bluuebunny/crossref_metadata_2025_split huggingface dataset:
Solubilization Kinetics of a Triglyceride/n-Alkane Mixture in a Non-ionic Surfactant Solution
Authors: Carroll B J , Doyle P J 
Published: April 2011

Abstract
The kinetics of solubilization in a non-ionic surfactant solution of pure n-hexadecane, pure triolein and a mixture of the two oils have been investigated. The rates were determined from observations of the dissolution of a single, microscopic droplet, using a drop-on-fibre technique. Conditions were such that negligible saturation of the micellar surfactant with solubilizate occurred. The rate of solubilization of each of the pure oils was found to be independent of time, hexadecane solubilization on a volume basis being about 8 times as rapid as that for triolein. The rate of solubilization of a mixture of the two oils, having a volume fraction 0.69 for triolein, was found to vary in the medium term, the rates apparently being steady both initially and (at a lower value) in the long term. These observations can be related quantitatively to the rates found for the pure oils.
The effect of hydrochlorothiazide on the composition of renal papillary interstitial fluid in the rat
Authors: Shirley D G , Skinner J , Walter S J 
Published: April 2011

Abstract
The effect of chronic hydrochlorothiazide administration on the composition of renal papillary interstitial fluid was investigated in the rat. Hydrochlorothiazide alone had no effect on papillary composition. However, when the sodium depletion that usually accompanies thiazide treatment was minimized by allowing the rats access to hypertonic NaCl solution, hydrochlorothiazide administration resulted in significant reductions in papillary osmolality, and sodium and potassium concentrations. It is suggested that the effects of hydrochlorothiazide on the renal papilla might be mediated by thiazide-induced hypokalaemia, and that under normal circumstances these effects are masked by the concomitant sodium depletion.
Twenty-one hormones fail to inhibit the brain to blood transport system for Tyr-MIF-1 and the enkephalins in mice
Authors: Banks William A , Kastin Abba J 
Published: April 2011

Abstract
Tyr-MIF-1 (Tyr-Pro-Leu-Gly-amide) and methionine enkephalin are transported intact across the blood-brain barrier by a saturable, stereospecific system. This system has been found to be modulated by a few non-peptide substances and by certain conditions such as ageing and some stresses. We investigated the possibility that hormones structurally unrelated to Tyr-MIF-1 and the enkephalins might also be capable of modulating this transport. Twenty-one hormones were tested including steroids, proteins, glycoproteins, peptides, and thyroid hormones, in doses ranging from 0.01 pmol to 1 nmol/mouse by injecting each hormone directly into the lateral ventricle simultaneously with [125I]Tyr-MIF-1. No clear effect on transport could be established for any of the substances at the doses tested. None of these substances seemed able to act as competitive inhibitors, to share their respective transport systems with Tyr-MIF-1, or to modulate immediately the saturable transport system.
Dopamine and apomorphine do not modulate the uptake of [3H]D-aspartate in the rat striatum in-vitro
Authors: O'Connor Ian , Cowburn Richard F , Hardy John A , Fowler Christopher J 
Published: April 2011

Abstract
Sodium-dependent [3H]D-aspartate uptake was measured in rat striatal homogenates. The uptake was inhibited by both L- and D-glutamate, with IC50 values of 5.6 and 224 μM, respectively. Dopamine (10−7–10−4 M), apomorphine (10−7 M), sulpiride (10−6 M) or a combination of dopamine and sulpiride were found not to affect the observed uptake of [3H]D-aspartate. Thus, the in-vitro dopaminergic modulation of high affinity glutamate uptake reported in the literature is not found when [3H]D-aspartate is used instead of [3H]L-glutamate.
Characterization of Sodium Carboxymethylcellulose-Gelatin Complex Coacervation by Chemical Analysis of the Coacervate and Equilibrium Fluid Phases
Authors: Koh Geok-Lay , Tucker Ian G 
Published: April 2011

