Finite dose pharmacokinetics of skin penetration.

Abstract:

:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of skin-vehicle parameters for large doses and, under certain conditions, can even reduce to the total excretory rate constant as the dose is decreased.

journal_name

J Pharm Sci

authors

Cooper ER,Berner B

doi

10.1002/jps.2600741018

subject

Has Abstract

pub_date

1985-10-01 00:00:00

pages

1100-2

issue

10

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)46914-X

journal_volume

74

pub_type

杂志文章
  • Detection of a minor amorphous phase in crystalline etoricoxib by dynamic mechanical analysis: comparison with Raman spectroscopy and modulated differential scanning calorimetry.

    abstract::Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22774

    authors: Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

    更新日期:2012-02-01 00:00:00

  • Preparation of pH-sensitive beads for NSAID using three-component gel systems.

    abstract::The aim of this study is to prepare novel pH-sensitive beads to obtain a gastric mucosa protective formulation and to ensure drug delivery into the intestine. Diclofenac sodium was used as a model drug. Bead formation was achieved by ionotropic gelation method using three-component gel system containing sodium alginat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21713

    authors: Fenyvesi Z,Auner A,Schmalz D,Pásztor E,Csóka G,Gyires K,Marton S,Klebovich I,Antal I

    更新日期:2009-11-01 00:00:00

  • Kinetics and stability of a multicomponent organophosphate antidote formulation in glass and plastic.

    abstract::An aqueous solution of trimedoxime bromide, atropine, and benactyzine hydrochloride was formulated to have maximum stability as an antidote in organophosphorus poisoning. The stability of the mixture in glass and plastic cartridges was determined. Glass cartridges were more desirable than plastic; there was less vapor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710315

    authors: Zvirblis P,Ellin RI

    更新日期:1982-03-01 00:00:00

  • Determination of the structural relaxation at the surface of amorphous solid dispersion using inverse gas chromatography.

    abstract::Amorphous dispersions provide an excellent way of increasing dissolution rates of poorly soluble drugs, but there may be concerns about stability. One way of assessing the stability of amorphous is the study of relaxation. In this study the relaxation at the surface of amorphous solid dispersions (SDs) was evaluated u...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21573

    authors: Hasegawa S,Ke P,Buckton G

    更新日期:2009-06-01 00:00:00

  • Compatibility, physical stability, and characterization of an IgG4 monoclonal antibody after dilution into different intravenous administration bags.

    abstract::The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23224

    authors: Kumru OS,Liu J,Ji JA,Cheng W,Wang YJ,Wang T,Joshi SB,Middaugh CR,Volkin DB

    更新日期:2012-10-01 00:00:00

  • Pharmacokinetic aspects of biotechnology products.

    abstract::In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.20125

    authors: Tang L,Persky AM,Hochhaus G,Meibohm B

    更新日期:2004-09-01 00:00:00

  • Fluorometric determination of trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles in biological materials.

    abstract::Interest in the 5-, 6-, and 7-trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles as potent, orally active anti-inflammatory agents required a method for their determination in serum, urine, and feces to permit studies of their absorption, metabolism, and excretion. A simple, rapid, sensitive, and specific pro...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600651218

    authors: Kaiser DG,Liggett WF,Forist AA

    更新日期:1976-12-01 00:00:00

  • Understanding disintegrant action by visualization.

    abstract::The aim of this study was to utilize high-speed video imaging for understanding the disintegrability of compacts and disintegrant action upon wetting. High-speed video imaging was used to visualize the disintegration of compacts and effect of wetting on free disintegrant particles. Acquired images were processed using...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23119

    authors: Desai PM,Liew CV,Heng PW

    更新日期:2012-06-01 00:00:00

  • Explication of Definitional Description and Empirical Use of Fraction of Orally Administered Drugs Absorbed From the Intestine (Fa) and Intestinal Availability (Fg): Effect of P-glycoprotein and CYP3A on Fa and Fg.

    abstract::Conventionally, it is believed that the fraction of orally administered drugs absorbed from the intestine (Fa) and intestinal availability (Fg) are independently determined by the apical membrane permeation and intestinal metabolism, respectively. However, the validity of this belief has not been well discussed, and F...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2015.11.005

    authors: Tanaka Y,Kitamura Y,Maeda K,Sugiyama Y

    更新日期:2016-02-01 00:00:00

  • Solubility and dissolution rate studies of ergotamine tartrate.

    abstract::The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690723

    authors: Anderson JR,Pitman IH

    更新日期:1980-07-01 00:00:00

  • A valid equation for the well-stirred perfusion limited physiologically based pharmacokinetic model that consistently accounts for the blood-tissue drug distribution in the organ and the corresponding valid equation for the steady state volume of distribu

    abstract::A consistent account of the assumptions of the well-stirred perfusion limited model leads to the equation for the organ tissue that does not coincide with that often presented in books and papers. The difference in pharmacokinetic profiles calculated by the valid and the commonly used equations could be quite signific...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21798

    authors: Berezhkovskiy LM

    更新日期:2010-01-01 00:00:00

  • The effects of substituted cyclodextrins on the colloidal and conformational stability of selected proteins.

