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1.
Electromagn Biol Med ; 39(4): 437-444, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-33021115

RESUMO

The objective of this study was to evaluate the effect of Capacitive and Resistive electric transfer (CRet)-combined exercise therapy for participants with non-specific chronic low back pain (NSCLBP). Twenty-six received only the exercise program (E group, n = 15), or received both CRet and the same exercise program (E+CRet group, n = 11). Pain intensity, functional disability and trunk function were measured pre-, and post-intervention and there was also a 1-month follow-up period. Data analysis was performed for each index using the Mann-Whitney U test for comparisons between two groups at each time point, and the Wilcoxon signed-rank test for comparison between each time point within the group. The results of this study indicate that pain intensity was improved in both groups at post-intervention, also, the effect continued during follow-up period. In addition, functional disability was significantly improved in the E+CRet group at the post-intervention and during the follow-up period. The intervention effect on NSCLBP was higher in the E+CRet group than the E group. CRet, which is a form of deep thermotherapy, combined with exercise have a possibility of more effectiveness than exercise alone.


Assuntos
Capacitância Elétrica , Terapia por Exercício/métodos , Dor Lombar/terapia , Adulto , Doença Crônica , Impedância Elétrica , Feminino , Humanos , Masculino
2.
J Sport Rehabil ; 29(5): 621-625, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31094624

RESUMO

CONTEXT: The functional movement screen (FMS) is an assessment tool for movement dysfunction, which is used to reduce the risk of injury. Although the relationship between the FMS composite score and injuries has been extensively studied, the association between FMS scores and injuries in only college basketball players remains unknown. OBJECTIVE: To examine the relationship between the FMS score and injuries in basketball players. DESIGN: Cross-sectional study. SETTING: University research laboratory. PARTICIPANTS: Eighty-one male college basketball players (average age 20.1 [1.3] y) participated. MAIN OUTCOME MEASURES: The FMS composite score was calculated from 7 movement tests. The incidence of injuries over a 1-year period prior to the test day was determined based on a questionnaire. Individuals were categorized into 2 groups: injury (with a serious basketball-related injury resulting in the loss of practice and game time for at least 4 wk) and noninjury groups. Mann-Whitney U and chi-square tests were used to evaluate group differences in the composite FMS and 7 movement scores, respectively. Furthermore, the scores significant on univariate analyses were submitted to a multivariate logistic analysis, adjusting for participant characteristics. RESULTS: The composite FMS scores of the 2 groups were not significantly different (P = .38). Among the 7 tasks, only the deep squat and hurdle step showed significant group differences (P = .03 and P = .001, respectively). The multivariate logistic analysis revealed that deep squat (odds ratio, 6.48; 95% confidence interval, 1.23-34.01; P = .03) and hurdle step scores (odds ratio, 25.80; 95% confidence interval, 1.81-368.73; P = .02) were significantly associated with injuries, even after adjustment for participant characteristics. CONCLUSIONS: Deep squat and hurdle step scores may be associated with injuries in basketball players. Further research should be conducted to confirm that these 2 scores can predict the incidence of injuries in basketball players.


Assuntos
Basquetebol/lesões , Transtornos dos Movimentos/diagnóstico , Movimento/fisiologia , Atletas , Traumatismos em Atletas/classificação , Traumatismos em Atletas/epidemiologia , Traumatismos em Atletas/etiologia , Estudos Transversais , Métodos Epidemiológicos , Humanos , Masculino , Exercício Pliométrico , Estudantes/estatística & dados numéricos , Fatores de Tempo , Universidades , Adulto Jovem
3.
Electromagn Biol Med ; 38(1): 48-54, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30663425