Abstract
The complex coacervation of sodium carboxymethylcellulose (SCMC) and gelatin has been characterized by chemical analyses of the coacervate and equilibrium fluid phases. The phenol-sulphuric acid (for SCMC) and Lowry (for gelatin) assays were used. Chemically analysed coacervate yield was used to predict optimum coacervation conditions, which occurred at a SCMC-gelatin mixing ratio of 3:7 at pH 3.5. The effects of pH, colloid mixing ratio and total colloid concentration on coacervate yield and composition were studied. The colloid mixing ratio, at which the peak coacervate yields occurred varied with coacervation pH. Increase in the total colloid concentration suppressed coacervation, resulting in a coacervate of higher water content. A similar coacervation mechanism was seen for two viscosity grades SCMC. However, because of the different degree of substitution of these two grades the SCMC-gelatin coacervates had different SCMC contents.
The Effects of Inclusions and Conditions of Storage on the Mechanical Properties of Maize Starch and Methylcellulose Films
Authors: Ononokpono Okon E , Spring M S 
Published: April 2011

Abstract
Films of methylcellulose and gelatinized maize starch were tested in tension, with and without 0.01–10% of additive in the film. The effects of these inclusions on the physical properties of the films have been found to be statistically significant in almost every case. The films, with and without inclusions, have also been conditioned at four different relative humidities and the behaviour of these films has also been considered. In general films were weakened by the presence of additives particularly at higher concentrations. The properties of methylcellulose films were changed most at specific concentrations of the inclusions, this effect was not found with maize starch films. Plasticization of maize starch films was not achieved.
The Distribution of Doxorubicin in Mice Following Administration in Niosomes
Authors: Rogerson A , Cummings J , Willmott N , Florence A T 
Published: April 2011

Abstract
Large multilamellar non-ionic surfactant vesicles (niosomes) with diameters of around 800–900 nm prepared from a C16 triglyceryl ether with and without cholesterol and containing doxorubicin (Adriamycin) were administered to S180 tumour-bearing NMRI mice by bolus injection. Although in-vitro drug release from cholesterol-containing niosomes is delayed, in-vivo there was little difference between the two preparations when plasma levels were compared. As previously observed, half-lives of the drug were prolonged compared with free solution profiles. Liver uptake was not significantly affected by niosome encapsulation of doxorubicin. There is minor accumulation of drug in the lung, perhaps because of aggregation of the vesicles and their physical entrapment. Tumour levels of drug were higher following administration of cholesterol-containing niosomes and this was reflected in the more effective reduction in tumour growth. Metabolism of doxorubicin is altered by niosomal administration, but more studies are required before the significance of the metabolic data can be assessed.
The effect of capsule size and density on transit through the proximal colon
Authors: Parker G , Wilson C G , Hardy J G 
Published: April 2011

Abstract
Colonic transit of radiolabeled capsules has been monitored in 18 healthy subjects using gamma scintigraphy. The capsules ranged in volume from 0.3–1.8 cm3 and in density from 0.7–1.5 gcm−3. The capsules were administered after an overnight fast and entered the colon, on average, 5 h after dosing. Transit rates through the proximal colon were independent of capsule density. Any effect due to capsule volume was small when compared with intersubject variations in transit rates. Within 10 h of entering the colon 80% of the units had reached the splenic flexure. These findings have implications in the design of non-disintegrating, sustained release dosage forms.
Paracetamol Confers Resistance to Ethanol-induced Gastric Mucosal Damage in Rats
Authors: Poon Y K , Cho C H , Ogle C W 
Published: April 2011

Abstract
Paracetamol given orally or subcutaneously did not produce any observable gastric mucosal damage, nor did it change the acidity of the residual secretion in rat stomachs. However, it delayed the gastric emptying rate and increased the residual volume of gastric secretion. Pretreatment with paracetamol 250 mg kg−1 significantly prevented ethanol-induced gastric ulceration. Although it did not influence ethanol-stimulated acid secretion, it increased the mucosal mucus content in the ethanol-treated animals. The findings suggest that the protective mechanism of paracetamol against ethanol-induced damage is likely to be due to improved gastric mucosal integrity, through an increase in the adherent mucosal mucus which protects the underlying delicate cellular structures.
Inhibition of the Multiplication of Enveloped and Non-enveloped Viruses by Glucosamine
Authors: Delgadillo R A , Berghe D A Vanden 
Published: April 2011

Abstract
Glucosamine can inhibit the development of viral cytopathogenic effect and the production of infective viral particles of both enveloped and non-enveloped viruses. The extent of antiviral activity is dependent on drug concentration, composition of the culture medium and type of cell host.
Actions of Buspirone in a Putative Model of Anxiety in the Mouse
Authors: Costall B , Kelly M E , Naylor R J , Onaivi E S 
Published: April 2011

