Solubility and partitioning. VII: Solubility of barbiturates in water.


:The solubility equation of Yalkowsky was used to estimate the aqueous solubility of 33 barbiturates in the temperature range of 5 to 45 degrees C. The equation was extended by adding a term which accounts for the effect of pH on the solubility of the drug. The extended equation is successful in estimating the aqueous solubility of this series of drugs under different conditions of temperature and pH. The results indicate that the extended equation can be used to estimate the aqueous solubility of nonelectrolytes as well as weak electrolytes.


J Pharm Sci


Pinal R,Yalkowsky SH




Has Abstract


1987-01-01 00:00:00














  • 2,5-Diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone II: Isolation and characterization of degradation products.

    abstract::A direct high-performance liquid chromatographic (HPLC) method was applied to monitor 2,5-diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone (I) and its degradation products in pharmaceutical vehicles at 25 +/- 0.1 degrees. At the optimal pH for stability of I, an increase in buffer concentration [phosphate and t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Poochikian GK,Kelley JA

    更新日期:1981-02-01 00:00:00

  • Effect of dispersion on the coloring properties of aluminum dye lakes.

    abstract::The effect of particle size on the coloring properties of aluminum dye lakes was studied. Lakes impart color by dispersion in the medium to be colored. Dispersion techniques were developed, using scanning electron micrographs for particle sizing. The color strength and the trichromatic colorimetric properties were cal...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wou LL,Mulley BA

    更新日期:1988-10-01 00:00:00

  • Adsorption of cationized bovine serum albumin onto epithelial crypt fractions of the rat colon.

    abstract::The purpose of the study was to characterize mucosal attachment of a cationized model protein, bovine serum albumin (BSA), onto the various fractions of colonic crypts epithelium in the rat. BSA was labeled with fluorescein isothiocyanate (FITC) and its surface net electric charge was modified from negative to positiv...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Blau S,Levin N,Schwartz B,Rubinstein A

    更新日期:2001-10-01 00:00:00

  • High-pressure liquid chromatographic determination of cimetidine in plasma and urine.

    abstract::An assay is described for the determination of the H2-receptor antagonist, cimetidine, in human plasma and urine. Alkalinized plasma or urine was extracted with methylene chloride, the organic phase was evaporated, and the reconstituted residue was analysed by high-pressure liquid chromatography (HPLC) using a reverse...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mihaly GW,Cockbain S,Jones DB,Hanson RG,Smallwood RA

    更新日期:1982-05-01 00:00:00

  • Intravascular bioresorbable polymeric stents: a potential alternative to current drug eluting metal stents.

    abstract::Stent implantation following angioplasty is the standard treatment of coronary artery disease necessitating interventional procedures. The use of stents as a platform for local drug delivery is a popular strategy to achieve local pharmacological treatment to the diseased artery. Drug eluting stents (DES) are now large...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Sharkawi T,Cornhill F,Lafont A,Sabaria P,Vert M

    更新日期:2007-11-01 00:00:00

  • Hypolipidemic activity of 6-amino-2-mercapto-5-methyl-pyrimidine-4-carboxylic acid and related derivatives in rodents.

    abstract::6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hall IH,Cocolas GH,Murthy AR,Rhyne KA,Knowles M

    更新日期:1985-07-01 00:00:00

  • Colorimetric assay of benzocaine and some dosage forms.

    abstract::A colorimetric procedure for benzocaine and a number of its dosage forms was developed; it offers improvement in ease, speed, and sensitivity over the official method. The method is based on the formation of a red Schiff base between benzocaine and p-dimethylaminocinnamaldehyde in a nonaqueous acidic medium. At the ma...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tan HS,Bruemmer GA,Shelton D

    更新日期:1977-07-01 00:00:00

  • Processing-induced phase transitions of theophylline--implications on the dissolution of theophylline tablets.

    abstract::Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tantry JS,Tank J,Suryanarayanan R

    更新日期:2007-05-01 00:00:00

  • Enhanced transdermal delivery of sex hormones in swine with a novel topical aerosol.

    abstract::This study investigated the enhanced transdermal delivery of testosterone (Tes) and estradiol (E2) in swine in vivo with novel metered-dose topical aerosols containing the penetration enhancer padimate O (PadO) and predicted the dose deliverable in humans from the calculated drug flux across the skin. Weanling swine w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Morgan TM,Parr RA,Reed BL,Finnin BC

