Prediction of xanthine solubilities using statistical techniques.

Abstract:

:Mixture response-surface methodology can be used as a technique to predict solubility in mixed solvent systems. The present report shows that if the intent is to predict solubility in nonideal solutions, mixture response-surface methodology is a better technique than one which assumes a particular mechanism to hold true. This is demonstrated by comparing the predictive ability of the mixture response-surface model with that of an extended Hildebrand approach to nonideal solutions. The nonideal systems are those used by Martin and co-workers involving the solubility of theobromine, caffeine, and theophylline in dioxane-water mixtures.

journal_name

J Pharm Sci

authors

Ochsner AB,Belloto RJ Jr,Sokoloski TD

doi

10.1002/jps.2600740206

subject

Has Abstract

pub_date

1985-02-01 00:00:00

pages

132-5

issue

2

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)46593-1

journal_volume

74

pub_type

杂志文章
  • Kinetic analysis of relationship between partition coefficient and biological response.

    abstract::Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700110

    authors: Cooper ER,Berner B,Bruce RD

    更新日期:1981-01-01 00:00:00

  • A Measurement and Modeling Study of Hair Partition of Neutral, Cationic, and Anionic Chemicals.

    abstract::Various neutral, cationic, and anionic chemicals contained in hair care products can be absorbed into hair fiber to modulate physicochemical properties such as color, strength, style, and volume. For environmental safety, there is also an interest in understanding hair absorption to wide chemical pollutants. There hav...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.12.010

    authors: Li L,Yang S,Chen T,Han L,Lian G

    更新日期:2018-04-01 00:00:00

  • Kinetics of drug-drug interactions in sheep: tolbutamide and sulfadimethoxine.

    abstract::The interaction between sulfadimethoxine and tolbutamide in sheep involving displacement from protein binding sites was investigated quantitatively. A 52% increase in the unbound plasma concentration of tolbutamide was observed in vitro at 37 degrees after the addition of sulfadimethoxine (100 microgram/ml) to sheep p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660803

    authors: Thiessen JJ,Rowland M

    更新日期:1977-08-01 00:00:00

  • Passive Immunotherapies Targeting Amyloid Beta and Tau Oligomers in Alzheimer's Disease.

    abstract::Alzheimer's disease (AD) is historically difficult to treat, in part because of the inaccessible nature of brain pathology. Amyloid beta and tau proteins drive pathology by forming toxic oligomers that eventually deposit as insoluble amyloid plaques and neurofibrillary tangles. Recent clinical studies suggest that eff...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.10.024

    authors: Vander Zanden CM,Chi EY

    更新日期:2020-01-01 00:00:00

  • Physicochemical properties of A-75998, an antagonist of luteinizing hormone releasing hormone.

    abstract::The physicochemical properties of A-75998, a synthetic antagonist of luteinizing hormone releasing hormone with potential for treatment of hormone-sensitive cancers and endometriosis, are described. An accelerated solution stability study indicated that the compound is relatively stable and showed a U-shaped pH-rate p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840810

    authors: Cannon JB,Krill SL,Porter WR

    更新日期:1995-08-01 00:00:00

  • Development of a nanofiltration process to improve the stability of a novel anti-MRSA carbapenem drug candidate.

    abstract::The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10084

    authors: Antonucci V,Yen D,Kelly J,Crocker L,Dienemann E,Miller R,Almarrsson O

    更新日期:2002-04-01 00:00:00

  • Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies.

    abstract::The clearance (Cl) and volume of distribution (V(ss)) of a lipophilic, lymphatically transported drug, halofantrine (Hf) have been evaluated after intravenous delivery to the systemic circulation in ex vivo lymph and plasma, and compared with the data obtained after administration of a lipid-based emulsion and a lipid...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23211

    authors: Caliph SM,Trevaskis NL,Charman WN,Porter CJ

    更新日期:2012-09-01 00:00:00

  • Simultaneous detection and analysis of protein aggregation and protein unfolding by size exclusion chromatography with post column addition of the fluorescent dye BisANS.

    abstract::For development and optimization of protein formulation sensitive analytical tools are required to follow both aggregation and changes in protein structure. The latter can be seen as the beginning of physical instability leading to aggregation. The focus of this work laid on the development of a novel analysis simulta...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22808

    authors: Printz M,Friess W

    更新日期:2012-02-01 00:00:00

  • Degradation kinetics and mechanisms of moricizine hydrochloride in acidic medium.

