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1.
Sci Rep ; 14(1): 8004, 2024 04 05.
Article in English | MEDLINE | ID: mdl-38580737

ABSTRACT

Pelvic fractures pose significant challenges in medical diagnosis due to the complex structure of the pelvic bones. Timely diagnosis of pelvic fractures is critical to reduce complications and mortality rates. While computed tomography (CT) is highly accurate in detecting pelvic fractures, the initial diagnostic procedure usually involves pelvic X-rays (PXR). In recent years, many deep learning-based methods have been developed utilizing ImageNet-based transfer learning for diagnosing hip and pelvic fractures. However, the ImageNet dataset contains natural RGB images which are different than PXR. In this study, we proposed a two-step transfer learning approach that improved the diagnosis of pelvic fractures in PXR images. The first step involved training a deep convolutional neural network (DCNN) using synthesized PXR images derived from 3D-CT by digitally reconstructed radiographs (DRR). In the second step, the classification layers of the DCNN were fine-tuned using acquired PXR images. The performance of the proposed method was compared with the conventional ImageNet-based transfer learning method. Experimental results demonstrated that the proposed DRR-based method, using 20 synthesized PXR images for each CT, achieved superior performance with the area under the receiver operating characteristic curves (AUROCs) of 0.9327 and 0.8014 for visible and invisible fractures, respectively. The ImageNet-based method yields AUROCs of 0.8908 and 0.7308 for visible and invisible fractures, respectively.


Subject(s)
Fractures, Bone , Neural Networks, Computer , Humans , X-Rays , Fractures, Bone/diagnostic imaging , Radiography , Tomography, X-Ray Computed/methods
2.
Surg Today ; 2024 Mar 04.
Article in English | MEDLINE | ID: mdl-38436719

ABSTRACT

PURPOSE: This study examined the impact of frailty and prefrailty on mid-term outcomes and rehabilitation courses after cardiac surgery. METHODS: A total of 261 patients (median age: 73 years; 30% female) who underwent elective cardiac surgery were enrolled in this study. The Japanese version of the Cardiovascular Health Study Frailty Index classified 86, 131, and 44 patients into frailty, prefrailty, and robust groups, respectively. We examined the recovery of walking ability, outcomes at discharge, mid-term all-cause mortality, and rehospitalization related to major adverse cardiovascular and cerebrovascular events (MACCE) across the three cohorts. RESULTS: The 3-year survival rates in the frailty, prefrailty, and robust groups were 87%, 97%, and 100%, respectively (p = 0.003). The free event rates of all-cause mortality and re-hospitalization related to MACCE were 59%, 79%, and 95%, respectively (p < 0.001), with a graded elevation in adjusted morbidity among patients in the prefrailty (hazard ratio [HR], 4.57; 95% confidence interval [CI], 1.08-19.4) and frailty (HR, 9.29; 95% CI 2.21-39.1) groups. Patients with frailty also experienced a delayed recovery of walking ability and a reduced number of patients with frailty were discharged home. CONCLUSION: Frailty and prefrailty adversely affect the mid-term prognosis and rehabilitation course after cardiac surgery.

3.
Hosp Top ; 101(1): 9-15, 2023.
Article in English | MEDLINE | ID: mdl-34592913

ABSTRACT

This study investigated nurses' and patients' perceptions of hospital room environment and patient pajama design. Nurses working in a Japanese university hospital and patients aged 20 and older were surveyed. Over 75% of patients rated the hospital environment and hospital rooms as "very good" or "good," but less than one in three nurses rated them similarly. Patients were more likely than nurses to rate rental pajamas as "very good" or "good." Contrary to the nurses, only about one in four patients valued wearing well-designed pajamas. Nurses' and patients' perceptions differed regarding hospital pajamas, but not about improving hospital rooms.


