bluuebunny/crossref_metadata_2025_split huggingface dataset:
Phosphocholine 2, 6-xylyl ether bromide: proton-phosphorus coupling constants and preliminary pharmacological assessment
Authors: Clark E R , Hughes I E 
Published: April 2011

Abstract
Phosphocholine 2, 6-xylyl ether bromide [PPP-trimethyl-2-(2, 6-xylyloxy)ethylphosphonium bromide], has been synthesized by reacting 2-(2, 6-xylyloxy)ethyl bromide with a solution of trimethyl-phosphine in phenol, but ethylenebis(trimethylphosphonium bromide), 1, 2-di(2, 6-xylyloxy)ethane and 2, 6-xylenol were the only reaction products identified when ether was used as solvent. The 2JPH and 3JPH coupling constants for these phosphonium salts have been determined. Although the phosphocholine xylyl ether blocks the Finkleman preparation in concentrations of 2–3 × 10−5 g/ml, this blockade does not have all the characteristics of the adrenergic neuron blockade produced by xylocholine.
The mode of action of insulin potentiation by mebanazine
Authors: Barrett A M 
Published: April 2011

Abstract
Chronic oral treatment of rats with mebanazine potentiated the hypoglycaemic response to insulin both in intensity and duration. A similar potentiation of intensity but not of duration was observed in pair-fed animals. In consequence, mebanazine-treated rats subjected to a 21 h fast before insulin died in hypoglycaemic coma whereas control and pair-fed animals did not. Intravenous glucose brought about a rapid return to consciousness in moribund mebanazine-treated rats in insulin coma but hyperglycaemic catecholamines did not. The observed hypoglycaemic unresponsiveness was not solely due to depletion of liver glycogen since both control and treated rats had undetectable levels of glycogen after fasting, yet only the treated animals died. Tissue levels of noradrenaline were raised by mebanazine treatment in brain, heart and liver but these enlarged stores were readily depleted by reserpine. A similar potentiation of hypoglycaemia was observed following chronic treatment of intact rats with tranylcypromine and of adreno-demedullated rats with guanethidine and bethanidine. No potentiation was observed with reserpine or α-methyldopa in either type of animal. Blood glucose was significantly raised by adrenaline and α-methylnoradrenaline, but not by octopamine. The observations support the hypothesis that hypoglycaemic unresponsiveness following chronic inhibition of monoamine oxidase is due to a replacement of noradrenaline in adrenergic neurons by octopamine. This substance is an ineffective hyperglycaemic agent and its physiological release in response to hypoglycaemia does not bring about a return to normoglycaemia.
Inhibition of enzymes by alkylsalicylic acids
Authors: McCoubrey A , Smith M H , Lane A C 
Published: April 2011

Abstract
5-n-Alkylsalicylates inhibited a variety of enzymes that transform acidic substances, viz. glucose-6-phosphate dehydrogenase, glyoxalase, xanthine oxidase, carbonic anhydrase and D-amino-acid oxidase. Inhibitory potency rose to a peak at the n-nonyl derivative. None of the tests were of value, either singly or in combination, as screening processes for anti-inflammatory activity. The comparable results with a trinitrobenzaldehyde reagent suggest that the various inhibitions arise by non-specific association of the drugs with arginine and lysine residues in proteins.
The effect of granule properties on the pore structure of tablets of sucrose and lactose
Authors: Ganderton D , Selkirk A B 
Published: April 2011

Abstract
Air permeability and liquid penetration of tablets of sucrose and lactose have been measured. The tablets had been compressed over a wide pressure range from granules which varied in bulk density, size and strength. The degree to which inter- and intra-granular pore structure within the tablet was sustained varied with these properties; low pressure, high density, high strength and large size promoting a more open but less uniform structure. Such structures allowed rapid penetration of liquid through a coarse pore network which isolated a large fraction of the total pore space. Thus tablets of high permeability gave low final degrees of saturation whereas less permeable tablets became fully saturated.
The effect of sodium salicylate on the binding of long-chain fatty acids to plasma proteins
Authors: Dawkins P D , McArthur J N , Smith M J H 
Published: April 2011

Abstract
Salicylate causes a release of palmitic, stearic, oleic and linolenic acids from their binding sites on human plasma proteins and bovine albumin. The implications of this finding with respect to other effects of salicylate on fatty acid metabolism are discussed.
Medicament release from fatty suppository bases
Authors: Baichwal Malati R , Lohit T V 
Published: April 2011

