Telmisartan, Amlodipine and Combination in Healthy Subjects

A Single-centre, Randomized, Open-label, Three-period Crossover Pharmacokinetic Study of 80 mg Telmisartan / 5 mg Amlodipine Fixed Dose Combination Compared With Its Monocomponents in Healthy Chinese Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01181011

Enrollment

Registered

2010-08-13

Start date

2010-08-31

Completion date

Unknown

Last updated

2014-07-24

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

To determine the pharmacokinetic profile of 80 mg telmisartan / 5 mg amlodipine (T80/A5) dose combination after single dose in healthy Chinese subjects. To determine whether a pharmacokinetic interaction exists between telmisartan and amlodipine, following single doses of 80mg telmisartan (T80), and 5 mg amlodipine (A5) tablet alone and in combination, in healthy Chinese subjects. To evaluate the safety and tolerability of T80 and A5 alone and in combination in healthy Chinese subjects.

Interventions

DRUGamlodipine/telmisartan/combination

patient would take amlodipine(5mg)/telmisartan(80mg)/combination(T80+A5mg) single dose in random order, and each dosage will be separated in 21 days interval.

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

1. Healthy males and females 2. Aged between 18 and 45 years 3. Body weight more than 50Kg , and Body Mass Index (BMI ) between 19 and 24 kg/m2

Exclusion criteria

1. Any finding of the medical examination deviating from normal and of clinical relevance 2. Any evidence of a clinically relevant concomitant disease 3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders 4. Surgery of the gastrointestinal tract (except appendectomy) 5. Diseases of the central nervous system or psychiatric disorders or neurological disorders 6. History of relevant orthostatic hypotension, fainting spells or blackouts. 7. Chronic or relevant acute infections 8. History of relevant allergy/hypersensitivity (including allergy to drug or its excipients) 9. Intake of drugs with a long half-life (\> 24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial 10. Use of drugs which might reasonably influence the results of the trial 11. Participation in another trial with an investigational drug within two months prior to administration or during the trial 12. Smoker 13. Inability to refrain from smoking during 24 hours prior to dosing and during the trial 14. Alcohol abuse or inability to stop alcoholic beverages for 24 hours prior to dosing and during the trial 15. Drug abuse 16. Blood donation (more than 100 mL within four weeks prior to administration or during the trial) 17. Excessive physical activities (within one week prior to administration or during the trial) 18. Any laboratory value outside the reference range that is of clinical relevance 19. Inability to comply with dietary regimen of trial site 20. A history of additional risk factors for torsade de pointes 21. Any history of relevant low blood pressure 22. Supine blood pressure at screening of systolic \<110 mm Hg and diastolic \< 60 mm Hg 23. History of urticaria 24. History of angioneurotic edema 25 Pregnancy / positive pregnancy test, or planning to become pregnant during the study or within 1 month of study completion 26\. No adequate contraception during the study and until 1 month of study completion 27. Lactation period

Design outcomes

Primary

Measure	Time frame
Area Under the Concentration-time Curve of Telmisartan in Plasma Over the Time Interval From 0 to the Time of the Last Quantifiable Data Point (AUC_0-tz)	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs
Area Under the Plasma Concentration-time Curve From the Time of Dosing to Infinity (AUC_0-∞) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs
The Maximum Observed Plasma Concentration (Cmax) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs
AUC_0-tz of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs
AUC_0-∞ of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs
Cmax of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days of wash-outs

Secondary

Measure	Time frame	Description
Tmax of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
λz of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
MRT_po of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
t_½ of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Time to Attain Cmax (Tmax) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
V_z/F of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Number of Participants With at Least One Treatment Emergent Adverse Event	4 weeks	—
Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	4 weeks	—
CL/F of Amlodipine	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Terminal Rate Constant in Plasma (λz) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	reflect the speed of drug elimination in vivo
Mean Residence Time of Telmisartan in the Body After Oral Administration (MRT_po)	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Elimination Half-life (t_½) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Apparent Clearance of Telmisartan in Plasma Following Extravascular Administration (CL/F)	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—
Apparent Volume of Distribution During the Terminal Phase λz Following an Extravascular Administration (V_z/F) of Telmisartan	3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs	—

Countries

China

Participant flow

Participants by arm

Arm	Count
All Participants all patients will be assigned to 6 treatment sequences. cross-over design was adopted to ensure each patient would take amlodipine/telmisartan/combination single dose in randomized order	28
Total	28

Withdrawals & dropouts

Period	Reason	FG000
Overall Study	Adverse Event	2
Overall Study	Lost to Follow-up	1

Baseline characteristics

Characteristic	All Participants
Age, Continuous	24 Years STANDARD_DEVIATION 2
Sex: Female, Male Female	10 Participants
Sex: Female, Male Male	18 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk
deaths Total, all-cause mortality	— / —	— / —	— / —
other Total, other adverse events	2 / 27	1 / 27	3 / 26
serious Total, serious adverse events	0 / 27	0 / 27	0 / 26

