Distribution and elimination of poly(methyl methacrylate) nanoparticles after subcutaneous administration to rats.


: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%/day via the feces and approximately 0.0005%/day via the urine) within 70 days. After 200 days, the fecal elimination increased exponentially until a greater than 100-fold increase was observed after 287 days in one rat. After this time, a tendency for an increase in fecal elimination was also observed in the other animals, and the radioactivity in all organs and tissue increased by approximately 100 times in all animals in comparison with the organ radioactivity determinations at earlier times.


J Pharm Sci


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




Has Abstract


1983-10-01 00:00:00














  • Nasal drug administration: potential for targeted central nervous system delivery.

    abstract::Nasal administration as a means of delivering therapeutic agents preferentially to the brain has gained significant recent interest. While some substrates appear to be delivered directly to the brain via this route, the mechanisms governing overall brain uptake and exposure remain unclear. Some substrates utilize the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Graff CL,Pollack GM

    更新日期:2005-06-01 00:00:00

  • Correlation of log P with molecular connectivity in hydroxyureas: influence of conformational system on log P.

    abstract::The correlation of log P (in octanol--water) with the nonempirical, topologically dependent, calculated molecular connectivity index (1chiv) delineates substituted hydroxyureas into two families of linearly related groups of compounds. The first group, composed of the 3-substituted ethyl, n-propyl, and n-butyl analogs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Parker GR

    更新日期:1978-04-01 00:00:00

  • Interactions of acetylcholine mustard with acetylcholinesterase.

    abstract::The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hudgins PM,Stubbins JF

    更新日期:1975-08-01 00:00:00

  • Monitoring the film coating unit operation and predicting drug dissolution using terahertz pulsed imaging.

    abstract::Understanding the coating unit operation is imperative to improve product quality and reduce output risks for coated solid dosage forms. Three batches of sustained-release tablets coated with the same process parameters (pan speed, spray rate, etc.) were subjected to terahertz pulsed imaging (TPI) analysis followed by...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ho L,Müller R,Gordon KC,Kleinebudde P,Pepper M,Rades T,Shen Y,Taday PF,Zeitler JA

    更新日期:2009-12-01 00:00:00

  • The effects of excipients on protein aggregation during agitation: an interfacial shear rheology study.

    abstract::We investigated the effects of excipients in solutions of keratinocyte growth factor 2 (KGF-2) on protein aggregation during agitation as well as on interfacial shear rheology at the air-water interface. Samples were incubated with or without agitation, and in the presence or absence of the excipients heparin, sucrose...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu L,Qi W,Schwartz DK,Randolph TW,Carpenter JF

    更新日期:2013-08-01 00:00:00

  • Drug release from hydrophilic matrices. 2. A mathematical model based on the polymer disentanglement concentration and the diffusion layer.

    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 ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ju RT,Nixon PR,Patel MV,Tong DM

    更新日期:1995-12-01 00:00:00

  • Binding of (+)- and (-)-isomers and racemate of etomoxir to human serum albumin and effect of stearic acid and stanozolol.

    abstract::Binding of (+)- and (-)-isomers and the racemate of sodium 2[6-(4-chlorophenoxy)-hexyl]-oxiran-2-carboxylate dihydrat (etomoxir) to the human serum albumin (HSA) was studied by the gel filtration method. The experimental results are presented graphically using the method of Scatchard. Measurements revealed the followi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vestemar V,Medic-Saric M,Rendic S

    更新日期:1994-04-01 00:00:00

  • Dissolution of theophylline monohydrate and anhydrous theophylline in buffer solutions.

    abstract::The dissolution kinetics of theophylline monohydrate and anhydrous theophylline were investigated with a rotating-disk apparatus in buffer solutions at 298 K under sink conditions. The observed dissolution rate of theophylline monohydrate under various conditions agreed well with predictions based on the Extended Simu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: de Smidt JH,Fokkens JG,Grijseels H,Crommelin DJ

    更新日期:1986-05-01 00:00:00

  • The Selection of a Pharmaceutical Salt-The Effect of the Acidity of the Counterion on Its Solubility and Potential Biopharmaceutical Performance.

