Pharmaceutical and pharmacokinetic characterization of a novel sublingual buprenorphine/naloxone tablet formulation in healthy volunteers

Figures & data

Table 1. Subject disposition.

	OX219-003	OX219-005
No. of subjects screened	130	80
No. of subjects randomized	60	28
Treated with OX219	53	28
Treated with Suboxone tablet	60	–
Treated with Suboxone film	–	27
No. of subjects completed	53	27

Table 2. Demographic data (randomized subjects).

	OX219-003, (N = 60)	OX219-005, (N = 28)
Sex*
Male	46 (76.7%)	19 (67.9%)
Female	14 (23.3%)	9 (32.1%)
Age [years]†	36 (11.2)	30 (9.2)
Weight [kg]†	75.7 (11.4)	76.7 (13.16)
Height [cm]†	173 (9.3)	173 (8.6)
BMI [kg/m^2]†	25.2 (2.85)	25.4 (2.86)
Race*
White	23 (38.3%)	16 (57.1%)
American Indian or Alaskan Native	2 (3.3%)	0 (0.0%)
Asian	3 (5.0%)	0 (0.0%)
Black or African American	23 (38.3%)	12 (42.9%)
Native Hawaiian or other Pacific Islander	3 (5.0%)	0 (0.0%)
Other	6 (10.0%)	0 (0.0%)
Ethnicity*
Hispanic or Latino	9 (15.0%)	1 (3.6%)
Not Hispanic or Latino	51 (85.0%)	27 (96.4%)

*n (%); †mean (SD).

Figure 1. Mean plasma concentration versus time curves, Study OX219-003. Error bars represent 1 SD.

Figure 2. Sublingual dissolve time. *Study OX219-003; † Study OX219-005.

Table 3. Sublingual dissolve time, acceptability and preference results.

	OX219	Suboxone tablet	Suboxone film	p
Study OX219-003
Sublingual dissolve time [min]*	5 (1–38)	12.5 (4–41)	–	<0.0001
Acceptability†
Taste NRS¶	6.4 (2.63)	4.2 (2.51)	–	<0.0001
Overall acceptability NRS¶	6.5 (2.43)	5.2 (2.68)	–	0.0003
Preference‡
Overall preference	41 (77.4%)	12 (22.6%)	–	<0.0001
Study OX219-005
Sublingual dissolve time [min]*	2.88 (0.83–13.38)	–	2.88 (0.88–20.50)	0.232
Acceptability†
Taste VAS§	62 (27.0)	–	26 (22.7)	<0.0001
Mouthfeel VAS§	59 (25.5)	–	48 (23.1)	0.0384
Ease of administration VAS||	16 (18.0)	–	20 (19.5)	0.0873
Overall acceptability VAS§	65 (20.8)	–	40 (26.1)	0.0002
Unpleasant aftertaste‡
None	16 (57.1%)	–	2 (7.4%)	ND
Mild	8 (28.6%)	–	10 (37.0%)	ND
Moderate	3 (10.7%)	–	7 (25.9%)	ND
Strong	1 (3.6%)	–	8 (29.6%)	ND
Preference‡
Taste preference	26 (96.3%)	–	1 (3.7%)	<0.0001
Mouthfeel preference	22 (81.5%)	–	5 (18.5%)	0.0011
Ease of drug adm. preference	24 (88.9%)	–	3 (11.1%)	<0.0001
Overall preference	24 (88.9%)	–	3 (11.1%)	<0.0001

*Median (min–max); †Mean (SD); ‡n (%); ND = “Not done”; ¶1 = “Extremely unpleasant”; 10 = “Extremely pleasant”; §0 mm = “Extremely unpleasant”; 100 mm = “Extremely pleasant”; ||0 mm = “Extremely easy”; 100 mm = “Extremely difficult.”

Figure 3. Distribution of acceptability ratings, *1 = “Extremely unpleasant”; 10 = “Extremely pleasant”; †0 mm = “Extremely unpleasant”; 100 mm = “Extremely pleasant”; ‡0 mm = “Extremely easy”; 100 mm = “Extremely difficult”.