Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers

Figures & data

Figure 1 Linear plot of mean plasma concentrations (μg/mL) versus time profile of diclofenac sodium for test and reference formulations in 10 obese (BMI > 25) male subjects under fasting conditions.

Abbreviations: SEM, standard error of mean; BMI, body mass index.

Table 1 Mean pharmacokinetic parameters in 10 obese male volunteers following intragluteal administration of the reference formulation (diclofenac sodium 75 mg/3 mL) and test formulation (diclofenac sodium 75 mg/1 mL)

Formulation A (reference)							Formulation B (test)
	Cmax (μg/mL)	Tmax (h)	AUC0–t (μg · h/mL)	AUC0–∞ (μg · h/mL)	t1/2 (h)	kel (h^−1)	Cmax (μg/mL)	Tmax (h)	AUC0–t (μg · h/mL)	AUC0–∞ (μg · h/mL)	t1/2 (h)	kel (h^−1)
Mean	0.93	1.08	2.73	3.75	5.93	0.12	1.30	0.50	2.71	3.71	6.30	0.11
SD	0.14	0.31	0.49	0.58	1.11	0.02	0.18	0.16	0.39	0.52	1.27	0.02
%CV	15.53	28.34	17.80	15.53	18.64	17.83	14.18	31.65	14.53	14.02	20.11	20.97

Abbreviations: C_max, maximum measured plasma concentration; T_max, time of maximum measured plasma concentration; AUC_0–t, area under the plasma concentration versus time curve from time zero to the last measurable concentration; AUC_0–∞, area under the plasma concentration versus time curve from zero to infinity; t _1/2, time required for the plasma drug concentration to decrease by one-half; k_el, apparent first order elimination or terminal rate constant; SD, standard deviation; %CV, coefficient of variation.

Table 2 Point estimate, 90% and 95% confidence intervals for the ratio of the product averages of test and reference formulations

Parameter	Point estimate test: Reference	90% confidence interval		95% confidence interval		P value
		Lower confidence limit	Upper confidence limit	Lower confidence limit	Upper confidence limit
Cmax	1.39	129.8	151.3	127.4	153.7	0.946
AUC0–t	0.993	94.6	104.4	93.5	105.7	0.135
AUC0–∞	0.989	92.9	106.08	91.5	107.8	0.193

Abbreviations: C_max, maximum measured plasma concentration; AUC_0–t, area under the plasma concentration versus time curve from time zero to the last measurable concentration; AUC_0–∞, area under the plasma concentration versus time curve from zero to infinity

Table 3 Summary statistics of diclofenac sodium in 10 obese adult subjects under fasting conditions

Parameters summary statistics	Product	Cmax	AUC0–t	AUC0–∞
		(μg/mL)	(μg · h/mL)	(μg · h/mL)
Geometric mean	Test	1.29	2.68	3.68
	Reference	0.92	2.69	3.71
LSM	Test	1.29	2.68	3.68
	Reference	0.92	2.69	3.71
LSM ratio B/A %		140.22	99.6	99.19
90% confidence interval: B/A
Lower limit		129.8	94.6	92.9
Upper limit		151.13	104.4	106.08
P value (ANOVA)
Period		>0.05	>0.05	>0.05
Formulation		>0.05	>0.05	>0.05
Sequence		>0.05	>0.05	>0.05
Intrasubject variability: %CV		9.18	5.92	7.95

Abbreviations: C_max, maximum measured plasma concentration; AUC_0–t, area under the plasma concentration versus time curve from time zero to the last measurable concentration; AUC_0–∞, area under the plasma concentration verses time curve from zero to infinity; LSM, least squares mean; A, reference product; B, test product; ANOVA, analysis of variance; B/A, bioavailability ratio test (B)/Reference (A); %CV, coefficient of variation.