Abstract：
:Human skin samples are permeable to theophylline delivered from 1.5% solutions in various alkanecarboxylic acids and their mixtures. The respective permeability coefficients of theophylline, calculated from steady-state flux, correlate negatively with the permeability coefficients of the donor carboxylic acids and positively with the excess free energy of theophylline in the donor phase, or "push" effect. An exception is propionic acid which enhances the penetration of theophylline by promoting its solubility in the skin-propionic acid medium through the "pull" effect. The two effects operate jointly in the delivery of theophylline from a mixture of propionic and a higher acid such as lauric, resulting in a much higher flux than expected from theory. The "push" effect can be estimated from the solubility parameters of theophylline and those of the holding phases even though regular solution behavior is not strictly obeyed. The increase in the permeability coefficient with partial molal volume of theophylline in the donor phase seems to reach an upper limit or decrease beyond 119 cm3.mol-1.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Kadir R,Stempler D,Liron Z,Cohen Sdoi
10.1002/jps.2600761004subject
Has Abstractpub_date
1987-10-01 00:00:00pages
774-9issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47531-8journal_volume
76pub_type
杂志文章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
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更新日期：1988-10-01 00:00:00
abstract：:There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...
journal_title：Journal of pharmaceutical sciences
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更新日期：2019-01-01 00:00:00
abstract：:Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, ...
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pub_type： 杂志文章
doi：10.1002/jps.10112
更新日期：2002-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2008-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670106
更新日期：1978-01-01 00:00:00
abstract：:NMR was used to study the binding of acetylcholine, atropine, and physostigmine to acetylcholinesterase. Changes in the linewidth of the N-methyl resonance of acetylcholine, resulting from association with the enzyme during hydrolysis, were utilized to study the enzyme-substrate interaction. Physostigmine inhibited th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640337
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abstract：:The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 day...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
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更新日期：1994-10-01 00:00:00
abstract：:A method is presented for encapsulating high molecular weight biological materials such as viral antigen, concanavalin A, and other proteins with cellulose acetate phthalate. The method is simple, inexpensive, and rapid; the process takes approximately 15 min. Capsules generated by this method are produced as microsph...
journal_title：Journal of pharmaceutical sciences
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更新日期：1984-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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abstract：:A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...
journal_title：Journal of pharmaceutical sciences
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更新日期：1982-03-01 00:00:00
abstract：:The degradation kinetics of metronidazole in aqueous solutions of pH 3.1 to 9.9 under accelerated storage conditions were studied. The stability of metronidazole in solutions containing propylene glycol or polyethylene glycol 400 was also investigated. The reaction order for metronidazole in these aqueous and solvent ...
journal_title：Journal of pharmaceutical sciences
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更新日期：1993-01-01 00:00:00
abstract：:Human papillomavirus (HPV) virus-like-particles (VLPs) produced by recombinant expression systems are promising vaccine candidates for prevention of cervical cancers as well as genital warts. At high protein concentrations, HPV VLPs, comprised of the viral capsid protein L1 and expressed and purified from yeast, are p...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20377
更新日期：2005-07-01 00:00:00
abstract：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20379
更新日期：2005-07-01 00:00:00
abstract：:In this study, powder surface imaging was utilized in evaluation of particle size-related segregation behavior of granules during vibration and tableting processes. Altogether, eight granule batches were manufactured using a fluidized bed granulator. The particle size distribution of each batch was measured with sieve...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23126
更新日期：2012-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9601187
更新日期：1996-10-01 00:00:00
abstract：:The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2014-02-01 00:00:00
abstract：:Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medi...
journal_title：Journal of pharmaceutical sciences
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更新日期：2008-06-01 00:00:00
abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...
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更新日期：2014-01-01 00:00:00
abstract：:The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs. The OMS was characterized as highly ordered mesoporous material with a narrow pore size distribution. Ezetimibe was loade...
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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更新日期：2010-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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更新日期：2002-02-01 00:00:00
abstract：:Hyperthermia (HT)-dependent cisplatin (CDDP) release and tumor CDDP level increase after the administration of thermosensitive, large unilamellar vesicles (LUVs: LUV-1 and LUV-2) and a thermosensitive, small unilamellar vesicle (SUV: SUV-1) were examined in comparison with those following administration of a non-therm...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600800604
更新日期：1991-06-01 00:00:00
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abstract：:The effect of dimethyl sulfoxide, dimethyl formamide, and dimethyl acetamide on the basal stratum corneum of excised nude mouse skin was investigated. All of these dipolar aprotic solvents caused a swelling of the basal stratum corneum cells and a disruption of the normal keratin pattern. This behavior suggests that d...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600770106
更新日期：1988-01-01 00:00:00
abstract：:A series of 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-2-acetic acids (3a-e) and 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-1-acetic acids (4a-e) were synthesized as semirigid analogues of tolmetin (1). These compounds were evaluated for their anti-inflammatory action by investigating their ability to block arachi...
journal_title：Journal of pharmaceutical sciences
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更新日期：1989-04-01 00:00:00
abstract：:In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.23221
更新日期：2012-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.24013
更新日期：2014-07-01 00:00:00
abstract：:Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600690934
更新日期：1980-09-01 00:00:00
abstract：:Pancreatic islet transplantation is a promising advanced therapy that has been used to treat patients suffering from diabetes type 1. Traditionally, pancreatic islets are infused via the portal vein, which is subsequently intended to engraft in the liver. Severe immunosuppressive treatments are necessary, however, to ...
journal_title：Journal of pharmaceutical sciences
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更新日期：2020-01-01 00:00:00
