• Archives of Pharmacal Research
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• v.3 no.1
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• pp.17-21
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• 1980

A sensitive spectrophotofluorometric method was developed for the analysis of 2[[3-(trifluoromethyl)phenyl]amino]-3-phridine carboxylic acid (I) in urine. The method is based on the fluoroscence behavior of the I-aluminum complex in absolute ethanol. This fluorophore has activation and emission wavelengths of 355 and 450 nm, respectively. Optimum conditions for the reaction were investigated. The fluorescence was linear in the range of 0.25 3.0 ug of I/ml. Replicate studies of spiked urine samples, each containing 2.5 ug of I/ml showed good precision with a relative standard deviation of 0.019. Overall recovery percent from five spiked urine samples was 99.4 $\pm$1.32%.

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.327-330
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• 1994

Bromolactonization of 2-substituted-1-cyclohexenyl-1-acetic acids with 1, 3-dibromo-5, 5-dime-thylhydantoin 9DBH) and potsssium tertiary butoxide (t-BuOK0 in anhydrous DMF was found to proceed in a highly regioselective manner. The reaction predominantly resulted in the formation of ${\betha}-lactones$ (greater than 96%).

• Archives of Pharmacal Research
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• v.15 no.2
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• pp.134-137
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• 1992

The effect of papaverine on the contractions induced by adrenergic neurotransmission in the isolated mouse vas deferens was investigated. Papaverine, $10^{-7}-10^{-5}$M, showed a dose-dependent and reversible inhibition on the induced contractions. When the frequency of stimulation was varied (2.5-20.0 Hz), the inhibitory effect tended to be marked at the lower frequencies.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1295-1301
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• 2004

The enantiomeric composition tests on flurbiprofen and ketoprofen present in patch products and in urine excretions following patch applications were performed as diastereomeric (R)-(+)- 1-phenylethylamides by achiral gas chromatography and by gas chromatography-mass spectrometry in selected ion monitoring mode. The method for determination of (R)- and (S)-enantiomers in the range from 0.1 to 5.0 ${\mu}$g was linear (r ${\ge}$ 0.9996) with acceptable precision (% RSD ${\le}$5.2) and accuracy (% RE = 0.6 ~ -2.4). The enantiomeric compositions of flurbiprofen in one patch product and of ketoprofen in five different products were identified to be racemic with relatively good precision (${\le}$ 6.4%). The urinary excretion level of (R)-flurbiprofen was two times higher than its antipode, while the comparable excretion levels of (R)- and (S)-enantiomers for ketoprofen were observed.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.81-86
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• 1986

The effect of imperatorin on hepatic microsomal mixed function oxidases (MF0) was investigated. On acute treatment, imperatorin (30 mg/kg, i.p) caused a significant reduction in activities of hepatic aminopyrine N-demethylase, hexobarbital hydroxylase and aniline hydroxylase as well as cytochrome p0450 content in rats and mice. Kinetic studies on rat liver enzymes revealed that imperatorin appeared to be a competitive inhibitor of aminopyrine N-demethylase (Ki,0.007 mM), whereas a non-competitive inhibitor of hexobarbital hydroxylase (Ki, 0.0148 mM). Imperatorin also inhibited non-competitively aniline metabolism (Ki 0.2 mM). Imperatorin binds to phenobarbital-induced cytochrome p-450 to give a typical type 1 binding sepctrum (max. 388nm, min 422 nm). Multiple administrations of imperatorin (30 mg/kg. i. p. daily for 7 days) to mice shortended markedly the duration of hexobarbital narcosis and increased activities of hepatic aminopyrine N-demethylase and hexobarbital hydroxylase and the level of cytochrome p-450 where as aniline hydroxylase activity was unaffected.

• Archives of Pharmacal Research
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• v.19 no.2
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• pp.100-105
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• 1996

Polyethylene glycols (PEGs; 400, 600, and 1000) were used to study the molecular weight (MW) permeability dependence in the rat ileal mucosa. Absorption of the PEGs was measured by following their recirculation perfusion over a 3 hr collection period. HPLC methods were used to separate and quantitate the individual oligomers present in the solution of PEGs mixtures (MW range 330 to 1 1 22 D). In the range studied, a distinct molecular weight cutoff was not identified. Corrected for the length of ileum used in the study, over the molecular weight range 330 to 1122 D, the apparent permeability $(P_{app)$ of PEG ranged from $3.2\pm0.06\times10_{-5} cm/sec(mean\pmSEM, n=7)\; to\; 0.1\pm0.02\times10^{-5} cm/sec.$ Also, it was observed that the apparent permeability was inversely proportional to approximately $MW^{2.4}$.

