bluuebunny/crossref_metadata_2025_split huggingface dataset:
Disposition of topically applied sodium cromoglycate in the albino rabbit eye
Authors: Lee Vincent H-L , Swarbrick James , Stratford Robert E , Morimoto Kim W 
Published: April 2011

Abstract
The influence of pH, tonicity, preservatives, polymers and instilled drop size on the disposition of sodium cromoglycate, an agent used in the prophylaxis of vernal keratoconjunctivitis, in the tear chamber of the albino rabbit eye has been examined. Radiotracer techniques were used throughout. The initial decline in concentration in the tear chamber was found to be unaffected by the presence of preservatives, pH, and tonicity over the ranges studied. However, significant increases in the residence time of sodium cromoglycate in the precorneal area were noted when a smaller instilled drop size was used and when 5% polyvinyl alcohol (PVA) was added to the aqueous vehicle. Tissue uptake was found to be greatest in the conjunctiva, followed by the cornea, the iris-ciliary body and the aqueous humor. In both the conjunctiva and the cornea, the addition of 5% PVA produced an elevation in the peak concentration of sodium cromoglycate and an increase in the time at which the peak concentration was achieved, indicating improved drug delivery to these sites.
Precorneal drainage of polyvinyl alcohol solutions in the rabbit assessed by gamma scintigraphy
Authors: Wilson C G , Olejnik O , Hardy J G 
Published: April 2011

Abstract
A method for monitoring the ocular distribution of solutions for ophthalmic use was developed using the technique of gamma scintigraphy. This method was used to monitor the effects of polyvinyl alcohol on the precorneal drainage of [99mTc]pertechnetate in the rabbit. The rate of drainage of solutions decreased on addition of PVA and precorneal residence of the marker was significantly prolonged, compared with saline controls, at a PVA concentration of 5% w/v. Increases in the activity in the inner canthal region mirrored the decrease in corneal counts. The method has a more general application for the study of ophthalmic formulations and devices in larger mammals and in man.
Particle size analysis of microcapsules
Authors: Morris Natalie J , Warburton B 
Published: April 2011

Abstract
To standardize the preparation of three-walled w/o/w microcapsules it was necessary to assess their particle size distribution, since they occur as both unicored and multicored types. The log-normal law, reported to be obeyed by many particulate systems, including microcapsules, was not applicable to the size data. A curve-fitting computer program using least squares minimization was used to assess the size distribution data. The models tested were the unimodal and bimodal log-normal distributions, the bimodal form being the most appropriate. Using the equations to the curves of best fit, the modal size and standard deviation of each population were estimated, and the relative percentages of unicored and multicored microcapsules could be deduced from an analysis of the bimodal curves in which they were represented as the sum of two constituent unimodal distributions.
Inhibition of bacterial DNA cytosine-5-methyltransferase by S-adenosyl-l-homocysteine and some related compounds
Authors: Crooks Peter A , Tribé Malcolm J , Pinney R J 
Published: April 2011

Abstract
S-Adenosyl-l-homocysteine and five related compounds have been evaluated as inhibitors of a DNA cytosine-5-methyltransferase. DNA methylation was assayed in cell extracts from E. coli strain J6-2 dcm+, proficient in DNA cytosine-5-methyltransferase activity, containing substrate DNA isolated from E. coli strain J6–2 dcm−, a strain deficient in DNA cytosine-5-methyltransferase. S-Adenosyl-l-homocysteine and its 7-deaza analogue, S-tubercidinylhomocysteine, were competitive inhibitors of DNA cytosine-5-methyltransferase with Ki’s of 14·2 and 17·6 μm, respectively, in the above enzyme assay.
An in-vitro model of intracellular bacterial infection using the murine macrophage cell line J774·2
Authors: Stevenson M , Baillie A J , Richards R M E 
Published: April 2011

Abstract
A simple model of intracellular bacterial infection based on the ability of the macrophage cell line J774·2 to phagocytose Escherichia coli in a reproducible manner is described. Viable counting of intracellular bacteria and microscopic examination of infected macrophage cultures after treatment with fluorescent E. coli antibody showed that the bacteria multiplied within the J774·2 cells. Viable intracellular bacteria may be used to study the activity of bactericidal and bacteriostatic drugs within the macrophage. The low apparent intracellular bactericidal activity of streptomycin, which was time- and concentration-dependent, accords with a low permeability of the J774·2 macrophages to this antibiotic. An exclusively intracellular infection could be achieved by inactivation of non-phagocytosed extracellular bacteria by streptomycin treatment of infected macrophage cultures. Under appropriate conditions intracellular bacterial viability was unaffected.
Modifications in prolactin binding capacity in the rat liver induced by non-steroidal anti-inflammatory drugs
Authors: Muccioli Giampiero , Bellussi Giuseppina , Lando Donata , Di Carlo Raffaele 
Published: April 2011