Outcome results

Primary

Area Under the Concentration-time Curve of Telmisartan in Plasma Over the Time Interval From 0 to the Time of the Last Quantifiable Data Point (AUC_0-tz)

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for AUC\_0-tz of Telmisartan

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Area Under the Concentration-time Curve of Telmisartan in Plasma Over the Time Interval From 0 to the Time of the Last Quantifiable Data Point (AUC_0-tz)	3200 ng·h/mL	Geometric Coefficient of Variation 74.7
Telmisartan 80mg	Area Under the Concentration-time Curve of Telmisartan in Plasma Over the Time Interval From 0 to the Time of the Last Quantifiable Data Point (AUC_0-tz)	2940 ng·h/mL	Geometric Coefficient of Variation 94.4

p-value: 0.010790% CI: [99.45, 119.95]ANCOVA

Primary

Area Under the Plasma Concentration-time Curve From the Time of Dosing to Infinity (AUC_0-∞) of Telmisartan

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for AUC\_0-∞ of Telmisartan

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Area Under the Plasma Concentration-time Curve From the Time of Dosing to Infinity (AUC_0-∞) of Telmisartan	3420 ng·h/mL	Geometric Coefficient of Variation 82.5
Telmisartan 80mg	Area Under the Plasma Concentration-time Curve From the Time of Dosing to Infinity (AUC_0-∞) of Telmisartan	3140 ng·h/mL	Geometric Coefficient of Variation 98.5

p-value: 0.013990% CI: [99.96, 120.71]ANCOVA

Primary

AUC_0-∞ of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for AUC\_0-∞ of Amlodipine

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	AUC_0-∞ of Amlodipine	225 ng·h/mL	Geometric Coefficient of Variation 27.1
Telmisartan 80mg	AUC_0-∞ of Amlodipine	210 ng·h/mL	Geometric Coefficient of Variation 30.9

p-value: 0.000695% CI: [102.1, 116]ANCOVA

Primary

AUC_0-tz of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for AUC\_0-tz of Amlodipine

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	AUC_0-tz of Amlodipine	206 ng·h/mL	Geometric Coefficient of Variation 28.6
Telmisartan 80mg	AUC_0-tz of Amlodipine	192 ng·h/mL	Geometric Coefficient of Variation 31

p-value: 0.001190% CI: [102.87, 117.07]ANCOVA

Primary

Cmax of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days of wash-outs

Population: All patients with values for Cmax of Amlodipine

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Cmax of Amlodipine	4.72 ng/mL	Geometric Coefficient of Variation 21.7
Telmisartan 80mg	Cmax of Amlodipine	4.43 ng/mL	Geometric Coefficient of Variation 27.3

p-value: 090% CI: [100.9, 112.9]ANCOVA

Primary

The Maximum Observed Plasma Concentration (Cmax) of Telmisartan

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for Cmax of Telmisartan

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	The Maximum Observed Plasma Concentration (Cmax) of Telmisartan	461 ng/mL	Geometric Coefficient of Variation 59.9
Telmisartan 80mg	The Maximum Observed Plasma Concentration (Cmax) of Telmisartan	480 ng/mL	Geometric Coefficient of Variation 78.3

p-value: 0.012690% CI: [84.643, 112.472]ANCOVA

Secondary

Apparent Clearance of Telmisartan in Plasma Following Extravascular Administration (CL/F)

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for CL/F of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Apparent Clearance of Telmisartan in Plasma Following Extravascular Administration (CL/F)	31.0 L/h	Standard Deviation 21.6
Telmisartan 80mg	Apparent Clearance of Telmisartan in Plasma Following Extravascular Administration (CL/F)	37.3 L/h	Standard Deviation 39.7

Secondary

Apparent Volume of Distribution During the Terminal Phase λz Following an Extravascular Administration (V_z/F) of Telmisartan

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for V\_z/F of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Apparent Volume of Distribution During the Terminal Phase λz Following an Extravascular Administration (V_z/F) of Telmisartan	1021 L	Standard Deviation 697
Telmisartan 80mg	Apparent Volume of Distribution During the Terminal Phase λz Following an Extravascular Administration (V_z/F) of Telmisartan	1135 L	Standard Deviation 1018

Secondary

CL/F of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for CL/F of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	CL/F of Amlodipine	22.7 L/h	Standard Deviation 6.3
Telmisartan 80mg	CL/F of Amlodipine	25.1 L/h	Standard Deviation 7.9

Secondary

Elimination Half-life (t_½) of Telmisartan

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for t\_½ of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Elimination Half-life (t_½) of Telmisartan	27.0 h	Standard Deviation 13.7
Telmisartan 80mg	Elimination Half-life (t_½) of Telmisartan	25.0 h	Standard Deviation 10.7

Secondary

Mean Residence Time of Telmisartan in the Body After Oral Administration (MRT_po)

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for MRT\_po of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Mean Residence Time of Telmisartan in the Body After Oral Administration (MRT_po)	20.0 h	Standard Deviation 4.8
Telmisartan 80mg	Mean Residence Time of Telmisartan in the Body After Oral Administration (MRT_po)	18.4 h	Standard Deviation 5.7

