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PubMed1982

Distribution of bile salts between 1-octanol and aqueous buffer.

The distribution of four bile salts: sodium cholate (I), sodium deoxycholate (II), sodium chenodeoxycholate (III), and sodium ursodeoxycholate (IV), between aqueous buffer and 1-octanol has been measured as a function of temperature between 25 and 55 degrees and as a function of bile salt concentration at concentrations less than 0.1 mole/liter in the aqueous phase. The distribution isotherms obtained have been explained on the basis of reversible association in the aqueous phase. The treatment assumes that the bile acid exists as a monomer in the organic phase, which is verified by vapor pressure osmometry. A graphical method has been employed to estimate the association constants in the aqueous phase for the various equilibria encountered. An aggregation number of four for IV and 12 for I, II, and III has been estimated. From the results, thermodynamic functions associated with the transfer of each of the bile salts from water to octanol and those associated with association processes in the aqueous phase were calculated. These results are consistent with previous findings that the premicellar association of bile salts occurs by hydrophobic interaction. The thermodynamics of transfer of bile salts revealed an unfavorable enthalpic and favorable entropic contribution for all four bile salts. However, for IV, which is an epimer of III, both enthalpic and entropic contributions are reduced, compared to III, suggesting a pronounced effect of stereochemical orientation on hydrophobic interaction.

1-Octanol↗
PubMed1983

Liquid crystal solubilization of cholesterol: potential method for gallstone dissolution.

Solubilization rate and phase equilibrium studies were conducted for cholesterol in aqueous sodium oleate solutions. The components interacted to form a lamellar liquid crystalline phase, and this phenomenon was investigated as a potential method for cholesterol gallstone dissolution. Phase equilibria data for cholesterol-sodium oleate-water showed that the mesophase contained approximately equimolar amounts of cholesterol and oleate with large amounts of water. The cholesterol solubilization rate from a static pellet in sodium oleate solutions was much faster than dissolution in sodium cholate solutions and was independent of oleate concentration from 2.5 to 10%. In these experiments, the medium became a cloudy dispersion of liquid crystalline phase in the micellar solutions. The rate-limiting step in the solubilization process appears to be dispersion of fragments from the liquid crystalline layer on the cholesterol surface. This hypothesis was consistent with the kinetic effects of viscosity, stirring rate, and oleate concentration. By converting cholesterol to a liquid crystalline phase, the solubilization process avoids the limitations for micellar solubility and interfacial resistance which control cholesterol dissolution in bile salt-containing media.

Cholelithiasis↗
PubMed1983

Effects of surfactants on the GI absorption of beta-lactam antibiotics in rats.

The effects of various nonionic and ionic surfactants and two bile salts (sodium cholate and sodium taurocholate) on the GI absorption of beta-lactam antibiotics were investigated using the in situ rat GI perfusion technique. Addition of 10 mM polyoxyethylene-23-lauryl ether in the perfusion solution reduced the absorption of propicillin by the stomach and markedly increased the absorption of propicillin and cefazolin by the small intestine. Ester-type nonionic surfactants and bile salts exerted no significant influence on the intestinal absorption of these antibiotics.

Animals↗
PubMed1988

Bile acid binding and hypocholesterolemic activity of a new anion exchange resin from 2-methylimidazol and epichlorohydrin.

A new anion exchange resin with an imidazolium salt on a epoxide polymer skeleton was synthesized. This white powder material was odorless and tasteless. The in vitro sodium cholate binding of this resin was much more potent than that of cholestyramine. The hypocholesterolemic activity of this resin in cholesterol-fed rabbits proved to be 4.3 times more potent than that of cholestyramine. These results suggest that effective reduction of plasma cholesterol may be achieved with lower doses of this resin.

Animals↗
PubMed1989

Self-association and solubility behaviors of a novel anticancer agent, brequinar sodium.

