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 solubilities. This study suggests that the Del Re method for calculating molecular charges and dipole moments also may be used, without appreciable change, to provide estimates of molecular refraction.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Cammarata Adoi
10.1002/jps.2600680713subject
Has Abstractpub_date
1979-07-01 00:00:00pages
839-42issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)42717-0journal_volume
68pub_type
杂志文章abstract::Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.11.033
更新日期:2016-09-01 00:00:00
abstract::Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C....
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670443
更新日期:1978-04-01 00:00:00
abstract::99mTc-N-(3-bromo-2,4,6-trimethylacetanilide)iminodiacetat e (I) and 99mTc-N-pyridoxyl-5-methyl-tryptophan (II) have been described as having optimal properties as hepatobiliary radiopharmaceuticals. This study compared specificity for hepatobiliary excretion, blood disappearance, rates of biliary appearance, and pharm...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731259
更新日期:1984-12-01 00:00:00
abstract::Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600790704
更新日期:1990-07-01 00:00:00
abstract::Chagas disease due to chronic infection with Trypanosoma cruzi is a neglected cause of heart disease, affecting approximately 6-10 million individuals in Latin America and elsewhere. T. cruzi Tc24, a calcium-binding protein in the flagellar pocket of the parasite, is a candidate antigen for an injectable therapeutic v...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.12.014
更新日期:2018-05-01 00:00:00
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
doi:10.1016/j.xphs.2019.11.018
更新日期:2020-03-01 00:00:00
abstract::Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.06.028
更新日期:2017-01-01 00:00:00
abstract::The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23994
更新日期:2014-07-01 00:00:00
abstract::The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690723
更新日期:1980-07-01 00:00:00
abstract::The effects of five conventional film-coating materials on tablet hardness were studied. Placebos showed apparently linear increases in hardness as coatings were applied. Completely coated samples exhibited hardness increases from 50 to 140%, with a corresponding 3% increase in tablet weight. Equations were derived re...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650908
更新日期:1976-09-01 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::Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.03.003
更新日期:2017-09-01 00:00:00
abstract::The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21372
更新日期:2008-12-01 00:00:00
abstract::The overall apparent first-order rate constants (Kab) of small intestinal absorption of sulfadiazine were determined in rats in situ at various pHs (4.01-7.42) of the recirculation fluids at 32 degrees. The purpose of the study was to verify our hypothesis that the rate-determining step for the absorption of sulfonami...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830208
更新日期:1994-02-01 00:00:00
abstract::Chlorpromazine-induced depression of rectal temperatures in rabbits kept at 20 degrees was used to determine relative biophasic drug levels corresponding to observed hypothermic response intensities, which then served to establish a triexponential linear mathematical model describing drug transference and drug action ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600651110
更新日期:1976-11-01 00:00:00
abstract::The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.10489
更新日期:2004-01-01 00:00:00
abstract::The mechanism of how poly(vinyl alcohol-co-acrylic acid-co-methyl methacrylate) (PVA copolymer) stabilizes an amorphous drug was investigated. Solid dispersions of PVA copolymer, poly(vinyl pyrrolidone) (PVP), and poly(vinyl pyrrolidone-co-vinyl acetate) (PVPVA) with indomethacin (IMC) were prepared. The glass transit...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24023
更新日期:2014-09-01 00:00:00
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
更新日期:1985-08-01 00:00:00
abstract::When heated at temperatures in excess of 100 degrees, the stability of neomycin in aqueous ophthalmic formulations was improved by the addition of edetate disodium (0.01%). As the exposure temperature was reduced, the degree of stability enhancement diminished until the effect was reversed, and addition of edetate dis...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700836
更新日期:1981-08-01 00:00:00
abstract::First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840504
更新日期:1995-05-01 00:00:00
abstract::Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1016/j.xphs.2018.03.009
更新日期:2018-07-01 00:00:00
abstract::The metabolic fate of aprophen hydrochloride (2-diethylaminoethyl 2,2-diphenylpropionate) was studied in rats after intravenous administration. Both 14C-labeled and unlabeled aprophen were used in these studies. Blood samples were collected and analyzed to determine the identities of the metabolites formed. Utilizing ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600770210
更新日期:1988-02-01 00:00:00
abstract::The aim of this study was to prepare and characterize thiolated chitosan (TC) nanoparticles (NPs) of tizanidine HCl (TZ) and to evaluate its transport across monolayer of RPMI 2650 cells (Human nasal septum carcinoma cell line) followed by assessment of their pharmacokinetic and pharmacodynamic attributes, after intra...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22780
更新日期:2012-02-01 00:00:00
abstract::The University of British Columbia (UBC) became the first university in Canada to develop a strategy for enhancing global access to its technologies. UBC's University-Industry Liaison Office, in collaboration with the UBC chapter of Universities Allied for Essential Medicines (UAEM), established a mandate and develope...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21495
更新日期:2009-03-01 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
abstract::Methods for the determination of diphenoxylate hydrochloride and atropine sulfate combinations in solutions and powdered tablet composites are presented. A semiautomated assay for diphenoxylate hydrochloride in individual tablets (content uniformity) also is presented. The USP XIX assays for these products are cumbers...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600661113
更新日期:1977-11-01 00:00:00
abstract::Scale up of pan coating process is of high importance to the pharmaceutical and food industry. The number of process variables and their interdependence in a pan coating process can make it a rather complex scale-up problem. This review discusses breaking down the coating process variables into three main categories: ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.24582
更新日期:2015-11-01 00:00:00
abstract::Dabrafenib is a small-molecule inhibitor of BRAF kinase activity that is currently being developed for the treatment of BRAF V600 mutation-positive melanoma. This clinical, open-label, two-cohort (n = 14 per cohort), randomized study was designed to evaluate the effect of drug substance particle size, and food on the ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,随机对照试验
doi:10.1002/jps.23519
更新日期:2013-09-01 00:00:00
abstract::Three polymorphs (forms I-III), a monohydrate (form S2), and three new solvates [4:1 hydrate (form S1), monohydrate (form S3), and methanol half-solvate (form S4)] were isolated and characterized by X-ray powder diffractometry (XRPD), IR spectroscopy, differential scanning calorimetry (DSC), hot stage microscopy, solu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600841007
更新日期:1995-10-01 00:00:00
abstract::In our previous research, cocaine applied intranasally in rats diffused or was transported directly from the nasal cavity to the brain. However, the direct nose-brain cocaine transport only contributes to an initial increase in the relative cocaine brain exposure. In this study, we have determined the nose-brain trans...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.1122
更新日期:2001-11-01 00:00:00