bluuebunny/crossref_metadata_2025_split huggingface dataset:
Interactions of parenteral solutions with sulphur-treated glass bottles
Authors: Passl W J 
Published: April 2011

Abstract
Concern about limited surface durability has been the main reason for recommendations by advisory committees and government health authorities, not to re-use sulphur-treated soda-lime glass (type II) bottles for intravenous solutions. In order to contribute specific data, the interactions of slightly acid and neutral parenteral solutions with ammonium sulphate-treated type II glass bottles have been investigated. It was established that the amounts of silica, sodium and calcium released into the solution are not greater than the potential background contamination from the raw materials. The number of particles in the solution was well below the limits set by the British Pharmacopoeia and not much higher than the lowest background count practically achievable. On an average, bottle surfaces released less material after the first time of use. Bottle-to-bottle variations revealed by scanning electron microscopy point at problems in achieving smooth, evenly surface-treated bottle surfaces during bottle manufacture.
Correlation of bioavailability in man with simulated absorption data for three doxantrazole preparations
Authors: Jones H , Bye A 
Published: April 2011

Abstract
The in vitro and in vivo availability of doxantrazole, a potential antiallergic compound has been evaluated. A solution was significantly less bioavailable than either tablet or suspension formulations and it is suggested that this is associated with the large volume of the solution vehicle altering the hydrophilicity of the gastrointestinal fluids. In vitro availability was determined from absorption rate constants and absorption profiles obtained using the Sartorius absorption and solubility simulators. A statistically significant correlation was found between the percentage absorbed in vitro at 1 h and both total urinary recovery and area under plasma curve values in vivo. It is considered that in vitro determination of diffusion through artificial lipid membranes may be a useful predictive method of in vivo availability.
Effects of acute or chronic administration of chlordiazepoxide on feeding parameters using two food textures in the rat
Authors: Cooper Steven J , Francis Raymond L 
Published: April 2011

Abstract
The effects of acute or chronic administration of chlordiazepoxide on several feeding parameters were studied in the rat. Given acutely, chlordiazepoxide reduced the rate of feeding, at lower dose levels (5·0 or 10·0 mg kg−1) tended to prolong feeding duration, and at a higher dose (15·0 mg kg−1) reduced the amount of food intake. Food texture can influence feeding parameters too; but the effects of the drug did not interact with the effects of food texture. After 9 daily injections of the drug, there were several indications of the development of tolerance to the effects of the drug on the feeding parameters. A possible role of 5-HT mechanisms in the reduction of eating rate produced by the drug is considered.
Catecholamine uptake blockade in anaesthetized dogs: influence on cardiovascular responses
Authors: Brown R A , Solca Anne M , Wilson J 
Published: April 2011

Abstract
The effects of differential and combined catecholamine uptake antagonism on cardiovascular responses of anaesthetized dogs to isoprenaline, noradrenaline, and electrical stimulation of the left ansa subclavia nerve have been studied. Uptake1 inhibition by cocaine HCl (5 mg kg−1 and 1 mg kg−1 every 45 min) enhanced responses to noradrenaline (0·1 to 2·0 μg kg−1 i.v.) and sympathetic nerve stimulation (1 to 20 Hz), but did not affect those to isoprenaline. Uptake2 inhibition by metanephrine (40 μg kg−1 min−1) enhanced cardiac responses to isoprenaline (0·05 to 1·0 μg kg−1 i.v.), but did not significantly alter those to noradrenaline or nerve stimulation. Responses to all agonist interventions were increased by the combined administration of cocaine and metanephrine. Cocaine preferentially enhanced the positive chronotropic cardiac response to noradrenaline, but metanephrine did not differentiate between heart rate and contractility. These results have been discussed in the light of the mechanism of drug action involved.
Effects of pyroxamidine and guanethidine on contractile responses to field stimulation and to noradrenaline in the anococcygeus muscle and vas deferens of the rat
Authors: Doggrell Sheila A 
Published: April 2011

