Modeling microstructure development and release kinetics in controlled drug release coatings.

Abstract:

:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are not well established. We apply a thermodynamically consistent model to probe the influence of drug-polymer chemistry (phobicity), drug loading, and evaporation rate on microstructure development during fabrication. For these structures, we compute release profiles for exposure to polymer-insoluble media and media in which the polymer readily dissolves. We find that with increasing drug-polymer phobicity, structural heterogeneities form at lower loadings and more rapid rates. The heterogeneities remain isolated and compact at low loadings and become interconnected as the drug to polymer ratio approaches 1.0. Release into polymer-insoluble media was dramatically enhanced by heterogeneities, resulting in up to a fourfold increase in drug release. In polymer-soluble media, however, heterogeneities diminished release. Although reductions of only 30% were typically observed, the absolute changes were much larger than observed in polymer-insoluble media. Our results suggest that improved comprehension and quantification of the physico-chemical properties in controlled release systems will enable the microstructure to be tailored to achieve desired responses that are insensitive to manufacturing variations.

journal_name

J Pharm Sci

authors

Saylor DM,Kim CS,Patwardhan DV,Warren JA

doi

10.1002/jps.21416

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

169-86

issue

1

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)32841-6

journal_volume

98

pub_type

杂志文章
  • Liposomes as carriers for topical and transdermal delivery.

    abstract::The delivery of active agents to the skin by liposome carriers is an interdisciplinary topic of great interest today. Data accumulated over the last decade strongly point to important advantages of these drug delivery systems. A symposium devoted to classic and new approaches in the use of liposomal systems was organi...

    journal_title:Journal of pharmaceutical sciences

    pub_type:

    doi:10.1002/jps.2600830902

    authors: Touitou E,Junginger HE,Weiner ND,Nagai T,Mezei M

    更新日期:1994-09-01 00:00:00

  • Concomitant adsorption and stability of some anthracycline antibiotics.

    abstract::Using liquid scintillation counting and liquid chromatographic techniques, it has been demonstrated that the anthracycline antibiotics, doxorubicin hydrochloride, N-trifluoroacetyladriamycin-14-valerate, and N-trifluoroacetyladriamycin-14-octanoate, can be strongly absorbed to the walls of containers, depending on the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600711011

    authors: Tomlinson E,Malspeis L

    更新日期:1982-10-01 00:00:00

  • GLC determination of methenamine in tablets.

    abstract::A rapid and sensitive GLC method was developed for the quantitative determination of methenamine in tablets. The method was shown to possess several advantages over the official NF assay. After dissolution of the whole tablet in absolute ethanol and addition of an internal standard (pentylenetetrazol), an aliquot was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660435

    authors: Strom JG Jr,Jun HW

    更新日期:1977-04-01 00:00:00

  • Iontophoretic transdermal delivery of sumatriptan: effect of current density and ionic strength.

    abstract::Iontophoretic transdermal delivery of sumatriptan was investigated in vitro. Among the conditions tested, 0.25 mA/cm2 and low ionic strength (NaCl 25 mM) was the best experimental condition to increase its transport across the skin. The flux increased 385-fold respective to passive diffusion, thus resulting in a trans...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20447

    authors: Femenía-Font A,Balaguer-Fernández C,Merino V,López-Castellano A

    更新日期:2005-10-01 00:00:00

  • On the mechanism and dynamics of uptake and permeation of polyether-copolyester dendrimers across an in vitro blood-brain barrier model.

    abstract::Dendrimers have emerged as a promising drug delivery system due to their well defined size, tailorability, and multifunctional nature. However, their application in brain delivery is relatively a new area of research. The present study was aimed at evaluating the uptake and permeation of polyether-copolyester (PEPE) d...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21669

    authors: Dhanikula RS,Hammady T,Hildgen P

    更新日期:2009-10-01 00:00:00

  • Fetal and maternal placental and nonplacental clearances of metoclopramide in chronically instrumented pregnant sheep.

    abstract::The placental and nonplacental clearances of metoclopramide were studied in nine chronically instrumented, near-term pregnant sheep using a two-compartment open model. Metoclopramide was administered to the ewe and fetus on separate occasions as an initial iv bolus loading dose followed by a constant-rate infusion, wi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600791204

    authors: Riggs KW,Rurak DW,Taylor SM,McErlane BA,McMorland GH,Axelson JE

    更新日期:1990-12-01 00:00:00

  • Deiodination kinetics of water-soluble radiopaques.

