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Penetration of minocycline hydrochloride into lung tissue and sputum
A Watanabe1, Y Anzai, K Niitsuma
1Department of Respiratory Oncology and Molecular Medicine, Institute of Development, Aging and Cancer, Tohoku University, Sendai, Japan.
Abstract:
Penetration of minocycline hydrochloride (MINO) into lung tissue and sputum was investigated. MINO (100 mg) was intravenously infused over 30 min to 14 patients before lung surgery: the concentration of MINO was determined in 16 lung tissue samples which were collected between 0.25 and 5.0 h after infusion. The mean concentration of MINO in lung tissue sample was 2.92 +/- 1.43 microg/g, and the mean lung tissue/plasma ratio of MINO concentration was 3.71 +/- 2.36. MINO was infused intravenously over 60 min twice daily to 5 patients with a chronic respiratory disease for 3-7 days. The concentration of MINO in sputum and in serum was determined on day 3. The mean maximum concentration of MINO in sputum sample was 2.12 +/- 2.20 microg/g, and the mean sputum/serum ratio of MINO concentration was 0.56 +/- 0.47. The concentration of MINO in sputum showed little time-related variation and remained as high as 0.74 microg/g until 10 h after infusion. The concentration of MINO in sputum and in serum after intravenous drip infusion was about twice as high as that after oral administration at the same dose. The breakpoint was 1.88 for MINO, as calculated by the formula established by the Japan Society of Chemotherapy.
Insights
Minocycline hydrochloride (MINO) effectively penetrates lung tissue and sputum, achieving higher concentrations via intravenous infusion compared to oral administration. This antibiotic demonstrates significant therapeutic potential for respiratory infections.
Area of Science:
- Pharmacology
- Respiratory Medicine
- Infectious Diseases
Background:
- Minocycline hydrochloride (MINO) is an antibiotic with potential applications in treating respiratory infections.
- Understanding drug penetration into lung tissue and sputum is crucial for optimizing antimicrobial therapy.
Purpose of the Study:
- To investigate the penetration of minocycline hydrochloride into lung tissue and sputum.
- To compare the pharmacokinetic profile of intravenous versus oral minocycline administration in respiratory patients.
Main Methods:
- Intravenous infusion of 100 mg minocycline hydrochloride in 14 patients undergoing lung surgery.
- Analysis of minocycline concentrations in lung tissue samples collected at various time points post-infusion.
- Intravenous infusion of minocycline hydrochloride in 5 patients with chronic respiratory disease, with subsequent analysis of sputum and serum concentrations.
Main Results:
- Mean minocycline concentration in lung tissue was 2.92 ± 1.43 µg/g, with a lung tissue/plasma ratio of 3.71 ± 2.36.
- Mean maximum minocycline concentration in sputum was 2.12 ± 2.20 µg/g, with a sputum/serum ratio of 0.56 ± 0.47.
- Intravenous administration resulted in approximately double the sputum and serum concentrations compared to oral administration.
Conclusions:
- Minocycline hydrochloride demonstrates good penetration into lung tissue and sputum.
- Intravenous administration of minocycline hydrochloride leads to higher drug concentrations in sputum and serum compared to oral administration.
- These findings support the potential efficacy of minocycline hydrochloride in treating respiratory tract infections.