RESUMO

This study aimed to investigate the acute effects of capacitive and resistive electric transfer (CRet) on Achilles tendon elongation during muscle contraction, as well as the circulation in the peritendinous region. Sixteen healthy men participated in this study. All 16 participants underwent 2 interventions: (1) CRet trial and (2) CRet without power (sham trial). Tendon elongation was measured four times. Using near-infrared spectroscopy, the blood circulation (volume of total-hemoglobin (Hb), oxygenated hemoglobin (oxy-Hb), and deoxygenated hemoglobin (deoxy-Hb)) was measured for 5 min before the intervention and for 30 min after the intervention. The differences between the measurements obtained before and after intervention were compared between the two interventions. The changes in tendon elongation and deoxy-Hb were not significantly different between the interventions. Total- and oxy-Hb were significantly increased in the CRet trial compared with the sham trial. In addition, the increases in total-Hb and oxy-Hb lasted for 30 min after the CRet intervention (CRet vs. sham: oxy-Hb: F = 8.063, p = 0.001, total-Hb: F = 4.564, p = 0.011). In conclusion, CRet significantly improved blood circulation in the peritendinous region.


Assuntos
Tendão do Calcâneo/anatomia & histologia , Tendão do Calcâneo/irrigação sanguínea , Capacitância Elétrica , Terapia por Estimulação Elétrica , Tendão do Calcâneo/metabolismo , Adulto , Circulação Sanguínea , Impedância Elétrica , Hemoglobinas/metabolismo , Humanos , Masculino
4.
J Phys Ther Sci ; 30(8): 978-983, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30154585

RESUMO

[Purpose] The association between foot injuries and foot alignment, including the transverse arch height (TAH) and asymmetry, was examined in athletes participating in college track events. [Participants and Methods] This study included 55 male athletes participating in a college track and field club. Data including demographic information and the incidence of foot injuries within a year prior to participation in this study were obtained via questionnaires. TAH and the medial longitudinal arch height during 10 and 90% loading, leg-heel alignment, and the heel angle were measured before calculating the asymmetry of each alignment parameter measured. Participants were categorized into an injury or a normal group. Unpaired t-tests were used to perform between-group comparisons for each alignment parameter measured and asymmetry. Additionally, logistic regression analysis was performed to identify factors associated with foot injuries after adjustment for demographic data. [Results] TAH asymmetry during 10 and 90% loading was significantly greater in the injury group. Further logistic regression analysis performed showed that only TAH asymmetry during 90% loading was significantly associated with foot injuries after adjustment for demographic data. [Conclusion] With regard to track events, a greater asymmetry of forefoot TAH in a weight-bearing position was observed to be associated with foot injuries.

5.
J Phys Ther Sci ; 30(5): 719-725, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29765189

RESUMO

[Purpose] This study aimed to clarify the effects of Capacitive and Resistive electric transfer (CRet) on changes in muscle flexibility and lumbopelvic alignment after fatiguing exercise. [Subjects and Methods] Twenty-two healthy males were assigned into either the CRet (n=11) or control (n=11) group. Fatiguing exercise and CRet intervention were applied at the quadriceps muscle of the participants' dominant legs. The Ely test, pelvic tilt, lumbar lordosis, and superficial temperature were measured before and after exercise and for 30 minutes after intervention. Statistical analysis was performed using one-way analysis of variance, with Tukey's post-hoc multiple comparison test to clarify within-group changes and Student's t-test to clarify between-group differences. [Results] The Ely test and pelvic tilt were significantly different in both groups after exercise, but there was no difference in the CRet group after intervention. Superficial temperature significantly increased in the CRet group for 30 minutes after intervention, in contrast to after the exercise and intervention in the control group. There was no significant between-group difference at any timepoint, except in superficial temperature. [Conclusion] CRet could effectively improve muscle flexibility and lumbopelvic alignment after fatiguing exercise.