Subject(s)
Clothing , Hospitals, General , Nursing Staff, Hospital , Humans , Attitude of Health Personnel , Hospitals, University , Surveys and Questionnaires , Japan , Patient Satisfaction
4.
J Clin Med ; 11(21)2022 Nov 04.
Article in English | MEDLINE | ID: mdl-36362775

ABSTRACT

Assisted reproductive technology (ART) has progressed rapidly, resulting in a great improvement in the clinical pregnancy ratio. When applying the protocol of piezo intracytoplasmic sperm injection (Piezo-ICSI), it is very important to puncture the zona pellucida and the oocyte cytoplasmic membrane without rupturing the oocyte cytoplasmic membrane. Previous studies have shown that the poor extensibility of the oocyte cytoplasmic membrane might be closely related to rupture. However, no consensus has been reached regarding how the quality of the oocyte for extensible ability or rupture possibility affects the surfaces of the oocyte on the microscopic frames. We conducted this study to provide evidence that artificial intelligence (AI) techniques are superior for predicting the tendency of oocyte rupture before puncturing on Piezo-ICSI. To inspect it, we provided a retrospective trial of 38 rupture oocytes and 55 nonruptured oocytes. This study marked the highest accuracy of 91.4% for predicting oocytes rupture using the support-vector machine method of machine learning. We conclude that AI technologies might serve an important role and provide a significant benefit to ART.

5.
Healthcare (Basel) ; 10(2)2022 Feb 16.
Article in English | MEDLINE | ID: mdl-35206991

ABSTRACT

It has recently been shown that the aging population is refractory to the maintenance of swallowing function, which can seriously affect quality of life. Singing and vocal training contribute to mastication, swallowing and respiratory function. Previous studies have shown that singers have better vocal cord health. No consensus has been reached as to how vocal training affects swallowing ability. Our study was designed to establish evidence that singers are statistically superior at inducing the swallowing reflex. To test our hypothesis, we undertook a clinical trial on 55 singers and 141 non-singers (mean age: 60.1 ± 11.7 years). This cross-sectional study with propensity score matching resulted in significant differences in a repetitive saliva swallowing test among singers: 7.1 ± 2.4, n = 53 vs. non-singers: 5.9 ± 1.9, n = 53, p < 0.05. We conclude that singing can serve an important role in stabilizing the impact of voluntary swallowing on speech.

6.
Dement Geriatr Cogn Disord ; 50(6): 554-558, 2021.
Article in English | MEDLINE | ID: mdl-34937029

ABSTRACT

INTRODUCTION: Postinspiratory activity, which is essential for laryngeal closure during swallowing to prevent aspiration of food into the airways, is reduced in a mouse model of tauopathy. Therefore, we hypothesized that patients at the stage of mild cognitive impairment (MCI) exhibit alterations in swallowing dynamics and coordination between swallowing and breathing. METHODS: We examined breathing-swallowing coordination in patients with MCI. Patients who scored ≥24 on the Mini-Mental State Examination and <26 on the Japanese version of the Montreal Cognitive Assessment were recruited at Sumoto Itsuki Hospital. Parameters associated with breathing-swallowing coordination were assessed using a combination of two sensors: a respiratory flow sensor and a piezoelectric sensor attached to the skin surface of the anterior neck. RESULTS: Nineteen patients met the criteria for MCI; 16 of these patients (79.5 ± 9.1 years old) scored <3 on the 10-item Eating Assessment Tool and were enrolled in the study. Their data were compared with those of an age-matched elderly cohort (79.9 ± 2.9 years old). The frequencies of swallowing during inspiration and swallowing immediately followed by inspiration in patients with MCI were 6.9% and 9.6%, respectively; these frequencies were not significantly different from those of the age-matched elderly cohort. However, the timing of swallowing in the respiratory cycle was significantly delayed in the MCI patients, and both time from the onset to the peak of laryngeal elevation and the duration between the onset of rapid laryngeal elevation and the time when the larynx returned to the resting position were significantly lengthened in this group. CONCLUSION: At the stage of MCI, breathing-swallowing coordination has already started to decline.


Subject(s)
Cognitive Dysfunction , Larynx , Aged , Animals , Deglutition , Humans , Mice , Respiration
7.
Sci Rep ; 11(1): 11716, 2021 06 03.
Article in English | MEDLINE | ID: mdl-34083655

