Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting-Point Microcrystalline Wax.

Abstract:

:It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled manner at 25°C. However, the mechanism of the drug release is still unclear. The objective of this study was to determine the mechanism of drug release from the WM particles using X-ray computed tomography. In the WM particles collected during dissolution tests at 25°C, the void space derived from drug release increased with increasing time, and there was no change in the structure, indicating that the WM particles released drug while maintaining the particle shape at 25°C. In the WM particles collected during dissolution tests at 37°C, the void space was confirmed at initial time point; however, at subsequent time points, the void space was disappeared, and the roughness of the surface was evident. This structural change may have blocked the conveyance pathway of the outer medium, which would inhibit the drug release. The difference between the drug-release mechanisms of the WM particles at the 2 temperatures will be valuable for developing cooling-triggered, temperature-sensitive formulations.

journal_name

J Pharm Sci

authors

Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

doi

10.1016/j.xphs.2019.01.010

subject

Has Abstract

pub_date

2019-06-01 00:00:00

pages

2086-2093

issue

6

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(19)30018-8

journal_volume

108

pub_type

杂志文章
  • 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

  • Novel Insights to Enhance Therapeutics With Acyclovir in the Management of Herpes Simplex Encephalitis.

    abstract::Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2021.01.003

    authors: Gurgel Assis MS,Fernandes Pedrosa TC,de Moraes FS,Caldeira TG,Pereira GR,de Souza J,Ruela ALM

    更新日期:2021-01-13 00:00:00

  • Forced degradation studies of corticosteroids with an alumina-steroid-ethanol model for predicting chemical stability and degradation products of pressurized metered-dose inhaler formulations.

    abstract::An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23111

    authors: Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

    更新日期:2012-06-01 00:00:00

  • Dose-dependent plasma clearance of MK-826, a carbapenem antibiotic, arising from concentration-dependent plasma protein binding in rats and monkeys.

    abstract::After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980232k

    authors: Wong BK,Bruhin PJ,Lin JH

    更新日期:1999-02-01 00:00:00

  • Use of fractal geometry to determine effects of surface morphology on drug dissolution.

    abstract::We extend and modify the Noyes-Whitney equation and the Hixon-Crowell cube root law to include surface roughness effects on the dissolution rate of drugs. The problem is treated theoretically in terms of the fractal reaction dimension, DR, of the effective surface which undergoes dissolution. Effects of changes in DR ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810111

    authors: Farin D,Avnir D

    更新日期:1992-01-01 00:00:00

  • Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery.

    abstract::The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1162

    authors: Kawakami S,Nishida K,Mukai T,Yamamura K,Kobayashi K,Sakaeda T,Nakamura J,Nakashima M,Sasaki H

    更新日期:2001-12-01 00:00:00

  • A physiologically based pharmacokinetic model of zidovudine (AZT) in the mouse: model development and scale-up to humans.

    abstract::After having been used in treating HIV infection for a decade, zidovudine (AZT) continues to be an essential component of antiretroviral regimens. Because antiviral responses and toxicity of AZT seem to be related to cells in specific target tissues, being able to understand and predict the distribution of AZT into di...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970243y

    authors: Chow HH

    更新日期:1997-11-01 00:00:00

  • Stereoselective pharmacokinetics and inversion of suprofen enantiomers in humans.

    abstract::The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600801116

    authors: Shinohara Y,Magara H,Baba S

    更新日期:1991-11-01 00:00:00

  • Understanding the Increased Aggregation Propensity of a Light-Exposed IgG1 Monoclonal Antibody Using Hydrogen Exchange Mass Spectrometry, Biophysical Characterization, and Structural Analysis.

    abstract::This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.01.017

    authors: Bommana R,Chai Q,Schöneich C,Weiss WF 4th,Majumdar R

    更新日期:2018-06-01 00:00:00

  • Crystal morphologies and polymorphs in tolbutamide microcrystalline powder.

