| Oral Delivery of Ionic Complex of Ceftriaxone with Bile Acid Derivative in Non-human Primates. | |
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MedLine Citation:
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PMID: 23292220 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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PURPOSE: Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS: Several bile acid derivatives were screened by measuring water solubility and partition coefficient of their complexes with CTO. The pharmacokinetic parameters of the selected CTO/HDCK ionic complex in monkeys were evaluated. The absorption pathway of CTO/HDCK complex was evaluated using Caco-2 cells and MDCK cells transfected with ASBT gene. RESULTS: HDCK enhanced the apparent membrane permeability of CTO 5.8-fold in the parallel artificial membrane permeability assay model. CTO/HDCK complex permeated Caco-2 cell via transcellular pathway, and interaction of the HDCK complex with ASBT was important to enhance uptake. When CTO/HDCK (equivalent to 50 mg/kg of ceftriaxone) formulated with lactose, poloxamer 407 and Labrasol was orally administered to monkeys, its maximum plasma concentration was 19.5 ± 1.8 μg/ml and oral bioavailability 28.5 ± 3.1%. CONCLUSIONS: The CTO/HDCK formulation could enhance oral bioavailability of CTO in non-human primates. This oral formulation could be an alternative to injectable CTO with enhanced clinical effects. |
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Authors:
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Ok-Cheol Jeon; Seung Rim Hwang; Taslim A Al-Hilal; Jin Woo Park; Hyun Tae Moon; Seulki Lee; Jae Hyung Park; Youngro Byun |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2013-1-5 |
Journal Detail:
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Title: Pharmaceutical research Volume: - ISSN: 1573-904X ISO Abbreviation: Pharm. Res. Publication Date: 2013 Jan |
Date Detail:
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Created Date: 2013-1-7 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Polymer Science and Engineering, Sungkyunkwan University, Suwon, 440-746, South Korea. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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