) by O-H⋯O, N-H⋯O and C-H⋯O hydrogen bonds. One of the hydroxyl groups is disordered over two positions, with occupancies of 0.643 (5) and 0.357 (5).

13.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 5): o1153, 2009 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-21583956

RESUMO

In the chiral title compound, C(38)H(28)O(4)P(2), the intra-molecular P⋯P separation is 3.671 (2) Šand the dihedral angle between the two benzene rings in the biphenyl unit is 77.9 (2)°.

14.
Zhonghua Bing Li Xue Za Zhi ; 34(12): 788-90, 2005 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-16545187

RESUMO

OBJECTIVE: To investigate the clinicopathologic features of gastrointestinal stromal tumors (GISTs) and to identify reliable prognostic parameters. METHODS: Fifty-nine GISTs were studied by immunostaining of CD117, CD34, SMA, desmin, S-100, bcl-2, and Ki-67. Histopathologic evaluations included tumor size, necrosis, histological growth patterns, mitotic activities and tumor lymphocytic infiltrate. The patients were clinically followed for 2 to 9 years. Univariate, multivariate and correlative statistical evaluations were used to analyze the data. RESULTS: Among the 59 patients, 40 were alive and 15 died of their tumors at follow-up, the remaining 4 patients died of other causes. Pathological parameters that correlated with prognosis included tumor sizes of more than 5 cm, tumor tissue necrosis, mitotic cell count equal or higher than 5 per 50 high power field, Ki-67 labeling index (LI) equal or higher than 5% and intense bcl-2 immunostaining. Multivariate analysis showed that the mitotic count and Ki-67 LI were independent prognostic indicators. There was a correlation between mitotic count and Ki-67 LI. CONCLUSIONS: Mitotic count and Ki-67 LI are the best predictors for a poor outcome of GIST after surgical treatment. Ki-67 immunostaining may substitute mitotic count as a useful prognostic parameter.


Assuntos
Ciclina D1/metabolismo , Tumores do Estroma Gastrointestinal/metabolismo , Antígeno Ki-67/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Proteínas Proto-Oncogênicas c-kit/metabolismo , Adolescente , Adulto , Idoso , Criança , Feminino , Seguimentos , Tumores do Estroma Gastrointestinal/patologia , Humanos , Masculino , Pessoa de Meia-Idade , Prognóstico
15.
Yao Xue Xue Bao ; 39(12): 993-6, 2004 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-15813028

RESUMO

AIM: To develop a rapid and sensitive LC/MS/MS method for the analysis of levodropropizine in plasma and study the pharmacokinetics of levodropropizine in healthy Chinese volunteers. METHODS: Levodropropizine and zolmitriptan (internal standard, IS) were extracted from plasma samples and chromatographed on a C18 column and detected using a tandem mass spectrometer with a TurboIon Spray ionization interface. Quantitation was performed using multiple reaction monitoring (MRM) of the transitions of the m/z 237 --> m/z 120 for levodropropizine and m/z 288 --> m/z 58 for the IS. RESULTS: The limit of quantification of the method for levodropropizine was 0.25 microg x L(-1). The assay was linear over the concentration range from 0.25 to 500.0 microg x L(-1) and intra- and inter-day precision over this range were < 11.4% with good accuracy. CONCLUSION: The method is shown to be accurate, and suitable for clinical pharmacokinetic study of levodropropizine.


Assuntos
Propilenoglicóis/sangue , Propilenoglicóis/farmacocinética , Administração Oral , Antitussígenos/sangue , Antitussígenos/farmacocinética , Área Sob a Curva , Cromatografia Líquida , Humanos , Masculino , Propilenoglicóis/administração & dosagem , Espectrometria de Massas por Ionização por Electrospray
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