ABSTRACT

Pelvic fracture is one of the leading causes of death in the elderly, carrying a high risk of death within 1 year of fracture. This study proposes an automated method to detect pelvic fractures on 3-dimensional computed tomography (3D-CT). Deep convolutional neural networks (DCNNs) have been used for lesion detection on 2D and 3D medical images. However, training a DCNN directly using 3D images is complicated, computationally costly, and requires large amounts of training data. We propose a method that evaluates multiple, 2D, real-time object detection systems (YOLOv3 models) in parallel, in which each YOLOv3 model is trained using differently orientated 2D slab images reconstructed from 3D-CT. We assume that an appropriate reconstruction orientation would exist to optimally characterize image features of bone fractures on 3D-CT. Multiple YOLOv3 models in parallel detect 2D fracture candidates in different orientations simultaneously. The 3D fracture region is then obtained by integrating the 2D fracture candidates. The proposed method was validated in 93 subjects with bone fractures. Area under the curve (AUC) was 0.824, with 0.805 recall and 0.907 precision. The AUC with a single orientation was 0.652. This method was then applied to 112 subjects without bone fractures to evaluate over-detection. The proposed method successfully detected no bone fractures in all except 4 non-fracture subjects (96.4%).


Subject(s)
Deep Learning , Fractures, Bone/diagnosis , Imaging, Three-Dimensional , Neural Networks, Computer , Pelvic Bones/diagnostic imaging , Pelvic Bones/pathology , Tomography, X-Ray Computed , Adult , Aged , Aged, 80 and over , Female , Humans , Image Processing, Computer-Assisted/methods , Imaging, Three-Dimensional/methods , Male , Middle Aged , Models, Theoretical , Reproducibility of Results , Sensitivity and Specificity , Tomography, X-Ray Computed/methods , Young Adult
8.
Tissue Eng Part C Methods ; 27(6): 349-356, 2021 06.
Article in English | MEDLINE | ID: mdl-33906381

ABSTRACT

Correct assessment of the bone healing process is required for the management of limb immobilization during the treatment of bone injuries, including fractures and defects. Although the monitoring of bone healing using ultrasound poses several advantages regarding cost and ionizing radiation exposure compared with other dominant imaging methods, such as radiography and computed tomography (CT), traditional ultrasound B-mode imaging lacks reliability and objectivity. However, the body structures can be quantitatively observed by ultrasound frequency-based methods, and therefore, the disadvantages of B-mode imaging can be overcome. In this study, we created a femoral bone hole model of a rat and observed the bone healing process using the quantitative ultrasound method and micro-CT, which provides a reliable assessment of the tissue microstructure of the bone. This study analyzed the correlation between these two assessments. The results revealed that the quantitative ultrasound measurements correlated with the CT measurements for rat bone healing. This ultrasound frequency-based method could have the potential to serve as a novel modality for quantitative monitoring of bone healing with the advantages of being less invasive and easily accessible. Impact statement Bone healing monitoring with ultrasound is advantageous as it is less invasive and easily accessible; however, the traditional B-mode method lacks reliability and objectivity. This study demonstrated that the proposed ultrasound frequency-based monitoring method can quantitatively observe bone healing and strongly correlates with the computed tomography measurements for rat bone healing. This method has the potential to become a reliable modality for monitoring bone healing.


Subject(s)
Fracture Healing , Fractures, Bone , Animals , Rats , Reproducibility of Results , Tomography, X-Ray Computed , Ultrasonography
9.
Int J Chron Obstruct Pulmon Dis ; 15: 1689-1696, 2020.
Article in English | MEDLINE | ID: mdl-32764914

ABSTRACT

Introduction: Dysphagia is a newly acknowledged multifactorial risk factor for the exacerbation of chronic obstructive pulmonary disease (COPD). Effective screening methods are awaited. We performed a prospective study to evaluate the impact of musculature and breathing-swallowing discoordination on the exacerbation of COPD with a novel swallowing monitor using a piezoelectric sensor. Patients and Methods: This was the second part of a prospective study of patients with COPD from the Iizuka COPD cohort. Seventy patients with stable COPD underwent dysphagia screening, skeletal muscle mass index (SMI) and tongue pressure measurements, and swallowed 3 mL and 30 mL of water while wearing a swallowing monitor. Patients were followed for one year. Results: During the follow-up period, 28 patients experienced exacerbations (E group), and 42 had none (non-E group). There was no significant difference in tongue pressure measurements between the two groups. The SMI in the E group was significantly lower than that in the non-E group. Among the swallowing monitor measurements, the 3 mL I-SW% (the percentage of swallows in which inspiration preceded the swallow [out of ten 3 mL swallows]) was significantly lower in the E group than in the non-E group. Conclusion: Breathing-swallowing coordination is an independent factor related to the exacerbation of COPD. Not only the presence of discoordination but also the inability to produce an airway protection mechanism may contribute to more frequent aspiration and exacerbations.


