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Pharmaceutics 2018, 10(3), 78; https://doi.org/10.3390/pharmaceutics10030078

Development and Evaluation of Raloxifene-Hydrochloride-Loaded Supersaturatable SMEDDS Containing an Acidifier

1
DMPK Group, Korea Institute of Toxicology, Daejeon 305-343, Korea
2
Pharvis R&D Department, Pharvis Korea Pharm., Ansan 425-100, Korea
3
Department of Pharmaceutics & Biotechnology, Konyang University, Daejeon 302-832, Korea
4
Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon 305-343, Korea
*
Author to whom correspondence should be addressed.
Received: 20 May 2018 / Revised: 25 June 2018 / Accepted: 26 June 2018 / Published: 29 June 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
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Abstract

Raloxifene hydrochloride (RLH) was formulated into a pH-modified supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) to increase drug solubility and dissolution rate. Optimal formulations of pH-modified S-SMEDDSs were developed by incorporating hydroxypropyl-cellulose-L as a precipitation inhibitor and phosphoric acid as a pH modifier (an acidifier). RLH was dissolved to greater extents by all pH-modified S-SMEDDSs compared with non-pH-modified S-SMEDDSs. In particular, phosphoric acid afforded greater drug dissolution than did the other acidifiers tested, perhaps because phosphoric acid better controlled the pH. More than 50% of the RLH was released from the pH-modified S-SMEDDS at pH 2.5 compared with only ~5% of the drug into aqueous buffer (pH 1.2 or 6.8) after dissolution of a conventional tablet. pH-modified S-SMEDDSs with a hydrophilic polymer and phosphoric acid improved the dissolution behavior of a drug exhibiting poor aqueous solubility. View Full-Text
Keywords: raloxifene; supersaturatable self-microemulsifying drug delivery system; microemulsion; solubility raloxifene; supersaturatable self-microemulsifying drug delivery system; microemulsion; solubility
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Lee, J.-H.; Kim, H.H.; Cho, Y.H.; Koo, T.-S.; Lee, G.W. Development and Evaluation of Raloxifene-Hydrochloride-Loaded Supersaturatable SMEDDS Containing an Acidifier. Pharmaceutics 2018, 10, 78.

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