Abstract
The effects of pyroxamidine (EMD 21192) and guanethidine on contractile responses were studied in the anococcygeus muscle and vas deferens of the rat. Pyroxamidine (10−6 and 10−5 M) and guanethidine (6 times 10−6 and 10−5 M) potentiated the responses to low concentrations of acetylcholine in the rat anococcygeus muscle. Following incubation of the muscle with 6-hydroxydopamine (10−3M for 3 h), pyroxamidine (10−5 M) and guanethidine (10−5 M) had no effect on responses to acetylcholine. This suggests that the potentiating effect of pyroxamidine and guanethidine on responses to acetylcholine is due to the release of subthreshold concentrations of noradrenaline.
In the anococcygeus, pyroxamidine (10−6 and 10−5 M) and guanethidine (10−6 and 10−5 M) inhibited responses to field stimulation and potentiated responses to exogenously applied (−)-noradrenaline. The responses to field stimulation in the vas deferens were also inhibited by 10−5M pyroxamidine and by 10−5 M guanethidine. 10−6 M guanethidine, but not 10−5 M pyroxamidine, potentiated responses to (−)-noradrenaline in the vas deferens. In the presence of nortriptyline (10−6 M), a potent inhibitor of neuronal uptake, the inhibitory effects of pyroxamidine and guanethidine on responses to field stimulation were reduced or reversed and these drugs had no effect on responses to (−)-noradrenaline. This suggests that pyroxamidine is a noradrenergic neuron blocker and that its action is dependent on continued neuronal uptake. Following 6-hydroxydopamine incubation, 10−5 M pyroxamidine and 10−5 M guanethidine inhibited the responses to (−)-noradrenaline in the rat anococcygeus muscle. Thus it seems likely, at high concentrations, that these compounds have postsynaptic blocking activity.
The neuromuscular and autonomic blocking activities of pancuronium, Org NC 45, and other pancuronium analogues, in the cat
Authors: Durant Nicholas N , Marshall Ian G , Savage David S , Nelson David J , Sleigh Thomas , Carlyle Ian C 
Published: April 2011

Abstract
Twenty-six mono-or bis-quaternary salts of 3,17-dioxy-2β,16β-dipiperidino-5α-androstanes (including pancuronium) and one 17-desoxy congener were tested for neuromuscular blocking and autonomic blocking activities in the chloralose-anaesthetized cat. The 17β-acetoxy series, all the members of which contain an acetylcholine-like fragment in the steroidal D-ring, was most selective for effecting neuromuscular blockade. The salient member of this series is 3α,17β-diacetoxy-2β,16β-dipiperidino-5α-androstane 16β-N-monomethobromide (Org NC 45) which is highly selective in blocking neuromuscular transmission in that a dose approximately sixty times greater than the neuromuscular blocking dose was required to block responses to vagal stimulation. In contrast, in doses sufficient to produce neuromuscular block, pancuronium simultaneously blocked responses to vagal stimulation. Moreover, pancuronium and Org NC 45 exhibited the same order of neuromuscular blocking activity and therefore the latter potentially represents a useful addition to the armamentarium of neuromuscular blocking agents currently in clinical use.
Effects of phenacetin, paracetamol and caffeine on the erosive activity of acetylsalicylic acid in the rat stomach: dose-response relationships, time course of erosion development and effects on acid secretion
Authors: Seegers A J M , Jager L P , van Noordwijk J 
Published: April 2011

Abstract
Adult male and female Wistar rats were equally susceptible to gastric injury induced with acetylsalicylic acid (aspirin). Both in male and in female rats simultaneous administration of caffeine and aspirin caused significantly more gastric erosions than the same dose of aspirin alone; likewise addition of paracetamol to aspirin decreased the incidence of gastric lesions in either sex, and addition of phenacetin to aspirin had no effect. The potentiation by caffeine and the inhibition by paracetamol were both dose-dependent and only markedly influenced the development of erosions after 3–4 h. Pretreatment with phenacetin or paracetamol 1 h before administration of aspirin did not affect its erosive activity. Administration of benorylate caused no more gastric erosions than the vehicle or than equivalent mixtures of aspirin and paracetamol. The histamine-stimulated acid output of the stomach during gastric perfusion with aspirin was rapidly diminished. Neither paracetamol nor caffeine initially affected this decrease in acid output. However, 30 min after perfusion with aspirin and caffeine, acid secretion increased approximately as strongly as after caffeine alone. Caffeine potentiates aspirin-induced erosions by its stimulatory effect on acid secretion whereas paracetamol inhibits these erosions by preventing their growth.
The photochemical stability of cis- and trans- isomers of tricyclic neuroleptic drugs
Authors: wan Po A Li , Irwin W J 
Published: April 2011

