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Effect of chloride ion on solubility and dissolution of a basic drug and salt form for oral delivery
RISE - Research Institutes of Sweden, Bioscience and Materials, Surface, Process and Formulation.
RISE - Research Institutes of Sweden, Bioscience and Materials, Surface, Process and Formulation. (Bioscience and Materials)ORCID iD: 0000-0003-3401-0728
RISE - Research Institutes of Sweden, Bioscience and Materials, Surface, Process and Formulation.
KI Karolinska Institute, Sweden.
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2018 (English)Conference paper, Poster (with or without abstract) (Other academic)
Abstract [en]

Introduction:

Chloride ions are the predominant anionic counter-ion present in vivo (intestine/ jejunum: 0.13M and stomach: 0.10M), significantly effecting solubility and dissolution of drugs for oral absorption1. Our group has recently discovered a novel small molecule, with good permeability but low aqueous solubility potentially limiting exposure after oral administration. It is a basic compound (pKa- 6-7) and provides opportunities to develop salt exploiting different counter-ions. Solubility is not only dependent on the ionization of the weak acid or weak base itself but also on the solubility of the counter ion pairs. Counter ion exchanges between salt forms or formation of hydrates is well known to occur in the gastrointestinal environment. If this happens, then formation of less soluble species can lead to in vivo precipitation of the drug.

Place, publisher, year, edition, pages
2018.
National Category
Basic Medicine
Identifiers
URN: urn:nbn:se:ri:diva-36479OAI: oai:DiVA.org:ri-36479DiVA, id: diva2:1265173
Conference
11th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology
Available from: 2018-11-22 Created: 2018-11-22 Last updated: 2018-12-06Bibliographically approved

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Schipper, Nicolaas

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