THE EFFECT OF RIFAMPICIN ON THE PHARMACOKINETIC PARAMETERS OF NIFEDIPINE IN HEALTHY VOLUNTEERS
THE EFFECT OF RIFAMPICIN ON THE PHARMACOKINETIC PARAMETERS OF NIFEDIPINE IN HEALTHY VOLUNTEERS
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Date
1995-03
Authors
USMAN, NDANUSA BABANDAKO
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Abstract
Quality assessment of the three brands of nifedipine
tablets/capsules were carried out. The identification tests,
chemical assay and melting point method, determination showed
that all the brands contained nifedipine as active ingredient.
The results are in line with BP 1988 Addendun 1990 specifications
for identification tests of nifedipine. Using U.V. spectroscopic
methods, the U.V. spectra of all brands compared well with that
of the reference with absorption maxima; at 206nm. 236nm and
344nm.
The estimated total content of active ingredient of the
brands of nifedipine using HPLC and U.V.- assay methods gave
results which complied with the BP 1988 specification for the
drug content (98 - 102%).
The disintegration time for all the three brands of the
nifedipine was less than 10 minutes. This result complied with
BP 1988 specification for tab 1et/capsules disintegration time of
not more than 15 minutes. The disssolution rate profiles of the
three brands are similar. All the brands released more than 70%
of their active ingredient in less than 30 minutes. These are
within the limit specification by BP 1988 - of 45 minutes.
The effect of a single oral dose of rifampicin 1200mg on the
pharmacokinetics parameters of nifedipine lOmg (Capsules) was
studied in a cross-over design in six healthy human volunteers
(Age 28 ± 6.3 years old and weight of 60.67 ± 3.50). The
pharmacokinetic parameters; such as tia(jg, Kabs , tlag , traax and Vd all
showed no significant difference between the studies. Thus the
absorption kinetics related parameters are not significantly
different between the studies. However, those kinetic parameters
related with metabolism and excretion kinetics showed significant
differences. AUC0 - M (relative bioavailability) was decreased by
62.2% (573.4 Vs 205.25 mg.hr/ml) P < 0.0001: t½ el. was decreased
by 67% (2.62 Vs 1.03 hr) P < 0.0001: ke,. was increased by 157%
(0.260 Vs 0.670 hr"1 ) P < 0.0001; ClT was increased by 194% (17.33
Vs 50.17 ml/min.kg) P < 0.0001: Cma¥ decreased by 67% (173.23 Vs
nidi
115.77 ng/ml ) P < 0.0001.
This study showed that rifampicin increases the metabolism
and elimination of nifedipine.
Description
A THESIS SUBMITTED TO THE POSTGRADUATE SCHOOL,
AHMADU BELLO UNIVERSITY, ZARIA, IN PARTIAL
FULFILLMENT OF THE REQUIREMENTS FOR THE
DEGREE OF MASTER OF SCIENCE IN
PHARMACEUTICAL ANALYSIS
DEPARTMENT OF PHARMACEUTICAL AND MEDICINAL CHEMISTRY,
FACULTY OF PHARMACEUTICAL SCIENCES,
AHMADU BELLO UNIVERSITY,
ZARIA - NIGERIA
MARCH, 1995
Keywords
EFFECT,, RIFAMPICIN,, PHARMACOKINETIC,, PARAMETERS,, NIFEDIPINE,, HEALTHY,, VOLUNTEERS.