    abstract::The effects of various types of substituted and nonsubstituted cyclodextrins (CDs) on the physical and colloidal stability of three different proteins were studied to further ascertain the mechanism by which cyclodextrins stabilize proteins. The three proteins examined in this study are the Clostridium difficile Toxoi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22053

    authors: Samra HS,He F,Bhambhani A,Pipkin JD,Zimmerer R,Joshi SB,Middaugh CR

    更新日期:2010-06-01 00:00:00

  • Solid-state dispersions employing urethan.

    abstract::The dissolution rates of a number of drug-urethan solid-state dispersion systems were studied. A marked enhancement of the initial dissolution rates of several poorly water-soluble drugs was found when they were incorporated into a urethan matrix by heat fusion. These differences were considerable when pure substances...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670332

    authors: Maulding HV

    更新日期:1978-03-01 00:00:00

  • Quantitative structure/property relationship analysis of Caco-2 permeability using a genetic algorithm-based partial least squares method.

    abstract::Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10214

    authors: Yamashita F,Wanchana S,Hashida M

    更新日期:2002-10-01 00:00:00

  • Model-independent steady-state plasma level predictions in autonomic nonlinear pharmacokinetics I: Derivation and theoretical analysis.

    abstract::Current drug level predictions in nonlinear pharmacokinetics are based on specific pharmacokinetic models in contrast to the model-independent (structureless), dose-linearity, and superposition principles used in linear pharmacokinetics. Such model-dependent methods may not provide reliable predictions due to their in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730614

    authors: Veng-Pedersen P

    更新日期:1984-06-01 00:00:00

  • Pharmacokinetics of dopamine-2 agonists in rats and dogs.

    abstract::The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600751002

    authors: Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

    更新日期:1986-10-01 00:00:00

  • Preparation and characterization of Apo2L/TNF-related apoptosis-inducing ligand-loaded human serum albumin nanoparticles with improved stability and tumor distribution.

    abstract::Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has received considerable attention as a potential anticancer agent. However, recombinant Apo2L/TRAIL has several limitations, which include a weak pharmacokinetic profile, namely, a short biological half-life and rapid renal clearance, and an inability t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22298

    authors: Kim TH,Jiang HH,Youn YS,Park CW,Lim SM,Jin CH,Tak KK,Lee HS,Lee KC

    更新日期:2011-02-01 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

  • Determination of mianserin and metabolites in plasma by liquid chromatography with electrochemical detection.

    abstract::A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710812

    authors: Suckow RF,Cooper TB,Quitkin FM,Stewart JW

    更新日期:1982-08-01 00:00:00

  • A site-directed mutagenesis study of drug-binding selectivity in genetic variants of human alpha(1)-acid glycoprotein.

    abstract::Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21697

    authors: Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

    更新日期:2009-11-01 00:00:00

  • Profile of P-glycoprotein distribution in the rat and its possible influence on the salbutamol intestinal absorption process.

    abstract::The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20071

    authors: Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

    更新日期:2004-06-01 00:00:00

  • Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effects of FcRn Inhibitors in Mice, Rats, and Monkeys.

    abstract::There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.065

    authors: Li T,Balthasar JP

    更新日期:2019-01-01 00:00:00

  • The Influence of In Vivo Metabolic Modifications on ADMET Properties of Green Tea Catechins-In Silico Analysis.

    abstract::The health effects of green tea are associated with catechins: (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin, (-)-epicatechin-3-O-gallate, and (-)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.07.026

    authors: Matić S,Jadrijević-Mladar Takač M,Barbarić M,Lučić B,Gall Trošelj K,Stepanić V

    更新日期:2018-11-01 00:00:00

  • Novel method of derivatization of an amidinourea (lidamidine) for GLC analysis.

    abstract::A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710327

    authors: Won CM,Zalipsky JJ,Patel DM,Grim WM

    更新日期:1982-03-01 00:00:00

  • Structural and thermal characterization of zolpidem hemitartrate hemihydrate (Form E) and its decomposition products by laboratory X-ray powder diffraction.

    abstract::The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21883

    authors: Halasz I,Dinnebier RE

    更新日期:2010-02-01 00:00:00

  • X-ray diffraction and infrared spectroscopy of N,N-dimethylformamide and dimethyl sulfoxide solvatomorphs of betulonic acid.

    abstract::X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23321

    authors: Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

    更新日期:2012-12-01 00:00:00

  • Tissue distribution of terbinafine in rats.

    abstract::Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1132

    authors: Hosseini-Yeganeh M,McLachlan AJ

    更新日期:2001-11-01 00:00:00

  • Development of a Stable Liquid Formulation for Live Attenuated Influenza Vaccine.

    abstract::Live attenuated influenza vaccine (LAIV) is considered one of the most effective vaccines and can be manufactured quickly and inexpensively to counter seasonal or pandemic influenza. Lyophilization is widely used in vaccine production. However, it requires a longer production cycle and large-scale equipment, thus posi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.02.017

    authors: Sun Y,Shen Z,Zhang C,Yi Y,Zhu K,Xu F,Kong W

    更新日期:2019-07-01 00:00:00

  • A novel method for the preparation of liposomes: freeze drying of monophase solutions.

    abstract::A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20055

    authors: Li C,Deng Y

    更新日期:2004-06-01 00:00:00

  • Metabolic fate and solubility of triamterene--not an explanation for triamterene nephrolithiasis.

    abstract::In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600750205

    authors: Sörgel F,Ettinger B,Benet LZ

    更新日期:1986-02-01 00:00:00