6.
J Phys Ther Sci ; 30(4): 630-635, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29706721

RESUMO

[Purpose] Few studies on the transverse arch (TA) in the forefoot have been conducted. The forefoot is where pains occur most frequently and is related to walking and balance; hence, paying attention to TA is vital. However, the relationship between TA and foot muscles has not been investigated. Therefore, this study aims to investigate muscles related to TA. [Subjects and Methods] Nineteen healthy young males were included. Measurements of their feet, excluding one foot with recent foot pain (n=37), were obtained. The height of TA (TAH) was measured in two ways: during 10% and 90% loading of body weight. The cross-sectional area and thickness of five muscles were measured: flexor digitorum longus, peroneus longus and brevis, flexor hallucis brevis, flexor digitorum brevis (FDB) and abductor hallucis (ABH). All measurements were performed with an ultrasound device. [Results] FDB and ABH were correlated with TAH during 10% and 90% loading after removing the effect of body mass index and age. The greater FDB and ABH, the higher TAH. [Conclusion] As FDB becomes larger, the second, third and fourth metatarsal heads are raised more. Furthermore, the height of the first metatarsal head is lowered by a larger ABH. These mechanisms may increase TAH.

7.
J Phys Ther Sci ; 30(2): 320-323, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29545704

RESUMO

[Purpose] Targeting university badminton players, this study investigated the relationship between agility, which is associated with performance in badminton, and lower limb muscle strength, and examined which muscles influence agility. [Subjects and Methods] A total of 23 male university badminton players were evaluated for side-shuffle test scores and lower limb strength. The relationships between agility, lower limb strength, and duration of experience playing badminton were evaluated using a correlation analysis. Moreover, the relationship between agility and lower limb strength was evaluated by partial correlation analysis, adjusting for the effects of experience of each badminton player. [Results] The agility score correlated with hip extension and ankle plantar flexion strength, with adjustment for badminton experience. [Conclusion] This study suggests that hip extension training and improvement in ankle plantar flexion strength may improve agility.

8.
J Foot Ankle Res ; 10: 17, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28416969

RESUMO

BACKGROUND: Forefoot structure is important to understand some foot problems such as hallux valgus and metatarsalgia. Ultrasonography (US) is a highly portable, noninvasive, low cost, and fast imaging method, especially when compared to magnetic resonance imaging (MRI), computed tomography (CT), and radiography. As the use of US for evaluating forefoot bony structure has not been validated, except for the presence of synovitis, erosions and bursitis within the forefoot in people with inflammatory arthritis, the purpose of this study was to determine whether US is a reliable method for evaluating forefoot structure. METHODS: Sixty feet (30 women, age = 40.1 ± 11.8 years) were examined by US and CT to assess agreement with CT and repeatability of US evaluation of the 2nd metatarsal head height, length between the medial sesamoid bone and 5th metatarsal head, transverse arch height, transverse arch index, sesamoid rotation angle, and area under the transverse arch. The measurement data were evaluated for agreement with CT using the intra-class correlation coefficient (ICC)3, 1, Pearson correlation coefficient, and Bland-Altman plot, and with ICC1, 1 for repeatability. RESULTS: The ICC3, 1 values of 0.78-0.89, Pearson correlation coefficient of 0.78-0.90, and Bland-Altman plots showed almost perfect agreements between the US and CT method for all parameters, except the area under the transverse arch (AUTA). The ICC1, 1 also showed perfect agreements (0.84-0.92) between two sets of US measurements in all parameters. CONCLUSIONS: The US evaluation of forefoot structure in the coronal plane showed good agreement with CT and repeatability of two ultrasonograms in adult women. This reliable evaluation method of forefoot structure can contribute to a quick clinical assessment screening for risk factors of foot problems such as hallux valgus and metatarsalgia. However, because of some limitations such as a lack of inter-observer reliability, more research is needed to validate US evaluation of forefoot structure. TRIAL REGISTRATION: The current study (trial registration number: R0297) was approved by the Ethical Committee for Human Experiments of Kyoto University (http://www.ec.med.kyoto-u.ac.jp) on December 3, 2015. The first participant in this study was enrolled on November 17, 2015 and retrospectively registered.