Abstract
Modifications in prolactin specific binding in the rat liver induced by different non-steroidal anti-inflammatory drugs (indomethacin, piroxicam, ketoprofen, phenylbutazone, mefenamic acid and acetylsalicylic acid) have been studied. All caused a dose-dependent inhibition of prolactin binding capacity whereas no change was found in dissociation constant values. The inhibitory effect is reversible and highly specific, since insulin binding to the same membrane preparation is not affected. The degree of inhibitory activity on prolactin binding is related to the anti-inflammatory activity of each drug, which supports the hypothesis of an involvement of prostaglandin synthesis.
Effect of secoverine and atropine on intestinal secretion and motor activity in the rat small intestine in-vivo
Authors: Greenwood B , Read N W , Hardcastle P T , Hardcastle J 
Published: April 2011

Abstract
The actions of secoverine and atropine on bethanechol-induced intestinal secretion, hypermotility and transintestinal potential difference were investigated in the rat jejunum in-vivo. Both secoverine (10−7 mol kg−1) and atropine (1·2 times 10−9 mol kg−1) inhibited motility at doses that did not affect secretion or transintestinal potential difference. However, secoverine was a less potent antagonist of all the bethanechol-induced changes than atropine. Increases in transintestinal potential difference were more closely related to production of fluid secretion than to increases in motility.
Distribution coefficients of atenolol and sotalol
Authors: Taylor P J , Cruickshank J M 
Published: April 2011

Abstract
The distribution coefficient (D) of atenolol is lower than that of sotalol, despite the latter’s lower partition coefficient (P). Since D is the relevant quantity under physiological conditions, it is re-established that atenolol is in practice the more hydrophilic. Because of the common confusion between P and D which this case exemplifies, the relation between them is set out.
The prolonged retention of sodium cromoglycate in the rabbit eye
Authors: Swarbrick James , Shrewsbury Robert P 
Published: April 2011

Abstract
The retention of sodium cromoglycate in the rabbit eye over a 6 h period following its administration in two different vehicles is reported. When formulated as a dispersion in a hypo-allergenic acetylated lanolin/paraffins base, prolonged retention was observed. Thus, the concentration of sodium cromoglycate in the tears, conjunctiva and cornea 6 h after administration equalled or exceeded the concentration obtained with an aqueous solution 1 h post-instillation.
Haemodynamic effects of bromocriptine in the conscious spontaneously hypertensive rat
Authors: Struyker-Boudier H A J , van Essen H , Smits J F M 
Published: April 2011

Abstract
The systemic haemodynamic effects of 0·3 mg kg−1 bromocriptine s.c. in conscious, chronically instrumented spontaneously hypertensive rats (SHR) has been investigated. Bromocriptine caused a gradual, long-lasting significant fall in mean arterial pressure with a maximum of 26 ± 3 mmHg (-17%). The fall was related to a significant decrease in stroke volume index (-9 ± 2 μl 100 g−1; -10%) and cardiac index (-3·9 ± 0·8 ml min−1 100 g−1; -12%). No significant changes in heart rate or total peripheral resistance index were observed. These data do not support previous suggestions that the antihypertensive effect of bromocriptine is caused by inhibition of the release of vasopressor substances. It is suggested that bromocriptine causes a reduction of venous return of the blood to the heart, possibly related to intrarenal effects.
Effects of 6-methoxytetrahydro-β-carboline on 5-hydroxytryptamine binding in rat brain
Authors: Taylor Dorothy L , Silverman Peter B , Ho Beng T 
Published: April 2011

Abstract
6-MeOTHBC competes for 5-HT binding sites in rat brain in-vitro and in-vivo. The β-carboline is significantly more active at the type 1 [3H]-5-HT, than the type 2 [3H]spiperone receptors, in-vitro. Following injection, 6-MeOTHBC significantly decreases [3H]-5-HT binding in the cortex. The ineffectiveness on [3H]spiperone binding in-vivo corresponds with the low affinity in-vitro. The effect of 6-MeOTHBC on central 5-HT binding may be a significant aspect of its 5-HT-ergic activity.
Time-related effects of benzodiazepines on intestinal motility in conscious dogs
Authors: Fargeas M J , Fioramonti J , Bueno L 
Published: April 2011

