A Randomized, Crossover, Pharmacokinetic and Adhesion Performance Study of a Lidocaine Topical System 1.8% During Physical Activity and Heat Treatment in Healthy Subjects

Figures & data

Table 1 Demographics and Baseline Characteristics

	N=12
Age, years, mean±SD (range)	46.17±15.94 (19–62)
Sex, n, M/F	3/9
Race, n, Black/White	1/11
BMI, kg/m^2 (mean±SD)	27.81±2.91

Abbreviations: SD, standard deviation; BMI, body mass index.

Table 2 Summary Statistics of Pharmacokinetic Parameters of Lidocaine Topical System 1.8% with Physical Exercise, Heating, and Normal Conditions

Statistics		Cmax (ng/mL)	AUC0–t (h·ng/mL)	AUC0–∞ (h·ng/mL)	AUC% Extrapolation	tmax* (h)	Kel (h^–1)	t½ (h)
Treatment A	N	12	12	12	12	12	12	12
	Mean	90.48	1328.81	1344.08	1.36	9.00	0.13	5.60
	SD	25.413	461.660	458.187	2.211	9.00–18.00	0.024	1.113
	CV (%)	28.1	34.7	34.1	162.3	30.0	18.9	19.9
Treatment B	N	12	12	12	12	12	12	12
	Mean	160.28	1718.71	1731.272	0.90	9.00	0.14	5.39
	SD	100.061	1004.005	1005.036	1.112	9.00–16.05	0.029	1.338
	CV (%)	62.4	58.4	58.1	124.0	21.2	21.5	24.8
Treatment C	N	12	12	12	12	12	12	12
	Mean	97.59	1487.39	1501.10	1.07	11.50	0.14	5.23
	SD	36.869	590.007	588.428	1.535	9.00–14.00	0.030	1.203
	CV (%)	37.8	39.7	39.2	143.2	18.9	21.5	23.0

Notes: *For t_max, median and range have been represented instead of mean and SD. Treatment A: with physical exercise; Treatment B: with heating; Treatment C: under normal conditions.

Abbreviations: SD, standard deviation; CV, coefficient of variation.

Table 3 Geometric Least Square Mean, Ratios, 90% Confidence Interval, ISCV and Power for Lidocaine Topical System 1.8% (in Transformed Data)

Parameter	Geometric Mean			Intra-Subject CV (%)	(A/C) Ratio, %	90% Confidence Intervals (A/C)	(B/C) Ratio, %	90% Confidence Intervals (B/C)
	A	Treatment B	C
Cmax, ng/mL	87.27	134.44	91.72	24.4	95.14	80.30–112.73	146.57	123.71–173.66
AUC0–t, h·ng/mL	1264.16	1513.10	1400.70	17.9	90.25	79.65–102.26	108.02	95.34–122.40
AUC0–∞, h·ng/mL	1281.92	1526.88	1416.04	17.4	90.53	80.15–102.25	107.83	95.46–121.79

Notes: Treatment A: with physical exercise; Treatment B: with heating; Treatment C: under normal conditions.

Abbreviations: ISCV, intrasubject coefficient of variation; CV, coefficient of variation.

Figure 1 Mean plasma lidocaine concentration after application of three lidocaine topical systems (1.8%; 108 mg) vs time with physical exercise, heat exposure, and under normal conditions. Treatment A: with physical exercise; Treatment B: with heating; Treatment C: under normal conditions.

Table 4 Summary Statistics of Adhesion Performance Evaluation of Lidocaine Topical System 1.8% with Physical Exercise, Heating, and Normal Conditions

Statistics	Treatment*	N	Minimum	Maximum	Mean	SD	CV (%)
Adhesion Score	A	12	0	2	0.33	0.389	116.8
	B	12	0	1	0.07	0.132	190.3
	C	12	0	0	0.00	0.000	0

Notes: *Treatment A: with physical exercise; Treatment B: with heating; Treatment C: under normal conditions.

Abbreviations: SD, standard deviation; CV, coefficient of variation.

Table 5 Summary of Adverse Events

Subject Number	Period Number	Treatment Received	Adverse Event	Severity	Related to Drug
S04	III	B	Head cold	Mild	Not related
S05	I	B	Headache	Moderate	Possibly related
				Mild	Possibly related
	II	C	Headache	Moderate	Possibly related
S09	I (Washout)	A	Menstrual cramps	Mild	Not related
S12	I	A	Light headedness secondary to exercise	Mild	Not related

Notes: Treatment A: with physical exercise; Treatment B: with heating; Treatment C: under normal conditions.