    abstract::A roadmap for the selection of a pharmaceutical salt form for a development candidate is presented. The free base of the candidate did not have sufficient chemical stability for development. The initially selected salt form turned out to be undevelopable because it was unstable during scale-up synthesis and storage. T...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: He Y,Orton E,Yang D

    更新日期:2018-01-01 00:00:00

  • Slow motion picture of protein inactivation during single-droplet drying: a study of inactivation kinetics of L-glutamate dehydrogenase dried in an acoustic levitator.

    abstract::A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lorenzen E,Lee G

    更新日期:2012-06-01 00:00:00

  • Conformational color polymorphism and control of crystallization of 5-methyl-2-[(4-methyl-2-nitrophenyl)amino]-3-thiophenecarbonitrile.

    abstract::5-Methyl-2-[(4-methyl-2-nitrophenyl)amino]-3-thiophenecarbonitrile is an example of conformational and color polymorphism. The compound crystallizes in red (R), dark red (DR), light red (LR), and orange (O) modifications. There are two specific goals for this study. One is to characterize the complex thermodynamic rel...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: He X,Griesser UJ,Stowell JG,Borchardt TB,Byrn SR

    更新日期:2001-03-01 00:00:00

  • Hydrolysis and protein binding of melphalan.

    abstract::Melphalan (30 microgram/ml) is completely hydrolyzed in water at 37 degrees after 8 hr. At lower temperatures, hydrolysis proceeds at slower rates. The presence of bovine serum albumin retards hydrolysis of melphalan (30 microgram/ml) in water. The melphalan hydrolysis rate is directely releated to the bovine serum al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chang SY,Alberts DS,Farquhar D,Melnick LR,Walson PD,Salmon SE

    更新日期:1978-05-01 00:00:00

  • The biologic effects of growth factor-toxin conjugates in models of vascular injury depend on dose, mode of delivery, and animal species.

    abstract::Toxin-conjugates, complexes designed from the fusion of tissue toxins and pathology-specific ligands, offer the potential for targeted cytotoxic therapy. Some have postulated that the recurrent failure of these conjugates to exhibit benefit in animal models of vascular injury arose because the timing and frequency of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yu C,Cunningham M,Rogers C,Dinbergs ID,Edelman ER

    更新日期:1998-11-01 00:00:00

  • Enantiotropically-related polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid: crystal structures and multinuclear solid-state NMR.

    abstract::Single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), and solid-state NMR (SSNMR) techniques are used to analyze the structures of two nonsolvated polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid. These polymorphs are enantiotropically-related with a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vogt FG,Katrincic LM,Long ST,Mueller RL,Carlton RA,Sun YT,Johnson MN,Copley RC,Light ME

    更新日期:2008-11-01 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


    authors: Jenkins RG,Friedel RO

    更新日期:1978-01-01 00:00:00

  • Effect of Water on the Chemical Stability of Amorphous Pharmaceuticals: 2. Deamidation of Peptides and Proteins.

    abstract::Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ohtake S,Feng S,Shalaev E

    更新日期:2018-01-01 00:00:00

  • Agglomerative crystallization of ABT-510 in a partially miscible solvent system.

    abstract::A modification of wet agglomeration technique is developed and demonstrated by agglomerative crystallization process for a nonapeptide (ABT-510) to improve processing of needle like crystals. Our procedure involves exploiting partial miscibility of the crystallization solvent system for in situ generation of a wetting...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sheikh AY,Pal A,Viswanath S,Tolle JC

    更新日期:2008-03-01 00:00:00

  • Freeze-Drying Above the Glass Transition Temperature in Amorphous Protein Formulations While Maintaining Product Quality and Improving Process Efficiency.

    abstract::This study explored the ability to conduct primary drying during lyophilization at product temperatures above the glass transition temperature of the maximally freeze-concentrated solution (Tg′) in amorphous formulations for four proteins from three different classes. Drying above Tg′ resulted in significant reduction...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Depaz RA,Pansare S,Patel SM

