Plasma Pharmacokinetic Parameters of Dexamethasone Following Administration of a Dexamethasone Intracanalicular Insert in Healthy Adults

Figures & data

Figure 1 The dexamethasone insert is placed in the punctum and into the canaliculus.

Table 1 Demographics and Clinical Characteristics

Age, years
Mean	31.7
Median (min, max)	27 (19, 55)
Gender, n (%)
Male	5 (31.3)
Female	11 (68.7)
Height, Inches
Mean	65.7
Median (min, max)	65 (59, 74)
Weight, pounds
Mean	143.4
Median (min, max)	145 (108, 170)
Body Mass Index, kg/m^2
Mean	23.4
Median (min, max)	23.5 (19.5, 26.3)
Race and Ethnicity, n (%)
Caucasian	7 (43.7)
African American	5 (31.3)
Hispanic	4 (25.0)

Table 2 Individual Dexamethasone Plasma Concentrations

Subject	Hours Post-Insertion						Days Post-Insertion
	0	1	2	4	8	16	2	4	8	15	22	29
1	0	0	0	0	0	0.08	0	0.06	0	0	0	0
2	0	0	0	0	0	0	0	0	0.19	0	ND	ND
3	0	0	0	0	0	0	0	0	0.08	0	0	0
4	0	0	0	0.81	0.06	0.08	0.06	0.05	0	0	0	0
5	0	0	0	0	0.05	0.05	0	0	0	0	0	0
6	0	0	0	0	0	0	0	0	0	0	0	0
7	0	0	0	0	0.08	0.05	0.07	0.08	0	0	0	0
8	0	0	0	0	0.05	0	0	0	0.05	0	0	0
9	0	0	0	0	0	0	0	0	0.1	0	0	0
10	0	0	0	0	0	0	0	0	0	0	0	0
11	0	0	0	0	0	0	0	0	0	0	0	0
12	0	0	0	0	0	0	0	0.08	0	0	0	0
13	0	0	0	0	0	0	0	0	0	0	0	0
14	0	0	0	0.06	0	0	0	0	0	0	0	0
15	0	0	0	0	0	0	0	0	0.12	0	ND	ND
16	0	0	0	0	0	0	0	0	ND	0	0	0

Notes: Drug concentrations expressed as ng/mL. Values of 0 indicate drug concentrations below the lower level of quantitation (0.05 ng/mL).

Abbreviation: ND, not done.

Table 3 Pharmacokinetic Parameter Results by Subject

Subject	Cmax (ng/mL)	AUC0-last (h∙ng/mL)	Tmax (Hours)
1	0.082	6.37	16.57
2	0.19	4.46	143.58
3	0.081	3.91	166.5
4	0.81	4.37	4.02
5	0.052	0.49	15.33
6	0	0	NC^a
7	0.078	6.34	8.02
8	0.053	7.18	142.3
9	0.1	3.61	139.87
10	0	0	NC^a
11	0	0	NC^a
12	0.083	3.31	103.88
13	0	0	NC^a
14	0.064	0.12	7.73
15	0.12	3.8	163.9
16	0	0	NC^a

Note: ^aNC, not calculated because drug concentrations were below the lower limit of quantification for these subjects.

Table 4 Changes in Intraocular Pressure^a

	Study Eye	Non-Study Eye
Screening
Mean, mm Hg (SD)	16.2 (1.4)	16.6 (2.0)
Median (min, max)	16.0 (14, 19)	17.0 (13, 20)
Day 2
Mean, mm Hg (SD)	16.1 (2.0)	15.8 (2.1)
Median (min, max)	16.0 (13, 20)	16.0 (12, 20)
Day 4
Mean, mm Hg (SD)	16.4 (3.1)	15.8 (3.2)
Median (min, max)	15.5 (12, 23)	15.0 (11, 23)
Day 8
Mean, mm Hg (SD)	17.2 (3.5)	15.1 (2.2)
Median (min, max)	16.5 (11, 27)	16.0 (11, 18)
Day 15
Mean, mm Hg (SD)	18.1 (5.1)	15.1 (2.2)
Median (min, max)	17.0 (13, 34)	15.0 (12, 19)
Day 22
Mean, mm Hg (SD)	19.3 (3.2)	16.4 (2.8)
Median (min, max)	18.0 (16, 28)	16.5 (13, 23)
Day 29
Mean, mm Hg (SD)	18.5 (4.1)	15.2 (2.8)
Median (min, max)	17.5 (14, 27)	14.0 (10, 20)

Notes: ^aSafety population, n=16.

Table 5 Changes in Best-Corrected Visual Acuity^a

	Study Eye	Non-Study Eye
Screening
Mean, logMAR (SD)	0.036 (0.14)	−0.001 (0.13)
Median (min, max)	0.03 (−0.18, 0.30)	0 (−0.20, 0.22)
Day 15
Mean, logMAR (SD)	0.087 (0.12)	−0.020 (0.14)
Median (min, max)	0.04 (0.0, 0.22)	−0.02 (−0.26, 0.24)
Day 29
Mean, logMAR (SD)	0.015 (0.15)	0.001 (0.12)
Median (min, max)	−0.02 (−0.16, 0.38)	0.0 (−0.20, 0.20)

Notes: ^aSafety population, n=16.