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[Purpose] To clarify the motion-plane dependency of the range of dart throw motion and the effects of tendon action due to long finger flexors and extensors during the motion. [Subjects and Methods] Forty healthy subjects attended the experiment, and the active range of wrist motion in seven motion planes was measured with an originally designed apparatus. [Results] The reliability of the measurement was acceptable. The range of dart throw motion depended on the motion planes, with a maximum at around the motion plane of 45° from the sagittal plane (45° of pronation). The tendon action of long finger muscles was shown in dart throw motion except in 45° of pronation. [Conclusion] Motion-plane dependency of the range of dart throw motion exists in healthy subjects. The absence of tendon action due to finger extrinsic muscles in dart throw motion at 45° might be one of the causes of the advantage of dart throw motion.
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[Purposes] Although it is recommended to develop a habit of physical activities, there is no easy way to measure skeletal muscle mass in preschool children, which cause the difficulty of evaluation. The purpose of this study was to examine the validity of body composition including the skeletal muscle mass assessment using multi-frequency bioelectrical impedance analysis by comparing body fat mass obtained by using multi-frequency bioelectrical impedance analysis method and body mass index formulas. [Subjects and Methods] Ninety-four children were surveyed for age, height, weight, grip strength, maximum occlusal force, thickness of muscle and fat mass (masseter and lower limb), body fat mass, skeletal muscle mass, and calf circumference. We assessed additional parameters, which were thought to be related to skeletal muscle mass, to ensure validity. [Results] A strong correlation was found in body fat mass values obtained using the multi-frequency bioelectrical impedance analysis method and those obtained using the body mass index formulas. Additionally, strong correlation coefficients were found between the skeletal muscle mass/height obtained using the multi-frequency bioelectrical impedance analysis method and grip strength and calf circumference. [Conclusion] Our results indicate that skeletal muscle mass can be reliably measured using the multi-frequency bioelectrical impedance analysis method in preschool children.
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OBJECTIVE: To evaluate the immediate effect of repetitive wrist extension on grip strength in patients with distal radial fracture. DESIGN: Interventional study. SETTING: Patients who were admitted to a hospital department of occupational therapy. PARTICIPANTS: Consecutive patients with a unilateral distal radial fracture (N=28). INTERVENTION: Each patient was randomly allocated to either the experimental group (n=14) or the control group (n=14). The experimental group performed 30 repetitive wrist extensions with maximal isometric contraction of the extensors of their affected hands during a 6-minute intervention period, whereas the control group did not perform the exercise. MAIN OUTCOME MEASURES: Grip strength was measured just before and after the intervention period. Pain during grip strength measurements was also quantified using the visual analog scale. Wrist extension strength was measured 10 minutes after the grip strength measurement. RESULTS: Grip strength increased immediately after repetitive wrist extension in the experimental group, but it remained the same in the control group. Visual analog scale scores indicated that pain was relieved only in the experimental group. However, pain was unrelated to strength production. CONCLUSIONS: The intervention used in this study might be useful during physical examination to reveal the potential grip strength of patients. The intervention may also be an effective warm-up training procedure in preparation for conventional grip-strengthening exercises.
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Terapia por Exercício/métodos , Força da Mão/fisiologia , Fraturas do Rádio/reabilitação , Articulação do Punho/fisiologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Mãos , Humanos , Contração Isométrica , Masculino , Pessoa de Meia-Idade , Amplitude de Movimento ArticularRESUMO
The inclusion mode of Limaprost in the presence of α- and ß-cyclodextrins (CDs) was investigated to gain insight into the stabilization mechanism of Limaprost-alfadex upon the addition of ß-CD in the solid state. The inclusion sites of α- and ß-CDs were studied by NMR spectroscopic and kinetic methods. With the addition of α- and ß-CDs, displacements in (13)C chemical shifts of prostaglandin F2α (PGF2α) were observed in the ω-chain and the five-membered ring, respectively, of the drug. Similar shift changes were observed with the addition of both α- and ß-CDs. In two-dimensional (2D) (1)H-NMR spectra, intermolecular correlation peaks were observed between protons of PGF2α and protons of both α- and ß-CDs, suggesting that PGF2α interacts with α- and ß-CDs to form a ternary complex by including the ω-chain with the former CD and the five-membered ring with the latter. In kinetic studies in aqueous solution, Limaprost was degraded to 17S,20-dimethyl-trans-Δ(2)-PGA1 (11-deoxy-Δ(10)) and 17S,20-dimethyl-trans-Δ(2)-8-iso-PGE1 (8-iso). The addition of α-CD promoted the dehydration to 11-deoxy-Δ(10), while ß-CD promoted the isomerization to 8-iso, under these conditions. In the presence of both α- and ß-CDs, dehydration and isomerization were also accelerated, supporting the formation of the ternary Limaprost/α-CD/ß-CD complex.
