Vehicle effects in percutaneous absorption: in vitro study of influence of solvent power and microscopic viscosity of vehicle on benzocaine release from suspension hydrogels.


:The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutaneous absorption caused by changes in drug solubility and/or diffusivity in the vehicle. The effect of the additives on the release is expressed in terms of the relative released amount, i.e., the ratio, Q/Qw, of the amount of drug released from each additive-containing gel to the amount released at the same time from the additive-free gel. The experimental Q/Qw values are correlated with values calculated by a simple equation involving known or readily measurable parameters such as the drug concentration in the gel, the drug solubility in the pure liquid phase, and the viscosity of this phase. Derivation of such a relationship from a known equation describing the vehicle-controlled relase of suspended drugs was possible because an inverse proportionality was observed between drug diffusivity in the gels and the viscosity of the respective solvents. This relationship is interpreted with respect to current theories on drug diffusion in diluted gels.


J Pharm Sci


Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F




Has Abstract


1980-04-01 00:00:00














  • Calorimetric determination of the heat of precipitation of pseudoephedrine racemic compound--its agreement with the heat of solution.

    abstract::The heat of precipitation of dl-pseudoephedrine was determined by direct calorimetry using a Tronac isoperibolic calorimeter. The precipitation of dl-pseudoephedrine was induced by mixing aqueous solutions of the two enantiomers, namely, d- and l-pseudoephedrine, directly in the calorimeter. The molar heat of precipit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pudipeddi M,Sokoloski TD,Duddu SP,Carstensen JT

    更新日期:1995-10-01 00:00:00

  • Effect of basic cholane derivatives on intestinal cholic acid metabolism: in vitro and in vivo activity.

    abstract::A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

    更新日期:1992-03-01 00:00:00

  • Rational coformer or solvent selection for pharmaceutical cocrystallization or desolvation.

    abstract::It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , be...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Abramov YA,Loschen C,Klamt A

    更新日期:2012-10-01 00:00:00

  • Microencapsulation IV: Cross-linked hemoglobin microcapsules.

    abstract::Hemoglobin microcapsules were prepared through cross-linking of hemoglobin itself with various acyldichlorides. Variations in the reticulation conditions were preformed in order to ameliorate the oxygen dissociation curve, the mean diameter, and the possibility for the microcapsules to be lyophilized. With terephthalo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lévy MC,Rambourg P,Lévy J,Potron G

    更新日期:1982-07-01 00:00:00

  • Colorimetric determination of nadolol in tablets.

    abstract::Nadolol was extracted from tablet excipients with an acidic potassium chloride solution. The drug was oxidized with periodic acid, and the resulting aldehyde was reacted with 2,4-dinitrophenylhydrazine to form the corresponding hydrazone. Excess reagent was removed with a cupric chloride solution. The hydrazone was ex...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ivashikiv E

    更新日期:1978-07-01 00:00:00

  • Chlorthalidone analysis using carbonic anhydrase inhibition.

    abstract::Chlorthalidone was analyzed in the concentration range of 0.1-3.0 microgram/ml with a precision of +/- 0.05 microgram/ml. Chlorthalidone inhibition of the enzymatic hydrolysis rate of p-nitrophenyl acetate by bovine erythrocyte carbonic anhydrase was used as a basis for the determination. The amount of p-nitrophenol f...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Johnston MM,Li H,Mufson D

    更新日期:1977-12-01 00:00:00

  • Focused Ultrasound-Triggered Release of Tyrosine Kinase Inhibitor From Thermosensitive Liposomes for Treatment of Renal Cell Carcinoma.

    abstract::This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Abshire C,Murad HY,Arora JS,Liu J,Mandava SH,John VT,Khismatullin DB,Lee BR

    更新日期:2017-05-01 00:00:00

  • Stabilization and HPLC analysis of betamethasone sodium phosphate in plasma.

    abstract::The analysis of corticosteroid prodrugs in pharmacokinetic (PK) studies poses the risk of overestimation of corticosteroid concentrations due to in vitro hydrolysis of prodrugs after sample collection. This study tests the effectiveness of enzyme inhibitors as stabilizers for betamethasone sodium phosphate (BSP) in pr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Samtani MN,Schwab M,Nathanielsz PW,Jusko WJ