To aid in the selection of appropriate excipients to formulate brequinar sodium [6-fluoro-2-(2'-fluoro-1,1'-biphenyl-4-yl)-3-methyl-4-quinolinecarboxyli c acid sodium salt; DuP 785], studies were initiated to characterize thoroughly its solubility behavior. The measured solubilities at RT (approximately 23 degrees C) agreed with the theoretical values in the pH range from 0.5 to 7.2, but became significantly greater than theoretical values at pH values above 7.2. This deviation was likely due to the vertical stacking-type self-association between brequinar molecules in water. The NMR and pH methods determined a critical association concentration of 15 mg/mL. Sodium salicylate, which has been proven to interfere with molecular self-association, reduced drug solubility from 116 to 10 mg/mL. But urea, another deaggregative agent, gave about a twofold increase rather than a decrease in solubility. Addition of sodium chloride caused a 226-fold decrease in solubility. The apparent solubility product did not remain constant but decreased as sodium chloride concentration increased, suggesting that the added salt decreased the degree of self-association between brequinar molecules. Among four surfactants examined (a bile salt with a rigid fused ring versus three ordinary surfactants with a flexible chain structure), only sodium cholate significantly increased the aqueous solubility of brequinar sodium.

Antineoplastic Agents↗
PubMed1991

Dissolution rate of griseofulvin in bile salt solutions.

Bile salts increase the apparent solubility of lipophilic poorly water-soluble drugs like griseofulvin. In this study, the dissolution kinetics of griseofulvin in solutions of bile salts (sodium taurocholate and sodium cholate) were investigated. A rotating disk apparatus was chosen to monitor dissolution kinetics; it well-defined hydrodynamic conditions allowed for analysis of the behavior of bile salt micelles under different conditions. Griseofulvin solubility and dissolution rate increased with increasing bile salt concentration in the dissolution medium. The enhancement of the dissolution rate was not linearly related to the solubility increase, as diffusional transport of the solubilized drug proved to be less efficient than transport of the unsolubilized ("free") drug. The dissolution process proved to be controlled by convective diffusion. An analysis of the data with the phase separation model provided results for the micellar diffusion coefficient comparable with literature data obtained with different techniques.

Bile Acids and Salts↗
PubMed1991

Increasing the in vitro bile acid binding capacity of diethylaminoethylcellulose by quaternization.

Diethylaminoethylcellulose (DEAE-cellulose) was quaternized with methyl iodide (DEAE-cellulose-CH3I), and its in vitro binding capacity for sodium glycocholate, at room temperature, in water, Tris-HCl buffer (0.0015-0.0050 M, pH 7.0), and aqueous NaCl (0.0025 M) was determined by reversed-phase HPLC. Quaternization increased the in vitro bile salt binding capacity of DEAE-cellulose. On a molar basis, the binding capacity was greater than that of cholestyramine, a cholesterol-lowering agent. Increasing the ionic strength of the medium decreased the binding capacities, as expected if ionic interactions are important. However, conversion of DEAE-cellulose-CH3I to its chloride form did not change the binding capacity. The bile salt binding capacity of DEAE-cellulose-CH3I was similar for both sodium cholate and sodium glycocholate.

Adsorption↗
PubMed1992

Polymeric sorbents for bile acids. I: Comparison between cholestyramine and colestipol.

Isotherms for the sorption of bile acids at 20 degrees C, in tris(hydroxymethyl)aminomethane.HCl(tris) and KH2PO4-NaOH (phosphate) buffers (pH 7.4), indicate that the binding by cholestyramine and colestipol is mainly through ionic linkages, although hydrophobic interactions are also of importance. Cholestyramine has a higher sorption capacity for bile acids, in both buffers, than colestipol. The chloride form of cholestyramine has a higher capacity for cholate in tris buffer than the iodide form. Increased ionic strength of the medium leads to decreased amounts of sorption.

