Abstract：
:A novel application of attenuated total reflectance IR spectroscopy (ATR-IR) was used to monitor the outer several microns of the stratum corneum (SC) and, thereby, demonstrate enhanced percutaneous absorption in vivo in man. 4-Cyanophenol (CP) as a model permeant yielded a unique IR signal, distinct from those of the stratum corneum and the vehicle components. CP was administered for 1, 2, or 3 hr as a 10% (w/v) solution either in propylene glycol or in propylene glycol containing 5% (v/v) oleic acid. The absorbance at 2230 cm-1, which corresponded to C identical to N bond stretching, diminished significantly faster when CP was codelivered with oleic acid. An IR absorbance due primarily to propylene glycol at 1040 cm-1 (C-O stretching) also disappeared more quickly following application of the enhancer-containing solution. In addition, only the formulations with oleic acid induced a higher wavenumber shift in the frequency of the asymmetric C-H bond stretching absorbance. This change indicates increased lipid-chain disorder, the mechanism by which oleic acid is believed to cause enhanced drug transport across the stratum corneum. Therefore, ATR-IR permits one to examine noninvasively the kinetics, extent, and mechanism of percutaneous penetration enhancement in vivo in human subjects.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Mak VH,Potts RO,Guy RHdoi
10.1023/a:1015960815578subject
Has Abstractpub_date
1990-08-01 00:00:00pages
835-41issue
8eissn
0724-8741issn
1573-904Xjournal_volume
7pub_type
杂志文章abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9395-0
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:The relationship between rat intestinal permeability (Papp) of a range of hydrophilic probe molecules and probe geometry was examined. METHODS:Molecules studies included mannitol, the polyethylene glycols (PEGs) 400, 900, and 4000, the dextran conjugated dye Texas Red (MW 3000) and the polysaccharide inulin (M...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016091915733
更新日期：1996-10-01 00:00:00
abstract：PURPOSE:Interferon beta is commonly used as therapeutic in the first line of therapy for multiple sclerosis. However, depending on the product, it induces an antibody response in up to 60% of patients. This study evaluated the impact of therapy related factors like dose, route of administration and administration frequ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-0992-9
更新日期：2013-06-01 00:00:00
abstract：:Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015917023949
更新日期：1988-03-01 00:00:00
abstract：PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1094-4
更新日期：2013-10-01 00:00:00
abstract：PURPOSE:Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS:Nanofibr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2428-z
更新日期：2018-05-22 00:00:00
abstract：PURPOSE:To engineer optimized near-infrared (NIR) active thermosensitive liposomes to potentially achieve image-guided delivery of chemotherapeutic agents. METHODS:Thermosensitive liposomes were surface-coated with either polyethylene glycol or dextran. Differential scanning calorimetry and calcein release studies wer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0738-0
更新日期：2012-08-01 00:00:00
abstract：PURPOSE:To improve upon the theory of reasoned action and apply it to pharmaceutical research, we investigated the effects of relevant appraisals attributes, and past behavior of physicians on the use of drug information sources. We also examined the moderating effects of practice characteristics. METHODS:A mail quest...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012143915886
更新日期：1997-10-01 00:00:00
abstract：PURPOSE:The trial-and-error approach is still predominantly used in pharmaceutical development of nanosuspensions. Physicochemical dispersion stability is a primary focus and therefore, various analytical bulk methods are commonly employed. Clearly less attention is directed to surface changes of nanoparticles even tho...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2300-6
更新日期：2018-02-21 00:00:00
abstract：:The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018941810744
更新日期：1994-04-01 00:00:00
abstract：PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011071401306
更新日期：2001-03-01 00:00:00
abstract：PURPOSE:We prepared injectable microspheres for controlled release of TAK-029, a water-soluble GPIIb/IIIa antagonist and discussed the characteristics of controlled release from microspheres. METHODS:Copoly(dl-lactic/glycolic)acid (PLGA) microspheres were used for controlled release of TAK-029 [4-(4-amidinobenzoylglyc...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012190304074
更新日期：1997-09-01 00:00:00
abstract：PURPOSE:The aim of this work was to evaluate whether improved topical delivery of finasteride, focussed to the hair follicles of human scalp skin could be achieved with application of short durations of heat and use of specific chemical penetration enhancers. METHODS:Franz cell experiments with human scalp skin were p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02822-y