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Alprostadil/análogos & derivados , Água/química , alfa-Ciclodextrinas/química , beta-Ciclodextrinas/química , Alprostadil/química , Espectroscopia de Ressonância Magnética , Estrutura MolecularRESUMO
The purpose of the study was clarify the effect of the cathepsin K inhibitor ONO-5334 on bone resortion markers using sustained release (SR) formulations with different pharmacokinetic (PK) patterns, and identify the optimal SR formulation. The PK profiles and pharmacodynamic effect on bone resorption markers of 4 SR candidates formulations were evaluated in healthy postmenopausal women within a randomized, 2-part, open-label crossover study. In Part A, subject received a single dose of each formulation orally in the fed state. In Part B, two selected formulations were evaluated in the fasted state. From the results from Part A, C(max) was reduced and plasma concentrations of ONO-5334 were sustained with all SR formulations compared with an immediate release tablet. In pharmacodynamics, the level of C-terminal telopeptide of type I collagen (CTX) in serum and urine were inhibited with SR tablets rather than with granules. C max and area under the concentration-time curve from time 0 to the last measurable time point (AUC(0-t)) of SR tablets were higher than those of granules. From Part B, C max in the fasted condition was lower than that in the fed condition with two SR tablets. In contrast, C(24 h) in the fasted condition was slightly higher than that in the fed condition, but AUC(0-t) was similar. The inhibitory effect on CTX in serum and urine may depend on the PK pattern of ONO-5334. The SR tablets was well tolerated in postmenopausal women and has the optimal SR profiles on pharmacodynamics effect on bone resortion markers and PK profile. These results suggest that SR tablets of ONO-5334 are an excellent drug candidate for osteoporosis.
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Catepsina K/antagonistas & inibidores , Osteoporose/tratamento farmacológico , Tiazolidinas/uso terapêutico , Idoso , Idoso de 80 Anos ou mais , Estudos Cross-Over , Feminino , Humanos , Pessoa de Meia-IdadeRESUMO
Stabilization against humidity of Limaprost (a prostaglandin E1 derivative), which is currently marketed as Opalmon, was undertaken using ß-cyclodextrin (ß-CD). Aqueous solutions of Limaprost alfadex/dextran 40 were lyophilized with and without ß-CD. Limaprost alfadex lyophilized with ß-CD was more chemically stable in humid conditions than that without ß-CD. Moreover, the addition of ß-CD as an excipient to tablets of these lyophilized composites remarkably improved the stability of Limaprost, and Limaprost in this moisture-resistant formulation was chemically stable for 19 weeks at 30°C, 75% relative humidity (R.H.). Chemical analysis of Limaprost and its degradation products indicated that degradation proceeded in the inclusion form (i.e., within the CD cavity). Solid (2)H-NMR spectroscopic studies showed that ß-CD constrained the molecular mobility of water in the solid state. These results suggested that the stabilization of Limaprost by ß-CD was at least partly due to the restricted molecular mobility of water, which acted as a catalytic species for the degradation, and also to the protection of the five-membered ring of Limaprost from water catalytic dehydration through inclusion complex formation with ß-CD.
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Alprostadil/análogos & derivados , Excipientes/química , alfa-Ciclodextrinas/química , beta-Ciclodextrinas/química , Alprostadil/química , Dextranos/química , Estabilidade de Medicamentos , Liofilização , Umidade , ComprimidosRESUMO
The purpose of the present study was to describe kinetically and kinematically the control patterns of wheelchair wheelies, to clarify the relation between motion of the wheelchair and floor reaction force, to reveal movement strategies of the task, and to find useful parameters to understand the control and learning process of the skill. 10 healthy female Japanese students who were able to perform a 2-min. stationary wheelie participated in the experiments. Analysis of the 20-sec. wheelie performances suggested that (1) Center of Pressure is not a fundamental parameter for wheelie balance control, but may be the result of the control (2) the anteroposterior component of the floor reaction force is a fundamental parameter for analyzing the control of a wheelchair wheelie, and (3) angular velocity is used in the control of wheelie balance as a cue.
