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Background/Aims@#Tegoprazan, a novel potassium-competitive acid blocker, is expected to overcome the limitations of proton pump inhibitors and effectively control nocturnal acid breakthrough. To evaluate the pharmacodynamics of tegoprazan versus dexlansoprazole regarding nocturnal acid breakthrough in healthy subjects. @*Methods@#In a randomized, open-label, single-dose, balanced incomplete block crossover study, 24 healthy male volunteers were enrolled and randomized to receive oral tegoprazan (50, 100, or 200 mg) or dexlansoprazole (60 mg) during each of two administration periods, separated by a 7- to 10-day washout period. Blood samples were collected for pharmacokinetic parameter analysis; gastric monitoring was performed for pharmacodynamic parameter evaluation. @*Results@#All 24 subjects completed the study. Average maximum plasma concentration, area under the plasma concentration–time curve, and mean time with gastric pH >4 and pH >6 for tegoprazan demonstrated dose-dependent incremental increases. All the tegoprazan groups reached mean pH ≥4 within 2 hours, whereas the dexlansoprazole group required 7 hours after drug administration. Based on pharmacodynamic parameters up to 12 hours after evening dosing, 50, 100, and 200 mg of tegoprazan presented a stronger acid-suppressive effect than 60 mg of dexlansoprazole. Moreover, the dexlansoprazole group presented a comparable acid-suppressive effect with the tegoprazan groups 12 hours after dosing. @*Conclusions@#All the tegoprazan groups demonstrated a significantly faster onset of gastric pH increase and longer holding times above pH >4 and pH >6 up to 12 hours after evening dosing than the dexlansoprazole group.
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Ibandronate (a bisphosphonate) is commonly used as an treatment of osteoporosis in combination with vitamin D. Monthly DP-R206-a novel, fixed-dose combination tablet (150 mg ibandronate/24,000 IU vitamin D3)-was recently developed to enhance patient compliance. This open, randomized, two-period crossover study was conducted to compare the pharmacokinetics of ibandronate when administered as DP-R206 or 150 mg ibandronate to healthy adult volunteers. Each volunteer was randomly allocated to receive single-dose DP-R206 or ibandronate with a 28-day washout period between treatments. Blood samples were assessed using pharmacokinetic analysis. Plasma ibandronate concentrations were determined using liquid chromatography-tandem mass spectrometry. Safety and tolerability assessments were performed throughout the study. In total, 103 participants received the study drugs and 72 participants completed the study. The geometric mean ratios (DP-R206/ibandronate) of the maximum concentration (C(max)) and the area under the plasma concentration time curve from time zero to the last concentration (AUC(last)) values were 0.959 (90% CI: 0.820-1.120) and 0.924 (90% CI: 0.805-1.060), respectively. The frequencies of adverse events (AEs) and drug reactions were similar between treatment groups, and all AEs were recovered without sequalae. Ibandronate pharmacokinetics, tolerability, and safety are comparable when administered to healthy individuals, regardless if administered as DP-R206 or ibandronate.
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Adulto , Humanos , Estudos Cross-Over , Espectrometria de Massas , Osteoporose , Cooperação do Paciente , Farmacocinética , Plasma , Vitamina D , Vitaminas , VoluntáriosRESUMO
BACKGROUND: This clinical study was conducted to compare pharmacokinetics of eperisone and aceclofenac of HCP1104, a new fixed dose combination drug with those in co-administration of eperisone 50 mg and aceclofenac 100 mg. The study used a partial replicated study design to characterize intra-subject variability of eperisone when co-administrated with aceclofenac. METHODS: A partial replicated crossover design was employed in 30 subjects. Each subject received a single dose of co-administration of eperisone 50 mg and aceclofenac 100 mg on two occasions and a single dose of 1 capsule of HCP1104. Blood samples were obtained for 24 hrs after dosing, and plasma was assayed for eperisone and aceclofenac by Liquid chromatography-electrospray ionization-mass spectrometry. RESULTS: Using an average bioequivalence criterion, the 90 % confidence limits for Ln-transformed Cmax and AUClast for aceclofenac fell wihin the acceptable range of 80 - 125 %. Point estimates of eperisone AUClast and Cmax were 1.0152 and 1.0490, respectively and the 90 % confidence interval for Cmax was 0.8499 - 1.3025. The within-subject coefficient of variation of Cmax for the reference was 50.198 %. Acceptance range for eperisone Cmax based on new bioequivalence guidance for highly variable drugs was extended to 0.6984 - 1.4319. CONCLUSION: The extent of exposure and rate of absorption of both eperisone and aceclofenac with a single dose of HCP1104 capsule were equivalent to those with co-administration of a marketed eperisone 50 mg tablet and a marketed aceclofenac 100 mg tablet under fasting conditions in healthy adult males.