Abstract
In a two-compartment box divided into a dark area and a brightly illuminated white area, mice taken from a dark environment showed aversion to the light and exhibited preference for exploratory rearings and line crossings in the black area. The peripheral administration of buspirone, and its injection into the dorsal raphe nucleus, lead to an increased time spent in the white area associated with enhanced exploratory behaviour with a decreased incidence of rearings and line crossings in the black section. In contrast, the injection of 5-hydroxytryptamine and 2-methyl-5-hydroxytryptamine into the dorsal raphe nucleus increased exploratory behaviour in the black section with decreased activity in the white area: the effects of 2-methyl-5-hydroxytryptamine were antagonized by buspirone administered peripherally. Ritanserin, methysergide, metergoline and cyproheptadine failed, in non-sedative doses, to influence exploratory behaviour in the two-compartment system and ritanserin and methysergide also failed to antagonize the effects caused by 2-methyl-5-hydroxytryptamine. It is concluded that in the mouse model the ability of buspirone to reduce the aversive response to a brightly illuminated area may reflect an anxiolytic action, that the dorsal raphe nucleus may be an important locus of action, and that the effects of buspirone may reflect an interaction at 5-hydroxytryptamine receptors.
Characterization of the sphericity of particles by the one plane critical stability
Authors: Chapman S B , Rowe R C , Newton J M 
Published: April 2011

Abstract
A method has been developed to characterize the roundness of particles in terms of the angle necessary to tilt a plane such that the particles would roll, the ‘one plane critical stability’. The method is based on determination of the centre of gravity of the particle from a digitized image of the coordinates of its outline and computing the angle necessary to incline a plane such that the centre of gravity moves outside the boundary of the particle. The method is particularly applicable to differentiate between the various shapes formed during the production of spherical granules by extrusion/spheronization.
Actions of amrinone and milrinone on the guinea-pig ileum
Authors: Stone T W , Paton D M 
Published: April 2011

Abstract
The pharmacological activity of the cardiotonic agents amrinone and milrinone has been examined on the isolated guinea-pig ileum. Both compounds antagonised the presynaptic inhibitory action of adenosine on electrically evoked contractions, milrinone being the more potent. Higher concentrations of amrinone or milrinone produced contractions of the ileum which were prevented by atropine. Contractile responses to adenosine 5′-monophosphate were not inhibited by atropine. It is concluded that amrinone and milrinone can antagonise some effects of purines but this does not represent their only pharmacological action.
Evaluation of the Sorbent Suspension Reciprocating Dialyser in the Treatment of Overdose of Paracetamol and Phenobarbitone
Authors: Shihab-Eldeen Aida A , Peck Garnet E , Ash Stephen R , Kaufman Geraldine 
Published: April 2011

Abstract
Poisoning with paracetamol (acetaminophen) and phenobarbitone is a common occurrence in the United States and Europe. The removal efficiency of these drugs by a sorbent suspension reciprocating dialyser (SSRD) has been investigated. The SSRD is a parallel plate dialyser with a reciprocating blood flow and free mobile sorbent suspension composed of charcoal and zeolites. This arrangement provided a system with minimal sorbent saturation. High performance liquid chromatography was used for the quantification of the drugs in aqueous and serum fluids. The in-vitro removal efficiency of the dialyser was studied by dialysing a large volume of the drug in solution for 12 to 16 h. The removal efficiency remained relatively constant up to 10 h of dialysis. The in-vivo dialysis studies were performed using normal dogs. Large doses of the drugs were administered orally or intravenously to achieve high blood levels. The clearance values obtained from these studies were comparable with, or in excess of, the values reported in the literature for conventional dialysers. The major advantage of the SSRD is the ability of the unit to be used for prolonged dialysis and to provide a system with minimal sorbent saturation due to mixing and interchange of sorbent granules next to the membrane surface.
Cardiovascular and Renal Actions of Calcium Channel Blocker Chemical Subgroups: a Search for Renal Specificity
Authors: Barrett Richard J , Wright Kathryn F , Taylor David R , Proakis Anthony G 
Published: April 2011