    abstract::Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690616

    authors: Wang YC

    更新日期:1980-06-01 00:00:00

  • High-performance liquid chromatographic determination of 4-amino-5-chloro-N-[(1-ethylimidazolin-2-yl)methyl]-2-methoxybenzamide and its metabolite in biological fluids. Applications in pharmacokinetic studies.

    abstract::A high-performance liquid chromatographic method with spectrofluorometric detection has been developed for the analysis of a new substituted benzamide and its metabolite in body fluids. The detection was performed at 270 nm for excitation, and 370 nm for emission. The proposed technique is selective, reliable, and sen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790617

    authors: Bressolle F,Bres J,Moulin A

    更新日期:1990-06-01 00:00:00

  • Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

    abstract::The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680208

    authors: Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

    更新日期:1979-02-01 00:00:00

  • Quantification of phencyclidine in mainstream smoke and identification of phenylcyclohex-1-ene as pyrolysis product.

    abstract::Parsley cigarettes containing [3H]phencyclidine were machine smoked, and the mainstream smoke was trapped in glass wool filters. Radioactivity was extracted from these filters with chloroform. The average recoveries of radioactivity were 76, 85, 70, and 69% for cigarettes containing 3, 10, 30, and 50 mg of [3H]phencyc...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700908

    authors: Freeman AS,Martin BR

    更新日期:1981-09-01 00:00:00

  • Gas chromatographic determination of a diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids.

    abstract::A method for the measurement of a potential diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids is described. The procedure involves the addition of a related internal standard to the specimens followed by extraction of the acids into...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730234

    authors: Weidner LL,Zacchei AG

    更新日期:1984-02-01 00:00:00

  • Verification and validation of computational models used in biopharmaceutical manufacturing: Potential application of the ASME Verification and Validation 40 standard and FDA proposed AI/ML model life cycle management framework.

    abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2021.01.016

    authors: Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

    更新日期:2021-01-22 00:00:00

  • Do multidrug resistance-associated protein-1 and -2 play any role in the elimination of estradiol-17 beta-glucuronide and 2,4-dinitrophenyl-S-glutathione across the blood-cerebrospinal fluid barrier?

    abstract::The purpose of this study was to examine the role of multidrug resistance-associated protein-1 and -2 (Mrp1 and Mrp2) in the efflux transport of organic anions across the blood-cerebrospinal fluid (CSF) barrier. The CSF concentration of estradiol-17beta-glucuronide (E(2)17betaG) and 2,4-dinitrophenyl-S-glutathione (DN...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10521

    authors: Lee YJ,Kusuhara H,Sugiyama Y

    更新日期:2004-01-01 00:00:00

  • Very rapid dissolution is not needed to guarantee bioequivalence for biopharmaceutics classification system (BCS) I drugs.

    abstract::Currently, the EMEA, FDA, and WHO as regulatory authorities accept rapidly dissolving (>85% dissolved in 30 min) biopharmaceutics classification system (BCS) I drug products for biowaiver candidates. In the draft EMEA guideline the requirement has been set tighter, that is, the drug product should be very rapidly diss...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21879

    authors: Kortejärvi H,Shawahna R,Koski A,Malkki J,Ojala K,Yliperttula M

    更新日期:2010-02-01 00:00:00

  • Synthesis and cytotoxic evaluation of some cyclic arylidene ketones and related oximes, oxime esters, and analogs.

    abstract::A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the alpha,beta-unsaturated ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830619

    authors: Dimmock JR,Sidhu KK,Chen M,Li J,Quail JW,Allen TM,Kao GY

    更新日期:1994-06-01 00:00:00

  • Development of aqueous parenteral formulations for carbamazepine through the use of modified cyclodextrins.

    abstract::The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800420

    authors: Brewster ME,Anderson WR,Estes KS,Bodor N

    更新日期:1991-04-01 00:00:00

  • Utilising Magnetically Isolated Lysosomes for Direct Quantification of Intralysosomal Drug Concentrations by LC-MS/MS Analysis: An Investigatory Study With Imipramine.

    abstract::Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.05.026

    authors: Francis L,Harrell A,Hallifax D,Galetin A

    更新日期:2020-09-01 00:00:00

  • Rapid pKa estimation using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection.

    abstract::A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20275

    authors: Zhou C,Jin Y,Kenseth JR,Stella M,Wehmeyer KR,Heineman WR

    更新日期:2005-03-01 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

  • Solubility in binary solvent systems: 8. Estimation of binary alkane plus p-dioxane solvent nonideality from measured anthracene solubilities.

