• Journal of Pharmaceutical Investigation
• /
• 제32권1호
• /
• pp.47-54
• /
• 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.

• 대한화학회지
• /
• 제34권2호
• /
• pp.184-188
• /
• 1990

치환 phenacyl bromide와 imidazole과의 반응 및 phenacyl bromide와 치환imidazole과의 반응속도를 전기전도도법으로 측정하였다. 반응속도는 phenacyl bromide의 전자 끄는기에 의하여 촉진되었으며 이 반응은 linear free energy relationship과 isokinetic relationship에 잘 맞았다. 반응속도와 imidazole의 pKa사이에는 Bronsted rule이 잘 적용되었으나 2-methylimidazole의 경우에는 위치장애현상으로 인해 여기서 벗어났다. Acetonitrile 용매하에서는 methanol 용매하에서보다 Kirkwood식에서 예상되는 것보다 훨씬 빠르게 반응속도가 관찰되었다.

• 대한화학회지
• /
• 제13권3호
• /
• pp.215-219
• /
• 1969

Methanol을 溶媒로 한 thiourea와 m- 또는 p- 置換 benzyl bromide 類 와의 反應速度를 電氣傳導度法으로 測定하였다. Hammett 置換基定數와 Log k 와의 關係를 調査한 結果 benzyl bromide에 對한 thiourea의 $SN_2$反應에 있어서 C-Br結合의 解離가 이 反應의 律速段階임을 알 수 있었다. 電子供與基와 電子吸引基는 다같이 反應速度에 定量的인 影響을 주었으나 그 樣式은 서로 달랐다. 이 結果에 符合되는 反應 메카니즘을 考察하였다. 몇 가지 熱力學的 파라미터로 求하였다.

• 상하수도학회지
• /
• 제13권3호
• /
• pp.83-90
• /
• 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.

• Archives of Pharmacal Research
• /
• 제14권3호
• /
• pp.266-270
• /
• 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.

• Archives of Pharmacal Research
• /
• 제26권12호
• /
• pp.990-996
• /
• 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.

• 대한화학회지
• /
• 제9권3호
• /
• pp.124-127
• /
• 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.

• 대한화학회지
• /
• 제13권1호
• /
• pp.1-4
• /
• 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.

• Bulletin of the Korean Chemical Society
• /
• 제3권4호
• /
• pp.144-148
• /
• 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.

• Nuclear Engineering and Technology
• /
• 제1권2호
• /
• pp.87-90
• /
• 1969

Trans-cinnamyl chloride와 bromide의 방사성 Cl$^{-}$, Br$^{-}$ 및 I$^{-}$와의 교환 반응을 아세톤 용액에서 반응속도론적으로 연구하였다. 상대적인 할로겐 이온들의 친핵성과 이탈능을 HSAB 원리를 이용하여 논의하였다.