• Title/Summary/Keyword: Bromide

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Bioequivalence of Alpit Tablet to Algiron Tablet (Cimetropium Bromide 50 mg) (알기론 정(브롬화 시메트로피움 50 mg)에 대한 알피트 정의 생물학적 동등성)

  • Cho, Hea-Young;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.32 no.1
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    • pp.47-54
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    • 2002
  • Cimetropium bromide, a quaternary ammonium compound which is chemically related to scopolamine, exhibits its antispasmodic activity by competing with acetylcholine for the muscarinic receptors of the smooth muscle of gastrointestinal tract. The drug has been used for the treatment of various disorders involving spasms of the musculature of the gastrointestinal, biliary and genitourinary tracts. The purpose of the present study was to evaluate the bioequivalence of two cimetropium bromide tablets, $Algiron^{TM}$ (Boehringer Ingelheim Korea Ltd.) and $Alpit^{TM}$ (Hana Pharmaceutical Co., Ltd.), according to the prior and revised guidelines of Korea Food and Drug Administration (KFDA). The cimetropium bromide release from the two cimetropium bromide tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty normal male volunteers, $25.25{\pm}2.10$ years in age and $65.76{\pm}6.39$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three tablets containing 50 mg of cimetropium bromide per tablet were orally administered, blood was taken at predetermined time intervals and the concentrations of cimetropium bromide in serum were determined using HPLC method with UV detector. The dissolution profiles of two cimetropium bromide tablets were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using non-transformed and logarithmically transformed $AUC_t\;and\;C_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on the $Algiron^{TM}$ were 2.19%, -5.97% and 3.49%, respectively. Minimum detectable differences $({\Delta})\;at \;{\alpha}=0.05\;and\;1-{\beta}=0.8$ were less than 20% (e.g., 13.71 %, 19.05% and 15.11% for $AUC_t,\;C_{max}\;and\;T_{max}$, respectively). The powers $(1-{\beta})\;at\;{\alpha}=0.05,\;{\Delta}=0.2\;for\;AUC_t$, $C_{max}\;and\;T_{max}$ were 97.79%, 83.22% and 95.60%, respectively. The 90% confidence intervals were within ${\pm}20%$ (e.g., $-5.84{\sim}10.21,\;-17.11{\sim}5.18\;and\;-5.35{\sim}12.33\;for\;AUC_t,\;C_{max}\;and\;T_{max}$, respectively). There were no sequence effect between two tablets in logarithmically transformed $AUC_t\;and\;C_{max}$. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) (e.g., $0.94{\sim}1.10\;and\;0.85{\sim}1.05\;for\;AUC_t\;and\;C_{max}$, respectively). Two parameters met the criteria of prior and revised KFDA guideline for bioequivalence, indicating that $Alpit^{TM}$ tablet is bioequivalent to $Algiron^{TM}$ tablet.

Kinetics of Reactions of Phenacyl Bromides with Imidazoles (치환 브롬화페나실과 이미다졸류의 반응에 대한 반응속도론적 연구)

  • Im, Dong Sun;Gwon, Jong U;Kim, Chang Seok;Hong, Soon Yung
    • Journal of the Korean Chemical Society
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    • v.34 no.2
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    • pp.184-188
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    • 1990
  • Rates for reactions of substituted phenacyl bromides with imidazole and those of substituted imidazoles with phenacyl bromide were measured by an electric conductivity method. The rates were accelerated by electron-withdrawing substituents of phenacyl bromide and these reactions obeyed well both the linear free energy relationship and the isokinetic relationship. The relation between pKa's of substituted imidazoles and reaction constants fit the Bronsted rule. However, the case of 2-methylimidazole deviated far from this rule exerting steric hindrance. The reaction proceeded much faster in acetonitrile than in methanol and the observed ratio, k2 (acetonitrile)/k2 (methanol), was considerably larger than the value calculated from the Kirkwood equation.

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Kinetics of the Reaction of Benzyl Bromides with Thiourea (Benzyl Bromide 類와 Thiourea의 反應에 關한 反應速度論的 硏究)

  • Yoh, Soo-Dong;Lee, Dae-Soo;Hong, Soon-Yung
    • Journal of the Korean Chemical Society
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    • v.13 no.3
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    • pp.215-219
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    • 1969
  • The kinetics of the reaction of m-or p-substituted benzyl bromides with thiourea in methanol at 35.0$^{\circ}$were determined by an electric conductivity method. According to a plot of log k against the Hammett substituent constants, C-Br bond cleavage in benzyl bromide is postulated to be a rate determining step at the SN2 reaction of benzyl bromide with thiourea. Both electron-donating substituents and electron-withdrawing substituents quantitatively affected the rate of reaction, but each in a different manner. A mechanistic possibility was proposed to account for the results. Some activation parameters were also calculated.

