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Effects of Sodium Taurocholate on the Absorption of Inhaled 99mTc-DTPA

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Purpose

The effects of a natural surface-active agent, sodium taurocholate (NaTC), on the absorption of a hydrophilic solute, technetium-99m-labelled diethylene triamine pentaacetic acid (99mTc-DTPA), deposited at various sites within the airways were evaluated in this open, cross-over, and single-dose study.

Methods

Nine healthy non-smokers received 99mTc-DTPA with or without the addition of NaTC, administered as an oropharyngeal aerosol and as nebulized large and fine droplet-sized pulmonary aerosols delivered by Pari and UltraVent nebulizers inhaled at fairly rapid and slow flows, respectively. Plasma concentration versus time profiles and 24-h urinary excretion of radioactivity were assessed. Further, 99mTc-labelled human serum albumin nanocolloidal particles (99mTc-Nanocoll) were administered with or without NaTC by Pari and followed by repeated chest γ-imaging.

Results

NaTC changed no pharmacokinetic parameters for oropharyngeal 99mTc-DTPA. Independent of intrapulmonary 99mTc-DTPA deposition pattern, NaTC reduced T max (Pari: −0.8 h; UltraVent: −1.5 h) and mean absorption time (MAT) (−0.4 h; −0.7 h), and increased bioavailability (+13%; +44%) and dose-adjusted C max (+54%; +103%). NaTC decreased the pulmonary 99mTc-Nanocoll disappearance half-life from 8 h and 45 min to 4 h and 19 min.

Conclusions

Our findings suggest that NaTC increases both rate and extent of 99mTc-DTPA absorption throughout the lower airways, without changing 99mTc-DTPA absorption in the oral cavity.

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Abbreviations

DTPA:

diethylene triamine pentaacetic acid

ELF:

epithelial lining fluid

MCC:

mucociliary clearance

PI:

penetration index

99mTc:

technetium-99m

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Acknowledgments

We would like to thank biomedical laboratory technologists Birgit Andersson, Eva Jeremiasson, Anita Kvist, and Åsa Wickman for skilful contributions to the performance of this study.

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Authors and Affiliations

  1. AstraZeneca R&D Lund, SE-221 87, Lund, Sweden

    Eva Bondesson & Thomas Bengtsson

  2. Lund University, Department of Clinical Sciences, Malmö, Clinical Physiology and Nuclear Medicine Unit, Malmö University Hospital, SE-205 02, Malmö, Sweden

    Eva Bondesson, Lars-Erik Nilsson & Per Wollmer

Authors
  1. Eva Bondesson
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  2. Thomas Bengtsson
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  3. Lars-Erik Nilsson
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  4. Per Wollmer
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Correspondence to Eva Bondesson.

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Bondesson, E., Bengtsson, T., Nilsson, LE. et al. Effects of Sodium Taurocholate on the Absorption of Inhaled 99mTc-DTPA. Pharm Res 23, 2122–2128 (2006). https://doi.org/10.1007/s11095-006-9013-6

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  • DOI: https://doi.org/10.1007/s11095-006-9013-6

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