Abstract
The consistency in terms of viscosity index and the rheology of mixtures of cacao butter with different fats was examined with a Stormer viscometer. Most bases showed shear rate thickening at low stresses and marked fall in consistency between 35°–40°. The drug release from them was related inversely to the consistency of the bases.
Pharmacological actions of phosphocholine 2,6-xylyl ether bromide (phospho-TM10; PTM10)
Authors: Hughes I E 
Published: April 2011

Abstract
PPP-Trimethyl-2-(2,6-xylyloxy)ethylphosphonium bromide (PTM10; phospho-TM10), the phosphorus analogue of xylocholine (TM10), has been found to possess local anaesthetic, α-adrenoceptor and ganglion blocking properties. It also shows a blocking action at the neuromuscular junction but has no detectable adrenergic neuron blocking properties. The relation of these results to the ‘cholinergic link” hypothesis of Burn and Rand is discussed.
The influence of angiotensin on the uptake of noradrenaline by the isolated heart of the rabbit
Authors: Schümann H J , Starke K , Werner U , Hellerforth R 
Published: April 2011

Abstract
The influence of angiotensin on the removal of noradrenaline (10 ng/ml) from the perfusion medium and on the net-uptake of noradrenaline (5 and 20 μg/ml) was examined in the rabbit isolated heart. Concentrations of angiotensin, known to augment the output of noradrenaline from rabbit heart during sympathetic nerve stimulation, did not inhibit the removal of infused noradrenaline from the perfusion fluid. Only very high concentrations of angiotensin (13 μg/ml) significantly diminished the loss of noradrenaline. The positive inotropic effect of noradrenaline was not potentiated by angiotensin. On the other hand, cocaine, in doses which enhance the output of noradrenaline during sympathetic stimulation greatly reduced the loss of noradrenaline from the perfusion fluid. Neither angiotensin (130 ng/ml) nor metanephrine (5 and 20 μg/ml) significantly influenced the net-uptake of noradrenaline from high concentrations. The observations made support the assumption that an increase of transmitter liberation rather than inhibition of transmitter inactivation is responsible for the increase caused by angiotensin in the output of noradrenaline during stimulation of sympathetic nerves.
The compression properties of lactose
Authors: Alpar Oya , Hersey J A , Shotton E 
Published: April 2011

Abstract
The tabletting characteristics of crystalline and spray dried lactose under direct compression have been examined together with the effect of particle size, shape and storage of the powders. The results indicated that the particle size had little effect, although there was a general tendency for the compact strength to increase as the particle size decreased. On the other hand, the particle shape and storage of the powder influenced the strength of the tablets and the force lost to the die wall. The 22 μm and 35 μm fractions of spray dried lactose—especially the latter—were almost entirely very regular spherical particles which resulted in the strongest tablets, whereas fractions below or above contained many more angular particles resulting in weaker tablets. Storage of the small particle size fraction of the crystalline material appeared to induce aggregation, and on compaction, a harder tablet was formed, accompanied by a decrease in the force lost to the die wall.
The alkaloidal pattern in the leaves, stem-bark and root-bark of Mitragyna species from Ghana
Authors: Shellard E J , Sarpong K 
Published: April 2011

Abstract
The leaves, stem-bark and root-bark of Mitragyna ciliata, M. inermis and M. stipulosa have been examined quantitatively and qualitatively for alkaloids. In addition, the plant parts of M. stipulosa collected at 12 regular monthly intervals have been similarly examined. The presence of mitraphylline in the leaves of this plant and the absence of indole alkaloids was confirmed. The predominant leaf alkaloids are oxindoles of the A series, those of the stem- and root-bark, oxindoles of the B series. Whereas the general alkaloidal pattern of M. ciliata appears similar to that of M. inermis rather than M. stipulosa, a more detailed study suggests that M. ciliata and M. inermis have a distinctly different metabolic pattern in relation to the C(9)-OMe alkaloids.
Physico-chemical studies of analgesics. The protein-binding of some p-substituted acetanilides
Authors: Dearden J C , Tomlinson Eric 
Published: April 2011