Abstract
The effects of diazepam and GABA on intestinal motility were investigated in fasted dogs fitted with strain-gauge transducers. Injected intravenously at 9.00 and 16.00 h, diazepam (0·5 mg kg−1) affected intestinal motility only during darkness i.e. from 19.00 to 7.00 h. These jejunal motor effects which were mimicked by GABA, (0·3 mg kg−1 i.v.) corresponded to a disruption of the migrating myoelectric complex (MMC) with an increased contractile activity. These results demonstrate that benzodiazepines affect the intestinal motility in dog and suggest that the effects are related to sleep-stages.
Suppression of laxative action of phenolphthalein by orally-administered indomethacin or aspirin
Authors: Capasso F , Mascolo N , Autore G , Duraccio M R 
Published: April 2011

Abstract
Oral administration of phenolphthalein produced a dose-dependent increase of wet faeces excreted by mice. The response to phenolphthalein was reduced by pretreatment with indomethacin, aspirin or polyphloretin phosphate (PPP), but not with benoxaprofen. These findings support the view that the effect of phenolphthalein may be suppressed by PG synthetase inhibitors (indomethacin, aspirin) and by PPP.
Potentiation of cyclo(N-methyl-Tyr-Arg)-induced antinociceptive activity by thyrotropin-releasing hormone in mice
Authors: Kawamura Shunsuke , Sakurada Shinobu , Sakurada Tsukasa , Kisara Kensuke , Akutsu Yasuyuki , Sasaki Yusuke , Suzuki Kenji 
Published: April 2011

Abstract
The effect of thyrotropin-releasing hormone (TRH) and its metabolite, cyclo(His-Pro) (C.HP), on cyclo(N-methyl-Tyr-Arg) (C.NMTA)-induced antinociception as measured by the tail-pressure test in mice has been examined. C.NMTA-induced antinociception was significantly potentiated by simultaneously intracerebroventricular or intraperitoneal injection of TRH (approximately 20–50%) in a dose-dependent manner, whereas the effect of morphine was not influenced significantly by TRH. C.HP had no significant effect on the antinociceptive response induced by C.NMTA or morphine. It is concluded that the mechanism of C.NMTA-induced antinociception may be involved in TRH neuronal system in the brain.
Vehicle effects in ophthalmic bioavailability: An evaluation of polymeric inserts containing pilocarpine
Authors: Saettone M F , Giannaccini B , Chetoni P , GALLI G , Chiellini E 
Published: April 2011

Abstract
A series of polymeric ophthalmic inserts containing pilocarpine were formulated with four different types of polyvinyl alcohol, PVA, and two types of hydroxypropylcellulose. Pilocarpine was present as the nitrate, or as the salt with polyacrylic acid, PAA. In-vivo miosis vs time experiments on albino rabbits, showed that all inserts increased significantly the bioavailability of pilocarpine, with respect to a standard solution of pilocarpine nitrate. Two PVA inserts, containing the PAA-salt of pilocarpine, were particularly effective. The preparations were also submitted to in-vitro release tests and to differential scanning calorimetry, to ascertain the release mechanism, and to verify, via the thermal behaviour, possible interactions between drug and polymers. The chemical and physicochemical factors, most likely to influence the ophthalmic bioavailability of pilocarpine from the present preparations, are briefly reviewed.
Lignocaine kinetics in the rat
Authors: Supradist S , Notarianni L J , Bennett P N 
Published: April 2011

Abstract
After intravenous injection of lignocaine 2·5, 5·0 or 10·0 mg kg−1 in the rat blood concentration declined in a bi-exponential manner. The data were analysed according to a two-compartment open model with elimination from the central compartment. Analysis of variance revealed no significant differences in k12, k21, k13, t1/2α, t1/2β, AUC or in the volume constants for the different doses used. After lignocaine 50·0, 70·0 or 90·0 mg kg−1 by mouth there was no significant change in t1/2β for the different doses or in peak plasma concentration normalized for dose. For both routes of administration blood concentration-time curves were superimposible and AUC was linearly related to dose. Renal excretion was negligible. Systemic availability of lignocaine was the lowest of species so far studied (mean 0·019 ± 0·001) did not alter with dose, and was very similar to the values in the literature quoted for the isolated perfused liver. Clearance of lignocaine related to anticipated liver mass was almost identical to the values for liver blood flow quoted using other techniques. The data indicated high hepatic extraction of lignocaine by the intact rat and the absence of dose dependency within the range studied.
Effect of some benzodiazepines on peripheral neuromuscular function in the rat in-vitro hemidiaphragm preparation
Authors: Driessen J J , Vree T B , Booij L H D J , Van Der Pol F M , Crul J F 
Published: April 2011

