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RETRACTED ARTICLE

Oral delivery of low-molecular-weight heparin using sodium caprate as absorption enhancer reaches therapeutic levels.
J Drug Target 2005; 13(10):573-83JD

Abstract

The primary objective of this study was to evaluate sodium caprate as an oral penetration enhancer for low molecular weight heparin (LMWH), ardeparin. In vitro studies using Caco-2 cell monolayer indicated that 0.0625% of sodium caprate gave approximately 2-fold enhancement of ardeparin compared to negative control with almost 100% cell survival as evaluated by MTT cytotoxicity assay. In vivo studies in rats with ardeparin (1,200 IU/kg) and sodium caprate (100 mg/kg) led to a relative bioavailability of 27% with plasma anti-factor Xa levels within the therapeutic range (>0.2 IU/ml). Moreover, under these conditions, histological examination provided evidence that there was no damage to the gastrointestinal wall. Regional permeability studies using rat intestine indicated the colon as the region of maximum permeation. These results suggest that, at the dose administered, sodium caprate acts as a relatively safe and efficient absorption enhancer in the quest for alternatives for the oral delivery of LMWH.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, 79106, USA.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Retracted Publication

Language

eng

PubMed ID

16390818

Citation

Motlekar, Nusrat A., et al. "Oral Delivery of Low-molecular-weight Heparin Using Sodium Caprate as Absorption Enhancer Reaches Therapeutic Levels." Journal of Drug Targeting, vol. 13, no. 10, 2005, pp. 573-83.
Motlekar NA, Srivenugopal KS, Wachtel MS, et al. Oral delivery of low-molecular-weight heparin using sodium caprate as absorption enhancer reaches therapeutic levels. J Drug Target. 2005;13(10):573-83.
Motlekar, N. A., Srivenugopal, K. S., Wachtel, M. S., & Youan, B. B. (2005). Oral delivery of low-molecular-weight heparin using sodium caprate as absorption enhancer reaches therapeutic levels. Journal of Drug Targeting, 13(10), pp. 573-83.
Motlekar NA, et al. Oral Delivery of Low-molecular-weight Heparin Using Sodium Caprate as Absorption Enhancer Reaches Therapeutic Levels. J Drug Target. 2005;13(10):573-83. PubMed PMID: 16390818.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Oral delivery of low-molecular-weight heparin using sodium caprate as absorption enhancer reaches therapeutic levels. AU - Motlekar,Nusrat A, AU - Srivenugopal,Kalkunte S, AU - Wachtel,Mitchell S, AU - Youan,Bi-Botti C, PY - 2006/1/5/pubmed PY - 2006/2/14/medline PY - 2006/1/5/entrez SP - 573 EP - 83 JF - Journal of drug targeting JO - J Drug Target VL - 13 IS - 10 N2 - The primary objective of this study was to evaluate sodium caprate as an oral penetration enhancer for low molecular weight heparin (LMWH), ardeparin. In vitro studies using Caco-2 cell monolayer indicated that 0.0625% of sodium caprate gave approximately 2-fold enhancement of ardeparin compared to negative control with almost 100% cell survival as evaluated by MTT cytotoxicity assay. In vivo studies in rats with ardeparin (1,200 IU/kg) and sodium caprate (100 mg/kg) led to a relative bioavailability of 27% with plasma anti-factor Xa levels within the therapeutic range (>0.2 IU/ml). Moreover, under these conditions, histological examination provided evidence that there was no damage to the gastrointestinal wall. Regional permeability studies using rat intestine indicated the colon as the region of maximum permeation. These results suggest that, at the dose administered, sodium caprate acts as a relatively safe and efficient absorption enhancer in the quest for alternatives for the oral delivery of LMWH. SN - 1061-186X UR - https://www.unboundmedicine.com/medline/citation/16390818/Oral_delivery_of_low-molecular-weight_heparin_using_sodium_caprate_as_absorption_enhancer_reaches_therapeutic_levels L2 - http://www.tandfonline.com/doi/full/10.1080/10611860500471906 DB - PRIME DP - Unbound Medicine ER -