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  • 1
    Electronic Resource
    Electronic Resource
    Paramagnetically enhanced relaxation of nuclear spins. Measurement of diffusion (1979)
    s.l. : American Chemical Society
    The @journal of physical chemistry 〈Washington, DC〉 83 (1979), S. 1401-1405 
    Details
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/j100474a010
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  • 2
    Electronic Resource
    Electronic Resource
    The electron spin resonance line width method for measuring diffusion. A critique (1979)
    s.l. : American Chemical Society
    The @journal of physical chemistry 〈Washington, DC〉 83 (1979), S. 1406-1412 
    Details
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/j100474a011
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  • 3
    Electronic Resource
    Electronic Resource
    Human Transbuccal Absorption of Diclofenac Sodium from a Prototype Hydrogel Delivery Device (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 126-129 
    Details
    ISSN: 1573-904X
    Keywords: buccal delivery ; diclofenac sodium ; human clinical ; hydrogel device
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The buccal delivery of the nonsteroidal antiinflammatory drug, diclofenac sodium (Voltaren), from a prototype hydrogel was studied in man in a randomized crossover design of buccal delivery and i.v. infusion. After a 30-min delay, plasma levels of diclofenac increased to near steady-state levels of 100 ng/ml by 3 hr. With each subject serving as his own control, the i.v. infusion data facilitated the calculation of a mean steady-state flux of diclofenac sodium of 2.1 ± 0.6 mg/cm2-hr across human buccal mucosa and a time lag of 1.0 ± 0.5 hr. The large flux of this ionized species indicates that the traditional lipoidal model of buccal permeation based on the partition coefficient is inadequate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018941517355
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  • 4
    Electronic Resource
    Electronic Resource
    Transbuccal Delivery of Acyclovir: I. In Vitro Determination of Routes of Buccal Transport (1998)
    Springer
    Pharmaceutical research 15 (1998), S. 1182-1188 
    Details
    ISSN: 1573-904X
    Keywords: acyclovir ; membrane transport ; buccal mucosal delivery ; in vitropermeation ; zwitterion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To determine the major routes of buccal transport of acyclovir and to examine the effects of pH and permeation enhancer on drug permeation. Methods. Permeation of acyclovir across porcine buccal mucosa was studied by using side-by-side flow through diffusion cells at 37°C. The permeability of acyclovir was determined at pH range of 3.3 to 8.8. Permeability of different ionic species was calculated by fitting the permeation data to a mathematical model. Acyclovir was quantified using HPLC. Results. Higher steady state fluxes were observed at pH 3.3 and 8.8. The partition coefficient (1-octanol/buffer) and the solubility of acyclovir showed the same pH dependent profile as that of drug permeation. In the presence of sodium glycocholate (NaGC) (2−100 mM), the permeability of acyclovir across buccal mucosa was increased 2 to 9 times. This enhancement was independent of pH and reached a plateau above the critical micelle concentration of NaGC. The permeabilities of anionic, cationic, and zwitterionic species were 3.83 × 10−5, 4.33 × 10−5, and 6.24 × 10−6cm/sec, respectively. Conclusions. The in vitropermeability of acyclovir across porcine buccal mucosa and the octanol-water partitioning of the drug were pH dependent. A model of the paracellular permeation of the anionic, cationic, and zwitterionic forms of acyclovir is consistent with these data. The paracellular route was the primary route of buccal transport of acyclovir, and the enhancement of transbuccal transport of acyclovir by sodium glycocholate (NaGC) appeared to operate via this paracellular route.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011927521627
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  • 5
    Electronic Resource
    Electronic Resource
    Influence of Skin Irritants on Percutaneous Absorption (1993)
    Springer
    Pharmaceutical research 10 (1993), S. 1756-1759 
    Details
    ISSN: 1573-904X
    Keywords: skin irritation ; percutaneous absorption ; norephedrine ; imipramine ; hydrocortisone ; caffeine ; indomethacin ; transepidermal water loss ; skin pH
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effects of the application of skin irritants on the in vitro percutaneous absorption of three model compounds of diverse physico-chemical properties, caffeine, indomethacin, and hydrocortisone, were investigated. Norephedrine and imipramine, basic drugs with a known skin irritation potential, were employed to damage the skin. Treatment with norephedrine increased the permeation of caffeine and hydrocortisone by two- to fourfold, while absorption of indomethacin declined an order of magnitude. A similar result was obtained for the effect of treatment with imipramine on transport of caffeine. Pretreatment with imipramine promoted hydrocortisone absorption 10-fold but, unlike norephedrine, did not alter indomethacin permeation. While both treatments in vivo caused an increase (norephedrine 〉 imipramine) in the pH on the surface of skin and after tape-stripping the skin, only norephedrine caused changes in transepidermal water loss in vivo in man. Since imipramine was the more severe irritant as judged by erythema, alterations by irritants of barrier function appeared rather complex.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018978232145
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  • 6
    Electronic Resource
    Electronic Resource
    Upper and lower limits of human skin electrical resistance in lontophoresis (1993)
    Hoboken, NJ : Wiley-Blackwell
    AIChE Journal 39 (1993), S. 2011-2018 
    Details
    ISSN: 0001-1541
    Keywords: Chemistry ; Chemical Engineering
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: The time-dependent electrical resistance of human cadaver skin was shown to be bound by an upper limit at equilibrium and a lower limit at steady state. The time to reach steady state from any initial condition by applying a current was much shorter than the recovery to equilibrium, due to different driving forces. The ratio of the equilibrium to the solution resistances increased with the salt concentration in free solution. This equilibrium relative resistance was sensitive to skin variability, primarily due to its dependence on porosity and pore geometry. A model was developed relating the equilibrium relative resistance to the structural properties of skin. The estimated pore radius of 25 × 10-10 m from the equilibrium resistance data is consistent with the average pore radius of human skin reported in the literature. In contrast, the steady-state resistance could be several orders of magnitude lower than the equilibrium resistance and depended on current density and salt concentration but not on the history of prior exposures of a skin sample to a current. This difference can greatly reduce the power requirement for iontophoresis and can make this technology more practical. A linear relationship was found between the logarithm of the steady-state relative resistance (skin/solution resistances) and the logarithm of the current density divided by the salt concentration. The slope of -0.65 was in excellent agreement with the theoretical slope of -2/3 that was derived for the convective transport of ions in a charged pore under a constant current.