    abstract::The degradation kinetics of moricizine hydrochloride (1) were examined over a pH range of 0.6 to 6.0 at an ionic strength of 0.3 and 60 degrees C. The disappearance of intact 1 was followed by a stability-indicating HPLC assay. The degradation products, which had approximate solubilities of less than 100 micrograms/mL...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810625

    authors: King SP,Sigvardson KW,Dudzinski J,Torosian G

    更新日期:1992-06-01 00:00:00

  • Anticonvulsant activity and selective inhibition of nicotinamide adenine dinucleotide-dependent oxidations by 10-(2-arylimino-3-acetylamino-4-thiazolidonyl) phenothiazines.

    abstract::Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650319

    authors: Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

    更新日期:1976-03-01 00:00:00

  • Inhibitory effect of valsartan on the intestinal absorption and renal excretion of bestatin in rats.

    abstract::Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically unders...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23805

    authors: Huo X,Liu Q,Wang C,Meng Q,Sun H,Peng J,Ma X,Sun P,Liu K

    更新日期:2014-02-01 00:00:00

  • Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

    abstract::The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680208

    authors: Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

    更新日期:1979-02-01 00:00:00

  • Liquid membrane phenomenon in diuretics.

    abstract::Surface activity and critical micelle concentrations are reported for two diuretic drugs, furosemide and triamterene. The drugs generate a liquid membrane on a supporting membrane. Transport of chloride, sodium, and potassium ions through the liquid membranes generated by the drugs was studied. The data suggest that t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731123

    authors: Bhise SB,Bhattacharjee D,Srivastava RC

    更新日期:1984-11-01 00:00:00

  • Determination of the permeability characteristics of two sulfenamide prodrugs of linezolid across Caco-2 cells.

    abstract::The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across Caco-2 cell monolayers. Both prodrugs were found to convert to linezolid in th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23084

    authors: Nti-Addae KW,Guarino VR,Dalwadi G,Stella VJ

    更新日期:2012-09-01 00:00:00

  • Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.

    abstract::In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21464

    authors: Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY

    更新日期:2009-02-01 00:00:00

  • Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery.

    abstract::The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1162

    authors: Kawakami S,Nishida K,Mukai T,Yamamura K,Kobayashi K,Sakaeda T,Nakamura J,Nakashima M,Sasaki H

    更新日期:2001-12-01 00:00:00

  • Thermodynamic analysis of energy dissipation by pharmaceutical tablets during stress unloading.

    abstract::A thermodynamic analysis of the energy transformations occurring within pharmaceutical tablets during the unloading phase of compaction was performed on Avicel, calcium phosphate, acetaminophen, and calcium oxalate. This analysis was based on viscoelastic stress data collected using an instrumented rotary press and wa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830629

    authors: Hoag SW,Rippie EG

    更新日期:1994-06-01 00:00:00

  • Quantitative expression of human drug transporter proteins in lung tissues: analysis of regional, gender, and interindividual differences by liquid chromatography-tandem mass spectrometry.

    abstract::The purpose of the present study was to clarify the expression levels of transporter proteins in human lung tissue and to analyze regional and interindividual differences in primary cultured epithelial cells. Organic cation/carnitine tranporter 1 (OCTN1) protein expression was highest (2.08 ± 1.19 fmol/μg protein) in ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23606

    authors: Sakamoto A,Matsumaru T,Yamamura N,Uchida Y,Tachikawa M,Ohtsuki S,Terasaki T

    更新日期:2013-09-01 00:00:00

  • Potency of synthetic luteinizing hormone releasing hormone preparations in rat anterior pituitary cell cultures.

    abstract::Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660319

    authors: Dermody WC,Pastushok CA,Sakowski R,Vaitkus JW,Reel JR

    更新日期:1977-03-01 00:00:00

  • Relative bioavailability of commercially available ibuprofen oral dosage forms in humans.

    abstract::Two human bioavailability studies were conducted to assess the in vivo performances of recently marketed 200-, 300-, and 400-mg ibuprofen capsules relative to the innovator's 300- and 400-mg tablets when administered as single oral 300- or 400-mg doses. An ibuprofen oral solution was also administered in each trial. W...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710920

    authors: Gillespie WR,DiSanto AR,Monovich RE,Albert KS

    更新日期:1982-09-01 00:00:00

  • Application of neural networks to pharmacodynamics.