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.24-27
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• 2003

A furanofuranoid lignan glycoside, with radical scavenging on peroxynitrite, total reactive oxygen species (ROS) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical, was isolated from the rhizome of Salvia miltiorrhiza and characterized as (+)-1-hydroxypinoresinol-1-Ο-$\beta$-D-glucoside based on spectroscopic evidence. The compound exhibited peroxynitrite, total ROS and DPPH radical scavenging activities with $IC_{50}$ values of 3.23$\pm$0.04, 2.26$\pm$0.07 and 32.3$\pm$0.13 $\mu$M, respectively. Penicillamine, Trolox (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid) and L-ascorbic acid, acting as positive controls, showed radical scavenging activities with $IC_{50}$ values of 6.72$\pm$0.25, 1.43$\pm$0.04 and 11.4$\pm$0.07 $\mu$M, respectively.

• Archives of Pharmacal Research
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• v.9 no.4
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• pp.229-232
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• 1986

Three inexpensive oxidation reagents, namely pyridinium chlorochromate, chromium trioxide-dipyridine and nicotinium dichromate were utilized for oxidation of carbohydrates in 78-92% yield. Hydration could be eliminated in the oxidation of pentopyranosides and hexopyranosides, while pentofuranosides had a tendency to be easily hydrated during the oxidation. In the carbon-13 n. m. r. study, the carbonyl function resulted from the oxidation affected on the chemical shifts of $\alpha$- and $\beta$-carbons of methyl 3. 4-O-isopropylidene-$\beta$-D-arabinopyranosid-2-ulose (8) and 1,2 : 4, 5-di-O-isopropylidene-$\beta$-D-erythro-2, 3-hexodiulo-2, 6-pyranose (10) to slightly down fields (0.7-2.6 p. p. m.) compared with the chemical shifts before oxidation. While the carbonyl groups of 1. 2-O-isopropylidene-5-O-ethyloxycarbonyl-$\alpha$-D-erythro-pentofuran-3-ulose (4) and methyl 3, 5-0-isopropylidene-$\alpha$-D-threo-pentofuranosid-2-ulose (6) pushed the $\alpha$-carbons to up fields (3, 2-18.3 p. p. m. However, the order of signals on the spectra before and after oxidation remained unaltered.

• Archives of Pharmacal Research
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• v.3 no.1
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• pp.37-49
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• 1980

Chlorpropamide, $C_{10}H_{13}N_{2}O_{3}SCI$, forms orthofombic crystals of space group $P_{2}_{ 1}2_{1}2_{1}$ with a 9.066 $\pm$ 0.004, b = 5.218 $\pm$ 0.003, c = 26, 604 $\pm$, 0.008 $\AA$, and four molecules per cell. Three dimensional photographic data were collected with Mo-K$\alpha$ radiation. The structure was determined using Patterson, Fourier and Difference syntheses methods and refined by the block-diagonal least-squares methods with anisotropic thermal parameters for all nonhydrogen atoms and isotropic thermal parameters for all hydrogen atomes. The final R value was 0.10 for the 1823 observed independent reflections. The dihedral angle between the planes through the benzene ring and the urea goup is 99$^{\circ}$. The conformational angle formed by the projection of the S-C(1) with that of N(1)-C(7) when the projection is taken along the S-N(1) bond is 76$^{\circ}$. The molecule appears to form with neighbouring molecules two hydrogen bonds, N(1)..H...O(3) and N(2)-H...0(2) of lengths 2.774 and 2.954$\AA$ respectively related by screw diads parallel to the a axis. Adjacent molecules parallel to b and c axis are bound together by van der Wasls forces.

• Archives of Pharmacal Research
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• v.29 no.2
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• pp.178-182
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• 2006

Four crystal forms of cephradine were isolated by recrystallization and characterized by powder X-ray diffractometry, differential scanning calorimetry, and thermogravimetric analysis. The dissolution patterns of four crystal forms of cephradine were studied in water at $37{\pm}0.5^{\circ}C$, 90 rpm for 120 min. The amount dissolved at 120 min was highest for Form 1 ($100\%$), followed by Form 3 ($98.9\%$), Form 4 ($77.83\%$), and Form 2 ($75.55\%$). After storage for two months at $0\%$ RH (silica gel, $20^{\circ}C$), $52\%$ RH (saturated solution of $Na_{2}Cr_{2}O_{7}{\cdot}2H_{2}O/20^{\circ}C$), and $95\%$ RH (saturated solution of $Na_{2}HPO_{4}/20^{\circ}C$), none of the crystal forms showed transformation.