Abstract
The irradiation of the tranquillizers flupenthixol, clopenthixol and chlorprothixene has been found to induce rapid cis-trans isomerization. The composition of the photostationary mixture is not that of the batch drug and hence this process may affect the activity. Further decomposition to a thioxanthone derivative occurs rapidly in the presence of air. Exclusion of oxygen, however, does not prevent further degradation and a slower secondary isomerization is observed on prolonged irradiation. Doxepin and dothiepin also undergo analogous reactions but the isomerizations are much slower and the oxidative degradation yields many products.
Stereoselective actions of substituted benzamide drugs on cerebral dopamine mechanisms
Authors: Jenner P , Clow A , Reavill C , Theodorou A , Marsden C D 
Published: April 2011

Abstract
Apomorphine-induced locomotor activity in reserpine-pretreated mice was antagonized by pretreatment with (-)-sulpiride and (-)-sultopride. The (+)-enantiomers were inactive. Apomorphine- and amphetamine-induced stereotyped behaviour in rats were antagonized by (-)-sultopride but not by the (+)-enantiomer. Neither enantiomer of sulpiride prevented the onset of the stereotyped response. Both (-)-sulpiride and (-)-sultopride induced increases in striatal and mesolimbic HVA and DOPAC concentrations; (+)-sultopride elevated striatal and mesolimbic DOPAC concentrations but not HVA, while (+)-sulpiride had no effect on HVA or DOPAC in either area. Dopamine concentrations were reduced by the enantiomers of sultopride but not by sulpiride. Low concentrations (10−9 −10−66 M) of the (-)-enantiomers of both drugs displaced [3 H]spiperone from its specific binding site in rat striatal preparations, but the (+)-enantiomers were 40 and 100 times less active. However, neither enantiomer of either drug anatagonized the dopamine-induced stimulation of adenylate cyclase in rat striatal preparations. The data suggest that the central pharmacological activity of sulpiride and sultopride resides in the (-)-enantiomers and that this activity occurs at cerebral dopamine receptors not dependent on adenylate cyclase for functional activity.
Ethanol-stimulated acid secretion in the isolated whole stomach of the rat
Authors: Bunce K T , Parsons M E 
Published: April 2011

Abstract
The application of ethanol to the serosal surface of the isolated whole rat stomach stimulated a high rate of acid secretion, with a maximum response being obtained to 4 % v/v ethanol. This acid response to ethanol was not inhibited by high concentrations (1 mM) of atropine or cimetidine, indicating that the response was probably not mediated by either histamine, gastrin or acetylcholine. These results using the secretory antagonists were confirmed by experiments in an isolated gastric mucosa preparation. The acid response to ethanol was significantly, but not completely inhibited by 10 mM thiocyanate, indicating the existence of an acid component of non-parietal cell origin in the mucosal bathing solution. However, analysis of the mucosal solution failed to reveal the presence of an acidic metabolite of ethanol.
The Clark plot: a semi-historical case study
Authors: Stone Mervyn 
Published: April 2011

Abstract
A study has been made of the origins of the quantitative theory of simple competitive antagonism as manifest in the papers of Gaddum and of Clark. The classical data of Clark on the antagonism of acetylcholine by atropine were reanalysed by recently developed computer-based methods. It was seen how close Clark came to initiating a method having the following significant advantages over the Schild plot: (i) symmetrical treatment with respect to the control (zero antagonist) data; (ii) absence of difficulty with the cases where an estimated dose-ratio is less than unity; (iii) straightforward calculation of approximate standard errors for departure from overall simple competitivity at each antagonist level including control.
Metabolism of thymoxamine: identification of metabolites in rat
Authors: Feniou C , Neau B , Prat G , Cheze C , Fauran F , Roquebert J 
Published: April 2011

Abstract
Thymoxamine hydrochloride administered by mouth to rats at 25 or 100 mg kg−1 was excreted in the urine as the deacetyl and N-demethyl-deacetyl metabolites. These were completely sulpho- and glucuronoconjugated at 25 mg kg−1 but only partially so at the higher dose. Thymoxamine deacetylation in vitro is catalysed by plasma and hepatic cytosol esterases and the deacetyl metabolite undergoes N-demethylation catalysed by the cytochrome P 450 hepatic microsome mixed function monooxygenase system. Because of the rapidity of the deacetylation it is concluded that thymoxamine is a prodrug leading in vivo to the active deacetyl thymoxamine.
The determination of ethoxylated non-ionic surfactants in wool grease
Authors: Christoe J R , Evans D J 
Published: April 2011