    Additional Material: 8 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/aic.690391211
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  • 7
    Electronic Resource
    Electronic Resource
    Variational analysis of the transdermal delivery rate from two prototypical ethanol-water nitroglycerin TTS devices and Transderm-Nitro 10 in the normal population (1992)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 20 (1992), S. 443-459 
    Details
    ISSN: 1573-8744
    Keywords: nitroglycerin ; transdermal delivery ; random intersubject and intrasubject variance ; fixed effect variance ; variational stability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The performance of two prototypical ethanol-water flux-enhanced transdermal therapeutic systems were compared to the performance of commercial Transderm-Nitro 10. This was a single- center, open- label, three- treatment, randomized crossover study in six healthy subjects who completed the study. Concurrent with each transdermal treatment, an infusion of the stable isotope [15N]3-nitroglycerin was administered. The use of double isotope methodology was incorporated into this study to minimize the variation introduced by fixed-effect error on the evaluation of transdermal flux. The objectives of this study were to isolate experimentally and characterize the average flux enhancement of each prototype, to determine the temporal profile of delivery, and to evaluate the components of variance of drug delivery from each transdermal system. The results of this study showed that the two flux-enhanced transdermal systems with different fill volumes both produced flux enhancement factors of 2 to 3 relative to Transderm-Nitro 10. Prototype B demonstrated a 57% reduction in intersubject variation relative to Transderm-Nitro 10 indicative of enhanced control of drug permeation across a subject population. Prototype A, while reducing intersubject variations, was less than optimal. Both prototypes demonstrated comparable intrasubject variation relative to Transderm-Nitro 10, indicating similar stability for within-subject transdermal drug delivery. The flux enhancement and variational properties of Prototype B were consistent with those intended based on mechanistic considerations of mutual nitroglycerin and ethanol- coupled transdermal delivery.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061465
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  • 8
    Electronic Resource
    Electronic Resource
    The Relationship of pK a and Acute Skin Irritation in Man (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 660-663 
    Details
    ISSN: 1573-904X
    Keywords: skin irritation ; pK a ; pH, skin permeation ; chemical structure/irritation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The relationship between pK a and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15–88 µg/cm2/hr). Skin irritation and pK a are correlated for pK a ≤ 4. Laser Doppler velocimetric assessment of skin blood flow, color meter readings, erythema, edema, and the primary irritation index are all linearly correlated and related to pK a, erythema at 24 hr appears to be the most sensitive parameter to variation in pK a when pK a ≤ 4.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015931105660
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  • 9
    Electronic Resource
    Electronic Resource
    Steady-State Pharmacokinetics and Pharmacodynamics of Benazeprilat in Spontaneously Hypertensive Rats (SHR) and Wistar–Kyoto (WKY) Rats (1991)
    Springer
    Pharmaceutical research 8 (1991), S. 883-887 
    Details
    ISSN: 1573-904X
    Keywords: benazepril ; benazeprilat ; pharmacokinetics ; pharmacodynamics ; steady state ; i.v. infusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effects of the simultaneous steady-state intravenous infusion of benazeprilat, the active metabolite of benazepril HC1, and angiotensin I (AI) on mean arterial blood pressure were investigated in the conscious, unrestrained spontaneously hypertensive rat (SHR) and its normotensive parent strain, the Wistar–Kyoto (WKY) rat. A competitive inhibition model is applied and the limits of its validity are discussed. Deviations from the model are apparent at high drug infusion rates and may relate to the effect of benazeprilat on the clearance of AI. The strains differ in the amounts of angiotensin converting enzyme (ACE) or responsiveness to angiotensin II (AII), the drug clearances, and either the pharmacology or the distribution of the drug. Since the latter two differences are drug dependent, prediction between strains is rendered difficult. This steady-state approach relates the hypertension in the SHR to the amount of ACE or responsiveness to AII and renal function.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015803529013
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  • 10
    Electronic Resource
    Electronic Resource
    Copolymers of (±)2-ethylhexyl acrylate and 3-[3,3,3-trimethyl-1,1-bis (trimethylsiloxy) disiloxanyl] propyl methacrylate (1997)
    Bognor Regis [u.a.] : Wiley-Blackwell
    Journal of Polymer Science Part A: Polymer Chemistry 35 (1997), S. 3571-3574 
    Details
    ISSN: 0887-624X
    Keywords: copolymerization ; reactivity ratios ; Q-e values ; pressure-sensitive adhesive ; 3-[3,3,3- trimethyl- 1,1-bis (trimethylsiloxy) disiloxanyl] propyl methacrylate ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Statistical copolymers of (±)2-ethylhexyl acrylate and 3-[3,3,3-trimethyl- 1,1-bis (trimethylsiloxy) disiloxanyl] propyl methacrylate were synthesized and the reactivity ratios and the Q and e values were calculated. The glass transition temperatures of the copolymers were in good agreement with the predictions of Fox's equation and Wood's formula. © 1997 John Wiley & Sons, Inc. J Polym Sci A: Polym Chem 35: 3571-3574, 1997
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
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