    abstract::The growing interest of pharmaceutical companies toward the crystal morphology prediction of active pharmaceutical ingredients is a consequence of the dramatic effect of the crystal habit on the tableting behavior of drugs. In order to help the optimization of the industrial process, molecular mechanics calculations t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23334

    authors: Li Destri G,Marrazzo A,Rescifina A,Punzo F

    更新日期:2013-01-01 00:00:00

  • Bioavailability and efficacy of antisense morpholino oligomers targeted to c-myc and cytochrome P-450 3A2 following oral administration in rats.

    abstract::Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10088

    authors: Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

    更新日期:2002-04-01 00:00:00

  • Effect of benzalkonium chloride/EDTA on the ocular bioavailability of ketorolac tromethamine following ocular instillation to normal and de-epithelialized corneas of rabbits.

    abstract::This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9504189

    authors: Madhu C,Rix PJ,Shackleton MJ,Nguyen TG,Tang-Liu DD

    更新日期:1996-04-01 00:00:00

  • Stereoselective disposition of the geometric isomers of a novel lipoxygenase cyclo-oxygenase inhibitor in dog and photochemical interconversion of its isomers.

    abstract::A sensitive (10 ng/mL) and specific high-performance liquid chromatographic (HPLC) assay, with electrochemical (EC) detection, for the geometric isomers of 3-hydroxy-N-(2-phenyl-2-(2-thienyl)ethenyl-5-(trifluoromethyl)benzo(b) thiophene-2-carboxamide in dog and human plasma has been developed. Both isomers strongly ab...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600771014

    authors: Matuszewski BK,Kanovsky SM,Constanzer ML,Yeh KC,Bayne WF

    更新日期:1988-10-01 00:00:00

  • Effect of thermodynamic activities of the unionized and ionized species on drug flux across buccal mucosa.

    abstract::The objective of this work was to delineate the contribution of thermodynamic activities of ionized and unionized species on buccal drug permeation. The flux and permeability of a model acidic (nimesulide) and basic (bupivacaine) drug were determined across porcine buccal mucosa at different pH conditions. Thermodynam...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21301

    authors: Kokate A,Li X,Singh P,Jasti BR

    更新日期:2008-10-01 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

    doi:10.1002/jps.2600820211

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

    更新日期:1993-02-01 00:00:00

  • Shear-induced degradation of plasmid DNA.

    abstract::The majority of gene therapy clinical trials use plasmid DNA that is susceptible to shear-induced degradation. Many processing steps in the extraction, purification, and preparation of plasmid-based therapeutics can impart significant shear stress that can fracture the phosphodiester backbone of polynucleotides, and r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.10140

    authors: Lengsfeld CS,Anchordoquy TJ

    更新日期:2002-07-01 00:00:00

  • In vitro photodecomposition of uric acid in presence of riboflavin II.

    abstract::In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600661115

    authors: Newburger J,Combs AB,Hsu TF

    更新日期:1977-11-01 00:00:00

  • Polyanhydride microsphere formulation by solvent extraction.

    abstract::A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770811

    authors: Bindschaedler C,Leong K,Mathiowitz E,Langer R

    更新日期:1988-08-01 00:00:00

  • Analysis of tricyclic antidepressants in human plasma by GLC--chemical-ionization mass spectrometry with selected ion monitoring.

    abstract::A method is described for the analysis of amitriptyline, doxepin, imipramine, nortriptyline, desmethyldoxepin, desipramine, and protriptyline in human plasma utlizing GLC-chemical-ionization mass spectrometry with selected ion monitoring. The assay is highly specific and is quantitative to at least 1 ng/ml with a stan...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670106

    authors: Jenkins RG,Friedel RO

    更新日期:1978-01-01 00:00:00

  • Overall monotropic behavior of a metastable phase of biclotymol, 2,2'-methylenebis(4-chloro-3-methyl-isopropylphenol), inferred from experimental and topological construction of the related P-T state diagram.

    abstract::The melt from the usual monoclinic phase (Phase I) of biclotymol (T(fusI) = 400.5 +/- 1.0 K, Delta(fus)H(I) = 36.6 +/- 0.9 kJ mol(-1)) recrystallizes into another phase, Phase II, that melts at T(fusII) = 373.8 +/- 0.2 K (Delta(fus)H(II) = 28.8 +/- 1.0 kJ mol(-1)). The transformation of Phase II into Phase I is found ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21285

    authors: Céolin R,Tamarit JL,Barrio M,López DO,Nicolaï B,Veglio N,Perrin MA,Espeau P