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Fenômenos Biomecânicos , Cinestesia , Destreza Motora , Orientação , Equilíbrio Postural , Cadeiras de Rodas , Adolescente , Feminino , Gravitação , Humanos , Suporte de Carga , Adulto JovemRESUMO
The effect of polymeric pharmaceutical excipients on the degradation of limaprost by hydrolysis was assessed by near infrared (NIR) spectroscopy and spin-spin relaxation time (T(2)) measurements of proton NMR. Freeze-dried limaprost-alfadex formulated with various polymeric pharmaceutical excipients was exposed under humidified condition at 25 degrees C and 75% relative humidity. The freeze-dried limaprost-alfadex formulated with cellulose derivatives, hydroxypropylmethylcellulose (HPMC) and hydroxypropylcellulose (HPC-L), degraded easily. However, degradation was suppressed in samples formulated with polysaccharides, dextran40, dextrin, and pullulan, although the water sorption was more than 10% (w/w). A second-derivative NIR study showed the changes in the water mobility in the mixtures. The absorption peak near 1900nm, which was assigned to water with high mobility, was observed in the humidified HPMC and HPC-L. The proton NMR spin-spin relaxation time measurements indicated that the structural relaxation of a polymeric excipient changed upon humidification. The polysaccharides showed only Gaussian relaxations, but the cellulose derivatives showed Lorentzian relaxations and Gaussian relaxations. The T(2) values of the Gaussian relaxation in HPMC and HPC-L were higher than those in dextran40, dextrin, and pullulan throughout the humidifying period. The higher molecular mobility of HPMC and HPC-L is related to the mobility of water, which may accelerate limaprost degradation.
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Alprostadil/análogos & derivados , Alprostadil/administração & dosagem , Alprostadil/química , Estabilidade de Medicamentos , Liofilização , Concentração de Íons de Hidrogênio , Espectroscopia de Ressonância Magnética , Espectroscopia de Luz Próxima ao InfravermelhoRESUMO
Limaprost/α-cyclodextrin (CD)/ß-CD ternary inclusion complex was prepared by freeze-drying a solution containing all three components. Under humid conditions, limaprost was more stable in the ternary α-/ß-CD inclusion complex than in the binary α- or ß-CD complex. Specifically, during storage at 30°C/75% relative humidity (R.H.) for 4 weeks, about 19% of limaprost degraded into 17S,20-dimethyl-trans-Δ(2)-prostaglandin A1 (referred as 11-deoxy-Δ(10)) in the ß-CD complex, 8.1% degraded in the α-CD complex, and only 2.2% degraded in the α-/ß-CD complex. The mechanism of limaprost stabilization in the presence of both CDs was investigated by Raman and solid-state NMR spectroscopy and powder X-ray diffractometry. The fast degradation of limaprost to 11-deoxy-Δ(10) in the ß-CD complex was due to the rapid crystallization of ß-CD from the complex, liberating the free amorphous drug, which is susceptible to degradation. The dissociation and crystallization of ß-CD from the inclusion complex were suppressed by freeze-drying limaprost in the presence of both α- and ß-CDs. In addition, the interaction between limaprost and the two CDs was reinforced by inclusion of different moieties of limaprost: α-CD predominantly included the alkyl ω-chain, whereas ß-CD included the five-membered ring. Thus, a stable ternary inclusion complex was formed that included limaprost, maintaining the amorphous state of the complex and dramatically stabilizing the drug under humid conditions.