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Adulto , Humanos , Masculino , Absorção , Estudos Cross-Over , Jejum , Farmacocinética , Plasma , Análise Espectral , Equivalência TerapêuticaRESUMO
BACKGROUND: Bivalirudin is a direct thrombin inhibitor for patients with unstable angina undergoing percutaneous coronary intervention. METHODS: A sensitive liquid chromatography-tandem mass spectrometry (LC/MS/MS) method was developed and validated for the determination of bivalirudin, in human plasma using nafarelin as internal standard (IS). Chromatographic separation was performed using a Shiseido MG3 mm column (2.0 x 50 mm) with a gradient mobile phase consisting of water and acetonitrile containing 0.1 % formic acid at a flow rate of 0.4 mL/min, and total run time was within 5 min. Detection and quantification was performed by the mass spectrometer using a multiple reaction-monitoring mode at m/z 1091.0 --> 650.3 for bivalirudin, and m/z 662.1 --> 249.3 for IS. RESULTS: The assay was linear over a concentration range of 10 - 10000 ng/mL with a lower limit of quantification of 10 ng/mL in human plasma. CONCLUSION: This method was successfully applied for pharmacokinetics study after intravenous administration of bivalirudin to healthy Korean male volunteers.
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Humanos , Masculino , Administração Intravenosa , Angina Instável , Cromatografia Líquida , Espectrometria de Massas , Métodos , Nafarelina , Intervenção Coronária Percutânea , Farmacocinética , Plasma , Trombina , ÁguaRESUMO
BACKGROUND: Amlodipine is a third-generation dihydropyridine calcium channel blocker for treating hypertension. Though marketed primarily as a besylate salt, there have been some efforts to find other comparable salts. Among them, maleate is the salt that has been considered favorable for many drugs. The aim of this study was to compare the pharmacokinetics, as well as safety and tolerability of amlodipine maleate with amlodipine besylate. METHODS: This study was open, randomized, two-period crossover design investigated in twelve healthy male volunteers over a 144 h period after administrating two forms of amlodipine 5 mg, respectively. Each period was separated with 2 weeks. Plasma concentrations of amlodipine were determined by liquid chromatography-tandem mass spectrometry. Safety profiles were assessed by vital signs, physical examinations, electrocardiograms, laboratory testing and adverse events monitoring. RESULTS: All subjects were completed this study. Geometric mean ratios (GMRs) of amlodipine maleate/amlodipine besylate of Cmax and AUClast for amlodipine were 0.92 (90 % confidence interval, 0.81 ~ 1.05) and 1.05 (0.96 ~ 1.16), respectively. No serious adverse events were reported, and no clinically relevant changes were observed in safety profiles during this trial. CONCLUSION: Pharmacokinetics, tolerability and the safety were comparable between amlodipine maleate and amlodipine besylate in healthy individuals.
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Humanos , Masculino , Anlodipino , Canais de Cálcio , Estudos Cross-Over , Di-Hidropiridinas , Eletrocardiografia , Ácido gama-Aminobutírico , Hipertensão , Maleatos , Espectrometria de Massas , Exame Físico , Plasma , Sais , Sinais VitaisRESUMO
Axillary osmidrosis is caused by excessive secretion of apocrine sweat gland and can cause extreme difficulty in social activities. The surgical removal of apocrine glands has been thought as an effective method. But this classical treatment results in many complications such as scarring, hematoma, skin necrosis and these complications have not been solved yet. Recently radiofrequency surgery as a minimally invasive technique is used for the treatment of snoring, benign prostate hypertrophy, hepatoma, reduction of masseter muscle and gastrocnemius muscle. From June, 2004 to March, 2005, 10 patients with axillary osmidrosis were treated by radiofrequency thermal ablation(PMC-1000). The generator was set to level 6-8 and the duration of time was 1.0 seconds. The maximum number of treatment sessions were two. The mean postoperative follow-up period was about average 6 month ranged from 2 to 9 month. The skin necrosis was developed in 2 patients. All patients were satisfied or partially satisfied with the results. Although suitable radiofrequency power and heating duration have not been defined yet, which is mandatory in order to obtain the best results, the radiofrequecy could be a safe and effective treatment modality for axillary osmidrosis with a good clinical outcome and few complications.
