Effect of lipophilicity on the bioavailability of drugs after percutaneous administration by dissolving microneedles.

abstract：:A method that accurately indicates the end-point of precipitation reactions by the measurement of the relative intensity of the scattered light in the titrate is presented. A new nephelometric titrator with an internal nephelometric sensor has been devised. The work of the titrator including the sensor and change in t...

journal_title：Journal of pharmaceutical sciences

authors： Zhan X,Li C,Li Z,Yang X,Zhong S,Yi T

更新日期：2004-02-01 00:00:00

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

authors： Ivashikiv E

更新日期：1978-07-01 00:00:00

abstract：:Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...

journal_title：Journal of pharmaceutical sciences

authors： Lee YC,Zhou G,Ikeda C,Chouzouri G,Howell L

更新日期：2019-03-01 00:00:00

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

authors： Mager DE,Jusko WJ

更新日期：2002-11-01 00:00:00

abstract：:Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs). This study was aimed to investigate the effect of solid-liquid interactions of an encapsulated ASD on drug release. Drug release profiles of a molecularly interacting amorphous celecoxib solid...

journal_title：Journal of pharmaceutical sciences

authors： Puri V,Dantuluri AK,Bansal AK

更新日期：2011-06-01 00:00:00

abstract：:Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent. Oral administration of allopurinol in a polyethylene glycol suspension, to which allopurinol may be reversibly...

journal_title：Journal of pharmaceutical sciences

authors： Patel VS,Kramer WG

更新日期：1986-03-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00

abstract：:3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

更新日期：1984-07-01 00:00:00

abstract：:The molecular modeling program SYBYL was used to simulate the adsorption of various barbiturates by an activated charcoal surface. The compounds barbituric acid (BA), barbital (B), phenobarbital (PB), mephobarbital (M), and primidone (Pr) were modeled, and their structures were energetically minimized. These structure...

journal_title：Journal of pharmaceutical sciences

authors： Wurster DE,Kolling WM,Knosp BM

更新日期：1994-12-01 00:00:00

abstract：:The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

journal_title：Journal of pharmaceutical sciences

authors： Wang DP,Tu YH,Allen LV Jr

更新日期：1988-11-01 00:00:00

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

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

更新日期：1991-01-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 00:00:00

abstract：:Poly(methyl [1-14C]methacrylate) nanoparticles were injected subcutaneously into rats. Almost all of the radioactivity stayed at the injection site. After an initial urinary and fecal excretion of approximately 1% of the administered dose per day, the rate of elimination dropped to a low level (approximately 0.005%/da...

journal_title：Journal of pharmaceutical sciences

authors： Kreuter J,Nefzger M,Liehl E,Czok R,Voges R

更新日期：1983-10-01 00:00:00

abstract：:A simple and sensitive assay for quantitating 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (1; BMY 26517) in human plasma was developed using high-performance liquid chromatography with fluorescence detection. The method involves precipitation of protein and reversed-phase chromatography. The method i...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Pittman KA,Dandekar KA

更新日期：1987-12-01 00:00:00

abstract：:Acrylic acid-esterified starch was produced by reacting starch with acrylic acid chloride. This reaction was rapid and easy to control. Introduction of acrylic groups into starch reduced the enzymatic degradability of starch (e.g., with 12 acrylic groups/100 glucose residues, approximately 75% of the degradation produ...

journal_title：Journal of pharmaceutical sciences

authors： Laakso T,Sjöholm I

更新日期：1987-12-01 00:00:00

abstract：:Many pharmaceuticals are formulated as powders to aid drug delivery. A major problem is how to produce powders having high purity, controlled morphology, and retained bioactivity. We demonstrate the use of supercritical carbon dioxide as an antisolvent for meeting this need for two model drug systems, quercetin, a spa...

journal_title：Journal of pharmaceutical sciences

authors： Jacobson GB,Shinde R,McCullough RL,Cheng NJ,Creasman A,Beyene A,Hickerson RP,Quan C,Turner C,Kaspar RL,Contag CH,Zare RN

更新日期：2010-06-01 00:00:00

abstract：:A new indole based chalcone molecule MOMIPP induced methuosis mediated cell death in gliobastoma and other cancer cell lines. But the drug was insoluble in water and had a very short plasma half-life. The purpose of this work was to develop a formulation that can provide sustained levels of MOMIPP in vivo. Initial stu...