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Alprostadil/análogos & derivados , Alprostadil/química , alfa-Ciclodextrinas/química , beta-Ciclodextrinas/química , Química Farmacêutica/métodos , Cristalização/métodos , Excipientes/química , Liofilização/métodos , Espectroscopia de Ressonância Magnética/métodos , Soluções Farmacêuticas/química , SolubilidadeRESUMO
Whereas many researchers have examined the transition from quiet posture to dynamic state, study of the initiation of lateral weight-transfer during sitting has only begun recently. This action is included in many tasks performed in our daily living, i.e., reaching, dressing, looking backwards, lying down, and shuffling the buttocks. The present study was designed to describe lateral weight-transfer movements of healthy adults, kinematically and kinetically, and to clarify the strategies and speed dependency of lateral weight-transfer initiation during sitting. Seven healthy Japanese male students without orthopaedic or neurological disorders participated. Their lateral weight-transfer movements were measured during sitting, using two force platforms and a 3-dimensional analysis system. Analysis showed that there appear to be two strategies for the initiation of the task: one is the lateral bending of trunk toward the weight-transfer side, and the other is a coordinated reciprocal leg action of both legs. A combination of these strategies is used in a trade-off fashion during natural motions. These results are clinically important for the assessment and therapy of patients with sitting problems.
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Peso Corporal , Postura , Transferência de Experiência , Adulto , Fenômenos Biomecânicos , Humanos , Cinética , MasculinoRESUMO
We studied the effects of dextran, dextrin, and disintegrants on the chemical stability of Opalmon tablets containing Limaprost-alfadex (Limaprost/alpha-cyclodextrin complex) and found that the addition of dextran or dextrin significantly improved the chemical stability of Opalmon tablets under high humidity, compared to lactose. We also examined how dextran stabilizes Limaprost in Opalmon tablets and studied the formulation of Opalmon tablets in order to achieve higher chemical stability, rapid dissolution and reduced stickiness. The results suggested that dextran increases stabilization after moisture adsorption by decreasing the dissociation of Limaprost-alfadex to the free drug and alpha-cyclodextrin in the dextran matrix, when compared with the lactose matrix. The stickiness of Opalmon tablets containing dextran and dextrin was negligible when dextran and dextrin amounted to less than 20% of the formulation. By selecting a proper disintegrant, we obtained Opalmon tablets with higher chemical stability and rapid dissolution properties.
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Alprostadil/análogos & derivados , Desintegrinas/farmacocinética , Polissacarídeos/farmacocinética , alfa-Ciclodextrinas/farmacocinética , Alprostadil/química , Alprostadil/farmacocinética , Dextranos/química , Dextranos/farmacocinética , Dextrinas/química , Dextrinas/farmacocinética , Desintegrinas/química , Excipientes , Umidade , Estrutura Molecular , Solubilidade , Comprimidos , alfa-Ciclodextrinas/químicaRESUMO
In stability studies on moisture-resistant Opalmon tablets in press-through-packages (PTP), which were placed in aluminum bags, we found that the degradation rate of the dextran formulation is faster than that of the lactose formulation. The fast degradation of the dextran formulation is attributed to residual moisture in the package because drying the tablets before packaging suppressed the degradation and there is a good correlation between the stability of the drug and the water-activity of the tablets. Therefore, we developed a new drying method for the tablets, i.e. the rotary vacuum drying method, and investigated the effects of the operating conditions such as heating temperature, rotation speed, and vacuum degree on the drying time, and the appearance of the tablets. Using the rotary vacuum drying method, the tablets were dried over a short time (30 min) on a mass production scale so that the water activity was less than 0.03. Furthermore, the tablets suffered negligible damage such as breaking and chipping during the drying process. These results indicate that the rotary vacuum drying method is useful for drying tablets on mass production scales.
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Comprimidos/química , Dextranos/química , Estabilidade de Medicamentos , Temperatura Alta , UmidadeRESUMO
The purpose of this study was to describe a rolling motion, which is common in normal adults and patients with motor disorder, and to try to understand the mechanism of the motion. Ten healthy young adults participated in the experiment and were requested to roll from supine to side-lying by pressing the floor with their contra-lateral foot. Their motions in the task were measured with a 3-D analysis system and a force platform. The hip abduction-adduction angle was at around the neutral position and was approximately constant throughout the rolling motion. The hip rotation angle was at a neutral or slightly internally rotated position at the beginning of the motion, and it externally rotated linearly toward the end of the rolling motion. These patterns were thought to be mechanically the most effective for the subjects to perform the motion as was also indicated by the kinetic analysis.