The results of study showed no significant differences on the stability of eye drop preparation containing vitamin B5 kept in neutral glass bottle and in PE vial. Light and high temperature make impact on the stability of the preparation so it needs to be kept from light in a cool place. With selected formula, the eye drop containing vitamin B5 kept in PE vial has stability at least 12 months at room conditions
Ophthalmic Solutions ; Pantothenic Acid

The most important and widely-prescribed drug for anticoagulation is a vitamin K antagonist such as warfarin although it has several limitations in clinical use. New oral anticoagulants (NOACs) have been developed to overcome these problems. The clinical efficacy and safety of dabigatran, rivaroxaban, and apixaban have been shown to be superior to warfarin through large-scale clinical trials. These NOACs can replace warfarin in significant proportions of patients with non-valvular atrial fibrillation to prevent stroke. Recent management guidelines for atrial fibrillation have already recommended NOACs for stroke prevention instead of warfarin. Future clinical studies should resolve the limitations of NOACs and try to extend their clinical indications.
Anticoagulants ; Atrial Fibrillation ; Benzimidazoles ; beta-Alanine ; Dabigatran ; Humans ; Morpholines ; Pyrazoles ; Pyridones ; Rivaroxaban ; Stroke ; Thiophenes ; Vitamin K ; Warfarin

The effects of carnosine and related compounds (CRCs) including anserine, homocarnosine, histidine, and beta-alanine on monosaccharide autoxidation and H2O2 formation were investigated. The incubation of CRCs with D-glucose, D-glucosamine, and D, L-glyceraldehyde at 37degreeC increased the absorption maxima at 285 nm, 273 nm, and 290 ~ 330 nm, respectively. D, L-glyceraldehyde was the most reactive sugar with CRCs. The presence of copper strongly stimulated the reaction of carnosine and anserine with D-glucose or D-glucosamine. Carnosine and anserine stimulated H2O2 formation from D-glucose autoxidation in a dose-dependent manner in the presence of 10 muM Cu (II). The presence of human serum albumin (HSA) decreased their effect on H2O2 formation. Carnosine and anserine has a biphasic effect on alpha-ketoaldehyde formation from glucose autoxidation. CRCs inhibited glycation of HSA as determined by hydroxymethyl furfural, lysine residue with free epsilon-amino group, and fructosamine assay. These results suggest that CRCs may be protective against diabetic complications by reacting with sugars and protecting glycation of protein.
Absorption ; Anserine ; beta-Alanine ; Carbohydrates ; Carnosine* ; Copper ; Diabetes Complications ; Free Radicals ; Fructosamine ; Furaldehyde ; Glucose ; Histidine ; Humans ; Lysine ; Serum Albumin

Pivotal clinical trials testing the efficacy of new antithrombotics for the prevention of stroke and systemic embolism in patients with atrial fibrillation have been published since the release of the first edition of Korean clinical practice guidelines for primary stroke prevention. From July 2007 to August 2012, 5 clinical studies and update of guidelines in Europe and North America were identified through systematic search. In patients with atrial fibrillation who were unsuitable for warfarin, the combination of clopidogrel and aspirin reduced the risk of stroke at the cost of increased major bleedings as compared to aspirin. In patients with nonvalvular atrial fibrillation and risk factors for stroke, new oral anticoagulants, dabigatran, rivaroxaban and apixaban, were as effective as or more effective than warfarin in preventing stroke or systemic embolism. The risks of major bleeding with novel anticoagulants were similar to or lower than that of warfarin. Particularly, the risk of intracranial bleeding was significantly lower with novel anticoagulants than with warfarin. In this report, we summarized the new evidences and updated our recommendations for primary stroke prevention in patients with atrial fibrillation.
Anticoagulants ; Aspirin ; Atrial Fibrillation ; Benzimidazoles ; beta-Alanine ; Embolism ; Europe ; Hemorrhage ; Humans ; Morpholines ; North America ; Primary Prevention ; Pyrazoles ; Pyridones ; Risk Factors ; Stroke ; Thiophenes ; Ticlopidine ; Warfarin ; Dabigatran ; Rivaroxaban

As an important material in pharmaceutical and chemical industry, β-alanine was mainly produced by chemical methods. L-aspartate-α-decarboxylase could catalyze the α-decarboxylation from L-aspartate to β-alanine. Determinations for specific activities of PanDs from Escherichia coli, Corynebacterium glutamicum and Bacillus subtilis were performed in this study (0.98 U/mg, 7.52 U/mg and 8.4 U/mg respectively). The optimal temperature and pH of PanDs from C. glutamicum and B. subtilis were 65 degrees C, pH 6.5 and 60 degrees C, pH 6.5 respectively. According to our research, PanD from B. subtilis could be more appropriate for industrial application because of the higher activity and thermostability when compared to PanDs from E. coli and C. glutamicum which had been the most studied. We also analyzed and discussed the special post-translation self-cleavage phenomenon and the mechanism based inactivation.
Bacillus subtilis ; enzymology ; Bacterial Proteins ; genetics ; metabolism ; Corynebacterium glutamicum ; enzymology ; Escherichia coli ; enzymology ; Glutamate Decarboxylase ; genetics ; metabolism ; Industrial Microbiology ; Temperature ; beta-Alanine