Abstract
The binding of fifteen p-substituted acetanilides to bovine serum albumin is examined at pH 7·2. An excellent correlation is obtained between the binding enthalpy and Hammett’s substituent constant, s̀. This is interpreted to mean that the binding is non-specific in nature. A very good correlation is also obtained between the entropy of binding and s̀, which suggests that the extent of hydration of unbound drug is a function of the charge separation within the drug molecule. Of the compounds examined, those that have been used clinically as analgesics possess the best thermodynamic properties, being neither so fully bound as to give low free drug concentrations in the bloodstream, nor so little bound that there is no sustained action.
The effect of rate of loading on the strength of tablets
Authors: Rees J E , Hersey J A , Cole E T 
Published: April 2011

Abstract
The breaking strength of tablets containing lactose and microcrystalline cellulose has been determined using an Instron Universal Testing Instrument at loading rates corresponding to cross-head movements of 0·05 to 5·0 cm min−1. For tablets of 2 to 30 kg, nominal strength, an increase in the loading rate produced a significant increase in the breaking strength, although the absolute increase in the mean strength value was only 2 kg for the strongest tablets. The standard deviation of replicate values was apparently unaffected by loading rate. Results obtained using the motorized Heberlein and Erweka instruments to determine the strength of compressed tablets, indicated that discrepancies in the strength values may be partially attributed to differences in the rates of loading.
An investigation of the pore structure of tablets of sucrose and lactose by mercury porosimetry
Authors: Selkirk Alastair B , Ganderton David 
Published: April 2011

Abstract
The pore structure of tablets has been investigated by mercury porosimetry. Tablets, when prepared from ungranulated powder, showed a narrow pore size distribution, the mode of which decreased from 9 to 1 μm over the pressure range studied. Granulation caused the size distribution of tablet pores to widen. Large robust granules, compressed at low pressures, gave tablets with a bimodal pore size distribution. Decrease in granule size and strength, promoted a more uniform tablet structure and fine, friable, granules, compressed at high pressures, gave tablets with almost the same structure as those prepared from ungranulated powder.
An infrared study of solute-solvent interactions of testosterone propionate
Authors: James K C , Noyce P R 
Published: April 2011

Abstract
Interactions between testosterone propionate and 10 different organic solvents have been investigated by observing the shifts of the stretching frequencies of the ketone and ester carbonyl groups. The shifts are shown to be approximately proportional to the degree of deviation from regular solution behaviour. The solvents are classified into three groups and the possible interactions in each discussed.
Adsorption of non-ionic surfactants at the griseofulvin-solution interface
Authors: Elworthy P H , Guthrie W G 
Published: April 2011

Abstract
The adsorption from solution onto griseofulvin powder of a series of non-ionic detergents of the polyoxyethylene glycol mono alkyl ether type is described. Results are also given for polyethylene glycol 400 and a new detergent, pentaerythritol mono-n-octyl ether, whose synthesis and purification is reported. The effect of temperature on the adsorption is studied and possible explanations of the variation of adsorption with temperature are based on the orientation of the molecules at the interface; this is deduced from measured molecular areas.
The use of a bromide ion selective electrode for the measurement of counter-ion activity in cationic surfactant solutions
Authors: Pearson J T , Humphreys K J 
Published: April 2011

Abstract
A bromide ion selective electrode has been used in conjunction with a saturated calomel reference electrode to measure bromide ion activity in solutions of n-decyl, n-dodecyl, n-tetradecyl and n-hexadecyl 1-trimethylammonium bromides at 30°; the critical micelle concentrations of the surfactants were measured by electrical conductance. Calibration of the electrode pair in potassium bromide solutions produced a linear response over the range 0·5 to 5·0p Bra− with a slope of 59·1 mV for a 10-fold change in activity. Results for the surfactants were treated to give values for the degree of micellar dissociation; literature values for this quantity reveal wide variation depending on the technique used.
On the release of drug from hard gelatin capsules
Authors: Newton J M , Rowley G 
Published: April 2011

Abstract
The effect of particle size and packing on the in vitro release of a water-insoluble hydrophobic drug from hard gelatin capsules has been related to the liquid permeability of powder beds of similar porosities. Drug release and permeability decrease with a decrease in particle size and porosity of the powder bed. A simple moist granulation process transforms a non-permeable powder bed, which allows low drug release, into one with high permeability and high drug release.
The absorption and excretion of carbenoxolone in man
Authors: Downer H D , Galloway R W , Horwich L , Parke D V 
Published: April 2011