    更新日期:2004-03-01 00:00:00

  • Effect of temperature on binding of warfarin by human serum albumin.

    abstract::The in vitro binding of warfarin by human serum albumin was studied at various temperatures and at pH 7.4 by a frontal gel filtration technique. The results can be best described in terms of a two class-of-binding site model, in which the numbers of primary and secondary sites are constrained to the average values for...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Oester YT,Keresztes-Nagy S,Mais RF,Becktel J,Zaroslinski JF

    更新日期:1976-11-01 00:00:00

  • Soft gelatin capsules II: Oxygen permeability study of capsule shells.

    abstract::A method is reported for studying the effects of several factors at room temperature on the oxygen permeability of soft gelatin capsule shell films. The method involves the use of a permeability cell assembly and the spectrophotometric determïnation of oxygen with an alkaline pyrogallic acid solution. Factors investig...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hom FS,Veresh SA,Ebert WR

    更新日期:1975-05-01 00:00:00

  • Possible changes in luminal surface charge densities of small intestine membrane in the 4-7.4 pH range exhibit varied influence on the absorption rate constants of the ionized and un-ionized species of sulfadiazine in rats.

    abstract::The overall apparent first-order rate constants (Kab) of small intestinal absorption of sulfadiazine were determined in rats in situ at various pHs (4.01-7.42) of the recirculation fluids at 32 degrees. The purpose of the study was to verify our hypothesis that the rate-determining step for the absorption of sulfonami...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chow SL,Nagwekar JB

    更新日期:1994-02-01 00:00:00

  • Liquid chromatographic assay and disposition of carvedilol in healthy volunteers.

    abstract::Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Varin F,Cubeddu LX,Powell JR

    更新日期:1986-12-01 00:00:00

  • Preparation and characterization of quercetin nanocrystals.

    abstract::This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

    更新日期:2011-06-01 00:00:00

  • Stable isotope coadministration methodology for the estimation of the fraction of imipramine metabolized to desipramine.

    abstract::The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sasaki Y,Shinohara Y,Baba S

    更新日期:1990-02-01 00:00:00

  • Thermodynamics of water-solid interactions in crystalline and amorphous pharmaceutical materials.

    abstract::Pharmaceutical materials, crystalline and amorphous, sorb water from the atmosphere, which affects critical factors in the development of drugs, such as the selection of drug substance crystal form, compatibility with excipients, dosage form selection, packaging, and product shelf-life. It is common practice to quanti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sacchetti M

    更新日期:2014-09-01 00:00:00

  • Effect of absorbents on water vapor transmission of free and applied polymer films.

    abstract::The influence of different types of absorbents on moisture transmission through free (cast films) and applied (coated tablets) polymer films was investigated. In free film studies, lubricated granulations were considered to be the absorbent. The compressed tablet was considered to be the absorbent in applied film stud...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amann AH

    更新日期:1976-04-01 00:00:00

  • Partial permselective coating adds an osmotic contribution to drug release from swellable matrixes.

    abstract::A swellable matrix tablet is described which is partially coated with cellulose acetate (CA) to obtain a film having the shape of a cup, whose permeability to water and solutes was altered by mixing increasing amounts of poly(ethylene glycol) 400 (PEG). The drug-release mechanism from such systems was assessed by carr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Catellani PL,Colombo P,Peppas NA,Santi P,Bettini R

    更新日期:1998-06-01 00:00:00

  • Synthesis and bioevaluation of a series of fatty acid esters of p-[N,N-bis(2-chloroethyl)amino]phenol.

    abstract::A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that of phenol mustard in H...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wynn JE,Caldwell ML,Robinson JR,Beamer RL,Bauguess CT

    更新日期:1982-07-01 00:00:00

  • Development of a targeted polymorph screening approach for a complex polymorphic and highly solvating API.

    abstract::Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

    更新日期:2010-09-01 00:00:00

  • A physicochemical basis for the extensive intestinal lymphatic transport of a poorly lipid soluble antimalarial, halofantrine hydrochloride, after postprandial administration to dogs.

    abstract::The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Khoo SM,Prankerd RJ,Edwards GA,Porter CJ,Charman WN