Abstract
The effect of equimolar cumulative concentrations of 11 different benzodiazepines on the indirectly evoked twitch contraction was investigated in the rat in-vitro phrenic nervehemidiaphragm preparation. Depending on the pattern of the concentration-response curves two groups of benzodiazepines can be distinguished: (i) a first group with a biphasic action, e.g. potentiation of twitch tension in low concentrations and depression of twitch tension in high concentrations, and (ii) a second group with primary depression of twitch tension with increasing concentrations. All of the tested compounds ultimately caused a 100% depression of twitch tension at concentrations ranging from 0·175 to 0·35 mmol litre−1. Although this peripheral effect of benzodiazepines on neuromuscular function is not the main site of action of these compounds, there are enough arguments to state that it is not a simple toxic effect. There is some evidence from this study that the peripheral component of the benzodiazepine effect on muscle relaxation may involve a multi- rather than one single receptor system.
Xylan–-a possible filler and disintegrant for tablets
Authors: Juslin M , Paronen P 
Published: April 2011

Abstract
Xylan, a novel possible adjuvant for tablets was tested and compared with modified starch, Sta-Rx 1500, for weight variation, strength and disintegration of tablets. There was no remarkable difference in weight variation between the tablets of the corresponding compositions. The tablets containing xylan were stronger and disintegrated more rapidly than those containing modified starch.
Effects of freezing on human skin permeability
Authors: Harrison S M , Barry B W , Dugard P H 
Published: April 2011

Abstract
The percutaneous absorption of water was measured in-vitro at 30 °C for pale caucasian abdominal skin which had been stored at −20 °C for up to 466 days and compared with fresh skin. Prolonged freezing of the skin did not affect the absorption of water which had a mean permeability coefficient of 1·71 ± 0·62 times 10−3 cm h−1 (180 diffusion experiments with 39 skin specimens). No significant difference was found between the absorption of water through human skin which was fresh or had been frozen. The mean permeability coefficient for skin which had not been frozen was 1·30 ± 0·55 times 10−3 cm h−1 for 6 skin specimens.
Acetylcholine-induced inhibition of responses to field stimulation in rabbit pulmonary artery is unaffected by endothelium removal
Authors: Loiacono R E , Story D F 
Published: April 2011

Abstract
Acetylcholine (0·01–10 μmol litre−1) relaxed normal rings (endothelium-retained) of rabbit pulmonary artery precontracted with clonidine (10 μmol litre−1) while preparations with the endothelium removed responded with contraction only. Removal of the endothelium had no effect on contractions of the preparation to clonidine or field stimulation of the adventitial nerves (2 Hz, 10 s). Furthermore, the inhibitory effect of acetylcholine (0·3 and 1·0 μmol litre−1) on contractions induced by field stimulation was not influenced by the vascular endothelium.
The effect of levamisole on gastric ulcers induced in the rat by anti−inflammatory and necrotizing agents
Authors: Evangelista S , Maggi C A , Meli A 
Published: April 2011

Abstract
Levamisole, in doses similar to those required to observe immunostimulation in animals, antagonized dose−dependently, in rats, gastric ulcers produced by necrotizing agents (HCl and ethanol) and NSAIDs (indomethacin and piroxicam) without affecting the anti−inflammatory properties of these latter drugs.
Preliminary study of the disposition in man of acebutolol and its metabolite, diacetolol, using a new stereoselective hplc method
Authors: Sankey M G , Gulaid A , Kaye C M 
Published: April 2011

Abstract
A new stereospecific hplc method that is capable of simultaneously quantitating the S-(-)- and R−(+)−enantiomers of acebutolol and its major metabolite, diacetolol, in plasma and urine, is described. When applied to the assay of biological fluids collected during single and chronic oral dosing with acebutolol (Sectral), this procedure failed to reveal any important stereoselectivity in the disposition of either acebutolol or diacetolol in man. This may occur because acebutolol is metabolized by hydrolysis and N-acetylation, whereas the other β−blockers which exhibit some degree of stereoselective disposition (e.g. metoprolol and propranolol) are primarily metabolized by oxidation.
A contribution, from a possible local anaesthetic action, to the effects of yohimbine on evoked noradrenaline overflow
Authors: Goodall Jacqueline , Hagan R M , Hughes I E 
Published: April 2011

