• 약학회지
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• 제13권1호
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• pp.1-15
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• 1969

A new method of qualitative and quantitative determination of barbiturates in the pharmaceuticals by means of $\alpha$-picoline-copper (II) was studied. Barbiturates in the pharmaceuticals were dissolved in the mixed solvent of 33% $\alpha$-picoline-Carbontetrachloride to yield Complex Compounds of barbiturates-copper (II)-$\alpha$-picoline. Complex Compounds of barbiturates show uniformly maximum absorption at the wavelength of 540m.mu. and wre to be identified at the concentration of 1 X 10$^{-4}$ Mole, and also was to be quantitatively determined at the concentration of 1 X 10$^{-3}$ Mole. By this method barbiturates in the pharmaceuticals could be determined in the presence of various compounds such as sulpyrine, isopropylantipyrine, antipyrine, phenacetin and etc. But Barbiturates could be also determined by this method after seperation with aminopyrine, acetaminophen, acetylsalicylic acid and etc. by column chromatography. And barbiturates and acetylsalicylic acid could be also determined by simultaneous equation while their complex compounds show uniformly each maximum absorption at the Wavelength of 540 m${\mu}$ and 620 m${\mu}$. I.R. spectra of these complex compounds show identification of Barbiturates derivatives. The composition ratio of these complex compounds were : barbiturates : Cu : ${\alpha}$-picoline=2:1:2.

• Archives of Pharmacal Research
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• 제15권3호
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• pp.196-203
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• 1992

Intramolecular excimer formation of 1, 3-di(1-pyrenyl)propane (Py-3-Py) and fluorescence polarization of 1, 6-diphenyl-1, 3, 5-hexatriene (DPH) were used to investigate the effects of barbiturates on the fluidity of model membranes of phosphatidycholine (SPMVPC), phosphatidylserine (SPMVPS), and phosphatidylinositol (SPMVPI) fractions of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex. In a dose-dependent manner, barbiturates decreased the excimer to monomer fluorescence intensity ratio (I'/I) of Py-3-Py and increased the anisotropy(r), rotational relaxation time (P), limiting anisotropy $(r_infty)$, and order parameter (S) of DPH in SPMVPC, SPMVPS and SPMVPI. This indicates that barbiturates decreased both the lateral and rotational diffusion of the probes in SPMVPC, SPMVPS and SPMVPI. The relative potencies of barbiturates in ordering the membranes were in the order: pentobarbital > hexobarbital > amobarbital > phenobarbital. This order correlates well with the anesthetic potencies of barbiturates and the potencies for enhancement of $\gamma$-aminobutyric acid-stimulated chloride uptake. Thus, it is strongly suggested that a close relationship might exist between the membrane ordering effects of barbiturates and the chloride fluxes across SPMV.

• Archives of Pharmacal Research
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• 제9권3호
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• pp.131-138
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• 1986

A specific and sensitive gas chromatographic (GC) procedure with the flame photometric detector (FPD) was developed for determination of barbiturates such as barbital, allobarbital, secobarbital, phenobarbital and thiopental in plasma. In order to evaluate the performance of the FPD, the results were campared with those of the flame ionization detector (FID). After extraction of barbiturates from plasma, the barbiturates were quantitatively N, N-dimethylthiometyl (MTM)-derivatized with methylthiomethyl chloride in 1, 8-diazabicyclo [5, 4, 0] undec-7-ene catalyst. The data indicate that the FPD is about 4 times more sensitive than the FID for barbiturates, although it is less reproducible. The FPD also produced chromatogram with less back ground for extracted plasma sample. The FPD also produced chromatogram with less background for extracted plasma sample. The minimum detectable amount of MTM-thiopental on 3% OV-225 column was 4, 4fmol and that of other MTM-barbiturate was about 10.0fmol.