    abstract::Neural networks (NN) are computational systems implemented in software or hardware that attempt to simulate the neurological processing abilities of biological systems. A synopsis is presented of the operational characteristics, structures, and applications of NN. The NN technology has primarily been aimed at recognit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820910

    authors: Veng-Pedersen P,Modi NB

    更新日期:1993-09-01 00:00:00

  • Limits on optimizing ocular drug delivery.

    abstract::The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800113

    authors: Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

    更新日期:1991-01-01 00:00:00

  • Adhesive tablet effective for treating canker sores in humans.

    abstract::A new mucoadhesive tablet, which releases natural active agents for pain reduction and rapid healing of canker sores, has been prepared and characterized. Adhesive tablets were prepared by compression molding of mixed powders of crosslinked polyacrylic acid and hydroxypropyl cellulose, absorbed with citrus oil and mag...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1002/jps.20193

    authors: Mizrahi B,Golenser J,Wolnerman JS,Domb AJ

    更新日期:2004-12-01 00:00:00

  • Explanation of the crystallization rate of amorphous nifedipine and phenobarbital from their molecular mobility as measured by (13)C nuclear magnetic resonance relaxation time and the relaxation time obtained from the heating rate dependence of the glass

    abstract::To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1033

    authors: Aso Y,Yoshioka S,Kojima S

    更新日期:2001-06-01 00:00:00

  • Stability of Ceftazidime Pentahydrate Investigated by Thermal Analysis Techniques.

    abstract::Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.11.018

    authors: Alves de Santana MS,Santiago de Oliveira Y,de Castro Fonseca J,Ferreira WC,Neto VS,Ayala AP

    更新日期:2020-03-01 00:00:00

  • Enabling tablet product development of 5-fluorocytosine through integrated crystal and particle engineering.

    abstract::The antifungal drug, 5-fluorocytosine (FC), is marketed as a capsule (250 or 500 mg strength) instead of the preferred tablet dosage form. Through systematic characterization of solid-state properties, including mechanical properties, we identify tabletability and poor physical stability of FC as the problems that lik...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23876

    authors: Perumalla SR,Sun CC

    更新日期:2014-04-01 00:00:00

  • Quantitative structure-pharmacokinetic/pharmacodynamic relationships of corticosteroids in man.

    abstract::The purpose of this study was to develop quantitative structure-activity/pharmacokinetic relationships (QSAR/QSPKR) for 11 selected corticosteroids in man. Multiple linear regression analysis with an automatic forward step-wise inclusion algorithm was used to construct QSAR/QSPKR models from molecular and submolecular...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10231

    authors: Mager DE,Jusko WJ

    更新日期:2002-11-01 00:00:00

  • Utilization of Zwitterion-based solutions to dissect the relative effects of solution pH and ionic strength on the aggregation behavior and conformational stability of a fusion protein.

    abstract::Solution pH and ionic strength (I) have complex effects on protein stability. We developed an experimental approach based on exploitation of the zwitterionic characteristic of amino acid molecules to probe the relative contribution from each. A variety of types of amino acid solutions were adopted to investigate the e...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24118

    authors: Zhou R,Nashine V,Palm T,Gandhi R,Adams M

    更新日期:2014-10-01 00:00:00

  • Impact of Processing Conditions on Inter-tablet Coating Thickness Variations Measured by Terahertz In-Line Sensing.

    abstract::A novel in-line technique utilising pulsed terahertz radiation for direct measurement of the film coating thickness of individual tablets during the coating process was previously developed and demonstrated on a production-scale coater. Here, we use this technique to monitor the evolution of tablet film coating thickn...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24503

    authors: Lin H,May RK,Evans MJ,Zhong S,Gladden LF,Shen Y,Zeitler JA

    更新日期:2015-08-01 00:00:00

  • Inclusion complexation of heptakis(2,6-di-O-ethyl)-beta-cyclodextrin with tiaprofenic acid: pharmacokinetic consequences of a pH-dependent release and stereoselective dissolution.

    abstract::beta-Cyclodextrin was ethylated at the 2- and 6-hydroxyl positions. Diethyl sulfate was employed as an alkylating reagent. NMR spectra data indicate that heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (DCD) is the principal component of the product obtained. In addition, the FAB mass spectra obtained in nitrobenzyl alcoho...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840819

    authors: Vakily M,Pasutto FM,Daneshtalab M,Jamali F

    更新日期:1995-08-01 00:00:00