The impact of polymeric excipients on the particle size of poorly soluble drugs after pH-induced precipitation
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F16%3A43902088" target="_blank" >RIV/60461373:22340/16:43902088 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.ejps.2016.08.028" target="_blank" >http://dx.doi.org/10.1016/j.ejps.2016.08.028</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejps.2016.08.028" target="_blank" >10.1016/j.ejps.2016.08.028</a>
Alternative languages
Result language
angličtina
Original language name
The impact of polymeric excipients on the particle size of poorly soluble drugs after pH-induced precipitation
Original language description
Active pharmaceutical ingredients (APIs) with strongly pH-dependent aqueous solubility can face the problem of precipitating from solution when the pH changes from acidic in the stomach to neutral in the intestine. The present work investigates the effect of two polymeric excipients ? polyvinylpyrrolidone (PVP) and Soluplus ? on the ability to either prevent precipitation, or to control the size distribution of precipitated particles when precipitation cannot be prevented. Two different APIs were compared, Dabigatran etexilate mesylate and Rilpivirine hydrochloride. The effect of excipient concentration on the precipitation behaviour during pH titration was systematically investigated and qualitatively different trends were observed: in case of Soluplus, which forms a micellar solution when critical micelle concentration is exceeded, precipitation was inhibited in the case of Dabigatran etexilate, which partitioned into the micelles. On the other hand, Rilpivirine precipitated independently of Soluplus concentration. In the case of PVP, which does not form micelles, precipitation could not be avoided. Increased polymer concentration, however prevented the aggregation of precipitated particles into larger cluster. The observed effect of PVP was especially pronounced for Rilpivirine. The main conclusion of this study is that a suitably chosen polymeric excipient can either prevent precipitation altogether or reduce the size of the resulting particles. The mechanism of action, however, seems-specific to a given molecule. It was also shown that the polymer-stabilised particles have a potential to redissolve. ? 2016 Elsevier B.V.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CI - Industrial chemistry and chemical engineering
OECD FORD branch
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Result continuities
Project
<a href="/en/project/GA13-37055S" target="_blank" >GA13-37055S: Remote Control of Adhesion and Reaction-Diffusion Process in Structured Microparticles</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach
Others
Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
European Journal of Pharmaceutical Sciences
ISSN
0928-0987
e-ISSN
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Volume of the periodical
95
Issue of the periodical within the volume
December 2016
Country of publishing house
US - UNITED STATES
Number of pages
7
Pages from-to
138-144
UT code for WoS article
000390505100017
EID of the result in the Scopus database
2-s2.0-84994246973