• 대한약리학회지
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• 제7권1호
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• pp.21-27
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• 1971

The effects of 5 different drugs (amphetamine, caffeine, serotonin, sod. salicylate and pentazocine) on the duration of action of two barbiturates (thiopental and pentobarbital) and an intravenous anesthetic (propanidid) were determined in rats. Duration of action was determined by the time elapsing between loss and return of the righting reflexes. All drugs were injected intraperitoneally except propanidid which was administered by the intravenous route. Preliminary experiments indicated that at a dose of 40 mg/kg either of the two barbiturates or propanidid produced loss of the righting reflexes without death. At this dose, however, the duration of action of propanidid was extremely short. However, this dose was selected for subsequent studies. 1. At the dose employed amphetamine shortened the sleeping time of three compounds. 2. Caffeine and theophylline shortened the sleeping time of thiopental and prolonged the duration of action of pentobarbital. 3. Serotonin had no effect on duration of action of the barbiturates but prolonged the sleeping time produced by propanidid. 4. Sod. salicylate significantly prolonged the sleeping time of the barbiturates whereas pentazocine exhibited this effect only in relation to thiopental.

• 한국축산식품학회지
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• 제37권6호
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• pp.847-854
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• 2017

A rapid, sensitive and specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of four barbiturates (phenobarbital, pentobarbital, amobarbital and secobarbital) in raw milk. The barbiturates were extracted using liquid-liquid extraction, ultrasonication and centrifugation, and purified on an SPE column. Analytes were separated by HPLC on a CSH C18 column eluted using an acetonitrile-water system with a linear gradient dilution programme, and detected by MS/MS. The recoveries of the barbiturates were 85.0-113.5%, and the intra- and inter-assay RSDs were less than 9.8% and 7.3%, respectively. The limit of detection was 5 ng/mL for all four of the barbiturates. The analytical method exhibited good linearity from 10 to 1000 ng/mL; the correlation coefficient ($r^2$) was greater than 0.9950 for each barbiturate. This method was also applied to the determination of barbiturates in real milk samples and was found to be suitable for the determination of veterinary drug residues in raw milk.

• Archives of Pharmacal Research
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• 제15권4호
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• pp.298-303
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• 1992

Synaptosomal plasma membrane vesicles (SPMV) were isolated from fresh bovine cerebral cortex. The effects of barbiturates on the rotational relaxation time of 1.6-diphenyl-1, 3, 5-hexatriene (DPH) in intact SPMV and model membranes of total lipids (SPMVTL) and phosphlipids (SPMVPL) extracted from SPMV were examined. Barbiturates decreased the rotational relaxation time of DPH in intact SPMV in a dose-dependent manner. In contrast, they did not affect the rotational relaxation time of DPH in SPMVTL and even dose-dependently increased the rotational relaxation time of DPH in SPMVPL.

• Archives of Pharmacal Research
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• 제13권3호
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• pp.246-251
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• 1990

Intermolecular interaction between barbiturates and membrane components such as phospholipid and cholesterol were investigated on $^1$H-NMR spectra and infrared spectra. According to previous reports, barbiturates interacted with phospholipid through intermolecular hydrogen bonds. We also investigated thi observation using dipalmitoyl-phosphatidylcholine (DPPC) as phospholipid in deuterochloroform, and characterized quantitatively. Also, the observed drug could interact with cholesterol which is one of the major components of biomembranes through hydrogen bonds. It was the carbonyl groups of barbiturate and the hydroxyl group of cholesterol that formed hydrogen bond complex. In addition to spectroscopic studies, we investigated the direct effect of phenobarbital on lipid multibilayer vesicles, whose compositions were varied, by calorimetric method. Phenobarbital caused a reduction in the temperature of phase transition of vesicles. These studies may provided a basis for interpreting the mode of action of barbiturates.