Assuntos
Pé/anatomia & histologia , Adulto , Pontos de Referência Anatômicos , Feminino , Pé/diagnóstico por imagem , Humanos , Masculino , Ossos do Metatarso/anatomia & histologia , Ossos do Metatarso/diagnóstico por imagem , Variações Dependentes do Observador , Reprodutibilidade dos Testes , Ossos Sesamoides/anatomia & histologia , Ossos Sesamoides/diagnóstico por imagem , Tomografia Computadorizada por Raios X , Ultrassonografia
9.
Int J Hyperthermia ; 33(6): 696-702, 2017 09.
Artigo em Inglês | MEDLINE | ID: mdl-28139939

RESUMO

PURPOSE: This study aims to evaluate the effects of Capacitive and Resistive electric transfer (CRet) and hotpack (HP) on haemoglobin saturation and tissue temperature. MATERIALS AND METHODS: The participants were 13 healthy males (mean age 24.5 ± 3.0). They underwent three interventions on different days: (1) CRet (CRet group), (2) HP (HP group) and (3) CRet without power (sham group). The intervention and measurement were applied at the lower paraspinal muscle. Indiba® active ProRecovery HCR902 was used in the CRet group, and the moist heat method was used in the HP group. Oxygenated, deoxygenated and total haemoglobin (oxy-Hb, deoxy-Hb, total-Hb) counts were measured before and after the 15-min interventions, together with the temperature at the skin surface, and at depths of 10 mm and 20 mm (ST, 10mmDT and 20mmDT, respectively). The haemoglobin saturation and tissue temperature were measured until 30 min after the intervention and were collected at 5-min intervals. Statistical analysis was performed for each index by using the Mann-Whitney U test for comparisons between all groups at each time point. RESULTS: Total-Hb and oxy-Hb were significantly higher in the CRet group than in the HP group continuously for 30 min after the intervention. The 10mmDT and 20mmDT were significantly higher in the CRet group than in the HP group from 10- to 30 min after intervention. CONCLUSIONS: The effect on haemoglobin saturation was higher in the CRet group than in the HP group. In addition, the CRet intervention warmed deep tissue more effectively than HP intervention.


Assuntos
Temperatura Corporal , Hemoglobinas/análise , Hipertermia Induzida , Adulto , Capacitância Elétrica , Impedância Elétrica , Temperatura Alta , Humanos , Masculino , Músculos Paraespinais , Adulto Jovem
10.
Biopharm Drug Dispos ; 36(1): 34-48, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25277346

RESUMO

The potent and selective phosphodiesterase 4 inhibitor ASP3258 is a novel therapeutic agent for asthma and chronic obstructive pulmonary disease (COPD). After a single oral administration to rats, ASP3258 is rapidly absorbed with a bioavailability of 106%. In situ absorption data indicated that ASP3258 is mainly absorbed in the small intestine. Tissue distribution data after oral administration of (14)C-ASP3258 showed rapid and extensive distribution to various tissues. Excluding the gastrointestinal tract, the tissues with the highest concentrations were liver, heart and plasma. Liquid chromatography-nuclear magnetic resonance spectroscopy data revealed that O-glucuronidation of the carboxylic acid moiety of ASP3258 (formation of an acyl glucuronide) plays a key role in metabolism. No indication was found that the acyl glucuronide reacted with proteins in plasma or tissues. When (14)C-ASP3258 was orally administered to intact rats, urinary and fecal excretion accounted for 1.3% and 100.6% of the administered radioactivity, respectively. After a single oral administration of (14)C-ASP3258 to bile-cannulated rats, urinary and biliary excretion accounted for 0.7% and 93.8% of the administered radioactivity, respectively. These findings suggest that fecal excretion via bile plays an important role in the elimination of ASP3258-derived radioactivity. In vitro metabolic profiles were relatively similar among the species examined, suggesting that our findings in rats may help us to understand pharmacokinetics, efficacy and safety profiles in humans and other species.


