Pharmacokinetics of a Sustained-Release Dosage Form of Isosorbide Dinitrate (Frandol<SUP>®</SUP>)
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A sustained-release dosage form of isosorbide dinitrate (Frandol<SUP>®</SUP>) has been developed for the purpose of prolonging the preventive effect of isosorbide dinitrate (ISDN) against attacks of angina pectoris.<BR>According to the JP IX disintegration test (with slight modification), the dissolution rate of Frandol was slow, with a 50% dissolution time of about 3 hr on the other hand, disintegration of the standard tablet (Nitorol<SUP>®</SUP>) was very rapid, almost entirely dissolving within 10 min.<BR>After administration of Frandol (20 mg) to six healthy volunteers, the plasma level of ISDN slowly increased to the maximum level at 3 hr and remained at a high level for 6 to 8 hr. However, after administration of the standard tablet (5 mg), the plasma level of ISDN rapidly increased to the maximum level within 30 min, but thereafter decreased rapidly.<BR>According to the pharmacokinetic analysis based on a two-compartment open model, the bioavailability of ISDN after dosing of the standerd tablet was about 7%, while the bioavailability of Frandol relative to the standard tablet was 95%.<BR>Computer-simulated pharmacokinetic data at the steady-states by repeated administrations of the standard tablet (8 hr interval) and Frandol (12 hr interval) were as follows: the average plasma concentrations of ISDN with the standard tablet and Frandol were 0.93 and 2.56 ng/ml, respectively ; and the minimum plasma concentrations with the standard tablet and Frandol were 0.11 and 1.40 ng/ ml, respectively ; and the maximum plasma concentrations with the standard tablet and Frandol were 5.32 and 3.52 ng/ml, respectively.<BR>These results indicated that Frandol may be an ideal sustained-release dosage form of ISDN for the prevention of angina pectoris, since the plasma ISDN level is maintained at a high level constantly without the production of an excessively high plasma level.
- 一般社団法人 日本臨床薬理学会の論文
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- Pharmacokinetics of a Sustained-Release Dosage Form of Isosorbide Dinitrate (Frandol®)
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