Pharmacokinetics of radioimmunotherapeutic agent of direct labeling mAb 188Re-HAb18

Table 1 Biodistribution of ¹⁸⁸Re-HAb18 F(ab’)₂ in hepatoma-bearing nude mice

Tissue	T(post-inj)/h	188Re-HAb18 F(ab’)2
		%ID·g-1(-x±s)	T/NT ratio
Tumor	1	3.01 ± 0.89	ND
	4	3.94 ± 0.82	ND
	18	3.43 ± 0.28	ND
	24	1.96 ± 0.43	ND
	48	0.99 ± 0.32	ND
Blood	1	4.58 ± 0.63	0.66
	4	1.83 ± 0.10	2.15
	18	0.21 ± 0.04	16.30
	24	0.18 ± 0.03	10.90
	48	0.05 ± 0.01	19.80
Heart	1	1.60 ± 0.38	1.88
	4	0.80 ± 0.10	4.92
	18	0.36 ± 0.03	9.53
	24	0.30 ± 0.02	6.53
	48	0.21 ± 0.03	4.71
Liver	1	2.07 ± 0.40	1.45
	4	1.57 ± 0.31	2.51
	18	0.77 ± 0.12	4.45
	24	0.66 ± 0.10	2.97
	48	0.47 ± 0.13	2.11
Spleen	1	1.22 ± 0.25	2.47
	4	0.91 ± 0.22	4.33
	18	0.47 ± 0.07	7.30
	24	0.45 ± 0.08	4.36
	48	0.41 ± 0.10	2.40
Lung	1	1.45 ± 0.23	2.08
	4	0.86 ± 0.29	4.58
	18	0.19 ± 0.04	18.10
	24	0.18 ± 0.04	10.90
	48	0.14 ± 0.05	7.07
Kidney	1	59.81 ± 14.52	0.05
	4	47.83 ± 12.87	0.08
	18	18.72 ± 4.94	0.18
	24	15.80 ± 0.99	0.12
	48	7.31 ± 2.10	0.13
Large	1	1.36 ± 0.38	2.21
intestine	4	0.93 ± 0.24	4.24
	18	0.57 ± 0.06	6.02
	24	0.45 ± 0.00	4.36
	48	0.18 ± 0.03	5.50
Small	1	1.61 ± 0.43	1.87
intestine	4	0.88 ± 0.29	4.24
	18	0.33 ± 0.05	10.40
	24	0.29 ± 0.05	6.76
	48	0.13 ± 0.05	7.62
Muscle	1	0.74 ± 0.29	4.07
	4	0.44 ± 0.12	8.95
	18	0.19 ± 0.08	18.10
	24	0.16 ± 0.06	12.25
	48	0.05 ± 0.02	19.80
Bone	1	1.03 ± 0.31	2.92
	4	0.68 ± 0.12	5.79
	18	0.31 ± 0.09	11.06
	24	0.27 ± 0.02	7.26
	48	0.16 ± 0.02	6.19

ND: not done

Table 2 Criteria for goodness of fitting for mean

REC No.	Mean No	WT	No. of camp	Weighted sum of squarers	R	R Squares	Goodness of fit	Max error C-CI	Max error %	AIC
1	1	1	1	0.672E-01	0.9993	0.9955	0.150	0.18	100.00	-9.499
2	1	1/c	1	0.329E+00	0.9856	0.9781	0.331	0.52	99.1	-1.560
3	1	1/cc	1	0.119E+01	0.9200	0.9207	0.630	3.58	78.2	4.877

Table 3 Pharmacokinetic parameters of ¹⁸⁸Re-HAb18 F(ab’)₂ in hepatoma-bearing nude mice

Parameter	Unit	Value	Standard error
C0	1 × 109 Bq·L-1	6.18	3.14E-01
Ke	h-1	0.30	2.88E-02
Vd	1 × 10-9 L·Bq-1	1.49
T1/2(Ke)	h	2.29
AUC	1 × 109 Bq·h·L-1	20.49
CL	1 × 10-3 L·h-1	0.45

CO: Concentration at zero time Ke: Elimination rate constant; Vd: Apparent volume of distribution T_1/2: Half-life time; AUC: Area under the curve CL: Clearance.

Table 4 Effect of various concentration of SnCl₂ and GH on free ¹⁸⁸ReO₄ amounts, colloid amounts and labeling efficiency

Concentration		188ReO-4	Colloid	Labelingfficiency(%)
aSnCl2 (g·L-1)	8	0.3	3.6	90.9
	4	0.4	2.8	90.1
	2	9.7	2.1	82.7
	1	21.8	1.2	71.2
bGH (mol·L-1)	0.8	1.1	1.1	91.7
	0.4	12.5	2.5	78.8
	0.2	16.6	2.8	72.7
	0.1	20.6	4.1	71.3

^aMolar ratio of 2-ME: F(ab’)₂ = 400:1,Concentration of GH = 0.5 mol·L^{-1 b}Molar ratio of 2-ME: F(ab’)₂ = 400:1,Concentration of SnCl₂ = 2 g·L^-1