    更新日期:2008-09-01 00:00:00

  • An Extrusion Spheronization Approach to Enable a High Drug Load Formulation of a Poorly Soluble Drug with a Low Melting Surfactant.

    abstract::Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24585

    authors: Tatavarti A,Kesisoglou F

    更新日期:2015-11-01 00:00:00

  • Agglomeration of mesoporous silica by melt and steam granulation. part II: screening of steam granulation process variables using a factorial design.

    abstract::The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was selected as the model com...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23699

    authors: Vialpando M,Albertini B,Passerini N,Vander Heyden Y,Rombaut P,Martens JA,Van Den Mooter G

    更新日期:2013-11-01 00:00:00

  • Experimental evaluation of three single-particle dissolution models.

    abstract::The dissolution of the 60-85-mesh fraction os recording, flow-through dissolution apparatus equipped with a dissolution cell; it was particularly suitable for kinetic analysis of multiparticulate systems. By using a time-scaling approach, experimental data are compared with theoretical calculations to evaluate, quanti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600651007

    authors: Pedersen PV,Brown KF

    更新日期:1976-10-01 00:00:00

  • Development of oral liquid dosage forms of acetazolamide.

    abstract::Two oral liquid dosage forms of acetazolamide have been developed. Using the solubility profiles, polyethylene glycol 400 (7%, v/v) was used as the solubilizing agent and propylene glycol (53%, v/v) as the cosolvent to keep acetazolamide in solution. Because of the bitter taste of acetazolamide, sweetening agents (sim...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790919

    authors: Parasrampuria J,Das Gupta V

    更新日期:1990-09-01 00:00:00

  • An investigation into the melting behavior of binary mixes and solid dispersions of paracetamol and PEG 4000.

    abstract::The melting behavior of paracetamol and polyethylene glycol (PEG) 4000, both individually and as binary systems, has been studied using differential scanning calorimetry. The appearance of the PEG peaks was shown to be highly dependent on scanning rate, with evidence for the existence of once-folded and extended chain...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970137w

    authors: Lloyd GR,Craig DQ,Smith A

    更新日期:1997-09-01 00:00:00

  • Drug delivery trends in clinical trials and translational medicine: evaluation of pharmacokinetic properties in special populations.

    abstract::In spite of the recent advances in technology to optimize the absorption, distribution, metabolism and elimination (ADME) properties of new and promising medicinal products to reduce clinical failures, the investigation of drug disposition in the pediatric and elderly populations continues to be under evaluated. With ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.22253

    authors: Chien JY,Ho RJ

    更新日期:2011-01-01 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

  • Perforated coated tablets for controlled release of drugs at a constant rate.

    abstract::Tablets with a central hole and a water-impermeable coating were prepared. These perforated coated tablets (PCTs) dissolve and release drug through the central hole only. In vitro release of the model drugs sodium benzoate and benzamide from PCTs occurred at a constant rate up to 80% release. The zero-order release ra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770408

    authors: Hansson AG,Giardino A,Cardinal JR,Curatolo W

    更新日期:1988-04-01 00:00:00

  • Pharmacology of malnutrition III: binding of digoxin to normal and kwashiorkor serum.

    abstract::Digoxin binding to normal and kwashiorkor serum was studied and found to be inferior in the latter. Digoxin should be used with care in hypoalbuminemic patients. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650629

    authors: Buchanan N,Van der Walt LA,Strickwold B

    更新日期:1976-06-01 00:00:00

  • Simultaneous GLC determination of methyl salicylate and menthol in a topical analgesic formulation.

    abstract::A simultaneous GLC determination for methyl salicylate and menthol in a topical analgesic formulation is reported. n-Nonadecane is used as the internal standard. The method is rapid, accurate, precise, and selective in the presence of salicylic acid and ethyl salicylate. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680431

    authors: Sapio JP,Sethachutkul K,Moody JE

    更新日期:1979-04-01 00:00:00