Absorption↗
PubMed1994

Oral administration of insulin in solid form to nondiabetic and diabetic dogs.

It was previously demonstrated that a biologically active insulin could cross the mucosal membrane in the gut by using surface active substances. In this report we describe studies in which insulin administered orally, in a solid formulation, was effectively absorbed in the canine model. The insulin was mixed with cholate and soybean trypsin inhibitor. It was delivered orally, as enterocoated microtablets, to nondiabetic and diabetic (pancreatectomized) dogs in a fasting state. The time interval between the administration of the drug and the beginning of a decrease in the plasma glucose levels was 60-140 min. This decrease reached a minimum level of 20-40 % of the initial values and lasted for more than 90 min following administration of the drug. In this model a pronounced increment in plasma insulin levels was shown prior to the drop of plasma glucose concentrations. It is concluded that with this novel oral insulin formulation a beneficial biological effect can be achieved in the treatment of diabetes.

Administration, Oral↗
PubMed1994

Dissolution kinetics of griseofulvin in mixed micellar solutions.

The dissolution kinetics of the poorly water soluble, lipophilic model drug substance griseofulvin were studied in solutions containing simple and mixed micelles of sodium cholate (BS) and phosphatidylcholine (PC). Variables under investigation were the concentration of BS and the ratio PC/BS. A rotating disk apparatus was used to monitor the dissolution process. With this method, (mixed) micellar diffusion coefficients could be calculated and some detailed information about the physicochemical behavior and composition of mixed PC/BS micelles could be derived.

Bile Acids and Salts↗
PubMed1995

Experimental evaluation of a model for predicting micellar composition and concentration of monomeric species in bile salt binary mixtures.

The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on which the presumed validity of this model was based are discussed. The following binary mixtures were investigated: sodium chenodeoxycholate with cholate, ursocholate and ursodeoxycholate, either unconjugated or conjugated with taurine and glycine at different mole fractions (0, 0.25, 0.5, 0.75, 1) in 0.15 M NaCl. For these mixtures, experimentally determined data were in good agreement with values predicted by the theoretical model: both the cmc and the surface tension at this concentration of the mixtures were intermediate between those of the two pure bile salts; also, as the total bile salt concentration increased, the mixed micelles became enriched with the bile salt having the highest cmc, whereas the total monomer activity, determined by a potentiometric method employing a bile salt-selective electrode, increased only slightly. To test this model in an in vitro system, surface tension was also measured in ox bile samples that were enriched by 50% with sodium ursodeoxycholate, chenodeoxycholate, or their taurine amidates. The cmc and the surface tension at this concentration of the artificial bile increased when enriched with a bile salt with a cmc higher than that of endogenous salts (e.g. ursodeoxycholate versus taurocholate), whereas the reverse occurred for mixtures enriched with a bile salt with a lower cmc, such as chenodeoxycholate.(ABSTRACT TRUNCATED AT 250 WORDS)

Bile Acids and Salts↗
PubMed1975

Studies of the oligomycin-sensitive ATPase from yeast mitochondria. Reconstitution of ATP-32Pi exchange in the presence of phospholipids.

A purified preparation of the oligomycin-sensitive ATPase from yeast mitochondria has been shown to elicit an oligomycin- and uncoupler-senstitive ATP-32Pi exchange in the presence of phospholipids. Reconstitution was normally achieved by dialysis of an ATPase-phospholipid-cholate mixture. Following this procedure, vesicles with diameters between 200 and 1,500 A were seen by electron microscopy. As in mitochondria, ATPase activity in the reconstituted system was stimulated by a range of uncouplers which inhibited ATP-32Pi exchange. These and other findings suggest that the coupling mechanism may still be intact within the ATPase complex.

Adenosine Triphosphatases↗
PubMed1978

Resistance of the intact and reconstituted adipocyte hexose transport system to irreversible inhibition by sulfhydryl and amino reagents.