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Characteristics of Trihalomethanes (THM) Formation for Groundwater in the Northeasthern Area of Cheju Island (제주도 북동부지역 지하수의 Trihalomethanes (THM) 생성 특성)

  • Song, Young-Cheol;Oh, Youn-Keun;Kam, Sang-Kyu
    • Journal of Korean Society of Water and Wastewater
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    • v.13 no.3
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    • pp.83-90
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    • 1999
  • This study was carried out to investigate the characteristics of trihalomethane (THM) formation from chlorination of groundwater in the northeastern area of Cheju Island. Effects of total organic carbon (TOC) and bromide in groundwater on the THM formation were studied. Samples were taken from two regions withe altitude. The concentrations of TOC and bromide in groundwater were higher at the regions of lower altitude, especially at the altitude below 50m. Generally the THM formation in GA region containing a high TOC was higher than that in GB region containing a relatively high bromide. At the altitude below 100m, the formation of total and brominated THM was highest at GB region. The most part of THM formation was brominated THM at GB region. The formation ratio of chloroform and brominated THM was similar to the others. Among the brominated THM, dibromochloromethane and bromoform in GB region were containing high bromide. Bromodichloromethane and dibromochloromethane in GA region were containing low bromide. At the altitude above 200m, chloroform was formed mainly. Comparing the ratio of brominated THM of total THM in Cheju Island with that in other areas, Seoul and Pusan, it can be konwn that the former showing 51.3% was much higher than the latter showing 6.7% and 28.8%, respectively.

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Synthesis of C-(2-Furyl)-N-(4-nitrophenyl)methanohydrazonyl Bromide. Reactions with Nucleophiles and Active Methylene Compounds

  • Hassaneen, Hamdi M.;Shawali, Ahmad S.;Elwan, Nehal M.;Ibrahim, Al Hossien A.
    • Archives of Pharmacal Research
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    • v.14 no.3
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    • pp.266-270
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    • 1991
  • Synthesis of C-(2-furyl)-N-(4-nitrophenyl)methanohydrazonyl bromide 2 is described. Treatment of 2 with uncleophiles affords the corresponding substitution products 3-7. Also, compound 2 reacts with selenocyanate anion and thiocyanate anion and give the corresponding selenadiazoline and thiadiazoline 8 and 9, respectively. Moreover, reaction of 2 with enolates of various active methylene compounds afforded the pyrazole derivatives 17-20.

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Synthesis of Novel Carboacyclic Nucleosides with Vinyl Bromide Moiety as Open-chain Analogues of Neplanocin A

  • Choi, Myung-Hee;Kim, Hee-Doo
    • Archives of Pharmacal Research
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    • v.26 no.12
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    • pp.990-996
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    • 2003
  • A novel carboacyclic nucleoside analogue, 9-[2-bromo-4-hydroxy-3-hydroxymethyl-2-butenyl] adenine, and its derivatives were designed and synthesized as open-chain analogues of neplanocin A. The syntheses were accomplished via the coupling of adenine or pyrimidine bases to the key intermediate allylic bromide 7. The bromide 7 was prepared from epichlorohydrin in a seven step process in a 54% overall yield. The synthesized compounds were evaluated for their antiviral activity against the polio virus, HSV and HIV.

The Surface Tension and the C. M. C. of the Solution of Dodecylpyridinium Bromide (Dodecylpyridinium Bromide 溶液의 表面張力과 C. M. C.)

  • Han, Man-Un;Lee, Chong-Man;Kim, Tae-Woo
    • Journal of the Korean Chemical Society
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    • v.9 no.3
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    • pp.124-127
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    • 1965
  • The surface tension of the solution of dodecylpridinium bromide was measured by the ring method over the range $25^{\circ}\; to\; 45^{\circ}C.$ The critical micelle concentration was determined from the change of the surface tension of solution with concentration. The temperature dependence of the critical micelle concentration was also investigated. The result was compared with Adderson and Taylor's data determined by the conductivity method.

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The Effect of Temperature on the Critical Micelle Concentration of Hexadecyl Trimethyl Ammonium Bromide (界面活性劑 Hexadecyl Trimethyl Ammonium Bromide의 C. M. C. 의 溫度效果)

  • Kun Moo Lee
    • Journal of the Korean Chemical Society
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    • v.13 no.1
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    • pp.1-4
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    • 1969
  • Temperature effect on the critical micelle concentration of hexadecyl trimetyl ammonium bromide over the range of $2^{\circ}-50^{\circ}C$ has been investigated by the method of electrical conductivity. The values obtained have been formulated as a power series in T. Several thermodynamic parameters have been calculated for the temparature range examined and their values have been discussed in the light of current theories on the participation of solvent in micelle formation.

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Kinetic Study on Bromine-Exchange Reaction of Antimony Tribromide with t-Butyl Bromide in Nitrobenzene and in 1, 2, 4-Trichlorobenzene$^*$

  • Choi, Sang-Up;Pae, Young-Il
    • Bulletin of the Korean Chemical Society
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    • v.3 no.4
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    • pp.144-148
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    • 1982
  • The kinetic study on the bromine-exchange reaction of antimony tribromide with t-butyl bromide in nitrobenzene or 1,2,4-trichlorobenzene has been carried out, using Br-82 labelled antimony tribromide. The results show that the exchange reaction is first order with respect to t-butyl bromide and 1.5th order with respect to antimony tribromide. It is assumed that the 1.5th order indicates the coexistance of first- and second-order kinetics. Reaction mechanisms for the exchange reaction are proposed.

Halogen Exchange Reactions of Cinnamyl Halides

  • Lee, Bon-Su;Lee, Ikchoon
    • Nuclear Engineering and Technology
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    • v.1 no.2
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    • pp.87-90
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    • 1969
  • Halogen exchange reactions of trans-cinnnamyl chloride and bromide with radioactive chloride, bromide and iodide ions in acetone have teen studied. Relative nucleophilicity of halide ions and relative leaving ability have been discussed invoking the principle of HSAB.

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