Secondary

MRT_po of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for MRT\_po of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	MRT_po of Amlodipine	44.3 h	Standard Deviation 7
Telmisartan 80mg	MRT_po of Amlodipine	43.7 h	Standard Deviation 7.6

Secondary

Number of Participants With at Least One Treatment Emergent Adverse Event

Time frame: 4 weeks

Population: Treated set

Arm	Measure	Value (NUMBER)
Telmisartan 80mg, Amlodipine 5mg	Number of Participants With at Least One Treatment Emergent Adverse Event	4 Participants
Telmisartan 80mg	Number of Participants With at Least One Treatment Emergent Adverse Event	2 Participants
Amlodipine 5mg	Number of Participants With at Least One Treatment Emergent Adverse Event	4 Participants

Secondary

Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities

Time frame: 4 weeks

Population: Treated set

Arm	Measure	Group	Value (NUMBER)
Telmisartan 80mg, Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	ECG abnormalities	0 Participants
Telmisartan 80mg, Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Vital signs abnormalities	0 Participants
Telmisartan 80mg, Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Physical finding abnormalities	0 Participants
Telmisartan 80mg, Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Laboratory finding abnormalities	1 Participants
Telmisartan 80mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Laboratory finding abnormalities	1 Participants
Telmisartan 80mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	ECG abnormalities	0 Participants
Telmisartan 80mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Physical finding abnormalities	0 Participants
Telmisartan 80mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Vital signs abnormalities	0 Participants
Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Laboratory finding abnormalities	0 Participants
Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Vital signs abnormalities	0 Participants
Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	Physical finding abnormalities	0 Participants
Amlodipine 5mg	Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities	ECG abnormalities	0 Participants

Secondary

t_½ of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for t\_½ of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	t_½ of Amlodipine	38.8 h	Standard Deviation 7.6
Telmisartan 80mg	t_½ of Amlodipine	38.6 h	Standard Deviation 7.5

Secondary

Terminal Rate Constant in Plasma (λz) of Telmisartan

reflect the speed of drug elimination in vivo

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for λz of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Terminal Rate Constant in Plasma (λz) of Telmisartan	0.0305 1/h	Standard Deviation 0.0114
Telmisartan 80mg	Terminal Rate Constant in Plasma (λz) of Telmisartan	0.0323 1/h	Standard Deviation 0.0124

Secondary

Time to Attain Cmax (Tmax) of Telmisartan

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for tmax of Telmisartan

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Time to Attain Cmax (Tmax) of Telmisartan	1.22 h	Standard Deviation 0.58
Telmisartan 80mg	Time to Attain Cmax (Tmax) of Telmisartan	1.16 h	Standard Deviation 0.76

Secondary

Tmax of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for tmax of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	Tmax of Amlodipine	6.88 h	Standard Deviation 1.74
Telmisartan 80mg	Tmax of Amlodipine	7.20 h	Standard Deviation 1.63

Secondary

V_z/F of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for V\_z/F of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	V_z/F of Amlodipine	1241 L	Standard Deviation 313
Telmisartan 80mg	V_z/F of Amlodipine	1353 L	Standard Deviation 369

Secondary

λz of Amlodipine

Time frame: 3 periods of single-dose treatment (8 days of sampling) separated by 21 days wash-outs

Population: All patients with values for λz of Amlodipine

Arm	Measure	Value (MEAN)	Dispersion
Telmisartan 80mg, Amlodipine 5mg	λz of Amlodipine	0.0305 1/h	Standard Deviation 0.0114
Telmisartan 80mg	λz of Amlodipine	0.0323 1/h	Standard Deviation 0.0124

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026

Telmisartan, Amlodipine and Combination in Healthy Subjects

Conditions

Brief summary

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Area Under the Concentration-time Curve of Telmisartan in Plasma Over the Time Interval From 0 to the Time of the Last Quantifiable Data Point (AUC_0-tz)

Area Under the Plasma Concentration-time Curve From the Time of Dosing to Infinity (AUC_0-∞) of Telmisartan

AUC_0-∞ of Amlodipine

AUC_0-tz of Amlodipine

Cmax of Amlodipine

The Maximum Observed Plasma Concentration (Cmax) of Telmisartan

Apparent Clearance of Telmisartan in Plasma Following Extravascular Administration (CL/F)

Apparent Volume of Distribution During the Terminal Phase λz Following an Extravascular Administration (V_z/F) of Telmisartan

CL/F of Amlodipine

Elimination Half-life (t_½) of Telmisartan

Mean Residence Time of Telmisartan in the Body After Oral Administration (MRT_po)

MRT_po of Amlodipine

Number of Participants With at Least One Treatment Emergent Adverse Event

Number of Participants With Clinically Relevant Findings in Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities

t_½ of Amlodipine

Terminal Rate Constant in Plasma (λz) of Telmisartan

Time to Attain Cmax (Tmax) of Telmisartan

Tmax of Amlodipine

V_z/F of Amlodipine

λz of Amlodipine