BACKGROUND AND OBJECTIVES: The prevalence of atrial fibrillation (AF) doubles in the extreme elderly and is higher than in the rest of the population. Warfarin therapy to prevent thromboembolic events secondary to AF is often underutilized and under-prescribed in this subgroup, due to the fear of bleeding and other complications. Newer oral anticoagulants such as rivaroxaban and dabigatran offer alternative therapeutic options for the extreme elderly. We review the clinical trial data of these newer agents in the extreme elderly population. SUBJECTS AND METHODS: The primary literature was identified through PubMed, using the following search terms: anticoagulation, rivaroxaban, dabigatran, warfarin, elderly, AF, bleeding, stroke, and aging. Additional references were identified through the review of references from the articles obtained. We included clinical studies evaluating anticoagulation therapies in AF. Selection emphasis was placed on those evaluating anticoagulation in the elderly population. RESULTS: Dabigatran and rivaroxaban have predictable, dose-proportional pharmacokinetic and pharmacodynamic properties, which make them favorable options for the elderly. Fewer monitoring parameters and drug interactions allow for the greater ease of use. A landmark trial shows that the rate of intracranial hemorrhage with dabigatran is lower in this population compared to warfarin. However, the data is based on a small number of subjects enrolled in the clinical trials. As such, the real-world use of these agents may not replicate the published rates of bleeding and thrombosis in the study populations. CONCLUSION: More research is needed in this area, specifically in this population, before newer agents such as rivaroxaban and dabigatran are widely recommended for use in the extreme elderly patients.
Aged ; Aging ; Anticoagulants ; Atrial Fibrillation ; Benzimidazoles ; beta-Alanine ; Drug Interactions ; Hemorrhage ; Humans ; Intracranial Hemorrhages ; Morpholines ; Prevalence ; Stroke ; Thiophenes ; Thrombosis ; Warfarin ; Dabigatran ; Rivaroxaban

BACKGROUND: The intrathecal (IT) administration of glycine or GABAA receptor antagonist result in a touch evoked allodynia through disinhibition in the spinal cord. Glycine is an inhibitory neurotransmitter that appears to be important in sensory processing in the spinal cord. This study was aimed to evaluate the effect of glycine-related amino acids on antagonizing the effects of IT strychnine (STR) or bicuculline (BIC) when each amino acid was administered in combination with STR or BIC. METHODS: A total of 174 male ICR mice were randomized to receive an IT injection of equimolar dose of glycine, betaine, beta-alanine, or taurine in combination with STR or BIC. Agitation in response to innocuous stimulation with a von Frey filament after IT injection was assessed. The pain index in hot-plate test were observed after it injection. The effect of it muscimol in combination with str or bic were also observed. RESULTS: The allodynia induced by STR was relieved by high dose of glycine or betaine. But, allodynia induced by BIC was not relieved by any amino acid. Whereas the STR-induced thermal hyperalgesia was only relieved by high dose of taurine at 120 min after IT injection, the BIC-induced one was relieved by not only high dose of taurine at 120 min but also low dose of glycine or betaine at 60 min after IT injection. The BIC-induced allodynia and thermal hyperalgesia was relieved by IT muscimol. CONCLUSIONS: This study suggests that IT glycine and related amino acids can reduce the allodynic and hyperalgesic action of STR or BIC in mice.
Amino Acids ; Animals ; beta-Alanine ; Betaine ; Bicuculline ; Dihydroergotamine ; Glycine ; Humans ; Hyperalgesia ; Male ; Mice ; Mice, Inbred ICR ; Muscimol ; Neurotransmitter Agents ; Nitrogen Mustard Compounds ; Spinal Cord ; Strychnine ; Taurine