Abstract
Blood, urine and bile concentrations of carbenoxolone have been measured after oral dosage to patients. The compound is rapidly absorbed attaining high blood concentrations and, as with rats, is excreted mostly in the bile, with only traces (2% of the dose) appearing in the urine. Blood concentrations of the drug generally exhibit two maxima, at 1–2 and 3–6 h after dosage, which are taken to indicate enterohepatic circulation of the biliary-excreted conjugates. As absorption of orally administered carbenoxolone is so rapid and does not occur when the gastric contents have pH &gt;2, it is inferred that the major site of absorption is the stomach. The high blood concentrations of carbenoxolone (60% of the dose present in the blood) are probably due to a high degree of binding of the drug to the plasma proteins. In contrast to the rat, in which carbenoxolone is largely hydrolysed to β-glycyrrhetic acid before absorption, in man carbenoxolone is absorbed largely unchanged and is excreted in the bile as the glucuronide. Gastric absorption of carbenoxolone may be necessary for the increased production of gastric mucus observed with the drug and hence is necessary for its gastric ulcer-healing activity.
The effect of nialamide, pargyline and tranylcypromine on the removal of amphetamine by the perfused liver
Authors: Trinker Fedora R , Rand M J 
Published: April 2011

Abstract
Nialamide, pargyline and tranylcypromine, three monoamine oxidase inhibiting drugs, and the microsomal enzyme inhibitor SKF 525-A significantly decreased the amount of amphetamine removed from the portal circulation of the isolated perfused liver of the cat. The enhancement of the vascular actions and toxicity of amphetamine by monoamine oxidase inhibitors could be explained in terms of these findings.
The effects of temperature on the critical micelle concentrations of alkyl α-picolinium bromides
Authors: Adderson J E , Taylor H 
Published: April 2011

Abstract
The temperature dependence of the critical micelle concentrations of decyl, dodecyl and tetradecyl α-picolinium bromides has been determined by measurement of conductance. Constants for the equation relating log. CMC and alkyl chain length have been calculated for the temperature range 5° to 70°, in increments of 5°. An estimate of the effect of temperature upon the degree of counterion binding is recorded. Thermodynamic parameters have been calculated using the uncharged phase-separation model and a theoretical interpretation of the process of micellization given.
Moisture uptake and tensile strength of bulk solids
Authors: Eaves T , Jones T M 
Published: April 2011

Abstract
An apparatus is described in which bulk solid handling properties can be examined over a wide range of humidities. It is shown that constant temperature and relative humidity can be maintained. The apparatus can also be used to study the effect of cycles of humidity changes. The rate of moisture uptake by loosely packed and tapped beds of six pharmaceutical materials was found to be dependent upon bed depth but independent of bulk density. The tensile strengths of the bulk solids changed when they were subjected to high relative humidities.
Salicylate and enzymes
Authors: SMITH M J H , DAWKINS P D 
Published: April 2011

Abstract
Salicylate inhibits the activities of a number of cellular enzymes and in some instances the mechanisms of inhibition have been established (Smith, 1968a). Reported inhibitory actions of the salicylate ion on important enzyme systems in vitro are now reviewed and assessed in relation to the known clinical and toxic effects of the drug.
The significance of differences in the potency of enantiomers of anti-acetylcholine drugs
Authors: BRIMBLECOMBE R W , INCH D M GREEN T D , THOMPSON PAMELA B J 
Published: April 2011

Abstract
The anti-acetylcholine potencies of the dimethylaminoethyl and N/-methyl piperidin-4-yl esters of R and S 2-cyclohexyl-2-hydroxy-2-phenylacetic acid and their quaternary derivatives have been measured by in vitro and in vivo procedures. The R-enantiomer of dimethylaminoethyl-2-cyclohexyl-2-hydroxy-2-phenylacetate was approximately 100 times more active than the corresponding S-enantiomer both in vivo and in vitro. In contrast, the differences in potencies of the enantiomers of the other compounds were smaller in vivo than in vitro and moreover, the in vivo differences in potency decreased as the potency of the racemates increased. The relevance of these results to general studies of enantiomeric differences is discussed.
The identification of tablets and capsules containing barbiturates by MATR infrared spectroscopy
Authors: ATKINSON J E 
Published: April 2011

Abstract
The technique of MATR infrared spectroscopy has been used to record the infrared spectra of a variety of barbiturate-containing tablets and capsules. The production of different spectra for preparations containing different active ingredients, and the absence of spectral variations arising from the source of manufacture and the presence of tablet and capsule additives, indicate the technique to have possible application in the identification of tablets and capsules, especially where only small samples (1–2 mg) are available.
The gas-liquid chromatographic estimation of phenacetin and paracetamol in plasma and urine
Authors: PRESCOTT L F 
Published: April 2011