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Humanos , Glândulas Apócrinas , Carcinoma Hepatocelular , Cicatriz , Seguimentos , Calefação , Hematoma , Temperatura Alta , Hipertrofia , Músculo Masseter , Músculo Esquelético , Necrose , Próstata , Pele , Ronco , Glândulas SudoríparasRESUMO
Craniosynostosis refers to the premature fusion of single or multiple sutures of the cranial base or vault. It causes restriction of cranium and brain growth and variable morphologic deformity. Inadequate intracranial volume for rapid brain growth brings about increased intracranial pressure and functional impairment. To solve this problem, the key is the surgical decompression and insurance of adequate intracranial volume. Traditional surgical approach is frontal advancement with cranial vault remodeling, but has drawbacks such as invasiveness, long operation time, large amount of hemorrhage, difficult postoperative care, and frequent complications. Recently, distraction osteogenesis is used for the treatment of craniosynostosis. So, we compared cranial distraction osteogenesis with traditional cranioplasty about merits and drawbacks and present the effectiveness of cranial distraction osteogenesis. In a comparative study of cranioplasty and distraction osteogenesis, clinical documents and pre/ postoperative X-ray and CT scans of 12 brachycephaly patients were reviewed. From April, 1994 to October, 2001, 8 patients were treated with traditional cranioplasty and 4 patients were treated with distraction osteogenesis. We achieved not only an increase in intracranial volume but also merits such as a reduction in operation time and bleeding, easy postoperative care and low complication rate with distraction osteogenesis.
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Humanos , Encéfalo , Anormalidades Congênitas , Craniossinostoses , Descompressão Cirúrgica , Hemorragia , Seguro , Pressão Intracraniana , Osteogênese por Distração , Cuidados Pós-Operatórios , Crânio , Base do Crânio , Suturas , Tomografia Computadorizada por Raios XRESUMO
There are several factors to be considered while performing reduction mammoplasty in patients having giant breast with severe breast ptosis. These are degrees of breast ptosis, location of newly created nipple areolar complex, preservation of sensation, symmetry of both breasts, amount of breast tissues to be resected, and finally the postoperative scar. Among the above factors, postoperative scar seems to be the major problem that patients complain about. So several methods have been investigated in time to minimize the scar. Authors have performed 3cases of reduction mammoplasty in patients with severe ptotic large breast by applying the method of umbilicus creation in abdominoplasty, so that only periareolar and submammary scars remained without a vertical scar. The age were between 33 and 43 years old. Mean follow up period was about 6.5 months. Amount of the resected mammary tissues was about 750-1350g. Periareolar deepithelialization was made about 8cm diameter for better cirulation to the nipple areolar complex and wider contact area thus enhancing the stabilization and survival of the nipple areolar complex. Only 1 case with partial deepithelialization of the areola occurred but completely healed within 1 month. Patients were pleased with natural shape and size of the breast and the sensation of the nipple areolar complex was restored completely in all cases after surgery. Authors have performed reduction mammoplasty without leaving the vertical scar which considered to be the major problems of the classical methods. Other problems such as insufficient reduction, flattening of the breast and severe wrinkles around the nipple were also solved. This method not only improve the aesthetic importance but also minimize the functional complications such as sensory loss and difficulty in lactation.