Sensitivity of the adipocyte D-glucose transport system in intact plasma membranes or following solubilization and reconstruction into phospholipid vesicles to several protein-modifying reagents was investigated. When intact plasma membranes were incubated with N-ethylmaleimide (20 mM) or fluorodinitrobenzene (4 mM), D-glucose transport activity was virtually abolished. However, washing the membranes free of unreacted reagents restored transport activity, indicating that covalent interaction with the membrane did not mediate the transport inhibition. Reaction of [3H]N-ethylmaleimide with plasma membranes under similar conditions resulted in extensive labeling of all protein fractions resolved on dodecyl sulfate gels. Similarly, addition of N-ethylmaleimide to cholate-solubilized membrane protein had no effect on transport activity in artificial phospholipid vesicles reconstituted under conditions where the membrane protein was free of unreacted N-ethylmaleimide. Transport activity in plasma membranes was also inhibited by both reduced and oxidized dithiothreitol or glutathione (15 mM) in a readily reversible manner. consistent with a noncovalent mode of inhibition. Thus, the insulin-responsive adipocyte D-glucose transport system differs from the red cell hexose transport system in its remarkable insensitivity to modulation by covalent blockade of sulfhydryal or amino groups by the reagents studied.

Adipose Tissue↗
PubMed1979

Alkaline phosphatase of basal lateral and brush border plasma membranes from intestinal epithelium.

The alkaline phosphatase present on isolated brush border and basal lateral membranes of rat duodenal epithelium were examined by means of a variety of biochemical assays and physical methods. The two alkaline phosphatases have similar pH optima of 9.6--9.8, similar substrate km's for p-nitrophenyl phosphate (PNPP) of 71 micromolar, similar responses to the inhibitors 2-mercaptoethanol, theophylline, phenylalanine, and ethylenediaminetetraacetic acid (EDTA), similar sensitivities to calcium, magnesium, zinc, sodium, and potassium, and similar insensitivities to digestion with trypsin of papain. The two enzymes also exhibit similar molecular weights on SDS-polyacrylamide gels in the range 124,000--150,000, and both enzymes show an Rf value of 0.092 on Triton X-100 polyacrylamide gels, indicating similar intrinsic charges. The Vmax of the brush border enzyme is ten times greater than that of the basal lateral enzyme, 140 mumoles/mg-h as opposed to 14 mumoles/mg-h. The differences in Vmax are a reflection of the known distribution of alkaline phosphatase in rat duodenum, there being more alkaline phosphatase activity present on the brush border than on the basal lateral surface. One other major difference was observed between the two enzymes, the stimulation of the basal lateral and not the brush border alkaline phosphatase by SDS, Triton X-100, or cholate. We conclude that the enzymes are very similar to one another and probably perform similar membrane functions.

Alkaline Phosphatase↗
PubMed2005

Micellar electrokinetic chromatography for simultaneous determination of six corticosteroids in commercial pharmaceuticals.

We have developed a micellar electrokinetic chromatography (MEKC) method using bile salts for the simultaneous determination of six corticosteroids, including betamethasone, cortisone, prednisolone, 6alpha-methylprednisolone, triamcinolone, and prednisone. The separation was performed using borate buffer containing sodium cholate and sodium deoxycholate. Several parameters were studied, including bile salt concentrations, concentrations and pH of borate buffer, and analytical voltages. In method validation, calibration curves were linear over a range of 10-100 microM for each corticosteroid. The RSD (relative standard deviation) and RE (relative error) were all less than 5% for intra- and interday assays. The limit of detection of each analyte was 5 microM. The recoveries were greater than 95%. Application of this method for quality control of commercial tablets also proved to be feasible. All analytical values fall within the labeled amount of 90-110% for betamethasone and prednisolone, and of the labeled amount of 92.5-107.5% for 6alpha-methylprednisolone, as required by the United State Pharmacopeia 25 (USP 25).