Assuntos
Bile/metabolismo , Absorção Intestinal , Naftiridinas/farmacocinética , Inibidores da Fosfodiesterase 4/farmacocinética , Administração Oral , Animais , Disponibilidade Biológica , Cromatografia Líquida , Espectroscopia de Ressonância Magnética , Masculino , Naftiridinas/administração & dosagem , Inibidores da Fosfodiesterase 4/administração & dosagem , Ratos , Ratos Endogâmicos F344 , Distribuição Tecidual
11.
Dement Geriatr Cogn Dis Extra ; 3(1): 312-9, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24174926

RESUMO

AIM: The purpose of this prospective cohort study is to examine whether cognitive decline is an independent predictor of new long-term care insurance (LTCI) requirement certifications in Japan. METHODS: A total of 5,765 community-dwelling older Japanese adults who, at baseline, were independent in terms of their activities of daily living participated in this study and were followed up for 18 months. The outcome measure was the number of new LTCI requirement certifications during the 18-month period of the study. We collected demographic information through questionnaires and assessed cognitive skills with the Cognitive Performance Scale (CPS). The participants were divided into 3 groups according to CPS scores (0, 1, and 2 or greater). RESULTS: During the 18-month period, 399 subjects (6.9%) became newly certified for LTCI services. In a multivariate Cox proportional hazards model, older participants with a CPS score of 1 (adjusted HR: 1.39, 95% CI: 1.08-1.77) and 2 or greater (adjusted HR: 2.27, 95% CI: 1.74-2.96) were significantly more likely to receive an LTCI certification compared to those with a CPS score of 0. CONCLUSIONS: Cognitive decline is an independent predictor of new LTCI requirement certifications and the severity of cognitive decline in elderly adults is positively associated with receiving an LTCI requirement certification in Japan.

12.
Arch Gerontol Geriatr ; 57(3): 328-32, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23566448

RESUMO

CKD is associated with impairments in health status, physical function, and frailty. The aim of the current prospective cohort study was to determine whether CKD predicted new LTCI need certification among community-dwelling older Japanese adults. This was a prospective cohort study. We analyzed the cohort data from a prospective study, The Japan Multicenter Aging Cohort for Care Prevention (J-MACC). We followed 8063 elderly adults for 2 years, and we analyzed the relationship between CKD and LTCI need. The outcome studied was new certification for LTCI service need during a 2-year period. We measured serum creatinine (the estimated glomerular filtration rate; eGFR), serum albumin, frailty checklist scores, and body mass index. During the 2-year follow-up, 536 subjects (6.6%) were newly certified as needing LTCI services. We stratified the cohort according to eGFR quartile and performed multivariate analyses using an eGFR value of 71.4-83.6 ml/min/1.73 m(2) as a reference. We found that subjects with eGFR values <60.0 ml/min/1.73 m(2) had a significantly elevated risk of LTCI service need (adjusted hazard ratio: 1.44 [95% CI 1.12-1.86]). Our results indicate that CKD is independently associated with new LTCI service need certification and is an important marker of frailty in older adults.


Assuntos
Seguro de Assistência de Longo Prazo/estatística & dados numéricos , Insuficiência Renal Crônica/terapia , Idoso , Idoso de 80 Anos ou mais , Índice de Massa Corporal , Lista de Checagem , Creatinina/sangue , Definição da Elegibilidade/estatística & dados numéricos , Feminino , Idoso Fragilizado/estatística & dados numéricos , Avaliação Geriátrica , Taxa de Filtração Glomerular , Humanos , Japão/epidemiologia , Assistência de Longa Duração/estatística & dados numéricos , Masculino , Análise Multivariada , Estudos Prospectivos , Insuficiência Renal Crônica/epidemiologia , Fatores de Risco , Albumina Sérica/análise
13.
J Am Med Dir Assoc ; 13(6): 507-11, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22572554