Subject(s)
Deglutition , Pulmonary Disease, Chronic Obstructive , Humans , Pressure , Prospective Studies , Pulmonary Disease, Chronic Obstructive/diagnosis , Tongue
10.
IEEE Trans Biomed Eng ; 65(11): 2529-2541, 2018 11.
Article in English | MEDLINE | ID: mdl-29993526

ABSTRACT

OBJECTIVE: The aim of this research was to develop a swallowing assessment method to help prevent aspiration pneumonia. The method uses simple sensors to monitor swallowing function during an individual's daily life. METHODS: The key characteristics of our proposed method are as follows. First, we assess swallowing function by using respiratory flow, laryngeal motion, and swallowing sound signals recorded by simple sensors. Second, we classify whether the recorded signals correspond to healthy subjects or patients with dysphagia. Finally, we analyze the recorded signals using both a feature extraction method (linear predictive coding) and a machine learning method (support vector machine). RESULTS: Based on our experimental results for 140 healthy subjects (54.5 32.5 years old) and 52 patients with dysphagia (75.5 20.5 years old), our proposed method could achieve 82.4% sensitivity and 86.0% specificity. CONCLUSION: Although 20% of testing sample sets were erroneously classified, we conclude that our proposed method may facilitate screening examinations of swallowing function. SIGNIFICANCE: In combination with the portable sensors, our proposed method is worth utilizing for noninvasive swallowing assessment.


Subject(s)
Deglutition/physiology , Larynx/physiology , Machine Learning , Monitoring, Physiologic , Respiration , Signal Processing, Computer-Assisted , Adult , Aged , Aged, 80 and over , Deglutition Disorders/diagnosis , Deglutition Disorders/physiopathology , Female , Humans , Male , Middle Aged , Monitoring, Physiologic/instrumentation , Monitoring, Physiologic/methods , Young Adult
11.
Front Physiol ; 8: 676, 2017.
Article in English | MEDLINE | ID: mdl-28970804

ABSTRACT

Rationale: Swallowing during inspiration and swallowing immediately followed by inspiration increase the chances of aspiration and may cause disease exacerbation. However, the mechanisms by which such breathing-swallowing discoordination occurs are not well-understood. Objectives: We hypothesized that breathing-swallowing discoordination occurs when the timing of the swallow in the respiratory cycle is inappropriate. To test this hypothesis, we monitored respiration and swallowing activity in healthy subjects and in patients with dysphagia using a non-invasive swallowing monitoring system. Measurements and Main Results: The parameters measured included the timing of swallow in the respiratory cycle, swallowing latency (interval between the onset of respiratory pause and the onset of swallow), pause duration (duration of respiratory pause for swallowing), and the breathing-swallowing coordination pattern. We classified swallows that closely follow inspiration (I) as I-SW, whereas those that precede I as SW-I pattern. Patients with dysphagia had prolonged swallowing latency and pause duration, and tended to have I-SW or SW-I patterns reflecting breathing-swallows discoordination. Conclusions: We conclude that swallows at inappropriate timing in the respiratory cycle cause breathing-swallowing discoordination, and the prolongation of swallowing latency leads to delayed timing of the swallow, and results in an increase in the SW-I pattern in patients with dysphagia.

12.
BMJ Open Respir Res ; 4(1): e000202, 2017.
Article in English | MEDLINE | ID: mdl-28883930

ABSTRACT

INTRODUCTION: Impaired coordination between breathing and swallowing (breathing-swallowing discoordination) may be a significant risk factor for the exacerbation of chronic obstructive pulmonary disease (COPD). We examined breathing-swallowing discoordination in patients with COPD using a non-invasive and quantitative technique and determined its association with COPD exacerbation. METHODS: We recruited 65 stable outpatients with COPD who were enrolled in our prospective observational cohort study and did not manifest an apparent swallowing disorder. COPD exacerbation was monitored for 1 year before and 1 year after recruitment. Swallowing during inspiration (the I-SW pattern) and swallowing immediately followed by inspiration (the SW-I pattern) were identified. RESULTS: The mean frequency of the I-SW and/or SW-I patterns (I-SW/SW-I rate) was 21.5%±25.5%. During the 2-year observation period, 48 exacerbation incidents (25 patients) were identified. The I-SW/SW-I rate was significantly associated with the frequency of exacerbation. During the year following recruitment, patients with a higher I-SW/SW-I frequency using thicker test foods exhibited a significantly higher probability of future exacerbations (p=0.002, log-rank test). CONCLUSIONS: Breathing-swallowing discoordination is strongly associated with frequent exacerbations of COPD. Strategies that identify and improve breathing-swallowing coordination may be a new therapeutic treatment for patients with COPD.