    更新日期:1998-10-01 00:00:00

  • Physicochemical property modification strategies based on enzyme substrate specificities II: alpha-chymotrypsin hydrolysis of aspirin derivatives.

    abstract::Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Banerjee PK,Amidon GL

    更新日期:1981-12-01 00:00:00

  • Rapid colorimetric analysis of chlorhexidine in pharmaceutical preparations.

    abstract::A colorimetric determination of chlorhexidine is described. The method is based on the formation of a yellow complex between the drug and bromcresol green. The absorption peak of this complex, extracted by chloroform, is at 410 nm, and linear response is obtained from 2.5 to 30 micrograms of chlorhexidine/ml. The accu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Andermann G,Buhler MO,Erhart M

    更新日期:1980-02-01 00:00:00

  • Ocular pharmacokinetics of a novel tetrahydroquinoline analog in rabbit: absorption, disposition, and non-compartmental analysis.

    abstract::The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pamulapati CR,Schoenwald RD

    更新日期:2011-12-01 00:00:00

  • Econazole nitrate-loaded MCM-41 for an antifungal topical powder formulation.

    abstract::The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ambrogi V,Perioli L,Pagano C,Marmottini F,Moretti M,Mizzi F,Rossi C

    更新日期:2010-11-01 00:00:00

  • The Organic Anion-Transporting Peptide 2B1 Is Localized in the Basolateral Membrane of the Human Jejunum and Caco-2 Monolayers.

    abstract::The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. Although the expression and function of this solute carrier transporter is well characterized in the human liver and other tissues, little i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Keiser M,Kaltheuner L,Wildberg C,Müller J,Grube M,Partecke LI,Heidecke CD,Oswald S

    更新日期:2017-09-01 00:00:00

  • Anthrax vaccine powder formulations for nasal mucosal delivery.

    abstract::Anthrax remains a serious threat worldwide as a bioterror agent. A second-generation anthrax vaccine currently under clinical evaluation consists of a recombinant Protective Antigen (rPA) of Bacillus anthracis. We have previously demonstrated that complete protection against inhalational anthrax can be achieved in a r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jiang G,Joshi SB,Peek LJ,Brandau DT,Huang J,Ferriter MS,Woodley WD,Ford BM,Mar KD,Mikszta JA,Hwang CR,Ulrich R,Harvey NG,Middaugh CR,Sullivan VJ

    更新日期:2006-01-01 00:00:00

  • Phase distribution studies on an oil-water emulsion based on a eutectic mixture of lidocaine and prilocaine as the dispersed phase.

    abstract::The distribution conditions in oil-water emulsions prepared by emulsifying a 1:1 eutectic mixture of lidocaine and prilocaine with a nonionic surfactant in water were studied by membrane and gel filtration methods. In this system, the local anesthetics are considered to be freely dissolved, surfactant solubilized, and...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nyqvist-Mayer AA,Brodin AF,Frank SG

    更新日期:1985-11-01 00:00:00

  • Semi-automated protein binding methodology using equilibrium dialysis and a novel mixed-matrix cassette approach.

    abstract::A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Plise EG,Tran D,Salphati L

    更新日期:2010-12-01 00:00:00

  • Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors.

    abstract::The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shaik N,Pan G,Elmquist WF

    更新日期:2008-12-01 00:00:00

  • Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl methylcellulose matrix tablets using (SBE)(7m)-beta-cyclodextrin as a solubilizing agent.

    abstract::Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rao VM,Haslam JL,Stella VJ

    更新日期:2001-07-01 00:00:00

  • Bioavailability assessment under quasi- and nonsteady-state conditions III: Application.

    abstract::The applicability of bioavailability assessment at quasi- and nonsteady state is illustrated with data from a study comparing two formulations of amitriptyline hydrochloride in humans. Relative bioavailability as a function of the observed mean plasma concentrations may be expressed in closed form, provided the affect...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bondi JV,Hucker HB,Yeh KC,Kwan KC

    更新日期:1976-11-01 00:00:00

  • Expanding Bedside Filtration-A Powerful Tool to Protect Patients From Protein Aggregates.

    abstract::Protein immunogenicity is intensively researched by academics, biopharmaceutical companies, and authorities as it can compromise the safety and efficacy of a biopharmaceutical drug. So far, the exact protein aggregate properties inducing immune responses are not known. Possible protein-related factors could be size, c...