RESUMO

BACKGROUND: In Japan, older adults are assessed by frailty checklist for care prevention. However, the effect of care prevention programs in community-dwelling frail older adults is still unclear. OBJECTIVES: The purpose of this study was to investigate whether the care prevention program would reduce care and disability and to measure its cost-effectiveness in frail older adults. DESIGN: This is a prospective study using propensity score matching. SETTING AND SUBJECTS: A total of 610 community-dwelling older adults were recruited in 2 cities of Japan. INTERVENTION: Subjects in the exercise group (n = 305) attended physical exercise sessions once a week for 16 consecutive weeks. The exercise sessions were in a standardized format consisting of moderate-intensity aerobic exercise, progressive strength training, flexibility and balance exercises, and cool-down activities. The control group (n = 305) received only screening evaluation. MEASUREMENTS: Primary outcome was long term care insurance requirement certification during the 1-year follow-up period. Secondary outcome measurements were changes of frailty checklist, and care and medical cost. RESULTS: Twenty-five subjects (8.1%) in the exercise group and 55 (18%) in the control group were newly certified for long-term care insurance service requirement in 1 year after the intervention (RR = 2.16, 95% CI = 1.46-3.20). Consequently, the health care cost for the subjects in the exercise group was significantly lower than in the control group (P < .001). Moreover, subjects in the exercise group had significant improvements in total scores of the frailty checklist compared with the control group that worsened after 1 year (exercise group: from 7.41 ± 3.98 to 7.11 ± 4.00, control group: from 7.34 ± 4.27 to 8.02 ± 4.81, F = 12.84, P < .001). CONCLUSION: These results suggested that physical exercise is effective in preventing the progression of frailty and further disability in older adults living in the community. We could save heath care costs by our care prevention program.


Assuntos
Serviços de Saúde Comunitária/organização & administração , Terapia por Exercício/métodos , Idoso Fragilizado , Serviços de Saúde para Idosos/organização & administração , Prevenção Primária , Atividades Cotidianas , Idoso , Idoso de 80 Anos ou mais , Distribuição de Qui-Quadrado , Serviços de Saúde Comunitária/economia , Análise Custo-Benefício , Avaliação da Deficiência , Terapia por Exercício/economia , Feminino , Seguimentos , Avaliação Geriátrica , Serviços de Saúde para Idosos/economia , Humanos , Japão , Modelos Logísticos , Masculino , Avaliação de Processos e Resultados em Cuidados de Saúde , Estudos Prospectivos , Resultado do Tratamento
14.
Telemed J E Health ; 18(4): 292-6, 2012 May.
Artigo em Inglês | MEDLINE | ID: mdl-22400972

RESUMO

Smartphones are very common devices in daily life that have a built-in tri-axial accelerometer. Similar to previously developed accelerometers, smartphones can be used to assess gait patterns. However, few gait analyses have been performed using smartphones, and their reliability and validity have not been evaluated yet. The purpose of this study was to evaluate the reliability and validity of a smartphone accelerometer. Thirty healthy young adults participated in this study. They walked 20 m at their preferred speeds, and their trunk accelerations were measured using a smartphone and a tri-axial accelerometer that was secured over the L3 spinous process. We developed a gait analysis application and installed it in the smartphone to measure the acceleration. After signal processing, we calculated the gait parameters of each measurement terminal: peak frequency (PF), root mean square (RMS), autocorrelation peak (AC), and coefficient of variance (CV) of the acceleration peak intervals. Remarkable consistency was observed in the test-retest reliability of all the gait parameter results obtained by the smartphone (p<0.001). All the gait parameter results obtained by the smartphone showed statistically significant and considerable correlations with the same parameter results obtained by the tri-axial accelerometer (PF r=0.99, RMS r=0.89, AC r=0.85, CV r=0.82; p<0.01). Our study indicates that the smartphone with gait analysis application used in this study has the capacity to quantify gait parameters with a degree of accuracy that is comparable to that of the tri-axial accelerometer.


