Abstract:
:A GLC assay to quantitate the methaqualone metabolite 2-methyl-3-(2-hydroxymethylphenyl)-4(3H)-quinazolinone was developed. Standard curves were linear, and recovery of the metabolite from tissue homogenates averaged 89%. In vitro metabolism of methaqualone by the 10,000Xg supernatant fraction of rat liver homogenate was measured by monitoring metabolite formation with the GLC assay. Diphenhydramine inhibited the in vitro metabolism of methaqualone. The percentage inhibition increased with increasing diphenhydramine concentration. The significance of this inhibition in relation to use and abuse of methaqualone--diphenhydramine combinations is discussed.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Hindmarsh KW,Hamon NW,LeGatt DF,Wallace SMdoi
10.1002/jps.2600671114subject
Has Abstractpub_date
1978-11-01 00:00:00pages
1547-50issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(15)42314-7journal_volume
67pub_type
杂志文章abstract::Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600661223
更新日期:1977-12-01 00:00:00
abstract::Site I of human serum albumin is an important and complex region for high-affinity binding of drugs. Equilibrium dialysis showed independent binding of dansyl-L-asparagine (DNSA) and n-alkyl p-aminobenzoates (p-ABEs) to regions Ib and Ic, respectively, in the pH range 6.0-9.0. However, individual binding of DNSA incre...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.20203
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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
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doi:10.1021/js970137w
更新日期:1997-09-01 00:00:00
abstract::Dissolution profiles are classified in accordance with the shape of fractional dissolution rate function. This function is constant in time for the classical first-order model and, in this case, the dissolution is described by a monoexponential function. Therefore, any deviation of the fractional dissolution rate from...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.10419
更新日期:2003-08-01 00:00:00
abstract::Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.07.008
更新日期:2018-11-01 00:00:00
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
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doi:10.1002/jps.2600771014
更新日期:1988-10-01 00:00:00
abstract::The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...
journal_title:Journal of pharmaceutical sciences
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更新日期:2007-02-01 00:00:00
abstract::Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.10.008
更新日期:2017-02-01 00:00:00
abstract::Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...
journal_title:Journal of pharmaceutical sciences
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doi:10.1016/j.xphs.2015.10.001
更新日期:2016-03-01 00:00:00
abstract::A rapid, automated method for the determination of phenylbutazone in plasma and urine was developed. The method offers distinct advantages over earlier procedures and is particularly suitable for large-scale bioavailability studies. ...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600650117
更新日期:1976-01-01 00:00:00
abstract::Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.22695
更新日期:2011-11-01 00:00:00
abstract::A physically based method for arriving at topological indexes is described. The derived indexes correlate with molecular surface areas and with the molecular connectivity index. The newly derived index seems to account better for the expected distinctions among primary, secondary, and tertiary alcohol aqueous solubili...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680713
更新日期:1979-07-01 00:00:00
abstract::The pharmacokinetics of aniracetam (AP), a new cognitive performance enhancer, and its main metabolites was investigated after intravenous (iv) and oral administrations to rat. The plasma levels of AP, 4-p-anisamidobutyric acid (ABA), and p-anisic acid (AA) were determined simultaneously by the HPLC method. The plasma...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js970355p
更新日期:1998-05-01 00:00:00
abstract::The chromatographic retention behavior of dextromethorphan hydrobromide on an octadecylsilane column was investigated as a function of the pairing ion and the mobile phase composition. Dramatic increases in the capacity factor were observed with pairing ions containing more than eight carbons and with decreasing organ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600691207
更新日期:1980-12-01 00:00:00
abstract::The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.05.019
更新日期:2016-08-01 00:00:00
abstract::This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.01.027
更新日期:2017-05-01 00:00:00
abstract::In this study, we developed cationic microemulsions containing a protein transduction domain (penetratin) for optimizing paclitaxel localization within the skin. Microemulsions were prepared by mixing a surfactant blend (BRIJ:ethanol:propylene glycol 2:1:1, w/w/w) with monocaprylin (oil phase) at 1.3:1 ratio, and addi...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.23482
更新日期:2013-05-01 00:00:00
abstract::The purpose of the present study was to clarify the expression levels of transporter proteins in human lung tissue and to analyze regional and interindividual differences in primary cultured epithelial cells. Organic cation/carnitine tranporter 1 (OCTN1) protein expression was highest (2.08 ± 1.19 fmol/μg protein) in ...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.23606
更新日期:2013-09-01 00:00:00
abstract::Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,多中心研究,随机对照试验
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abstract::The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...
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abstract::A high-pressure liquid chromatographic procedure for quantitative dexamethasone and dexamethasone sodium phosphate determinations in all types of commercially available pharmaceutical dosage forms was developed. The method also separates dexamethasone from its phosphate salt and separates dexamethasone or its salt fro...
journal_title:Journal of pharmaceutical sciences
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abstract::The use of enzymes as therapeutics is very promising because of their catalytic activity and specificity. However, intracellular delivery of active enzymes is challenging due to their low stability and large size. The production of protein-enzyme nanoparticles was investigated with the goal of developing a protein car...
journal_title:Journal of pharmaceutical sciences
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abstract::This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...
journal_title:Journal of pharmaceutical sciences
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更新日期:2014-08-01 00:00:00
abstract::Adsorption isotherms for the diazepam-activated carbon system in simulated intestinal fluid (SIF), without pancreatin, and in SIF with different percentages of ethanol were determined as were the solubilities of diazepam in SIF and in SIF with different percentages of ethanol. The surface area of the activated carbon ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10454
更新日期:2003-10-01 00:00:00
abstract::Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
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更新日期:2012-02-01 00:00:00
abstract::Taraxacum mongolicum (TM), also known as dandelion, is a herb widely used in the East for its antibacterial activity. The high mineral content of TM presents a potential problem for the absorption of quinolone antibiotics. This study was undertaken to discern the significance of a drug-drug interaction between TM and ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980367q
更新日期:1999-06-01 00:00:00
abstract::The viscosity of xanthan gum solutions in the low shear region was investigated with the aid of a Couette instrument. All solutions were highly pseudoplastic . Solutions containing 0.3-0.5% of the gum exhibited a highly ordered phase at very low shear. Viscosity, the degree of pseudoplasticity , and the value of the t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600730410
更新日期:1984-04-01 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
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更新日期:1980-01-01 00:00:00
abstract::Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
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更新日期:1995-02-01 00:00:00
abstract::Biopharmaceutics Classification System and Biopharmaceutics Drug Distribution Classification System are complimentary, not competing, classification systems that aim to improve, simplify, and speed drug development. Although both systems are based on classifying drugs and new molecular entities into four categories us...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.23359
更新日期:2013-01-01 00:00:00