Pharmacokinetic profile of ENDUR-AMIDE® sustained-release niacinamide

Highlights

• Sustained-release ENDUR-AMIDE® and standard niacinamide pharmacokinetics studied in young men
• Low-dose preparations yield similar results
• High-dose preparations differ in several parameters (Cmax, AUC and Tmax)

Summary

The aim of this study was to compare the plasma pharmacokinetics of niacinamide (NAM) in humans given at two doses and in two different formulas.

Eight men, mean age 20 years (range 18-22 years) with an average body weight of 75 kg (range 66 to 68 kg) provided written informed consent and were enrolled in the study. The different doses and different preparations were studied in each study participant on four separate occasions, each separated by at least one week.

Two different preparations were studied:

1.  Standard NAM (pure powder)
2. Sustained-release NAM (ENDUR-AMIDE® tablet)

Each preparation was evaluated at a low dose and a high dose:

Low Dose:

1. Standard NAM: 2.5 mg/kg body weight of niacinamide
2. ENDUR-AMIDE®: 6.7 mg/kg body weight of niacinamide for a 75-kg person (one 500-mg tablet)

High Dose:

1. Standard NAM: 25 mg/kg body weight of niacinamide
2. ENDUR-AMIDE®: 26.6 mg/kg body weight of niacinamide for a 75-kg person (four 500-mg tablets)

Results indicate no significant differences between the kinetics of the low-dose preparations.

By contrast, the high-dose standard NAM preparation (25 mg/kg body weight) resulted in a significantly higher peak plasma concentration (Cmax), a significantly higher area under the plasma concentration-time curve (AUC), and a significantly lower time to peak concentration (Tmax) compared to the high-dose ENDUR-AMIDE® preparation.

 

Dose	Cmax (g/ml)	Tmax (h)	AUC (g/ml/h)	Plasma Half-life (h)
Low Standard	3.3 +/- 2.6	0.3 +/- 0.1	3.0 +/- 1.4	0.6 +/- 0.2
Low ENDUR-AMIDE®	2.1 +/- 0.7	1.0 +/- 0.8	4.5 +/- 2.2	1.0 +/- 0.5
High Standard	42.1 +/- 15.2	0.5 +/- 0.3	187.1 +/- 54.8	3.5 +/- 1.0
High ENDUR-AMIDE®	16.2 +/- 3.5*	1.9 +/- 1.2*	107.0 +/- 41.1**	2.7 +/- 1.6

Data are means +/- standard deviations; *P<.05; **P<.01 compared to standard niacinamide.

Reference

Petley A, Macklin B, Renwick AG, Wilkin TJ. The pharmacokinetics of nicotinamide in humans and rodents. Diabetes. 1995;44(2):152-155. PMID: 7859933.

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