    journal_title:Journal of pharmaceutical sciences

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    authors: Werner BP,Winter G

    更新日期:2018-11-01 00:00:00

  • Characterization of the properties of cocaine in blood: blood clearance, blood to plasma ratio, and plasma protein binding.

    abstract::As part of a study to examine cocaine disposition and interaction with ethanol, it was necessary to characterize various properties of cocaine in the blood of the experimental animal. All studies were conducted using blood from healthy adult male Sprague-Dawley rats. Cocaine was incubated in whole blood at 37 degrees ...

    journal_title:Journal of pharmaceutical sciences

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    authors: Sukbuntherng J,Martin DK,Pak Y,Mayersohn M

    更新日期:1996-06-01 00:00:00

  • Effects of solvent polarity on the acid dissociation constants of benzoic acids.

    abstract::The pKa values of benzoic acid, p-methylbenzoic, and p-aminobenzoic acid (PABA) were determined by potentiometric titration in mixtures of 0-0.5 volume fractions of various cosolvents and water. The differences between the aqueous and semiaqueous pKa values were similar for the three solutes at a particular cosolvent-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rubino JT,Berryhill WS

    更新日期:1986-02-01 00:00:00

  • Forced degradation studies of corticosteroids with an alumina-steroid-ethanol model for predicting chemical stability and degradation products of pressurized metered-dose inhaler formulations.

    abstract::An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

    更新日期:2012-06-01 00:00:00

  • Cytotoxic effects of methionine alkyl esters and amides in normal and neoplastic cell lines.

    abstract::Homologous series of L-methionine alkyl ester hydrochlorides and tosylates were synthesized and evaluated for in vitro growth inhibitory activity in Meth A sarcoma. Cytotoxicity, as determined by [3H]thymidine incorporation, was found to be directly proportional to alkyl chain length and surface tension lowering activ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Clement MA,Chapman JM,Roberts J

    更新日期:1989-06-01 00:00:00

  • Formation of a cyclic derivative of ethacrynic acid with diazomethane.

    abstract::Samples of ethacrynic acid were treated with methanol-hydrochloric acid or with diazomethane. GLC and mass spectrometric analysis indicated that the methanol-hydrochloric acid reaction gave the expected methyl ester, whereas diazomethane treatment gave a compound containing an additional 14 mass units. Accurate mass m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Midha KK,Hubbard JW,Charette C,Jun HW

    更新日期:1978-07-01 00:00:00

  • The use of N,N-diethyl-m-toluamide to enhance dermal and transdermal delivery of drugs.

    abstract::A dermal penetration enhancer has been found which improves the dermal delivery of a wide variety of drugs and at the same time has a history of low toxicity for human dermal application. N,N-Diethyl-m-toluamide (I) has been shown to improve the delivery of many drugs through hairless mouse skin in an in vitro diffusi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Windheuser JJ,Haslam JL,Caldwell L,Shaffer RD

    更新日期:1982-11-01 00:00:00

  • Solubility and mass and nuclear magnetic resonance spectroscopic studies on interaction of cyclosporin A with dimethyl-alpha- and -beta-cyclodextrins in aqueous solution.

    abstract::The interaction of cyclosporin A (CsA) with dimethyl-alpha- and -beta-cyclodextrins (DM-alpha-CyD and DM-beta-CyD) was investigated by the solubility method, electrospray ionization mass spectrometry (ESI-MS) and 1H-nuclear magnetic resonance spectroscopy (1H NMR). The extremely low solubility (1.9 x 10(-5) M at 25 de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Miyake K,Hirayama F,Uekama K

    更新日期:1999-01-01 00:00:00

  • pH-Sensitive cationic copolymers of different macromolecular architecture as potential dexamethasone sodium phosphate delivery systems.

    abstract::This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

    更新日期:2014-08-01 00:00:00

  • Oxidation of human insulin-like growth factor I in formulation studies. 3. Factorial experiments of the effects of ferric ions, EDTA, and visible light on methionine oxidation and covalent aggregation in aqueous solution.

    abstract::The influence of ferric ions, EDTA, and visible light on the oxidation of methionine and the covalent reducible and nonreducible dimerization in human Insulin-like Growth Factor I (hIGF-I) in aqueous (1 mM) phosphate buffer solution were studied. A reduced factorial experiment with two levels of each factor was used. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fransson JR

    更新日期:1997-09-01 00:00:00