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Adulto , Feminino , Humanos , Abdominoplastia , Mama , Cicatriz , Seguimentos , Lactação , Mamoplastia , Mamilos , Sensação , UmbigoRESUMO
The importance of dressing in the territory of plastic surgery has been greatly emphasized. Especially the tie-over dressing method is very effective method which has been widely used in the areas of skin graft, and after subcutaneous shaving for osmidrosis. However, the present tie-over dressing method, using cotton balls or gauze, is poses several problems. The damp areas produced by insufficient absorption of exudate, inappropriate and uneven pressure, and excessive pressure become susceptible to infection, conclusively leading to the decreased success rate. For the last three years, we have been using the sponge, replacing the cotton balls or gauze, in total 248 cases for compressive dressing of skin graft, conchal cartilage graft, dermofat graft and subcutaneous shaving of the osmidrosis. We conclude this new method has many benefits as well as the solutions to the problems of using cotton balls or gauze.
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Absorção , Bandagens , Cartilagem , Exsudatos e Transudatos , Poríferos , Pele , Cirurgia Plástica , TransplantesRESUMO
Neurofibromatosis is a syndrome of multiple neurofibromas, abnormal skin pigmentation and certain bony abnormalities. Sometimes the growth of plexiform neurofibromatosis on the face or trunk is centripetal and usually involves the mediastinum and skull base. However, it is very rare that neurofibromatosis involves the trigeminal ganglion. Its encroachment around the foramina of the skull base may induce facial palsy or conductive hearing loss. The guiding principle in the treatment of generalized neurofibromatosis is a radical excision with preservation of vital structures and an immediate reconstruction of the bony skeleton and soft tissue defect. The authors experienced 4 cases of neurofibromatosis involving the trigeminal ganglion. All had trigeminal symptoms for 3 to 4 years. These were severe headache and intractable trigeminal neuralgia. Tumors in all 4 cases were spread in the centripetal type from extracranial neurofibromatosis. The facial nerve was affected in 4 cases. Malignat Schwannoma occurred in 1 case. Accurate diagnosis and assessments were necessary with CT, MRI art oomputer-aided simulation design. Intraoperative bleeding was minimal with hypotensive anesthesia. Surgical approach to the middle cranial fossa involved temporary removal of the zygomatic arch and TMJ disarticulation with downward traction of the mandible. Satisfactory results have been obtained far 3 to 7 years(mean 5 years) follow-up.
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Anestesia , Fossa Craniana Média , Diagnóstico , Desarticulação , Nervo Facial , Paralisia Facial , Seguimentos , Cefaleia , Perda Auditiva Condutiva , Hemorragia , Imageamento por Ressonância Magnética , Mandíbula , Mediastino , Neurilemoma , Neurofibromatoses , Neurofibromatose 1 , Esqueleto , Pigmentação da Pele , Base do Crânio , Articulação Temporomandibular , Tração , Gânglio Trigeminal , Neuralgia do Trigêmeo , ZigomaRESUMO
Because deep forehead wrinkle is considered of concept against beauty, many considerations and trials to solve the problem has been done. Furthermore severely exaggerated forehead wrinkle that is accentuated with upward gaze, especially of younger persons is tremendous handicap socially and psychologically. In the persons with blepharoptosis, forehead wrinkle is created because of the compensatory action of frontalis muscle for the additional lift of inferiorly malpositioned upper eyelid. We experienced twenty three patients from February 1993 to April 1996. the average age of the patients was 22.5 years (range 15 to 34 years). There were 4 unilateral and 19 bilateral cases. Preoperative measurement of ptotic amount, levator function by Berke's method, and Margin limbal distance (MLD) were 2.1mm, 10.2mm, and 2.2mm respectively. And postoperative measurement of there were not ptotic, 14.2, and 6.2mm. We followed up 18 months in the mean. Most of the patients were corresponding to mild and borderline ptosis. We operated all the patients under the local anesthesia, which enable us to use the adjustable suture technique and overcome the pitfall of formular prediction. Simultaneously at the end of the procedure, double eyelid operations were done in the cases of oriental eye lid. As a results, correction of blepharoptosis, repositioning of abnormally elevated eyebrow, disappearance of forehead wrinkle, improvement of vision, and acquisition of adequate eyelid functionally and aesthetically were possible. On the other hand, we confronted 7 cases of mild complication. These were as follows ; transient lagophthalmost (4 cases), overcorrection(1 cases), unfercorrection(1 case), and asymmetry(1 case). Lagophthalmos was improved spontaneously after several months. We achieved satisfactory result using levator shortening without significant side effects and complications. This method is of great worth for the spontaneous resolution of the forehead wrinkle with undertectable blepharoptosis.