Adrenal Cortex Hormones↗
PubMed2005

Novel nonaqueous capillary electrophoresis separation and determination of bioactive flavone derivatives in Chinese herbs.

Nonaqueous CE (NACE) coupled to UV detection is described for the separation and determination of bioactive flavone derivatives in Chinese herbs extraction. After optimization of electrophoresis parameters, including the electrolyte nature and the organic solvent composition, a reliable separation of the analytes in an ACN/methanol (60:40, v/v) mixture containing 80 mM Tris and 10 mM sodium cholate was performed. The detection was performed at 254 nm. Method performances, including migration time and peak area reproducibility, linearity, sensitivity, and accuracy, were evaluated. The method was applied to determine bioactive flavone derivatives in seven Chinese herbs.

Drugs, Chinese Herbal↗
PubMed2006

Phanquinone as a suitable derivatization reagent in micellar electrokinetic chromatography and HPLC analysis of amino acids.

Phanquinone (chemically: 4,7-phenanthroline-5,6-dione) was applied as an original precolumn derivatization reagent for amino acids followed by separation using MEKC with UV detection (240 nm). The derivatization reaction was carried out at 68 degrees C in the presence of aqueous phosphate buffer (pH 8.0) and it was found to be complete after 30 min. Twelve derivatized standard amino acids were separated in about 22 min under MEKC conditions using sodium cholate (250 mM) as the surfactant in phosphate buffer (20 mM, pH 9.0). The developed method was validated for the analysis of D,L-phosphoserine (D,L-p-Ser) and L-glutamine (L-Gln); good linearity (r > 0.999) was achieved in the calibration range of 0.25-2.5 micromol/mL. The sensitivity of the MEKC method (LOD 0.1 micromol/mL; LOQ 0.25 micromol/mL, RSD% <5.0%, n = 3) was found to be adequate for quantitation of amino acids in pharmaceuticals. Quantitative applications of the validated MEKC method were carried out by the analysis of commercially available oral polyaminoacid formulations (tablets and extemporaneous solutions) containing L-Gln and D,L-p-Ser; the obtained results were found to be in agreement with those from a validated reference RP-HPLC method.

Amino Acids↗
PubMed1997

Quantitative liver function tests define the functional severity of liver disease in early-stage cirrhosis.

Some patients with early-stage cirrhosis preserve hepatic function, whereas others have little hepatic reserve and rapidly deteriorate. The aim of this study was to use quantitative tests of liver function (QLFTs) to define the degree of functional hepatic impairment in patients with early-stage cirrhosis (Child-Pugh score 5-7) and to determine whether the tests predicted subsequent hepatic decompensation. We recruited 10 cirrhotic (Cr) patients and 10 healthy controls (NI), who were well matched for race, age, weight, and gender. Clearances of caffeine (CF) and antipyrine (AP) after oral administration were measured from timed samples of saliva. The clearance of cholate (CA) was measured from serum samples obtained after simultaneous oral ([2,2,4,4-2H]CA) and intravenous ([24-13C]CA) administration. CA shunt was calculated as (Cl i.v./Clo x 100%). CF elimination rate (Cr v NI, mean +/- SD: 0.03 +/- 0.02 v 0.075 +/- 0.018 h-1, P < .0005) and AP clearance (24 +/- 16 v 40 +/- 7 mL/minute, P < .02) were reduced in Cr patients. CA shunt was increased in Cr patients (43 +/- 18 v 18 +/- 7%, P < .002). Five Cr patients decompensated during follow-up and had the worst CA shunts (76%, 66%, 51%, 48%, and 45%). Three subsequently received successful orthotopic liver transplantation, 1 died of hepatoma, and 1 is on the waiting list for transplantation. In conclusion, QLFTs define the degree of functional impairment in early cirrhosis and may identify Cr patients at greatest risk of decompensation who may require transplantation for survival.

Administration, Oral↗