Abstract
Both yohimbine (0·1 to 10 μm) and phentolamine (10 μm) increased the tritium overflow evoked by electrical stimulation (2·5 Hz, 1 ms, 15 V, for 90 s every 20 min) of mouse isolated vas deferens previously incubated with (–)−[3H]noradrenaline. At their maximally effective concentrations, phentolamine (10 μm) produced an effect that was sustained over the 2 h of the experiment while the effect of yohimbine (6 μm) decreased by about 60% over the first 40 min and was then sustained at a lower level. At higher concentrations of yohimbine, the increase in evoked tritium overflow was less marked and at the highest concentration tested (30 μm) evoked overflow was reduced below the levels seen before exposure to the drug. It is concluded that at concentrations maximally effective in inhibiting the presynaptic α−adrenoceptor−mediated mechanism controlling transmitter release, the known local anaesthetic effect of yohimbine may contribute to the overall effect on evoked transmitter overflow.
The use of phenothiazines to enhance the rectal absorption of water―soluble compounds
Authors: Fix Joseph A , Leppert Paula S , Porter Patricia A , Alexander Jose 
Published: April 2011

Abstract
The ability of phenothiazines to enhance the rectal absorption of sodium cefoxitin and gentamicin sulphate from aqueous formulations was examined in rats. In the absence of absorption―promoting adjuvants, sodium cefoxitin and gentamicin sulphate bioavailabilities from the rectal compartment were less than 5% of the corresponding intravenous administration. In aqueous microenemas containing 20 mg ml−1 phenothiazine, sodium cefoxitin bioavailability increased to 16–62%, while gentamicin sulphate bioavailability increased to 74–146%. The absorption―promoting potential of chlorpromazine and perphenazine was concentration―dependent, with significant increases in gentamicin sulphate absorption occurring with 1 mg ml−1 chlorpromazine or 2·5 mg ml−1 perphenazine. Maximal gentamicin sulphate bioavailability and serum concentrations were achieved with 10 mg ml−1 chlorpromazine or 20 mg ml−1 perphenazine. The findings indicate that the phenothiazines, which are well absorbed rectally, also significantly enhance the rectal absorption of watersoluble, poorly absorbed compounds.
Formation of encapsulated hydrophilic polymer beads by combined techniques of bead polymerization and phase separation
Authors: Suryakusuma H , Jun H W 
Published: April 2011

Abstract
A novel and rapid procedure for the preparation of hydrophilic polymer beads coated with ethyl cellulose has been developed. The coated polymer beads were prepared by combining techniques of bead polymerization and phase separation into a single step procedure. The final product has a size range of 200–1000 μm and consists of the core copolymer of 2-hydroxyethyl methacrylate—acrylamide and the barrier membrane of ethyl cellulose. Examination of beads in which amaranth dye was used as a model of active ingredient showed the dye to be uniformly distributed throughout the polymer matrix. Microscopic examination indicated that ethyl cellulose coated the core matrix. The effects of ethyl cellulose concentration, degree of agitation and molar ratio of monomers on the size of coated beads were investigated.
The preparation and characterization of ferrous sulphate hydrates
Authors: Mitchell A G 
Published: April 2011

Abstract
Ferrous sulphate BP, FeSO4, 7H2O, dehydrates to form FeSO4, 4H2O when the relative humidity (RH) is less than 65%, or on heating at 40 °C. The tetrahydrate was also prepared by recrystallization at 60 °C from aqeuous solutions of the sulphate. Commercial dried ferrous sulphate BP is FeSO4, H2O but the method of preparation given in the BP produces FeSO4, 4H2O which is the stable form at RH &lt; 65% (25 °C). A crystalline monohydrate was prepared either by heating the tetrahydrate on a boiling water bath to constant weight or heating the heptahydrate under vacuum at 60 °C in the presence of water vapour evolved from the water of crystallization. An X-ray amorphous form of FeSO4, H2O was made by heating the heptahydrate at 100 °C under vacuum with the removal of water vapour. Crystalline FeSO4, H2O rehydrates to the heptahydrate when RH &gt; 65% but the amorphous form recrystallizes as the stable tetrahydrate at RH &gt; 0 and &lt;65%. The various hydrates were characterized by DSC and X-ray diffraction. A simple procedure is described for obtaining data to construct a RH-composition phase diagram. The method combines measurement of any weight changes of each hydrate after storage at various controlled humidities together with a direct measurement of RH over the hydrate pairs. The thermal dehydration pathways are reported together with the RH-composition phase diagrams.