13.
Med Biol Eng Comput ; 55(6): 1001-1017, 2017 Jun.
Article in English | MEDLINE | ID: mdl-27665103

ABSTRACT

The assessment of swallowing function is important for the prevention of aspiration pneumonia. We developed a new swallowing monitoring system that uses respiratory flow, swallowing sound, and laryngeal motion. We applied this device to 11 healthy volunteers and 10 patients with dysphagia. Videofluoroscopy (VF) was conducted simultaneously with swallowing monitoring using our device. We measured laryngeal rising time (LRT), the time required for the larynx to elevate to the highest position, and laryngeal activation duration (LAD), the duration between the onset of rapid laryngeal elevation and the time when the larynx returned to the lowest position. In addition, we evaluated the coordination between swallowing and breathing. We found that LAD was correlated with a VF-derived parameter, pharyngeal response duration (PRD) in healthy subjects (LAD: 959 ± 259 ms vs. PRD: 1062 ± 149 ms, r = 0.60); however, this correlation was not found in the dysphagia patients. LRT was significantly prolonged in patients (healthy subjects: 320 ± 175 ms vs. PATIENTS: 465 ± 295 ms, P < 0.001, t test). Furthermore, frequency of swallowing immediately after inspiration was significantly increased in patients. Therefore, the new device may facilitate the assessment of some aspects of swallowing dysfunction.


Subject(s)
Deglutition Disorders/physiopathology , Deglutition/physiology , Larynx/physiology , Pharynx/physiology , Pulmonary Ventilation/physiology , Adult , Aged , Case-Control Studies , Female , Humans , Male , Motion , Respiration , Sound
14.
Magn Reson Med Sci ; 15(2): 212-9, 2016.
Article in English | MEDLINE | ID: mdl-26607809

ABSTRACT

PURPOSE: To evaluate morphological and signal intensity (SI) changes of placental insufficiency on magnetic resonance imaging (MRI) and to assess morphological changes and decreased flow voids (FVs) on T2-weighted rapid acquisition with relaxation enhancement (RARE) images for diagnosing placental insufficiency. METHODS: Fifty singleton fetuses underwent MRI using a 1.5-T MR scanner. Placental thickness, area, volume, SI, amniotic fluid SI, and size of FVs between the uterus and the placenta were measured on MR images. Two radiologists reviewed T2-weighted RARE images for globular appearance of the placenta and FVs between the uterus and the placenta. Data were analyzed using t-tests, McNemar's tests, and areas under the receiver operating characteristic curve (AUCs) at 5% level of significance. RESULTS: Twenty-five of the 50 pregnancies were categorized as having an insufficient placenta. Significant differences were observed between insufficient and normal placentas in mean placental thickness, area, volume, placenta to amniotic fluid SI ratio, and size of FVs (49.0 mm vs. 36.9 mm, 1.62 × 10(4) mm(2) vs. 2.67 × 10(4) mm(2), 5.13 × 10(5) mm(3) vs. 6.56 × 10(5) mm(3), 0.549 vs. 0.685, and 3.4 mm vs. 4.3 mm, respectively). The sensitivity and accuracy using globular appearance plus decreased FVs were greater than those using decreased FVs (P < 0.01). There was no significant difference among AUCs using globular appearance and decreased FVs, and globular appearance plus decreased FVs. CONCLUSIONS: Placental insufficiency was associated with placental thickness, area, volume, placenta to amniotic fluid SI ratio, and size of FVs. Evaluating FVs on T2-weighted RARE images can be useful for detecting placental insufficiency, particularly in placentas without globular appearance on MR images.


