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Formulation and Evaluation of Irinotecan Suppository for Rectal Administration

Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbi...

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Autores principales: Feng, Haiyang, Zhu, Yuping, Li, Dechuan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Korean Society of Applied Pharmacology 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3936431/
https://www.ncbi.nlm.nih.gov/pubmed/24596626
http://dx.doi.org/10.4062/biomolther.2013.087
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author Feng, Haiyang
Zhu, Yuping
Li, Dechuan
author_facet Feng, Haiyang
Zhu, Yuping
Li, Dechuan
author_sort Feng, Haiyang
collection PubMed
description Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbits was investigated. Following a single intravenous dose of irinotecan (50 mg/kg), the plasma irinotecan concentration demonstrated a bi-exponential decay, with a rapid decline over 15 min. C(max), t(1/2), AUC(0–30h) and AUC(0-∞) were 16.1 ± 2.7 g/ml, 7.6 ± 1.2 h, 71.3 ± 8.8 μg·h/ml and 82.3 ± 9.5 μg·h/ml, respectively. Following rectal administration of 100 mg/kg irinotecan, the plasma irinotecan concentration reached a peak of 5.3 ± 2.5 μg/ml at 4 h. The AUC(0–30h) and AUC(0-∞) were 32.2 ± 6.2 μg·h/ml and 41.6 ± 7.2 μg·h/ml, respectively. It representing ∼50.6% of the absolute bioavailability.
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spelling pubmed-39364312014-03-04 Formulation and Evaluation of Irinotecan Suppository for Rectal Administration Feng, Haiyang Zhu, Yuping Li, Dechuan Biomol Ther (Seoul) Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbits was investigated. Following a single intravenous dose of irinotecan (50 mg/kg), the plasma irinotecan concentration demonstrated a bi-exponential decay, with a rapid decline over 15 min. C(max), t(1/2), AUC(0–30h) and AUC(0-∞) were 16.1 ± 2.7 g/ml, 7.6 ± 1.2 h, 71.3 ± 8.8 μg·h/ml and 82.3 ± 9.5 μg·h/ml, respectively. Following rectal administration of 100 mg/kg irinotecan, the plasma irinotecan concentration reached a peak of 5.3 ± 2.5 μg/ml at 4 h. The AUC(0–30h) and AUC(0-∞) were 32.2 ± 6.2 μg·h/ml and 41.6 ± 7.2 μg·h/ml, respectively. It representing ∼50.6% of the absolute bioavailability. The Korean Society of Applied Pharmacology 2014-01 /pmc/articles/PMC3936431/ /pubmed/24596626 http://dx.doi.org/10.4062/biomolther.2013.087 Text en Copyright © 2014 The Korean Society of Applied Pharmacology This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Feng, Haiyang
Zhu, Yuping
Li, Dechuan
Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title_full Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title_fullStr Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title_full_unstemmed Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title_short Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
title_sort formulation and evaluation of irinotecan suppository for rectal administration
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3936431/
https://www.ncbi.nlm.nih.gov/pubmed/24596626
http://dx.doi.org/10.4062/biomolther.2013.087
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