Abstract
The diuretic and natriuretic responses to structurally distinct classes of Ca2+ channel blockers have been compared, to determine whether any agent provoked K+-sparing natriuresis, and to assess the relation of such responses with drug effects on blood pressure. Conscious normotensive Sprague-Dawley rats received vehicle or one of the following drugs in an oral saline load (40 mL kg−1): nifedipine, nimodipine, nitrendipine, prenylamine, cinnarizine, flunarizine, diltiazem, verapamil, hydrochlorothiazide, amiloride, or hydralazine, at doses from 0.316 to 100 mg kg−1. Urine was collected for 6 h. Blood pressure was monitored directly in parallel studies. Diltiazem (31.6, 100 mg kg−1) and flunarizine (100 mg kg−1) enhanced urine and electrolyte excretion in spite of marked hypotension; diltiazem was the only drug to produce dose-related renal responses. In contrast, equihypotensive doses of hydralazine and nifedipine produced overt urine and electrolyte retention. Nitrendipine and prenylamine (0.316 mg kg−1 each) produced slight diuresis or natriuresis without altering blood pressure; higher doses had no effect. The 31.6 mg kg−1 doses of verapamil, nitrendipine, and nimodipine markedly reduced blood pressure, but neither enhanced nor limited urine and electrolyte excretion. Cinnarizine failed to produce any cardiovascular or renal effects. Diuretic responses evoked by the Ca2+ channel blockers were not class-specific, showed no tendency towards sparing K+, were generally weaker than those produced by low doses of amiloride or hydrochlorothiazide, and were dissociable from drug-induced changes in blood pressure.
A Three Dimensional Receptor Model of the Dopamine D2 Receptor from Computer Graphic Analyses of D2 Agonists
Authors: Manallack David T , Beart Philip M 
Published: April 2011

Abstract
Four potent D2 agonists were employed to define a primary pharmacophore for the D2 receptor. Hypothetical receptor points, representing interaction points on a receptor were built on to each molecule. These points and the nitrogen atom were averaged to give the coordinates (Å) of the primary pharmacophore: R1 (0.00, 3.50, 0.00), R2 (0.00, −3.50, 0.00), R3 (5.79, 2.06, 0.00), and nitrogen (5.13, −0.63, 0.37). Eight structural classes of D2 agonists were then superimposed on to the primary pharmacophore to aid in the location of secondary binding sites. The secondary sites include two lipophilic clefts, an area of steric bulk, a region to hydrogen bond ‘meta’ hydroxy groups and a ‘critical region’ accepting methoxy and halogen substituents but not hydroxy substituents. The model has the potential to design and predict activity of novel D2 agonist compounds.
The stable prostacyclin-analogue, iloprost, unlike prostanoids and leukotrienes, potently stimulates cyclic adenosine monophosphate synthesis of primary astroglial cell cultures
Authors: Seregi Andras , Schobert Angelika , Hertting Georg 
Published: April 2011

Abstract
The effect of different eicosanoids on adenosine-3′, 5′-cyclic-monophosphate (cAMP) accumulation in primary astroglial cell cultures prepared from newborn rat brain was studied. The stable prostacyclin-analogue, iloprost, effectively stimulated cAMP synthesis in a concentratioin-dependent, saturable manner, the EC50 being about 3 × 10−8 M. Prostaglandin (PG) E2 was less potent, without reaching plateau even at 10−5 M. Prostaglandins D2 and F2α, and the stable thromboxane A2-analogue, U 46619, as well as leukotrienes (LT) B4, C4, D4 and E4 were not effective and did not attenuate basal or isoprenaline (10−8 M)-stimulated astroglial cAMP formation. This is the first indication for the existence of a prostacyclin receptor coupled positively to the adenylate cyclase in astrocytes. Other eicosanoids are unlikely to be involved in receptor-mediated regulation of astroglial cAMP levels.
Metabolism of fenfluramine to norfenfluramine in guinea-pigs
Authors: Fuller Ray W , Snoddy Harold D , Perry Kenneth W 
Published: April 2011

Abstract
After injection of fenfluramine into guinea-pigs, the N-dealkylated metabolite norfenfluramine was present in brain at higher concentrations and persisted longer than the parent drug, fenfluramine. Contrary to a claim in previous literature, the guinea-pig does metabolize fenfluramine to norfenfluramine, hence the ability of fenfluramine to cause acute and long-term depletion of brain 5-hydroxytryptamine in this species does not prove that fenfluramine, instead of nonfenfluramine, can produce these effects.
Cardiovascular effects of intracerebro-ventricular bradykinin and melittin in the rat
Authors: Thomas G Roger , Hiley C Robin 
Published: April 2011

