Plasma concentrations and ocular effects of cyclopentolate after ocular application of three formulations.

Abstract:

:1. Eight volunteers received in randomized order two 30 microliters drops of either 1% w/v cyclopentolate hydrochloride or a corresponding amount of cyclopentolate polygalacturonate in saline or in acetate buffer in one eye. Cyclopentolate concentrations in plasma were measured by a radioreceptor assay. 2. Peak plasma drug concentrations of about 3 ng ml-1 occurred within 30 min after all formulations. Occasionally, a second concentration peak in plasma, probably reflecting drug absorption from the gastrointestinal tract, was seen after 2 h. The mean elimination half-life of cyclopentolate was 111 min when all subjects and formulations were considered together. There were no statistically significant differences between the formulations with respect to the time-course of plasma drug concentration. 3. The maximal mydriatic effect was reached within about 15 min and was maintained for several hours, often being 1/3 of its peak value after 30 h. Similarly, an intense cycloplegic response was achieved within a few minutes, the peak changes in the near-point of vision being 9 to 10 dioptres. The cycloplegic response was more intense after one of the polygalacturonate complexes, especially at later time points.

journal_name

Br J Clin Pharmacol

authors

Lahdes K,Huupponen R,Kaila T,Monti D,Saettone MF,Salminen L

doi

10.1111/j.1365-2125.1993.tb04173.x

subject

Has Abstract

pub_date

1993-05-01 00:00:00

pages

479-83

issue

5

eissn

0306-5251

issn

1365-2125

journal_volume

35

pub_type

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