• 대한약리학회지
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• 제26권2호
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• pp.209-217
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• 1990

Barbiturates가 분자적 약리작용기전 탐구에 기초자료를 제공하기 위하여 소의 신선한 대뇌피질 synaptosomal plasma membrane vesicles로부터 분리제제한 phosphatidylethanolamine인공세포막(SPMVPE)의 유동성에 미치는 barbiturates의 영향을 형광 probe법으로 검색한 결과는 다음과 같다. 1. Pentobarbital, hexobarbital, amobarbital 및 phenobarbital이 기재한 순위로 SPMVPE내 Py-3-Py의 monomer 형광세기에 대한 excimer 형광세기의 비 (I'/I)를 감소시켰다. 2. Pentobarbital, hexobarbital, amobarbital 및 phenobarbital이 기재한 순위로 SPMVPE내 DPH의 polarization, anisotropy, limiting anisotropy, order parameter 및 rotational relaxation time을 증가시켰다. 3. 따라서 위에 제시한 barbiturates가 SPMVPE의 유동성을 유의성있게 감소시킨다는 것을 확인할 수가 있었다.

• 대한약리학회지
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• 제28권1호
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• pp.103-114
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• 1992

한국산 2년생 소의 신선한 대뇌피질로 부터 synaptosomal plasma membrane vesicles (SPMV)를 분리한 후 이 SPMV로 부터 추출한 총지질 (SPMVTL) 및 총인지질 (SPMVPL)로서 인공세포막을 제제하였다. SPMVTL 및 SPMVPL의 outer monolayer에 trinitrophenyl groups로 공유결합시킴으로써 형광 probe 1,6-diphenyl-1,3,5-hexatriene (DPH)의 outer monolayer 형광을 선택적으로 소광케한 후 SPMVTL 및 SPMVPL의 inner와 outer monolayer 사이의 비대칭적 유동성 존재 유무를 확인하였던 바 inner monolayer에 비하여 outer monolayer가 유동성이 크다는 것을 확인하였으며 SPMVTL에 비하여 SPMVPL의 유동성이 높았다. 뿐만 아니라 barbiturates는 SPMVTL의 유동성에 대하여는 유의성이 있을 만큼의 증감 효과를 나타내지 않았고 SPMVPL의 유동성은 감소시키되 주로 outer monolayer의 유동성을 감소시킨다는 것을 확인하였으며 barbiturates 종류에 따른 SPMVPL의 총유동성 감소의 크기는 pentobarbital > hexobarbital > amobarbital > phenobarbital의 순이었다.

• 대한약리학회지
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• 제31권3호
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• pp.271-278
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• 1995

Barbiturates의 분자적 약리학적 작용기전 연구에 기초자료를 제공키 위하여 본연구를 수행하였다. 분자적 약리작용 기전 연구에서는 무엇보다도 선행되어야 하는 것이 barbiturates가 신경세포막에서 어느 부위에 주로 분포되는가를 알아내는 데에 있다. 쥐(Rat)의 뇌로부터 분리한 synaptosomal plasma membrane vesicles (RSPMV)를 분리한 후 이 RSPMV 외측 단층(outer monolayer)의 소수성 부위와 친수성 부위에 barbiturates가 분포되는 경향을 형광 probe 법으로 검색하였다. 세포막 외측 단층의 친수성 부위에 분포되는 형광 probe N-octadecylnaphthyl-2-amino-6-sulfonic acid (ONS)와 소수성 부위에 분포되는 형광 probe12-(9-anthroyloxy)stearic acid (AS)를 각각 봉입한 후 형광소광법으로 barbiturates의 분포를 측정한 결과는 다음과 같다. 1) 대부분의 barbiturates가 RSPMV 외측 단층의 친수성 부위(표면)에 분포되고 소수성 부위 (hydrophobic region)에 극히 소량만이 분포된다는 것을 확인하였다. 2) 마취효과를 크게 일으키는 barbiturates일수록 소수성 부위에 분포되는 양이 증가하였다. barbiturates 종류에 따른 RSPMV 외측 단층 소수성 부위에의 분포 크기는 thiopental sodium > pentobarbital > hexobarbital > amobarbital > phenobarbital의 순위였다.