Abstract
The cardiovascular effects of intracerebroventricular (i.c.v.) bradykinin and melittin were investigated in the anaesthetized rat. Bradykinin, 30 μg, increased mean arterial pressure by 15 mmHg and this was the result of an increase in peripheral resistance; heart rate and cardiac output were unchanged. Tissue blood flow was lower in the skin and spleen in the animals given bradykinin than the controls. Significant increases in tissue vascular resistance occurred in the skin and several organs of the splanchnic region, the spleen, stomach, large intestine and the pancreas/mesentery. Melittin infusion gave a biphasic response in systemic blood pressure in which a depressor response was followed by a pressor phase; the pressor stage was accompanied by an increase in heart rate. Since melittin is a stimulant of membrane bound kallikrein, the results lend limited support to the hypothesis that there is a kallikrein-kinin system endogenous to the central nervous system which is involved in cardiovascular regulation.
Differences in the characteristics of opioid receptor binding in the rat and marmoset
Authors: Yeadon M , Kitchen I 
Published: April 2011

Abstract
The density of μ and δ opioid binding sites in homo-genates of rat and marmoset brain was determined using radio-labelled peptides with high receptor selectivity. In addition the affinity of μ and δ receptor binding of five drugs of the fentanyl series was measured. The ratio of μ:δ sites was similar within each species but the total receptor binding capacity in the rat was double that of the marmoset. The binding affinities for the δ site were dissimilar between the species and supports the hypothesis that the structure of this receptor shows phylogenetic differences. In contrast, μ site binding affinity was identical in rat and marmoset.
Prostaglandin synthetase inhibitors in feverfew
Authors: Pugh W J , Sambo K 
Published: April 2011

Abstract
The IC50 values for the in-vitro inhibition of the prostaglandin synthetase (bovine seminal vesicle mitochondrial fraction) mediated PGE2 production from arachidonic acid by parthenolide, michefuscalide and chrysanthenyl acetate were 11.0 ± 0.44, 121 ± 0.51 and 14.2 ± 0.58 μM (mean ± 95% confidence limits), respectively.
Thermal Characterization of Drug/Polymer and Excipient/Polymer Interactions in Some Film Coating Formulation
Authors: Okhamafe Augustine O , York P 
Published: April 2011

Abstract
Some probable consequences of the dissolution/migration of a major solid dosage component in or into an applied film coating during or after a film coating operation have been investigated using free films of hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) incorporating small amounts of either lactose (a diluent) or ephedrine hydrochloride (a drug). Intrinsic features of the films such as softening, glass transition, crystallinity and melting were examined by differential scanning calorimetry and thermomechanical analysis. Generally, the results indicate that ephedrine hydrochloride exhibited plasticizing activity in both HPMC and PVA films. On the other hand, incorporation of lactose produced an opposite effect (stiffening) in PVA films as demonstrated by increased glass transition temperature and crystallinity. On the basis of these findings, it was proposed that the undesired presence of a component of a solid dosage core in the applied film coating could significantly alter its end-use properties such as diffusivity and the incidence of film coating defects. It was also shown that the application of the relationship of Moelter & Schweizer (1949) in the evaluation of the plasticizer efficiency of non-homologous additives could pose problems of interpretation.
Chemical Reactivity of Aluminium-based Pharmaceutical Compounds used as Phosphate-binders
Authors: Cargill Robert W , Dutkowskij Michael , Prescott Ann , Fleming Laura W , Stewart William K 
Published: April 2011

Abstract
Several aluminium-containing substances, including antacids used as phosphate-binders in treating renal failure, have been analysed in-vitro under different pH conditions for the release of Al3+ ions and for binding of phosphate. Control experiments on different forms of pure aluminium hydroxide validated the methods. At pH 2 it was the most amorphous forms which released Al3+ most rapidly. These aluminium ions, available for absorption by the patient, were released from all antacids tested, but no firm phosphate-binding was detected while the pH remained at 2. Phosphate was bound at pH 8, by adsorption onto the surface of aluminium hydroxide. No significant amounts of free Al3+ exist in solution at pH 8, since at that pH aluminium hydroxide is precipitated. The most amorphous forms of this solid were the most efficient phosphate-binders. Alumino-silicate salts require prior exposure to acid to produce free Al3+ before they can act as phosphate-binders, whereas amorphous aluminium hydroxide acts as an efficient phosphate-binder without prior exposure to acid. Chemical principles are employed to show why aluminium release and phosphate-binding are separate and independent processes. Methods are proposed for maximizing the activity of phosphate- binders in-vivo, while minimising aluminium release.