Abstract
Surfactants in grease can be identified by dissolving the grease (5 g) in hexane-ethyl acetate (1: 1 v/v) and adding to silica gel (100–200 mesh), eluting first with solvent and then with 50% v/v aqueous ethanol, evaporating and extracting with acetone. After evaporation, the residue is heated at 130 °C for 2 h with the mixed anhydride of acetic acid and 4-toluene sulphonic acids (cleavage reagent) (3 ml) to give ethyleneglycol diacetate (EGD) and the corresponding acetate or phenolic derivatives of the hydrophobic portion of the surfactant. When cool, the mixture is diluted with water, added to Na2SO4 (anhyd.) neutralized with Na2CO3, extracted with ether, dried (Na2SO4), concentrated and a sample (3 μ1) gas chromatographed (glass column 1 m × 3 mm i.d., packed with 15% Carbowax 20M on Gas-Chrom Q, oven temp. 170 °C, inlet/outlet 210 °C, N2 carrier 30 ml min−1) and compared with g.c.s of known surfactants. Quantitatively, the grease (0·1-1·0g) is refluxed with cleavage reagent as above, cooled to 60 °C, distilled water (15 ml) added and the separated liquor centrifuged (3000 rev min−1, 5 min). The clarified liquor is added to Na2SO4 (anhyd.), neutralized and extracted with ethyl acetate and a sample (3 μl) chromatographed as above with oven temp. 150 °C. The concentration of surfactant can be determined from comparison of the height of the EGD peak (Rt 2.5 min) with heights from known amounts of the surfactant treated concurrently. The type of grease (commercial, lanolin B.P., and a methanol-soluble fraction of a commercial grease were examined) has no effect on the method.
A comparison of chemically defined and complex media for the production of Bacillus subtilis spores having reproducible resistance and germination characteristics
Authors: Hodges N A , Melling J , Parker S J 
Published: April 2011

Abstract
Spores of Bacillus subtilis were produced on five batches of Antibiotic Assay Medium No. 1 obtained from different suppliers, five batches obtained from a single supplier and five batches of a chemically defined liquid medium. The magnitude of the variation within each of the three groups was compared in terms of heat resistance, glutaraldehyde resistance, germination rate and sensitivity of germinated spores to neomycin. For all these parameters the degree of reproducibility achieved by using a chemically defined liquid medium was substantially better than that using batches of complex medium from a single supplier. Even larger variations in these parameters resulted when different suppliers were used. The value of defined media for the production of spore inocula to be used in sterilization control and similar procedures is discussed.
The influence of drug and diluent particle size on the in vitro release of drug from hard gelatin capsules
Authors: Newton J M , Bader F 
Published: April 2011

Abstract
The in vitro release of a drug from capsules containing different proportions of controlled particle size fractions of acetylsalicylic acid and lactose, has been assessed in terms of the time for 50% of the drug content of the capsule to be released into solution during a dissolution test (T50), and by a standard disintegration test. In general the two types of test gave closely related responses although some discrepancies existed with certain systems. For capsules containing only the drug, the value of T50 increased as the particle size of the drug decreased. The addition of lactose generally reduced the T50 value, the extent of the reduction showing greater dependence on the proportion of lactose added than its particle size. Capsule formulations containing 80% w/w of lactose had values of T50 which were independent of drug or diluent particle size. Capsule formulations containing lower proportions of lactose usually had an optimumcombination of particlesize fractions of drug and diluent for maximum drug release. The relationship between drug release and the porosity within the capsule was dependent on the particle size of the drug.
Assay of nicotine in biological materials: sources of contamination and their elimination
Authors: Feyerabend C , Russell M A H 
Published: April 2011

Abstract
A previous method for the measurement of nicotine in biological samples was subject to occasional interference from a contaminant which eluted simultaneously with the internal standard (quinoline). This has been rectified by substituting isoquinoline as the internal standard and modifying the operating conditions of gas chromatography. Other sources of contamination in nicotine assays such as the analytical reagents, the atmosphere and the sample itself are discussed in detail.
Some mechanisms which may modulate noradrenaline release in guinea-pig isolated ileum
Authors: Sanger G J , Watt A J 
Published: April 2011