更新日期：2020-05-31 00:00:00
abstract：PURPOSE:To compare the ability of alkyl-aryl isothiocyanates (ITCs) to increase the activities of the Phase 2 detoxification enzymes NAD[P]H:quinone acceptor oxidoreductase 1 (NQO1) and glutathione S-transferases (GST) in rat tissues in vivo and in cells in vitro. MATERIALS AND METHODS:Twelve alkyl-aryl ITCs and the f...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9595-2
更新日期：2008-09-01 00:00:00
abstract：:A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016346018962
更新日期：1984-11-01 00:00:00
abstract：PURPOSE:The purpose of the study is to characterize glycine crystallization during freezing of aqueous solutions as a function of the glycine salt form (i.e., neutral glycine, glycine hydrochloride, and sodium glycinate), pH, and ionic strength. METHODS:Crystallization was studied by thermal analysis, microscopy, x-ra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016223101872
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:The feasibility of using iontophoresis to enhance the permeation rate of a model peptide was investigated in vitro using hairless mouse skin. METHODS:Angiotensin 2 (AT 2) was employed as a permeant probe, using optimum iontophoresis conditions. A number of physicochemical parameters (donor ionic strength; vale...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016254230155
更新日期：1995-07-01 00:00:00
abstract：:Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-007-9431-0
更新日期：2008-03-01 00:00:00
abstract：PURPOSE:Topoisomerase II (Topo II) preferentially cuts DNA at alternating purine-pyrimidine repeats. Different Topo II poisons may affect Topo II to produce distinct drug-specific DNA cleavage patterns. GL331 is a new podophyllotoxin derivative exhibiting potent Topo II-poisoning activity. Therefore, the sequence selec...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011048831698
更新日期：2001-06-01 00:00:00
abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2466-6
更新日期：2018-08-20 00:00:00
abstract：:Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018926007902
更新日期：1994-09-01 00:00:00
abstract：PURPOSE:The lack of an in vivo diagnostic test for AD has prompted the targeting of amyloid plaques with diagnostic imaging probes. We describe the development of a contrast agent (CA) for magnetic resonance microimaging that utilizes the F(ab')2 fragment of a monoclonal antibody raised against fibrillar human Abeta42 ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9600-9
更新日期：2008-08-01 00:00:00
abstract：PURPOSE:A novel bioequivalence limit is proposed taking into account the therapeutic window. METHODS:The therapeutic range is introduced as the ratios maximum tolerated dose/therapeutic dose (MTD/D) and the therapeutic dose/lowest effective dose. The performance of the new acceptance range was compared with the method...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9680-6
更新日期：2008-11-01 00:00:00
abstract：PURPOSE:It is reported that the cerebrospinal fluid (CSF) to plasma unbound concentration ratio of fleroxacin at steady-state is approximately 0.5 in experimental animals. These results can be accounted for by assuming the presence of an active transport system for the efflux of this compound across the choroid plexus....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016081618149
更新日期：1996-04-01 00:00:00
abstract：:A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015865319250
更新日期：1992-07-01 00:00:00
abstract：PURPOSE:This paper attempts to correlate the hydrophobic contribution constants (faa) of 21 amino acids in small peptides with commonly used physiochemical parameters. These faa constants can then be used to predict hydrophobicity change in peptides when any one of the amino acid residue is substituted with another. M...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016008102587
更新日期：1996-08-01 00:00:00
abstract：PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011954800246
更新日期：1998-07-01 00:00:00
abstract：:(+)-Propranolol was infused at two rates into the pyloric vein (a portal vein tributary) of 15 male Sprague Dawley rats until apparent steady-state conditions were established (i.e., 8 hr at each rate). One group (n = 7) received the high dose (40 micrograms/min/kg) first, and in the other group (n = 8) the low dose (...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018921306200
更新日期：1994-03-01 00:00:00
abstract：:A procedure is described that is suitable for the radioimmunoassay (RIA) of 9-[(l,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) in plasma or serum at concentrations as low as 0.7 ng/ml (2.75 × 10(-9) M). Antiserum was prepared by coupling DHPG monohemisuccinate to bovine serum albumin and immunizing rabbits with the re...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016397520991
更新日期：1986-04-01 00:00:00
abstract：PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018959327311
更新日期：1999-09-01 00:00:00
