Impact of recovery on fraction unbound using equilibrium dialysis.

abstract：:To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

journal_title：Journal of pharmaceutical sciences

authors： Ito Y,Yoshimura M,Tanaka T,Takada K

更新日期：2012-03-01 00:00:00

abstract：:A high-speed liquid chromatographic system is described, which can be used for the simultaneous identification of the anabolic steroid methandrostenolone and its impurities and the quantitation of each of these compounds. Separation is effected by adsorption chromatography on a slurry-packed microparticulate silica ge...

journal_title：Journal of pharmaceutical sciences

authors： Butterfield AG,Lodge BA,Pound NJ,Sears RW

更新日期：1975-03-01 00:00:00

abstract：:The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

journal_title：Journal of pharmaceutical sciences

authors： Meffin PJ,Williams RL,Blaschke TF,Rowland M

更新日期：1977-01-01 00:00:00

abstract：:The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur wa...

journal_title：Journal of pharmaceutical sciences

authors： Ehlhardt WJ,Sullivan HR,Wood PG,Woodland JM,Hamilton M,Hamilton C,Cornpropst D,Grindey GB,Worzalla JF,Bewley JR

更新日期：1993-07-01 00:00:00

abstract：:Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...

journal_title：Journal of pharmaceutical sciences

authors： Grampp G,McElroy PL,Camblin G,Pollock A

更新日期：2018-06-01 00:00:00

abstract：:Dissolution profiles are classified in accordance with the shape of fractional dissolution rate function. This function is constant in time for the classical first-order model and, in this case, the dissolution is described by a monoexponential function. Therefore, any deviation of the fractional dissolution rate from...

journal_title：Journal of pharmaceutical sciences

authors： Lánský P,Weiss M

更新日期：2003-08-01 00:00:00

abstract：:With the introduction of Quality by Design (QbD) to the pharmaceutical industry, there has been an increased focus on understanding the nature of particles and composites, with the aim of understanding and modeling how they interact in complex systems, leading to robust dosage forms. Particle characterization tools ha...

journal_title：Journal of pharmaceutical sciences

authors： Gamble JF,Tobyn M,Hamey R

更新日期：2015-05-01 00:00:00

abstract：:Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...

journal_title：Journal of pharmaceutical sciences

authors： Ohta T,Hashida Y,Yamashita F,Hashida M

更新日期：2016-09-01 00:00:00

abstract：:A new High-performance liquid chromatographic (HPLC) method for the assay of sodium fusidate (I) or fusidic acid in dosage forms was developed and compared to a microbiological assay. A linear relationship was obtained between absolute peak area and amount of I(r = 0.99+) in the 50-1000-microgram/ml range. In the micr...

journal_title：Journal of pharmaceutical sciences

authors： Hikal AH,Shibl A,El-Hoofy S

更新日期：1982-11-01 00:00:00

abstract：:The full parameterization for the stratum corneum biphasic microtransport model presented previously in this Journal [95:620-648 (2006)] is developed through a combination of fundamental transport theory and calibration with existing data. Of the five microscopic transport properties, four (D(cor), K(cor/w), D(lip), K...

journal_title：Journal of pharmaceutical sciences

authors： Wang TF,Kasting GB,Nitsche JM

更新日期：2007-11-01 00:00:00

abstract：:Fifteen pyrimidine-related compounds were evaluated for their ability to inhibit enzymatic degradation of 5-fluoro-2'-deoxyuridine (FUdR). Acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil] showed the highest inhibitory effect on the phosphorolytic degradation of FUdR in various tissue homogenates derived fro...

journal_title：Journal of pharmaceutical sciences

authors： Kawaguchi T,Saito M,Saneyoshi M

更新日期：1988-11-01 00:00:00

abstract：:Cholesterol promotes basal and verapamil-induced ATPase activity of P-glycoprotein (P-gp). We investigated whether these effects are related to each other and to the impact of the sterol on bilayer fluidity and verapamil membrane affinity. P-gp was reconstituted in egg-phosphatidylcholine (PhC) liposomes with or witho...

journal_title：Journal of pharmaceutical sciences

authors： Belli S,Elsener PM,Wunderli-Allenspach H,Krämer SD

更新日期：2009-05-01 00:00:00

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 00:00:00

abstract：:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusua...

journal_title：Journal of pharmaceutical sciences

authors： Leong NJ,Prankerd RJ,Shackleford DM,Mcintosh MP

更新日期：2015-04-01 00:00:00

abstract：:In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hyd...

journal_title：Journal of pharmaceutical sciences

authors： Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

更新日期：1979-03-01 00:00:00

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

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

abstract：:The sensitivity of pharmacokinetic deconvolution algorithms with respect to simulated experimental error has been studied. Approximations of cumulative absorption profiles reconstructed from simulated data sets with normally distributed random error were compared with corresponding known input functions. The coinciden...

