Pharmacokinetics of nalbuphine hydrochloride extended release tablets in hemodialysis patients with exploratory effect on pruritus

Table 1 Mean pharmacokinetic parameters on day 1 and day 13 following multiple nalbuphine oral doses

Parameter	Statistics	Hemodialysis patients		Healthy subjects
		30 mg QD	180 mg BID	30 mg QD	180 mg BID
		Day 1	Day 13	Day 1	Day 13
AUC_inf (ng•h/mL)	N	4	4	7	8
	Mean	142.5	2635.38	49.53	588.40
	SD	33.28	2038.01	30.04	214.08
	CV%	23.4	77.3	60.7	36.4
AUC_last (ng•h/mL)	N	15	9	9	8
	Mean	73.43	1457.74	40.55	529.85
	SD	41.81	1016.26	22.96	179.93
	CV%	56.9	69.7	56.6	34.0
AUC_tau (ng•h/mL)	N	15	9	9	8
	Mean	43.2	760.87	31.53	351.15
	SD	24.97	538.28	16.93	118.21
	CV	57.8	70.7	53.7	33.7
ARAUC _tau ratio	Ratio of Mean	2.7	NA	1.6	NA
C_max (ng/mL)	N	15	9	9	8
	Mean	6.28	82.78	5.2	44.21
	SD	3.36	55.81	2.78	14.54
	CV	53.5	67.4	53.5	32.9
T_max (h)	N	15	9	9	8
	Min	1.0	2.0	2.0	2.0
	Median	5.0	5.0	3.0	4.0
	Max	18	7.1	5.0	6.0
T_1/2 (h)	N	4	4	7	8
	Mean	10.49	14.23	6.81	8.58
	SD	2.22	3.24	2.79	2.05
	CV	21.1	22.7	41.0	23.9

Subjects were titrated every 3–4 days from 30 mg QD on Day 1 to 30 mg BID then 60 mg BID, 120 mg BID and finally 180 mg BID over a 14-day period. Data shown for Day 1 and Day 13 only.
Abbreviations: ARAUC_tau accumulation ratio (mean AUC_tau Day 4/Mean AUC_tau Day 1), AUC_inf area under plasma concentration-time curve from time zero extrapolated to infinite time, AUC_last area under the plasma concentration-time curve from time zero to the last measureable concentration, AUC_tau area under plasma concentration-time curve over dosing interval (0-12 hr), BID twice daily, C_max maximum observed plasma concentration, CV coefficient of variation, ER extended release, h hour, Max maximum, Min minimum, n number of subjects, NA not applicable, QD once daily, T_max time of maximum observed plasma concentration, T_1/2 plasma half life.

ISSN: 1471-2369