Abstract
Methods are described for the gas-liquid chromatographic estimation of phenacetin and paracetamol in plasma and free and conjugated paracetamol in urine. p-Chloracetanilide and p-bromacetanilide were used as internal standards. The drugs were extracted with ethyl acetate and before chromatography were converted to trimethylsilyl derivatives with N,O-bis(trimethylsilyl)acetamide (simultaneous assay of phenacetin and free paracetamol in plasma), or N-trimethylsilylimidazole (assay of paracetamol alone). Phenacetin was extracted with chloroform and chromatographed directly. Paracetamol glucuronide and sulphate were hydrolysed enzymatically to the parent compound before extraction. Recovery of added phenacetin and paracetamol in plasma at concentrations of 1–100 μg/ml was complete, and the limit of detection of the drugs in plasma was 0.05 μg/ml.
The sizing of some powder and liquid sprays from pressurized packs by air sedimentation
Authors: HIRST CHRISTINE A , KAYE R C 
Published: April 2011

Abstract
The construction and testing of an apparatus suitable for the size analysis of certain pressurized sprays by air sedimentation is described. Talc spray size was related to the size of the talc used to prepare the pressurized pack. For other powders (UFI and neomycin sulphate) the sprays were much larger than the powder used to prepare the pack. The use of propellents of higher vapour pressures, higher pack temperatures and the addition of 0·5% sorbitan monolaurate resulted in smaller talc sprays. Talc spray size was increased by the addition of 0·5% isopropyl myristate. Increasing the viscosity of the liquid product and increasing the concentration of propellent gave a reduction in liquid spray size; for both liquid and talc sprays, smaller sprays resulted from the use of a valve housing with a vapour tap.
Effects of acetylsalicylic acid on serum protein binding and metabolism of tryptophan in man
Authors: SMITH HEATHER G , LAKATOS CLAIRE 
Published: April 2011

Abstract
In normal persons, ingestion of aspirin causes a release of tryptophan from its binding site on serum albumin. There is a fall in bound and total serum tryptophan concentrations and a rise in free tryptophan concentrations. The urinary excretion of 3-hydroxyanthranilic acid is decreased, that of xanthurenic acid is increased and that of 3-hydroxykynurenine was increased in 4 out of 6 subjects, indicating an effect on the enzyme systems involved in the metabolism of tryptophan. Conjugates of these metabolites were shown to interfere with the method of assay of the unconjugated hydroxy acids by column chromatography. To overcome this difficulty all urine samples were first boiled in molar hydrochloric acid to hydrolyse any conjugates present. Any results obtained using non-hydrolysed urines would be misleading. This work shows that it is important to take account of the drugs used in treatment before ascribing changes in tryptophan metabolism to pathological states.
Mass spectrometry of fluorinated corticosteroidal 1,4-dien-3-ones of the British Pharmacopoeia
Authors: LODGE B A , TOFT P 
Published: April 2011

Abstract
The mass spectrum of each of the B.P. 1968 fluorinated corticosteroidal 1,4-dien-3-ones is shown to be sufficiently characteristic to be of value as a means of identification. Mechanisms for the principal fragmentations are discussed.
Modifications of the responses to antidiuretic hormone by hydrolytic enzymes
Authors: CUTHBERT A W , PAINTER M E 
Published: April 2011

Abstract
Proteolytic enzymes (trypsin and α-chymotrypsin) and lipolytic enzymes (phospholipases A & C) have been used to treat both surfaces of the skins of frogs and toads. The effects of the enzymes on sodium transport (frog skin) and hydraulic flow (toad skin) have been measured, together with the effects on the responses to ADH. With the experimental conditions used, proteolytic enzymes reduced resting sodium transport but had no major effect on the responsiveness to ADH. Conversely these enzymes had no effect on resting hydraulic flow but reduced or abolished the responses to ADH. Phospholipases applied to the inner surfaces of skins affected neither water nor sodium movement but abolished the responses to ADH. Phospholipases applied to the outside enhanced the effect of ADH on water flow but had no effect on the increased sodium movement caused by ADH. The results are discussed in terms of the possible removal of calcium binding sites by phospholipases.