journal_title：Journal of pharmaceutical sciences

authors： Oppong F,Li Z,Fakhrabadi EA,Raorane T,Giri PM,Liberatore MW,Sarver JG,Trabbic CJ,Hosier CE,Erhardt PW,Maltese WA,Nesamony J

更新日期：2020-09-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 00:00:00

abstract：:Crystallization of polymorphs still has a touch of art, as even prior observations of polymorphs do not guarantee their crystallization. However, once crystals of various polymorphs have been obtained, their relative stabilities can be established with a straightforward thermodynamic approach even if the conclusion wi...

journal_title：Journal of pharmaceutical sciences

authors： Rietveld IB,Céolin R

更新日期：2015-12-01 00:00:00

abstract：:In this article, we show that crystalline lactulose can be amorphized directly in the solid state by mechanical milling. Moreover, compared to similar materials, the amorphization kinetics of lactulose is found to be very rapid and the amorphous state thus obtained appears to be very stable against recrystallization o...

journal_title：Journal of pharmaceutical sciences

authors： Ngono F,Willart JF,Cuello G,Jimenez-Ruiz M,Affouard F

更新日期：2019-02-01 00:00:00

abstract：:Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medi...

journal_title：Journal of pharmaceutical sciences

authors： He W,Jiang X,Zhang ZR

更新日期：2008-06-01 00:00:00

abstract：:As part of a series of articles in this special issue evaluating model IgG1-Fc glycoforms for biosimilarity analysis, 3 well-defined IgG1-Fc glycoforms (high mannose-Fc, Man5-Fc, and N-acetylglucosamine-Fc) and a nonglycosylated Fc protein (N297Q-Fc) were examined in this work to elucidate chemical degradation pathway...

journal_title：Journal of pharmaceutical sciences

authors： Mozziconacci O,Okbazghi S,More AS,Volkin DB,Tolbert T,Schöneich C

更新日期：2016-02-01 00:00:00

abstract：:An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...

journal_title：Journal of pharmaceutical sciences

authors： Metzler CM

更新日期：1987-07-01 00:00:00

abstract：:A physiological flow model was developed for the distribution of sulfathiazole residues in various tissues in swine. The approach was compartmental, in which the compartments and equilibrium constants had physiological meaning. Differential equations were developed, and appropriate parameter values and initial conditi...

journal_title：Journal of pharmaceutical sciences

authors： Duddy J,Hayden TL,Bourne DW,Fiske WD,Benedek IH,Stanley D,Gonzalez A,Heierman W

更新日期：1984-11-01 00:00:00

abstract：:The hydrogen-bonded interactions of chloral hydrate and halide ions have been investigated conductometrically at 25.00 degrees C in aqueous solutions. In spite of the strong competing effect of water, the 1:1 associates have relatively high stability constants, in the order of chloride greater than bromide greater tha...

journal_title：Journal of pharmaceutical sciences

authors： Barcza L,Lenner L

更新日期：1988-07-01 00:00:00

abstract：:It is understood that a potential issue for drugs with poor aqueous solubility is low oral absorption. If oral exposure issues arise when working with a low solubility drug candidate, the common action is to rely on enabling formulations to solve the issue. However, this approach becomes troublesome in the pre-clinica...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Sutherlin D,Pang J,Salphati L

更新日期：2016-06-01 00:00:00

abstract：:A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...

journal_title：Journal of pharmaceutical sciences

authors： Mayberry DO,Kowblansky M,Lane PA,Wray PE

更新日期：1990-08-01 00:00:00

abstract：:The ratio between ocular and systemic drug concentrations describes the relative safety of ophthalmic dosage forms of the same drug in terms of its systemic side effects. In this study, we evaluated the effects of epinephrine pretreatment and solution pH on the aqueous humor:plasma and iris-ciliary body:plasma ratios ...

journal_title：Journal of pharmaceutical sciences

authors： Kyyrönen K,Urtti A

更新日期：1990-08-01 00:00:00

abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

journal_title：Journal of pharmaceutical sciences

authors： Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

更新日期：1990-07-01 00:00:00