Trial Outcomes & Findings for Crossover, Single Dose, Two-stage Bioequivalence Study of SCMC-Lys Salt 1.35 g Powder vs SCMC-Lys Salt 90 mg/mL Syrup (NCT NCT02858193)

NCT ID: NCT02858193

Last Updated: 2024-11-18

Results Overview

Cmax = maximum plasma concentration. Cmax of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentrations of carbocysteine were measured in each study period at the timepoints hereunder reported. Arithmetic means+standard deviation are reported hereunder

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

30 participants

Primary outcome timeframe

pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Results posted on

2024-11-18

Participant Flow

30 healthy volunteers were randomized, receiving a single dose of test and reference treatment. Based on the cross-over design, a single dose of product was given orally in one of the two possible sequences: in the "test-reference" arm, subjects received SCMC-lys 1.35 g oral powder firstly and then the product Fluifort®. In the "reference-test" arm, subjects received reference product Fluifort® first, than SCMC-lys 1.35 g oral powder. A wash-out interval separated the 2 treatments.

Participant milestones

Participant milestones
Measure
Sequence "Test -Reference"
Participants first received a single oral dose of test product (1 sachet; 1.35 g of SCMC-lys) under fasting condition (day 1, Visit 3, 8:00 ± 1h ). After a wash-out period of at least 4 days the partecipants then received a single dose of the reference product Fluifort® syrup 90 mg SCMC-lys/mL (15 mL of syrup, 1.35 g of SCMC-lys) always under fasting conditions. There were no premature discontinuations during the study
Sequence "Reference - Test"
Participants first received a single oral dose of reference product Fluifort® syrup 90 mg SCMC-lys/mL (15 mL of syrup, 1.35 g of SCMC-lys) under fasting condition (day 1, Visit 3, 8:00 ± 1h ). After a wash-out period of at least 4 days the partecipants then received a single dose of the test product (1 sachet; 1.35 g of SCMC-lys) always under fasting conditions.
First Treatment Period
STARTED
15
15
First Treatment Period
COMPLETED
15
15
First Treatment Period
NOT COMPLETED
0
0
Washout Period (at Least 4 Days)
STARTED
15
15
Washout Period (at Least 4 Days)
COMPLETED
15
15
Washout Period (at Least 4 Days)
NOT COMPLETED
0
0
Second Treatment Period
STARTED
15
15
Second Treatment Period
COMPLETED
15
15
Second Treatment Period
NOT COMPLETED
0
0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Crossover, Single Dose, Two-stage Bioequivalence Study of SCMC-Lys Salt 1.35 g Powder vs SCMC-Lys Salt 90 mg/mL Syrup

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
All Study Partecipants
n=30 Participants
Enrolled population: all enrolled subjects. This analysis was used for the analysis of demographic, baseline and background characteristics. Safety population: all subjects who received at least one dose of investigational product.
Age, Categorical
<=18 years
0 Participants
n=93 Participants
Age, Categorical
Between 18 and 65 years
30 Participants
n=93 Participants
Age, Categorical
>=65 years
0 Participants
n=93 Participants
Age, Continuous
38.9 years
STANDARD_DEVIATION 10.6 • n=93 Participants
Sex: Female, Male
Female
12 Participants
n=93 Participants
Sex: Female, Male
Male
18 Participants
n=93 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=93 Participants
Race (NIH/OMB)
Asian
0 Participants
n=93 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=93 Participants
Race (NIH/OMB)
Black or African American
1 Participants
n=93 Participants
Race (NIH/OMB)
White
29 Participants
n=93 Participants
Race (NIH/OMB)
More than one race
0 Participants
n=93 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=93 Participants
Region of Enrollment
Switzerland
30 participants
n=93 Participants

PRIMARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results

Cmax = maximum plasma concentration. Cmax of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentrations of carbocysteine were measured in each study period at the timepoints hereunder reported. Arithmetic means+standard deviation are reported hereunder

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: Cmax
7.15 µg/mL
Standard Deviation 1.97
6.34 µg/mL
Standard Deviation 1.53

PRIMARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results

AUC0-t= area under the concentration-time curve from administration to the last observed concentration time t, calculated with the linear trapezoidal method. AUC0-t of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentration of carbocysteine were measured in each study period at the timepoints hereunder specified.Arithmetic means±standard deviation are reported hereunder Please note that AUC0-t was considered a reliable estimate of the extent of absorption if the ratio AUC0-t/AUC0-∞ equalled or exceeded a factor of 0.8, i.e. if %AUCextra was \<20%. Arithmetic means±standard deviation are reported hereunder

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: AUC0-t
26.73 µg/mL*h
Standard Deviation 5.95
24.36 µg/mL*h
Standard Deviation 5.35

SECONDARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results

AUC0-∞= Area under the concentration-time curve extrapolated to infinity, calculated, if feasible, as AUC0-t + Ct/λz, where Ct is the last measurable drug concentration. AUC0-∞of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentration of carbocysteine were measured in each study period at the timepoints hereunder specified. Arithmetic means±standard deviation are reported hereunder

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: AUC0-∞
27.23 µg/mLxh
Standard Deviation 6.06
24.85 µg/mLxh
Standard Deviation 5.52

SECONDARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results

Tmax = Time to achieve Cmax. Tmax (0-10hours) of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentration of carbocysteine were measured in each study period at the timepoints hereunder specified.

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: Tmax
1.72 h
Standard Deviation 0.43
1.85 h
Standard Deviation 0.60

SECONDARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results

t1/2= Half-life, calculated, if feasible, as ln2/λz. t1/2 (0-10 hours) of carbocysteine was calculated from plasma concentrations after single oral dose of test and reference products. Plasma concentration of carbocysteine were measured in each study period at the timepoints hereunder specified.

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: t1/2
1.51 h
Standard Deviation 0.24
1.50 h
Standard Deviation 0.21

SECONDARY outcome

Timeframe: pre-dose (0), 0.25 (15 min), 0.5 (30 min), 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 10 h post-dose

Population: PK population: all randomised subjects who fulfilled the study protocol requirements in terms of investigational medicinal product(s) intake and had evaluable PK data readouts for the planned treatment comparisons, with no major deviations that may affect the PK results µg/mL

Frel: Relative bioavailability, calculated as ratio AUC0-t (test)/ AUC0-t (reference)

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Carbocysteine Plasma PK Parameters: Frel
110.28 % of bioavailability
Standard Deviation 13.85

SECONDARY outcome

Timeframe: From the screening visit up to the final visit/ETV (i.e.up to 4 weeks)

Population: Safety population: all subject who received at least one dose of investigational product.

TEAE=Treatment Emergent Adverse Events. TEAEs were assessed throughout the study, from the screening to the final visit/early termination visit (ETV) which take place after visit 5 on day 1 of period 2, more precisely after the 10h blood sampling and vital sign.

Outcome measures

Outcome measures
Measure
SCMC-lys 1.35 g Oral Solution (Test Product)
n=30 Participants
SCMC-lys 1.35 g powder for oral solution in sachets each containing 1.35 g. One sachet of the powder of the test formulation 1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base was dissolved in 100 mL of hot (not boiling) still mineral water. Additional 100 mL of still mineral water at room temperature were added and mixed. The solution was swallowed and the glass was rinsed with 40 mL of still mineral water that was also drunk by the subjects. The final administered volume was 240 mL. All subjects were in fasting conditions from the evening before (at least 10 h, overnight). The final administered volume was 240 mL for both the test and reference treatments.
Fluifort® 90 mg/mL Syrup (Reference Product)
n=30 Participants
Fluifort® 90 mg/mL syrup (15 mL corresponding to 1.35 g SCMC-lys) Fifteen (15) mL of syrup (1.35 g of SCMC-lys corresponding to 750 mg of carbocysteine-free base) poured in a glass were drunk by the subjects. Afterward, the glass was rinsed twice with a volume of 100 mL and 125 mL of still mineral water and the rinses were drunk immediately by the subjects. The final administered volume was 240 mL for both the test and reference treatments.
Number of TEAEs
0 Number of events
0 Number of events

Adverse Events

SCMC-lys 1.35 g Oral Solution (Test Product)

Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths

Fluifort® 90 mg/mL Syrup (Reference Product)

Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Adverse event data not reported

Additional Information

Clinical Development & Operations

Dompé farmaceutici SpA

Phone: +39 02 583831

Results disclosure agreements

  • Principal investigator is a sponsor employee
  • Publication restrictions are in place