Effect of food on nifedipine pharmacokinetics

Abstract

The effect of food on the bioavailability of nifedipine (Procardia), 10 mg capsules, was studied. Each of 15 male volunteers received a single oral 10 mg dose with 120 ml water under three conditions: fasting, after a low-fat (high-carbohydrate) meal, and after a high-fat meal. An open, three-way Latin-square design was employed with a 4-day washout period between administrations. Serial blood samples were collected just before the dose (0 hour) and from 0 to 8 hours after administration. Nifedipine assays were performed by GLC/electron capture detection. Diet did not appreciably alter the AUC from 0 to 8 hours, the AUC from 0 to infinity, or the elimination half-life. The time to peak (tmax) and peak concentrations (Cmax) were significantly altered by food. The mean Cmax values for fasting, low-fat, and high-fat meals were 78.9, 42.2, and 58.7 ng/ml, respectively. The mean tmax values for these three conditions were 0.97, 1.89, and 1.07 hours, respectively. The results indicate that food, in particular a low-fat (high-carbohydrate) meal, slows the rate but does not alter the extent of nifedipine absorption. Insofar as certain side effects (e.g., flushing and headache) may be related to the high peak plasma levels associated with rapid absorption, administration with meals might serve to reduce the incidence of such effects. Clinical trials would be necessary to confirm this possibility. For the majority of patients on routine maintenance therapeutic regimens, nifedipine capsules may be administered without regard to food intake.

Pharmacokinetics of nifedipine in Taiwanese

“…The difference between the mean and median AUC of NF in Taiwan residents indicates that the data were not normally distributed but skewed. Our data showed significantly higher values of AUC than those for the British [9][10][11][12], Americans [2,15] and Germans [4], but lower than that of Nigerians [10]. No statistical difference was seen when compared with Indians [9], Mexicans [7,16] and Japanese [17] after the NF dose was normalized.…”

Food effect on the oral bioavailability of Manidipine: single dose, randomized, crossover study in healthy male subjects

“…The same findings were observed for the other dihydropyridine calcium antagonists as benidipine (16), felodipine (17), and nisoldipine (16), showing the same lipophilicity as manidipine (18). On the other hand, no significant food effect on the extent of absorption was observed for other less lipophilic dihydropyridine calcium antagonists as nifedipine (19,20,21,22,23), amlodipine (24,25,26), isradipine (27), and nilvadipine (28).…”

The influence of food on the pharmacokinetics of ‘biphasic’ nifedipine at steady state in normal subjects.

“…The first was carried out in patients with myocardial infarction where it was found that taking nifedipine following a light breakfast delayed both the rate of absorption and the peak concentration achieved (Hirasawa et al, 1985). Both the delay in achieving maximum concentration and the reduction in peak concentration when a nifedipine capsule is taken following food were confirmed in normal volunteers (Challenor et al, 1987;Reitberg et al, 1987). Recently, a 'biphasic' formulation of nifedipine has been developed which contains 5 mg 'rapid' release and 15 mg 'retarded' release drug.…”