Abstract：
:A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer chains detach off the gelled matrix. For (hydroxypropyl)methylcellulose (HPMC) in water, we estimate that rho p,dis scales with HPMC molecular weight, M, as rho p,dis varies M-0.8. Further, matrix dissolution is considered similar to the dissolution of an object immersed in a fluid. As a result, a diffusion layer separating the matrix from the bulk solution is incorporated into the transport regime. An anisotropic expansion model is also introduced to account for the anisotropic expansion of the matrix where surface area in the radial direction dominates over the axial surface area. The model predicts that the overall tablet size and the characteristic swelling time correlate with rho p,dis qualitatively. Two scaling laws are established for fractional polymer (mp(t)/mp(infinity)) and drug (md(t)/md(infinity)) released as mp(t)/mp(infinity) varies M-1.05 and md(t)/md(infinity) varies M-0.24, consistent with the limiting polymer molecular weight effect on drug release. Model predictions for polymer and drug release agree well with observations, within 15% error. Evolution of water concentration profiles and the detailed structure of a swollen matrix are discussed.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Ju RT,Nixon PR,Patel MV,Tong DMdoi
10.1002/jps.2600841214subject
Has Abstractpub_date
1995-12-01 00:00:00pages
1464-77issue
12eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49958-7journal_volume
84pub_type
杂志文章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
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更新日期：2019-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2007-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js950497o
更新日期：1996-10-01 00:00:00
abstract：:A pharmacokinetic model was developed describing the pharmacokinetics of stannous fluoride in human subjects after oral topical application of a stannous fluoride dentifrice. Twenty subjects participated in an investigation of an experimental dentifrice. Subjects rinsed their mouths with the experimental dentifrice sl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21691
更新日期：2009-10-01 00:00:00
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更新日期：2004-10-01 00:00:00
abstract：:The influences of 1-ethyl-, 1-butyl-, 1-hexyl-, and 1-octyl-2-pyrrolidone in their saline solutions on the transport of beta-estradiol, corticosterone, and hydrocortisone across hairless mouse skin under in vitro conditions have been investigated by the physical model approach. The experimental data were interpreted w...
journal_title：Journal of pharmaceutical sciences
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更新日期：1995-03-01 00:00:00
abstract：:Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21271
更新日期：2008-09-01 00:00:00
abstract：:A method has been developed for the estimation of the distribution coefficient (D), which considers the microspecies of a compound. D is calculated from the microscopic dissociation constants (microconstants), the partition coefficients of the microspecies, and the counterion concentration. A general equation for the ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js960177k
更新日期：1997-07-01 00:00:00
abstract：:A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...
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pub_type： 杂志文章
doi：10.1021/js980393o
更新日期：1999-07-01 00:00:00
abstract：:Fibril formation (aggregation) of human and bovine insulin and six human insulin mutants in hydrochloric acid were investigated by visual inspection, Thioflavin T fluorescence spectroscopy, transmission electron microscopy (TEM), and Fourier transform infrared (FTIR) spectroscopy. The fibrillation tendencies of the wi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10238
更新日期：2002-12-01 00:00:00
abstract：:During stability studies at high temperature (70 degrees C) and low relative humidity ( approximately 0%), the recovery of an asparagine containing hexapeptide (VYPNGA) and its known deamidation products from solid polyvinylpyrrolidone (PVP) matrices was incomplete. To determine the causes of this mass loss, formulati...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10316
更新日期：2003-03-01 00:00:00
abstract：:The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20667
更新日期：2006-08-01 00:00:00
abstract：:Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690205
更新日期：1980-02-01 00:00:00
abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600780308
更新日期：1989-03-01 00:00:00
abstract：:Magnetic resonance imaging (MRI) with chemical shift resolution is a recent extension of MRI and it provides information about species resolved molecular transport on the macroscopic scale in complex systems. In this contribution, we show that by using this novel method, one can predict the behavior of drug and food m...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20749
更新日期：2007-02-01 00:00:00
abstract：:Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9504245
更新日期：1996-07-01 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
pub_type： 杂志文章
doi：10.1002/jps.2600761216
更新日期：1987-12-01 00:00:00
abstract：:This work was to investigate the effects of particle size and paddle speed on the particle diffusional layer thickness h(app) in a USP dissolution apparatus II. After the determination of the powder dissolution rates of five size fractions of fenofibrate, including <20, 20-32, 32-45, 63-75, and 90-106 microm, the pres...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21345
更新日期：2008-11-01 00:00:00
abstract：:Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2017.04.035
更新日期：2017-09-01 00:00:00
abstract：:A stability-indicating analytical method is described for the simultaneous determination of nitrate, and if present, its reductive degradation product, nitrite, in toothpastes. Nitrate and nitrite were extracted from the toothpaste using distilled water and separated from other water-soluble excipients by two RP-8 col...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730740
更新日期：1984-07-01 00:00:00
abstract：:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/wat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js970218s
更新日期：1998-03-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690534
更新日期：1980-05-01 00:00:00
abstract：:A novel method for creating water soluble prodrugs of cisplatin analogues bearing chelating diamines is introduced. When 2-(amino-methyl)aniline is reacted with K2PtCl4 between a pH of 6 and 7, the neutral chelated complex [2-(aminomethyl)aniline)dichloroplatinum(II) (1) is isolated. On the other hand, when the comple...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840707
更新日期：1995-07-01 00:00:00
abstract：:Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js960276y
更新日期：1996-11-01 00:00:00
abstract：:The S6-(N-alkyl-N-alkoxycarbonyl)aminomethyl-6-MP (6-CARB-6-MP) prodrugs 5-20 were synthesized from the reaction of 6-MP with N-alkyl-N-alkyoxycarbonylaminomethyl chlorides (4) in dimethyl sulfoxide in overall yields of 5-62%, depending on the N-alkyl and the alkoxy groups involved. The derivatives were fully characte...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790116
更新日期：1990-01-01 00:00:00
abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24648
更新日期：2016-02-01 00:00:00
abstract：:The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690113
更新日期：1980-01-01 00:00:00
abstract：:Surfactants stabilize proteins through two major mechanisms: (1) their preferential location at nearby interfaces, in this way precluding protein adsorption; and/or (2) their association with protein into "complexes" that prevent proteins from interacting with surfaces as well as each other. However, selection of surf...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23908
更新日期：2014-05-01 00:00:00
abstract：:A new mucoadhesive tablet, which releases natural active agents for pain reduction and rapid healing of canker sores, has been prepared and characterized. Adhesive tablets were prepared by compression molding of mixed powders of crosslinked polyacrylic acid and hydroxypropyl cellulose, absorbed with citrus oil and mag...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.20193
更新日期：2004-12-01 00:00:00