    更新日期:2016-01-01 00:00:00

  • Pharmacokinetic study of methotrexate following intra-articular injection of methotrexate loaded poly(L-lactic acid) microspheres in rabbits.

    abstract::The pharmacokinetics and tissue distribution of methotrexate (MTX) were investigated following intra-articular injection of either MTX solution or controlled release MTX loaded microspheres in healthy rabbit joints. MTX solution or MTX loaded microspheres (size 30-100 mum) (10 mg MTX) was injected into the right knee ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liang LS,Wong W,Burt HM

    更新日期:2005-06-01 00:00:00

  • Regulation of Tight-Junction Integrity by Insulin in an In Vitro Model of Human Blood-Brain Barrier.

    abstract::Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

    更新日期:2017-09-01 00:00:00

  • Tensile strengths and hardness of tablets.

    abstract::The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jarosz PJ,Parrott EL

    更新日期:1982-06-01 00:00:00

  • GLC determination of (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine in human plasma and urine.

    abstract::(-)-1-Cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine (MK-160) was extracted from human plasma and urine with petroleum ether and quantitated by GLC using a nitrogen-sensitive detector. A homologue of the drug served as the internal standard. The method is specific for the d...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hucker HB,Hutt JE

    更新日期:1983-07-01 00:00:00

  • Variations in compaction behaviour for tablets of different size and shape, revealed by small-angle X-ray scattering.

    abstract::Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Laity PR,Han L,Elliott J,Cameron RE

    更新日期:2010-10-01 00:00:00

  • Stability of Ceftazidime Pentahydrate Investigated by Thermal Analysis Techniques.

    abstract::Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Alves de Santana MS,Santiago de Oliveira Y,de Castro Fonseca J,Ferreira WC,Neto VS,Ayala AP

    更新日期:2020-03-01 00:00:00

  • Fluoride remineralization of demineralized bovine tooth enamel and hydroxyapatite pellets.

    abstract::Both bovine enamel and hydroxyapatite pellets were remineralized in a fluoride-containing remineralization solution after prior demineralization for various lengths of time. In both the enamel and pellet systems, the degree of remineralization attainable was directly related to the extent of prior demineralization, al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yonese M,Fox JL,Nambu N,Hefferren JJ,Higuchi WI

    更新日期:1981-08-01 00:00:00

  • Effect of temperature and relative humidity on nitrazepam stability in solid state.

    abstract::The decomposition of a 1% dilution of nitrazepam in microcrystalline cellulose was established by quantitative determination of the two main breakdown products, 2-amino-5-nitrobenzophenone and 3-amino-6-nitro-4-phenyl-2(1H)-quinolone, using in situ diffuse reflectance measurements on thin-layer chromatograms. The deco...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Genton D,Kesselring UW

    更新日期:1977-05-01 00:00:00

  • Independence of antimineralocorticoid and catatoxic effects of various steroids.

    abstract::A series of unrelated steroids were tested for antimineralocorticoid activity by Kagawa's test in male rats and by modified test in female rats. Adrenalectomized male rats given 12 mcg desoxycorticosterone (DOC) and 2.5 ml normal saline received 1 mg of the test steroid, and their urine was analyzed for sodium and po...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Solymoss B,Krajny M,Varga S

    更新日期:1970-05-01 00:00:00

  • Predicting With Confidence: Using Conformal Prediction in Drug Discovery.

    abstract::One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

    更新日期:2021-01-01 00:00:00

  • Synthesis, cytotoxicity, and phase-solubility study of cyclodextrin click clusters.

    abstract::To explore the possibility of cyclodextrin click clusters (CCCs) as a new cyclodextrin-based excipient, we prepared three different CCCs; heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}-β-cyclodextrin (HT-β-CD), heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}{2,3-di-O-methyl}-β-cyclodextrin (...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Le HT,Jeon HM,Lim CW,Kim TW

    更新日期:2014-10-01 00:00:00

  • Cerebral kinetics of oxycodone in conscious sheep.

    abstract::Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

    更新日期:2006-08-01 00:00:00