Assuntos
Aceleração , Marcha , Telemedicina/instrumentação , Adolescente , Adulto , Fenômenos Biomecânicos , Feminino , Humanos , Japão , Masculino , Reprodutibilidade dos Testes , Processamento de Sinais Assistido por Computador , Telemedicina/métodos , Adulto Jovem
15.
Biopharm Drug Dispos ; 33(3): 160-9, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22374735

RESUMO

YM155 monobromide is a novel small-molecule survivin suppressant. The pharmacokinetics, distribution and excretion of YM155/[14C]YM155 were investigated using males and pregnant or lactating female rats after a single intravenous bolus administration. For the 0.1, 0.3 and 1 mg/kg YM155 doses given to male rats, increases in area under the plasma concentration-time curves were approximately proportional to the increase in the dose level. After administering [14C]YM155, radioactivity concentrations in the kidney and liver were highest among the tissues in both male and pregnant rats: e.g. 14.8- and 5.24-fold, respectively, and higher than in plasma at 0.1 h after dosing to male rats. The YM155 concentrations in the brain were lowest: 25-fold lower than in plasma. The transfer of radioactivity into fetuses was low (about 2-fold lower than in plasma). In lactating rats, the radioactivity was transferred into milk at a level 8- to 21-fold higher than for plasma. Radioactivity was primarily excreted in feces (64.0%) and urine (35.2%). The fecal excretion was considered to have occurred mainly by biliary excretion and partly by secretion across the gastrointestinal membrane from the blood to the lumen.


Assuntos
Antineoplásicos/farmacocinética , Imidazóis/farmacocinética , Lactação/metabolismo , Naftoquinonas/farmacocinética , Gravidez/metabolismo , Animais , Antineoplásicos/sangue , Antineoplásicos/urina , Bile/química , Proteínas Sanguíneas/metabolismo , Fezes/química , Feminino , Imidazóis/sangue , Imidazóis/urina , Masculino , Troca Materno-Fetal , Proteínas Associadas aos Microtúbulos/antagonistas & inibidores , Naftoquinonas/sangue , Naftoquinonas/urina , Placenta/metabolismo , Ratos , Ratos Sprague-Dawley , Survivina , Distribuição Tecidual
16.
Biopharm Drug Dispos ; 25(6): 253-60, 2004 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-15334624

RESUMO

YM466 is a novel factor Xa inhibitor for the treatment of thrombosis. The absorption, distribution, metabolism and excretion of YM466 were investigated in male Fisher rats after a single oral administration. YM466 was absorbed rapidly from all segments of the gastrointestinal tract except the stomach. After oral dosing, the plasma concentration of (14)C-YM466 reached a maximum within 0.5 h, and declined rapidly with an elimination half-life of 0.64 h. The unchanged YM466 accounted for almost all of its radioactivity, suggesting a minimal metabolism in rats. This was also supported by the finding that no metabolites were observed in bile and urine after oral dosing of (14)C-YM466. The distribution of (14)C-YM466 in tissue was evaluated and the liver and kidney were the organs with radioactivity concentrations consistently higher than that of plasma. Cumulative biliary and urinary excretion of radioactivity in bile duct-cannulated rats was 29.5% and 7.6%, respectively, indicating prominent excretion into bile after oral dosing. This was consistent with the finding that 76.1% and 25.2% of radioactivity dosed were excreted to faeces and urine, respectively, after i.v. dosing. These results suggest that YM466 was rapidly absorbed and then subjected to biliary excretion with a minimal metabolism after oral dosing to rats.


Assuntos
Inibidores do Fator Xa , Absorção Intestinal/efeitos dos fármacos , Naftalenos/farmacocinética , Piperidinas/farmacocinética , Administração Oral , Animais , Radioisótopos de Carbono , Cromatografia Líquida de Alta Pressão , Fezes/química , Meia-Vida , Injeções Intravenosas , Masculino , Naftalenos/sangue , Naftalenos/metabolismo , Piperidinas/sangue , Piperidinas/metabolismo , Ratos , Ratos Endogâmicos F344 , Fatores de Tempo , Distribuição Tecidual
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