Optimizing bioavailability of oral administration of small peptides through pharmacokinetic and pharmacodynamic parameters: the effect of water and timing of meal intake on oral delivery of Salmon Calcitonin.

Karsdal MA, Byrjalsen I, Riis BJ, Christiansen C

BMC clinical pharmacology9 Sept 2008Cited by 49 (Europe PMC)

PMID18782439PMCIDPMC2551583DOI10.1186/1472-6904-8-5PepBankPUB-18782439

Summary

BackgroundTo investigate the influence of water intake and dose timing on the pharmacokinetic and pharmacodynamic parameters of an oral formulation of salmon calcitonin (sCT).MethodsThe study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study. 56 healthy postmenopausal women were randomly assigned to receive five treatments. The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray), water volume given with the tablet (50 or 200 ml water), and time between dosing and meal (10, 30, or 60 minutes pre-meal). Plasma sCT levels and changes in the bone resorption (C-terminal telopeptide of collagen type I) was investigated. Trial regristration.ResultsOral delivery of 0.8 mg of sCT with 50 ml of water compared to that with 200 ml water resulted in a two-fold increase in maximum concentration (Cmax and AUC0-4) of plasma sCT but comparable time to reach maximum concentration (Tmax). The sCT AUC0-4 with 50 ml of water was 4-fold higher than that obtained with nasal calcitonin. The increased absorption of sCT resulted in increased efficacy demonstrated by AUC of the relative change of serum CTX-I measured in the 6 hours post dosing.Conclusion0.8 mg sCT with 50 ml of water taken 30 and 60 minutes prior to meal time resulted in optimal pharmacodynamic and pharmacokinetic parameters. The data suggest that this novel oral formulation may have improved absorption and reduction of bone resorption compared to that of the nasal form.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study5

5 results from studies that gave the peptide. 5 results from people.

01HumanRandomized controlled trialPharmacokinetics
In healthy postmenopausal women, oral salmon calcitonin with 50 ml water doubled Cmax compared with 200 ml water.
In plain wordsIn postmenopausal women, salmon calcitonin with 50 ml water doubled peak blood concentration compared with 200 ml water.
Peptide
Calcitonin-salmon
Outcome
IncreaseCmax by water volume
Study
n: not reported in source
Comparator
200 ml water
Analysis
Exploratory
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg · oralAs given in this study (human).
Measurements
Cmax fold change
2 fold
50 ml versus 200 ml water
Source sentences
Summary
Oral delivery of 0.8 mg of sCT with 50 ml of water compared to that with 200 ml water resulted in a two-fold increase in maximum concentration (Cmax and AUC0-4) of plasma sCT but comparable time to reach maximum concentration (Tmax).
3 context sentences(design, population, supporting numbers)
Summary · context
The study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study.
Summary · context
56 healthy postmenopausal women were randomly assigned to receive five treatments.
Summary · context
The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray)
Show in the study text Report a problemFND-1878243901
02HumanRandomized controlled trialPharmacokinetics
In healthy postmenopausal women, oral salmon calcitonin with 50 ml water doubled AUC0-4 compared with 200 ml water.
In plain wordsIn postmenopausal women, salmon calcitonin exposure doubled with 50 ml water compared with 200 ml water.
Peptide
Calcitonin-salmon
Outcome
IncreaseAUC by water volume
Study
n: not reported in source
Comparator
200 ml water
Analysis
Exploratory
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg · oralAs given in this study (human).
Measurements
AUC0-4 fold change
2 fold
50 ml versus 200 ml water
Source sentences
Summary
Oral delivery of 0.8 mg of sCT with 50 ml of water compared to that with 200 ml water resulted in a two-fold increase in maximum concentration (Cmax and AUC0-4) of plasma sCT but comparable time to reach maximum concentration (Tmax).
3 context sentences(design, population, supporting numbers)
Summary · context
The study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study.
Summary · context
56 healthy postmenopausal women were randomly assigned to receive five treatments.
Summary · context
The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray)
Show in the study text Report a problemFND-1878243902
03HumanRandomized controlled trialPharmacokinetics
In healthy postmenopausal women, salmon calcitonin Tmax was comparable with 50 and 200 ml water.
In plain wordsIn postmenopausal women, salmon calcitonin reached peak concentration at comparable times with 50 and 200 ml water.
Peptide
Calcitonin-salmon
Outcome
Direction not reportedTmax by water volume
Study
n: not reported in source
Comparator
200 ml water
Analysis
Exploratory
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg · oralAs given in this study (human).
Source sentences
Summary
Oral delivery of 0.8 mg of sCT with 50 ml of water compared to that with 200 ml water resulted in a two-fold increase in maximum concentration (Cmax and AUC0-4) of plasma sCT but comparable time to reach maximum concentration (Tmax).
3 context sentences(design, population, supporting numbers)
Summary · context
The study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study.
Summary · context
56 healthy postmenopausal women were randomly assigned to receive five treatments.
Summary · context
The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray)
Show in the study text Report a problemFND-1878243903
04HumanRandomized controlled trialPharmacokinetics
In healthy postmenopausal women, oral salmon calcitonin with 50 ml water produced 4-fold higher AUC0-4 than nasal calcitonin.
In plain wordsIn postmenopausal women, oral salmon calcitonin with 50 ml water produced 4-fold higher exposure than nasal calcitonin.
Peptide
Calcitonin-salmon
Outcome
IncreaseAUC versus nasal calcitonin
Study
n: not reported in source
Comparator
Nasal calcitonin
Analysis
Exploratory
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg · oralAs given in this study (human).
Measurements
AUC0-4 fold change
4 fold
oral with 50 ml water versus nasal calcitonin
Source sentences
Summary
The sCT AUC0-4 with 50 ml of water was 4-fold higher than that obtained with nasal calcitonin.
3 context sentences(design, population, supporting numbers)
Summary · context
The study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study.
Summary · context
56 healthy postmenopausal women were randomly assigned to receive five treatments.
Summary · context
The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray)
Show in the study text Report a problemFND-1878243904
05HumanRandomized controlled trialEfficacy outcome
In healthy postmenopausal women, increased salmon calcitonin absorption accompanied increased efficacy measured by serum CTX-I response AUC over 6 hours.
In plain wordsIn postmenopausal women, increased salmon calcitonin absorption accompanied a greater effect on a bone resorption marker.
Peptide
Calcitonin-salmon
Outcome
Direction not reportedSerum CTX-I response AUC
Study
n: not reported in source
Analysis
Exploratory
Outcome group
Bone and joint · Musculoskeletal
Studied dose
0.8 mg · oralAs given in this study (human).
Source sentences
Summary
The increased absorption of sCT resulted in increased efficacy demonstrated by AUC of the relative change of serum CTX-I measured in the 6 hours post dosing.
3 context sentences(design, population, supporting numbers)
Summary · context
The study was a randomized, partially-blind, placebo-controlled, single dose, exploratory crossover phase I study.
Summary · context
56 healthy postmenopausal women were randomly assigned to receive five treatments.
Summary · context
The treatments comprised a combination of study medication (SMC021 (0.8 mg sCT + 200 mg 5-CNAC), SMC021 placebo, or 200 IU Miacalcic NS nasal spray)
Show in the study text Report a problemFND-1878243905

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

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Version 2Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:35 UTC
First added · source update from Europe PMC

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