Subject(s)
Fetus/diagnostic imaging , Magnetic Resonance Imaging/methods , Placental Insufficiency/diagnostic imaging , Female , Humans , Pregnancy
15.
Article in English | MEDLINE | ID: mdl-24110121

ABSTRACT

This paper describes noninvasive cellular quantity measurement in Bone Marrow Stromal Cells/ ß-tricalcium phosphate. We attempt to identify cellular quantity with an ultrasonic system. The ultrasonic waves are reflected at boundaries where there is a difference in acoustic impedances of the materials on each side of the boundary. Therefore, we focus on the reflected signal. From the obtained ultrasonic data, we extract two features; amplitude and frequency. Amplitude is obtained from the raw ultrasonic wave, and frequency is calculated from frequency spectrum obtained by applying cross-spectrum method. Therefore, we suggest the superiority of frequency to analyze Bone Marrow Stromal Cells. This study shows the ability of intervention to produce the desired beneficial effect.


Subject(s)
Calcium Phosphates/chemistry , Mesenchymal Stem Cells/cytology , Animals , Bone Marrow Cells/cytology , Bone Marrow Cells/metabolism , Mesenchymal Stem Cells/metabolism , Rats, Sprague-Dawley , Reproducibility of Results , Tissue Engineering/methods , Ultrasonics/instrumentation , Ultrasonics/methods
16.
Yakugaku Zasshi ; 131(4): 629-34, 2011 Apr.
Article in Japanese | MEDLINE | ID: mdl-21467803

ABSTRACT

After solid dispersion systems of probucol-polyvinylpyrrolidone K30 (1 : 9 in weight ratio) were exposed to light (10000 lx) for 7 days, 84% of the probucol remained. Commercial probucol fine granules were thus fairly stable under light exposure. When solid dispersion systems were stored in heat-sealed packages at relative humidity (R.H.) of 75% and 92% for 30 days at 30°C, the weight of the samples increased by 22% and 43%, respectively. When these solid dispersion systems were dissolved in water, the probucol concentration decreased with the duration of storage. The crystalline nature of probucol in the solid dispersion systems could not be detected by powder X-ray diffraction or differential scanning calorimetry. After passing the dissolution medium through the membrane filter, retention time of the residue on the filter in the HPLC method corresponded to that of probucol. These results suggest that the partial crystallization of probucol in the solid dispersion systems may occur during storage under these conditions. Solid dispersion systems in heat-sealed packages were fairly stable when stored under room conditions or in light-resistant tightly sealed containers for 5 months.


Subject(s)
Povidone , Probucol , Calorimetry , Chromatography, High Pressure Liquid/methods , Crystallization , Dosage Forms , Drug Packaging , Drug Stability , Drug Storage , Humidity , Light/adverse effects , Povidone/radiation effects , Probucol/radiation effects , Solubility , Temperature , Time Factors , Water , X-Ray Diffraction
17.
Biol Pharm Bull ; 32(11): 1880-4, 2009 Nov.
Article in English | MEDLINE | ID: mdl-19881302

ABSTRACT

Disks of probucol and solid dispersion systems of probucol-polyvinylpyrrolidone (PVP) in various weight ratios were prepared. Dissolution of probucol was markedly increased in the solid dispersion systems in J.P. XV disintegration media No. 1 (pH 1.2) and No. 2 (pH 6.8). The concentrations of probucol after the dissolution of the disks of solid dispersion systems showed supersaturation. Following the administration of disks of solid dispersion systems in rabbits, a marked increase in the area under the plasma concentration time curve (AUC) was observed. When the weight ratio of PVP to probucol was larger, a larger AUC was observed. When disks of the 1 : 9 solid dispersion system (weight ratio of probucol : PVP=1 : 9) containing 50 and 100 mg probucol were respectively administered, AUC values were approximately proportional to the dose. AUC values following the administration of disks of the 1 : 9 solid dispersion systems containing 15 mg probucol (total weight: 150 mg) and 500 mg probucol were approximately equal. The mean half life (t(1/2)) was 12 h when disks of the 1 : 9 solid dispersion system were administered, whereas the t(1/2) was 35 h when probucol disks were administered. The markedly increased dissolution of probucol in solid dispersion systems resulted in a marked increase in its bioavailability.