    abstract::Experimental solubilities are reported for anthracene in binary solvent mixtures containing p-dioxane with n-hexane, cyclohexane, n-heptane, methylcyclohexane, n-octane, cyclooctane, and isooctane at 25 degrees C. Results of these measurements, used in conjunction with the nearly ideal binary solvent (NIBS) model, ena...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760807

    authors: Procyk AD,Bissell M,Street KW Jr,Acree WE Jr

    更新日期:1987-08-01 00:00:00

  • Heterogeneous nucleation-controlled particulate formation of recombinant human platelet-activating factor acetylhydrolase in pharmaceutical formulation.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.20237

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

    更新日期:2005-02-01 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

  • Quantitative (13)C Solid-State NMR Spectra by Multiple-Contact Cross-polarization for Drug Delivery: From Active Principles to Excipients and Drug Carriers.

    abstract::In this contribution, we present an analysis of the main parameters influencing the efficiency of the (1)H → (13)C multiple-contact cross-polarization nuclear magnetic resonance (NMR) experiment in the context of solid pharmaceutical materials. Using the optimum experimental conditions, quantitative (13)C NMR spectra ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.05.025

    authors: Saïdi F,Taulelle F,Martineau C

    更新日期:2016-08-01 00:00:00

  • Application of neural networks to pharmacodynamics.

    abstract::Neural networks (NN) are computational systems implemented in software or hardware that attempt to simulate the neurological processing abilities of biological systems. A synopsis is presented of the operational characteristics, structures, and applications of NN. The NN technology has primarily been aimed at recognit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820910

    authors: Veng-Pedersen P,Modi NB

    更新日期:1993-09-01 00:00:00

  • A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.

    abstract::CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.10.035

    authors: Liu T,Gobburu JVS

    更新日期:2018-03-01 00:00:00

  • Dynamics of disinfection of selected preservatives against Escherichia coli.

    abstract::Mathematical models were determined relating preservative concentration and D values (decimal reduction times at 25 degrees C; pH 6.9-7.1) against Escherichia coli in aqueous medium. Preservatives investigated were 2-bromo-2-nitro-1,3-propanediol (Bronopol), N-(hydroxymethyl)-N-(1,3-dihydroxymethyl-2, 5-dioxo-4-imidaz...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740820

    authors: Hurwitz SJ,McCarthy TJ

    更新日期:1985-08-01 00:00:00

  • Incidence of experimental fascioliasis on hepatic disposition of [3H]tetracycline and [14C]rafoxanide in rats.

    abstract::[7-3H]Tetracycline and [carbonyl-14C]rafoxanide were injected intravenously into anesthetized controls and rats in which experimental fascioliasis had been induced by 20 Fasciola hepatica metacercariae. The biliary excretion (1 and 3 h, respectively) of the radioactivity consisted of approximately 4% of the administer...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740921

    authors: Galtier P,Larrieu G,Franc M

    更新日期:1985-09-01 00:00:00

  • Simple procedure for determining octanol--aqueous partition, distribution, and ionization coefficients by reversed-phase high-pressure liquid chromatography.

    abstract::The described simple, accurate, and precise reversed-phase high-pressure liquid chromatographic procedure is in excellent agreement with 1-octanol shake-flask partition or distribution coefficients over a 3.5 log range. A chemically bonded octadecylsilane support is persilated and coated with 1-octanol. With 1-octanol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671008

    authors: Unger SH,Cook JR,Hollenberg JS

    更新日期:1978-10-01 00:00:00

  • Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus.

    abstract::Effects of the commercial drug zanamivir (Relenza) covalently attached to poly-l-glutamine on the infectivity of influenza A viruses are examined using the plaque reduction assay and binding affinity to viral neuraminidase (NA). These multivalent drug conjugates exhibit (i) up to a 20,000-fold improvement in anti-infl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22338

    authors: Weight AK,Haldar J,Alvarez de Cienfuegos L,Gubareva LV,Tumpey TM,Chen J,Klibanov AM

    更新日期:2011-03-01 00:00:00

  • ¹⁴N nuclear quadrupole resonance study of polymorphism in famotidine.

    abstract::(14)N nuclear quadrupole resonance (NQR) in two known polymorphs of famotidine was measured. At room temperature, seven quadrupolar sets of transition frequencies (ν(+), ν(-), and ν(0)) corresponding to seven different nitrogen sites in the crystal structure of each of the two polymorphs were found. This confirms the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23956

    authors: Luźnik J,Pirnat J,Jazbinšek V,Lavrič Z,Žagar V,Srčič S,Seliger J,Trontelj Z

    更新日期:2014-09-01 00:00:00