    更新日期:2002-03-01 00:00:00

  • Stabilizing effect of fructose on aqueous solutions of hydrocortisone.

    abstract::Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bansal NP,Holleran EM,Jarowski CI

    更新日期:1983-09-01 00:00:00

  • Potential antineoplastics I: substituted 3,5-dioxo-and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines.

    abstract::The synthesis of some 6-substituted 3,5-dioxo- and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines for possible antineoplastic activity is reported. The assigned structures were substantiated by IR, NMR, and mass spectral studies of representative members of the series. Four compounds were tested against P-388 lymph...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ibrahim el-SA,Shams el-Dine SA,Soliman FS,Labouta IM

    更新日期:1979-02-01 00:00:00

  • A novel approach to preparing water soluble prodrug forms of cisplatin analogues bearing chelating diamines.

    abstract::A novel method for creating water soluble prodrugs of cisplatin analogues bearing chelating diamines is introduced. When 2-(amino-methyl)aniline is reacted with K2PtCl4 between a pH of 6 and 7, the neutral chelated complex [2-(aminomethyl)aniline)dichloroplatinum(II) (1) is isolated. On the other hand, when the comple...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Köckerbauer R,Bednarski PJ

    更新日期:1995-07-01 00:00:00

  • The Role of Physiologically Based Oral Absorption Modelling in Formulation Development Under a Quality by Design Paradigm.

    abstract::Within the last decade, Quality by Design (QbD) has been getting increased attention in its implementation in the development of pharmaceutical drug products. Understanding of the impact of formulation composition and process on clinical performance is a centerpiece of QbD. Physiologically based pharmacokinetic modeli...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kesisoglou F

    更新日期:2017-04-01 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

  • Thermodynamics of the Enantiotropic Pharmaceutical Compound Benzocaine and Solubility in Pure Organic Solvents.

    abstract::The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cheuk D,Svärd M,Rasmuson ÅC

    更新日期:2020-11-01 00:00:00

  • Effect of repeated skin application on percutaneous absorption of salicylic acid.

    abstract::Various concentrations of salicylic acid in hydrophilic ointment were applied repeatedly at daily or weekly intervals to rats in vivo. Salicylic acid absorption through treated skin was monitored by determining the penetration fluxes of salicylic acid through skin excised at various times. A gradual decrease in the sa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Roberts MS,Harlock E

    更新日期:1978-12-01 00:00:00

  • Survival of Staphylococcus aureus in oral administration liquid medicaments and influence of count medium on survival.

    abstract::The survival of Staphylococcus aureus was studied in 30 oral administration liquid medicaments (15 syrups and 15 solutions) to determine the effectiveness of the preservatives, the influence of the culture medium used in the enumeration of the surviving microorganisms, and the loss of the enzyme coagulase, phosphatase...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vivar C,de la Rosa C,Mosso A

    更新日期:1993-02-01 00:00:00

  • Investigation of PEG crystallization in frozen PEG-sucrose-water solutions: II. Characterization of the equilibrium behavior during freeze-thawing.

    abstract::Our objective was to characterize, by DSC and XRD, the equilibrium thermal behavior of frozen aqueous solutions containing polyethylene glycol (PEG) and sucrose. Aqueous solutions of (i) PEG (2.5-50% w/w), (ii) sucrose (10% w/v) with different concentrations of PEG (1-20% w/v), and (iii) PEG (2% or 10% w/v) with diffe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bhatnagar BS,Martin SM,Teagarden DL,Shalaev EY,Suryanarayanan R

    更新日期:2010-11-01 00:00:00

  • Enhanced econazole penetration into human nail by 2-n-nonyl-1,3-dioxolane.

    abstract::This study determines the enhancing effects of 2-n-nonyl-1,3-dioxolane on the penetration of econazole, an antifungal drug, into the deeper layers of the human nail where fungal infection resides. Aliquots (10 microL) of Econail lacquer formulation containing 0.45 mg of [(14)C]-econazole with 18% 2-n-nonyl-1,3-dioxola...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hui X,Chan TC,Barbadillo S,Lee C,Maibach HI,Wester RC

    更新日期:2003-01-01 00:00:00