BACKGROUND: Iron overload is a risk factor affecting all patients with thalassemia intermedia (TI). We aimed to determine whether there is a relationship of serum ferritin (SF) and alanine aminotransferase (ALT) with liver iron concentration (LIC) determined by R2 magnetic resonance imaging (R2-MRI), to estimate the most relevant degree of iron overload and best time to chelate in patients with TI. METHODS: In this cross-sectional study, 119 patients with TI (mean age years) were randomly selected and compared with 120 patients who had a diagnosis of thalassemia major (TM). Correlations of LIC, as determined by R2-MRI, with SF and ALT levels, were assessed in all participants. A P-value < 0.05 was considered statistically significant. RESULTS: SF and LIC levels were lower in patients with TI than in those with TM; only ferritin values were significant. We found a statistically significant relationship between SF and LIC, with cut-off estimates of SF in patients with TI who had splenectomy and those who entered puberty spontaneously (916 and 940 ng/mL, respectively) with LIC >5 mg Fe/g dry weight (P < 0.0001). A significant relationship was also found for patients with TI who had elevated ALT level (63.5 U/L), of 3.15 times the upper normal laboratory limit, using a cut-off for LIC ≥5 mg Fe/g dry weight. CONCLUSION: We determined the cut-off values for ALT and SF indicating the best time to start iron chelation therapy in patients with TI, and found significant correlations among iron overload, SF, and ALT.
Adolescent ; Alanine Transaminase ; beta-Thalassemia* ; Chelation Therapy ; Cross-Sectional Studies ; Diagnosis ; Ferritins* ; Humans ; Iron Overload ; Iron* ; Liver* ; Magnetic Resonance Imaging ; Puberty ; Risk Factors ; Splenectomy ; Thalassemia*

The effect of buffer system, adjustment substance pH, pH of solution, antioxygen and antiseptic on the stability of eye drop solution with vitamin B5 was studied. The result: at pH 5,5, buffer system of acetat, of citrat and of phosphat strictly influence to the stability of eye drop solution containing vitamin B5. This solution also sustained with antioxygen dinatri edetat 0,02%, combining with natri metabisulfid 0,1% -0,3% don’t make increase the stability of product. The antiseptic of benzalkonium clorid and chlorobutanol don’t influence to the stability of this solution. But benzalkonium clorid is appropriate than chlorobutanol because of it don’t absorb through PE plastic, the antiseptic efficacy increase with the presence of dinatri edetat and this make increase the bioavailability of drug
Ophthalmic Solutions ; Pantothenic Acid ; Pharmaceutical Preparations

PURPOSE: The purposes of this study were to evaluate the biodistribution and effect of Ho-166 radionuclide by intra-arterial injection of the Ho-166 chitosan complex in dogs and to assess the clinical efficacy and side effects of this complex in the treatment of hepatocellular carcinoma (HCC). MATERIALS AND METHODS: In an experimental study, 20 mCi of Ho-166 chitosan complex was injected into the left hepatic artery of six adult dogs. The distribution of radioactivity in each organ was calculated using a gamma camera scan at regular intervals. A beta ray radioactivity count (cpm) of blood and urine was performed periodically, and hematologic and hepatic function were regularly assessed. At 4, 8 and 12 weeks after intra-arterial injection, bone marrow and liver were pathologically evaluated. Twenty-five patients with a single, nodular HCC mass 3 -9 cm in diameter were treated by intra-arterial injection of Ho-166 chitosan complex, and immediately after the procedure a gamma camera scan was obtained. A beta ray radioactivity count(cpm) of blood was performed periodically, hematologic and hepatic function were regularly evaluated, and CT scans and angiograms were obtained 3 months after the procedure. On the basis of the CT and angiographic findings, the treatment effects were classified as complete (CR), partial (PR) or non-response(NR). RESULTS: In the animal study, blood radioactivity peaked immediately after injection and then declined rapidly. Urinary excretion was 0.17%. The proportion of radioactivity in each organ per whole body was 25% in the left lobe of the liver, 7% in the right lobe, 3% in the lung, 1.4 -3% in the bladder, and 2% in bone. WBC and platelet counts declined maximally at 3 -4 weeks and recovered at 12 weeks. The cellularity of bone marrow was 25% at 4 weeks and 55% at 12 weeks, findings which correlated well with the observed hematologic changes. In the clinical study of 25 HCC patients, CR was achieved in 17 (68%) cases, PR in 5 (20%) and NR in 3 (12%). At gamma camera imaging immediately after treatment, tumor radioactivity was localized in 76% of cases. In six cases (24%) WBC and platelet counts decreased 50% or more compared with their pretreatment level. In 67 -75% of cases, SGOT and SGPT were, within 1 -3 days, 2 -3 times higher than their pre-treatment level, and recovered at post 4 weeks. CONCLUSION: Ho-166 chitosan complex administrated intra-arterially localized the target organ with minimal side effects, and we therefore suggest that it may be used in the treatment of nodular and hypervascular HCC. Further study of its dosimetry and possible hematologic side reactions is needed, however.
Adult ; Alanine Transaminase ; Animals ; Aspartate Aminotransferases ; Beta Particles ; Bone Marrow ; Carcinoma, Hepatocellular* ; Chitosan* ; Dogs ; Gamma Cameras ; Hepatic Artery ; Humans ; Injections, Intra-Arterial* ; Liver ; Lung ; Platelet Count ; Radioactivity ; Radionuclide Imaging ; Tomography, X-Ray Computed ; Urinary Bladder