Abstract：
:New butyrate derivatives were synthesized to investigate the residence time of potent butyric acid in vivo. These derivatives were triglycerides in which one, two, or three butyric acid molecules were bound to glycerol or to mono- and dipalmitic esters of glycerol. Pharmacokinetic studies showed that a constant plasma level of each compound was maintained for a long time; all molecules had identical volumes of distribution, but differed about their mean residence time. Triesters in which palmitic acid was present displayed no toxicity and seemed to be even more stable in the organism; this may be due to their adsorption on the tissue. Other triglycerides constituted by butyric acid and various long fatty acids may be synthesized and useful in long-term clinical treatment.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Planchon P,Pouillart P,Ronco G,Villa P,Pieri Fsubject
Has Abstractpub_date
1993-10-01 00:00:00pages
1046-8issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49250-0journal_volume
82pub_type
杂志文章abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641229
更新日期：1975-12-01 00:00:00
abstract：:Photoprotective potential and biological consequences (mutagenic potential) of octyl-dimethyl-PABA (ODP), titanium dioxide (TiO2 ), and montmorillonite (MMT) upon ultraviolet B (UVB) irradiation, alone and in different associations [physical mixtures (PMs)], were evaluated using a Saccharomyces cerevisiae ogg1 mutant ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24057
更新日期：2014-08-01 00:00:00
abstract：:The delivery of active agents to the skin by liposome carriers is an interdisciplinary topic of great interest today. Data accumulated over the last decade strongly point to important advantages of these drug delivery systems. A symposium devoted to classic and new approaches in the use of liposomal systems was organi...
journal_title：Journal of pharmaceutical sciences
pub_type：
doi：10.1002/jps.2600830902
更新日期：1994-09-01 00:00:00
abstract：:A procedure is described for TLC detection and differentiation of the butyrophenone-diphenylbutylpiperidine group and phenothiazine derivatives at the microgram level. A two-dimensional TLC method to separate butyrophenone and diphenylbutylpiperidine compounds is reported. A variety of possible detection reagents were...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680834
更新日期：1979-08-01 00:00:00
abstract：:The purpose of this study was to investigate the feasibility of delivering sinomenine hydrochloride (SH) transdermally using composite dissolving microneedles (DM) which integrated with liquid crystals (H2). The fabricated SH-loaded composite DM was evaluated for their appearance, mechanical strength, irritation, and ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.07.027
更新日期：2017-12-01 00:00:00
abstract：:A stability-specific high-pressure liquid chromatographic (HPLC) method was developed to assay intact chlorambucil (I) in the presence of its hydrolytic decomposition products. The HPLC method was used to follow the degradation kinetics of I over pH 1.0-10.0 in the presence of various buffers with and without added ch...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710113
更新日期：1982-01-01 00:00:00
abstract：:Low-density lipoproteins (LDLs), the physiological vehicles for lipids, are potentially useful drug delivery devices for (hydrophobic) drugs. The physicochemical characteristics of LDL loaded with the adriamycin derivative AD 32 or the N-mustard derivative WB 4291 were compared to that of native and reconstituted LDL ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840204
更新日期：1995-02-01 00:00:00
abstract：:The stability of therapeutic proteins formulated in prefilled syringes (PFS) may be negatively impacted by the exposure of protein molecules to silicone oil-water interfaces and air-water interfaces. In addition, agitation, such as that experienced during transportation, may increase the detrimental effects (i.e., pro...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23973
更新日期：2014-06-01 00:00:00
abstract：:To design safe, efficient synthetic gene therapy vectors, it is desirable to understand the intracellular mechanisms that facilitate their delivery from the cell surface to the nucleus. Elements of the cytoskeleton and molecular motor proteins are known to play a pivotal role in most intracellular active transport pro...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21106
更新日期：2008-04-01 00:00:00
abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640933
更新日期：1975-09-01 00:00:00
abstract：:The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840514
更新日期：1995-05-01 00:00:00
abstract：:The absorption of the model drug carbenoxolone was reevaluated using an in situ rat intestinal perfusion technique in which disappearance from the intestinal lumen, binding to the perfused jejunal segment, and appearance in the mesenteric (jejunal) vein were measured. The effect of the degree of ionization on these pr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790510
更新日期：1990-05-01 00:00:00
abstract：:Drug-induced phototoxic skin responses involves photoirritation, photoallergy, and photogenotoxicity. In the present study, we attempted to develop effective analytical tools to predict the photogenotoxic potential of pharmaceutical substances on the basis of their photobiological and DNA-binding properties. Photoclea...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21670
更新日期：2009-10-01 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 butamben has been measured gravimetrically in pure methanol, 1-propanol, 2-propanol, 1-butanol, and toluene over the temperature range 268-298 K. Polymorph transition and melting temperatures, associated enthalpy changes, and the heat capacity of the solid forms and the supercooled melt have been mea...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.02.013
更新日期：2019-07-01 00:00:00
abstract：:The applicability of bioavailability assessment at quasi- and nonsteady state is illustrated with data from a study comparing two formulations of amitriptyline hydrochloride in humans. Relative bioavailability as a function of the observed mean plasma concentrations may be expressed in closed form, provided the affect...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600651124
更新日期：1976-11-01 00:00:00
abstract：:A sensitive, simple, and rapid method for the quantitation of ibuprofen in plasma, using 1-(p-fluorobenzoyl)-5-methoxy-2-methylindole acetic acid as the internal standard, was developed. The method is based on reversed-phase high-pressure liquid chromatography with a mobile phase containing acetonitrile--0.1 M acetic ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700829
更新日期：1981-08-01 00:00:00
abstract：:In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispe...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24207
更新日期：2015-01-01 00:00:00
abstract：:Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23464
更新日期：2013-04-01 00:00:00
abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690905
更新日期：1980-09-01 00:00:00
abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670643
更新日期：1978-06-01 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：:To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22814
更新日期：2012-03-01 00:00:00
abstract：:The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.1080
更新日期：2001-09-01 00:00:00
abstract：:17-(allylamino)-17-demethoxygeldanamycin (17AAG) is a benzoquinone ansamycin Hsp90 inhibitor which has promising anticancer activity in vitro, in animal models and in clinical trials. 17AAG has poor water-solubility which is a potential problem for clinical formulation. The hydroquinone derivative of 17AAG, 17AAG hydr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21394
更新日期：2008-12-01 00:00:00
abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740819
更新日期：1985-08-01 00:00:00
abstract：:Anionic surfactants compromise skin's barrier function by damaging stratum corneum lipids and proteins. The objective of this study was to examine anionic surfactant-induced changes in the skin's polar and transcellular pathways and the resulting impact on surfactant penetration into the skin. Three anionic surfactant...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.06.030
更新日期：2019-11-01 00:00:00
abstract：:A high-performance liquid chromatographic method has been developed for the simultaneous determination of azobenzene and hydrazobenzene in phenylbutazone and sulfinpyrazone raw materials and formulations. The drug raw material or formulation is shaken with 1N NaOH and n-hexane and centrifuged. The n-hexane layer is in...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721032
更新日期：1983-10-01 00:00:00
abstract：:In iontophoresis, an electric field across the skin induces electromigration of exogenously applied and endogenously present ions. The approach can be used to improve dramatically drug delivery by elimination of competing co-ions in the externally applied formulation, as this maximizes the fraction of current carried ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20561
更新日期：2006-03-01 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
pub_type： 杂志文章
doi：10.1002/jps.2600840310
更新日期：1995-03-01 00:00:00
