Miglyol 840, propylene glycol diesters of caprylic and capric acids, in binary systems with ethanol markedly improved the in vitro skin permeation rate of several transdermal drug candidates such as tetrahydroaminoacridine (THA), diltiazem, atenolol, tazifylline and hydrocortisone, as compared to ethanol or Miglyol 840 alone across human and hairless mouse skin.The addition of ethanol to Miglyol 840 improved the drugs' skin permeation rates primarily as a result of increasing the drugs' solubilityThe addition of ethanol to Miglyol 840 also improved the relative permeation rate (permeation rate/initial concentration) of ethanol.No local irritation (erythema or edema) was noted over a 24 h period among four human volunteers wearing patches containing the binary vehicle, ethanol-Miglyol 840 (20:80 or 40:60).

1989-02-01·Methods and findings in experimental and clinical pharmacology

The reducing effects of tazifylline on histamine-induced bronchoconstriction in atopic asthmatics.

Article

作者: Reuter, C ; Stenius-Aarniala, B ; Harlow, B ; Kiviranta, K ; Scott, J

Percentage reductions in the peak flow rates to a standardized number of histamine inhalations were compared after 7 days of treatment with 10 mg bd tazifylline and after 7 days of placebo in a randomized crossover study in 11 male seasonal atopic asthmatics. After tazifylline, mean % reductions in peak flow rates were significantly lower than after placebo (p = 0.03). The effects of tazifylline had disappeared within 7 days of stopping treatment. Using a 50% decrease in bronchial reactivity as the criteria of "protection", 7 of the subjects were "protected" by tazifylline only and none by placebo only (p = 0.03).

1989-01-01·Biopharmaceutics & drug disposition4区 · 医学

Multiple‐dose pharmacokinetics of the new H₁‐receptor antagonist tazifylline in healthy volunteers

4区 · 医学

Article

作者: Auger, J. ; Pinhas, H. ; Dow, R. ; Jullien, I. ; McEwen, J. ; Cano, J. P. ; Iliadis, A. ; Bruno, R.

Abstract:

The multiple‐dose pharmacokinetics of the new H1‐receptor antagonist, tazifylline, were investigated in healthy volunteers. From single‐dose data, tazifylline appeared to be rapidly absorbed (median tmax of 0·6 h) and eliminated (t1/2 □ 1·0±0·2 h). However, plasma levels measured on days 3 and 8 of the multiple‐dose regimen (10 mg b.i.d. for 8 days) indicated moderate accumulation. A two‐compartment model best described multiple‐dose data with a terminal half‐life of 15·6 ± 7·6 h consistent with twice‐daily dosing of tazifylline.

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