Subject(s)
Anticholesteremic Agents/pharmacokinetics , Povidone/administration & dosage , Probucol/pharmacokinetics , Administration, Oral , Animals , Anticholesteremic Agents/administration & dosage , Anticholesteremic Agents/blood , Area Under Curve , Biological Availability , Male , Probucol/administration & dosage , Probucol/blood , Rabbits , Solubility
18.
Chem Pharm Bull (Tokyo) ; 57(2): 167-76, 2009 Feb.
Article in English | MEDLINE | ID: mdl-19182407

ABSTRACT

The Grignard, Wittig, Tebbe, Horner-Emmons, and Reformatsky reactions of the 4-oxoproline esters gave the corresponding 4-alylated or 4-alkylidenated products, respectively. The products were properly treated with bases to cause aromatization, giving 4-substituted pyrrole-2-carboxylic acid esters such as methyl 4-methylpyrrole-2-carboxylate, which is a trail pheromone of Atta texana.


Subject(s)
Pyrrolidonecarboxylic Acid/analogs & derivatives , Pyrrolidonecarboxylic Acid/chemistry , Alkylation , Cyclization , Indicators and Reagents , Magnetic Resonance Spectroscopy , Pheromones/chemistry
19.
Int J Pharm ; 339(1-2): 130-8, 2007 Jul 18.
Article in English | MEDLINE | ID: mdl-17398044

ABSTRACT

We investigated the effect of different dispersion methods on release behavior and efficacy onset following microparticle administration of buserelin acetate (BA) sustained-release injection. In this in vitro release study, the initial dispersion of BA increased with increased stirring speed (p<0.01). Stability of BA was studied over 7 days after BA release. The initial BA release rate was higher (p<0.01) after a 1-min vibration dispersion method (VDM) using a test tube mixer (2000 rpm) compared with the standard dispersion method (SDM) by hand. Without shaking, powder aggregation was observed, and BA release was lower than in either the SDM or VDM methods. In this study using 4-week-old Sprague-Dawley female rats, the initial plasma estrone (E(1)) concentrations were lower (p<0.05) in the VDM method than in the SDM method. Observations by optical microscope and scanning microscope showed no change in microparticle shape or distribution of size induced by SDM, VDM or the ultrasonication dispersion method. These results suggest that different dispersion methods do not change the shape and distribution of microparticle size, but clearly change the BA release rate and the transition in plasma E(1) concentrations that can affect drug efficacy.


Subject(s)
Buserelin/administration & dosage , Estrone/blood , Animals , Buserelin/analysis , Buserelin/chemistry , Chromatography, High Pressure Liquid , Down-Regulation , Female , Gonadotropin-Releasing Hormone/antagonists & inhibitors , Microscopy, Electron, Scanning , Microspheres , Rats , Rats, Sprague-Dawley , Solubility
20.
Biol Pharm Bull ; 25(12): 1614-8, 2002 Dec.
Article in English | MEDLINE | ID: mdl-12499650

ABSTRACT

The pharmacokinetics of ketotifen fumarate (KF) was examined after administration in rabbits through four different routes (intravenous, intranasal, oral and rectal). The time-course of the plasma concentration of KF after intravenous administration (1 mg/kg dose) fitted a two-compartment open model. KF was rapidly absorbed and showed a high plasma concentration within 0.33 h after intranasal administration. The absolute bioavailability of KF after intranasal administration was 66%. After oral administration at a dose of 1 mg/kg, the plasma concentration of KF was below the detection limit of HPLC analysis. Even at 5 mg/kg, the value of the area under the plasma concentration-time curve (AUC) after oral administration of KF was significantly lower than that after intranasal administration of 1 mg/kg. Oral bioavailability was only 8%. The very low bioavailability of KF after oral administration might be due to the first-pass effect in the liver. We also prepared suppositories containing KF (1 mg/kg) for rectal administration in rabbits. After rectal administration, KF was rapidly absorbed and its bioavailability was 34%. These results indicated that the intranasal route appears the most effective for administering KF, and that rectal administration may be superior to oral administration in terms of bioavailability.


Subject(s)
Ketotifen/administration & dosage , Ketotifen/pharmacokinetics , Administration, Intranasal , Administration, Oral , Administration, Rectal , Animals , Area Under Curve , Injections, Intravenous , Ketotifen/blood , Male , Rabbits
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