Literature DB >> 29352911

HPMCAS as an effective precipitation inhibitor in amorphous solid dispersions of the poorly soluble drug candesartan cilexetil.

Juliana Munari Oliveira Pinto1, Aline Franciane Leão1, Manoela Klüppel Riekes1, Maria Terezinha França1, Hellen Karine Stulzer2.   

Abstract

Among the strategies to improve the biopharmaceutic properties of poorly soluble drugs, Supersaturating Drug Delivery Systems like polymer-based amorphous solid dispersions (SD) have been successfully applied. The screening of appropriate polymeric carriers to compose SD is a crucial point on their development. In this study, hydroxypropylmethylcellulose (HPMC), hydroxypropylmethylcellulose acetate succinate (HPMCAS) types L, M and H and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SOL) were evaluated by in vitro supersaturation studies regarding their anti-precipitant ability on the poorly soluble drug candesartan cilexetil (CC) under two different media, including biorelevant conditions. According to the results, HPMCAS M was considered the best carrier to develop SD containing CC among all the polymers tested, due to its good anti-precipitant performance in both media. In addition, the medium used in the in vitro supersaturation studies played an important role on the results, and its selection should be carefully done.
Copyright © 2017. Published by Elsevier Ltd.

Entities:  

Keywords:  Biorelevant medium; Candesartan cilexetil; Hydroxypropylmethylcellulose acetate succinate; In vitro supersaturation study; Supersaturating drug delivery systems

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Substances:

Year:  2017        PMID: 29352911     DOI: 10.1016/j.carbpol.2017.12.052

Source DB:  PubMed          Journal:  Carbohydr Polym        ISSN: 0144-8617            Impact factor:   9.381


  4 in total

1.  Hypromellose acetate succinate based amorphous solid dispersions via hot melt extrusion: Effect of drug physicochemical properties.

Authors:  Sandeep Sarabu; Venkata Raman Kallakunta; Suresh Bandari; Amol Batra; Vivian Bi; Thomas Durig; Feng Zhang; Michael A Repka
Journal:  Carbohydr Polym       Date:  2020-01-10       Impact factor: 9.381

2.  Dual mechanism of microenvironmental pH modulation and foam melt extrusion to enhance performance of HPMCAS based amorphous solid dispersion.

Authors:  Anh Q Vo; Xin Feng; Jiaxiang Zhang; Feng Zhang; Michael A Repka
Journal:  Int J Pharm       Date:  2018-08-21       Impact factor: 5.875

3.  Hot-melt extruded hydroxypropyl methylcellulose acetate succinate based amorphous solid dispersions: Impact of polymeric combinations on supersaturation kinetics and dissolution performance.

Authors:  Arun Butreddy; Sandeep Sarabu; Mashan Almutairi; Srinivas Ajjarapu; Praveen Kolimi; Suresh Bandari; Michael A Repka
Journal:  Int J Pharm       Date:  2022-01-15       Impact factor: 6.510

4.  Improved Dissolution and Pharmacokinetics of Abiraterone through KinetiSol® Enabled Amorphous Solid Dispersions.

Authors:  Urvi Gala; Dave Miller; Robert O Williams
Journal:  Pharmaceutics       Date:  2020-04-14       Impact factor: 6.321

  4 in total

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