Abstract
Guinea-pig isolated ileum pre-incubated with [3 H]noradrenaline, released 3 H-label during coaxial stimulation at 3·2-12·8 Hz. This evoked 3 H-overflow seems due to nerve stimulation, and may be frequency-dependent. The 3 H-overflow evoked by coaxial stimulation was increased with 2·6 μM phentolamine, reduced at threshold stimulation by 0·56 μM prostaglandin E1, but the tendency for 2·8 μM indomethacin to increase the evoked 3 H-overflow was not statistically significant. The results indicate that the release of noradrenaline from guinea-pig ileum may be modulated by activation of presynaptic α-adrenoceptors, whereas prostaglandins act mainly at a postsynaptic site to modulate the sympathetic response.
Evidence for a direct anti-inflammatory action of calcitonin: inhibition of histamine-induced mouse pinnal oedema by porcine calcitonin
Authors: Strettle R J , Bates R F L , Buckley G A 
Published: April 2011

Abstract
Porcine calcitonin (PCT) caused a potent inhibition of histamine-induced vascular leakage in the mouse pinna. These effects were observed at doses of PCT lower than those required to affect plasma calcium concentrations. In contrast PCT did not inhibit responses of the mouse pinna to 5-hydroxytryptamine despite observed falls in plasma calcium concentrations. It would appear that PCT inhibits histamine-induced oedema in the mouse by a direct action which may partially or fully explain the anti-inflammatory action of PCT, observed by other workers, in some acute inflammatory conditions.
The effects of theophylline and caffeine on thermoregulatory functions of rats at different ambient temperatures
Authors: Lin M T , Chandra A , Liu G G 
Published: April 2011

Abstract
Both systemic and central administration of theophylline and caffeine produced a dose-dependent rise in rectal temperature at ambient temperatures of 8, 22 and 30°C. The hyperthermia in response to either xanthine was brought about by an increase in metabolic heat production. In addition, their administration produced behavioral excitation, cutaneous vasodilation (as estimated by an increase in the foot and tail skin temperatures) and diuresis. There was no change in respiratory evaporative heat loss. Probably, the hyperthermia induced by the two drugs was due to behavioral excitation leading to an increased metabolism at the ambient temperatures studied. Furthermore, either destruction of central catecholaminergic nerve fibres (with 6-hydroxydopamine) or blockade of α-adrenergic and dopaminergic (with phentolamine and haloperidol) receptors antagonized the xanthine-induced hyperthermia. The data suggest that these xanthines elicit a central activation of both adrenergic and dopaminergic receptors via release of endogenous catecholamines that leads to behavioral excitation and hyperthermia in rats.
Solubility in amide-water cosolvent systems: a thermodynamic view
Authors: Lindstrom Richard E , Lee Chi Ho 
Published: April 2011

Abstract
The solubility of methyl p-hydroxybenzoate was determined in a series of amide-water cosolvents in the temperature range 25–40 °C. Thermodynamic values for the transfer of the ester between the cosolvent system were calculated using a method which permits a focus on the effects of amide alkylation. The results are interpreted in terms of hydrophobic bonding principles which suggest that the alkyl groups on the amide detract from amide-water interaction and enhance amide-ester interaction.
Identification of in vivo liver metabolites of Δ1 -tetrahydrocannabinol, cannabidiol, and cannabinol produced by the guinea-pig
Authors: Harvey D J , Martin B R , Paton W D M 
Published: April 2011

Abstract
The metabolites of Δ1 -trahydrocannabinol (Δ1 -THC), cannabidiol (CBD), and cannabinol (CBN) produced in vivo by the guinea-pig have been studied by combined gas-liquid chromatography-mass spectrometry. 45 metabolites of Δ1 -THC were identified of which 12 have not been reported before. Several other metabolites were detected but not identified. The major metabolic routes involved allylic and aliphatic hydroxylations, oxidations to ketones and acids, oxidative degradation of the side-chain presumably by the β-oxidation pathway, and formation of glucuronide conjugates. Di- and tri-substituted metabolites were abundant. The metabolism differed considerably from that observed in mouse and rat in that 1″- and 6β-hydroxylation and oxidative degradation of the side-chain were major metabolic pathways. 1″-Hydroxy-Δ1 -THC was found as a pair of diasteroisomers. Similar metabolic pathways were observed with CBD; twenty metabolites were identified of which two were new. Only 6 metabolites of CBN were identified. These were mainly mono-substituted in the same positions as were observed with Δ1 -THC and CBD.