journal_title：Journal of pharmaceutical sciences

authors： Süverkrüp R,Bonnacker I,Raubach HJ

更新日期：1989-11-01 00:00:00

abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...

journal_title：Journal of pharmaceutical sciences

authors： Kinoshita H,Nakamaru R,Tanaka S,Tohira Y,Sawada M

更新日期：1986-07-01 00:00:00

abstract：:Clinical lots of recombinant human platelet-activating factor acetylhydrolase (rhPAF-AH) were prepared in a lyophilized formulation. After reconstitution with sterile water for injection to form an aqueous solution (10 mM sodium citrate, 7.5 w/v% sucrose, and 0.1 w/v% Pluronic-F68, pH 6.5), a few visible, slowly growi...

journal_title：Journal of pharmaceutical sciences

authors： Chi EY,Weickmann J,Carpenter JF,Manning MC,Randolph TW

更新日期：2005-02-01 00:00:00

abstract：:A high-performance liquid chromatographic method was developed for the simultaneous determination of azobenzene, hydrazobenzene, and four other decomposition products in phenylbutazone injectable formulations. Separation was achieved on a C18 column, with 0.1 M Tris-citrate buffer (pH 5.25) and acetonitrile (52:48), a...

journal_title：Journal of pharmaceutical sciences

authors： Fabre H,Hussam-Eddine N,Mandrou B

更新日期：1984-12-01 00:00:00

abstract：:A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...

journal_title：Journal of pharmaceutical sciences

authors： Clark CR,McMillian CL

更新日期：1990-03-01 00:00:00

abstract：:Studies directed at the synthesis of tetracycline ring A analogs are described. 4-Carbethoxycyclohexane-1,3-dione was converted to the ethyl urethan dispiro[1,3-dioxolane-2,2'-cyclohexane-4',2"(1,3)-dioxolane]-1'-carbamic acid ethyl ester via the dispiro[1,3-dioxolane-2,2'-cyclohexane-4'-2"(1,3)-dioxolane]-1'-carboxyl...

journal_title：Journal of pharmaceutical sciences

authors： Moskalyk RE,Mak AL,Chatten LG,Locock RA

更新日期：1981-05-01 00:00:00

abstract：:Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...

journal_title：Journal of pharmaceutical sciences

authors： Perevozchikova T,Nanda H,Nesta DP,Roberts CJ

更新日期：2015-06-01 00:00:00

abstract：:The increased incidence of human immunodeficiency virus infection in women has identified an urgent need to develop a female-controlled method to prevent acquisition of human immunodeficiency virus and other sexually transmitted diseases. Women would apply the product intravaginally before intercourse. Development of ...

journal_title：Journal of pharmaceutical sciences

authors： Sassi AB,McCullough KD,Cost MR,Hillier SL,Rohan LC

更新日期：2004-08-01 00:00:00

abstract：:A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and c...

journal_title：Journal of pharmaceutical sciences

authors： Yu D,Wong J,Matsuda Y,Fox JL,Higuchi WI,Otsuka M

更新日期：1992-06-01 00:00:00

abstract：:We investigated the effects of excipients in solutions of keratinocyte growth factor 2 (KGF-2) on protein aggregation during agitation as well as on interfacial shear rheology at the air-water interface. Samples were incubated with or without agitation, and in the presence or absence of the excipients heparin, sucrose...

journal_title：Journal of pharmaceutical sciences

authors： Liu L,Qi W,Schwartz DK,Randolph TW,Carpenter JF

更新日期：2013-08-01 00:00:00

abstract：:The recombinant fusion proteins hybrid 1 [H1 (Ag85B-ESAT-6)] and hybrid 56 [H56 (Ag85B-ESAT-6-Rv2660c)] derived from Mycobacterium tuberculosis are promising antigens for subunit vaccines against tuberculosis. Both antigens are early batches of antigens to be enrolled in human clinical trials and it is therefore impor...

journal_title：Journal of pharmaceutical sciences

authors： Hamborg M,Kramer R,Schanté CE,Agger EM,Christensen D,Jorgensen L,Foged C,Middaugh CR

更新日期：2013-10-01 00:00:00

abstract：:This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

journal_title：Journal of pharmaceutical sciences

authors： Jong T,Li J,Morton DA,Zhou QT,Larson I

更新日期：2016-03-01 00:00:00

abstract：:Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...

journal_title：Journal of pharmaceutical sciences

authors： Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Y

更新日期：2007-06-01 00:00:00

abstract：:Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...

journal_title：Journal of pharmaceutical sciences

authors： Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda T

更新日期：1996-09-01 00:00:00