Impact of Bile Salts on Solution Crystal Growth Rate and Residual Supersaturation of an Active Pharmaceutical Ingredient
Rattachement africain : us, gb. Niveau de preuve : code pays fourni par la source.
Le résumé fourni par la source
Supersaturating formulations have become a popular approach to address the issue of inadequate aqueous solubility for small molecules. Given that prevention of nucleation may not be always possible, it is of particular interest to control crystal growth from supersaturated solutions in order to maximize the extent of oral absorption of therapeutic agents. Bile salts are endogenous surfactants that are present in biorelevant dissolution media and can have direct impact on the in vivo performance of therapeutic agents due to their presence in the gastrointestinal tract. In this study, an in situ common history seeding method was implemented to provide seeds that better mimic crystals formed from aqueous supersaturated solutions. By forming seeds in situ and then regenerating supersaturation, we were able to probe the influence of biorelevant bile salts on telaprevir crystal growth rates and secondary nucleation. The extent of growth inhibition was found to vary with bile salt chemistry and aggregation level. It was also noted that sodium taurocholate and sodium taurochenodeoxycholate inhibited secondary nucleation of telaprevir from highly supersaturated solutions. The impact of bile salts on crystal growth and secondary nucleation is of relevance for improved understanding of precipitation kinetics of supersaturating dosage forms.
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Le contrôle bibliographique ouvert
DOI retrouvé dans Crossref DOI retrouvé ; titre concordant.
- Titre Crossref
- Impact of Bile Salts on Solution Crystal Growth Rate and Residual Supersaturation of an Active Pharmaceutical Ingredient
- Date Crossref
- 18/05/2017
- Éditeur
- American Chemical Society (ACS)
- Type
- journal-article
Ce recoupement confirme des métadonnées liées au DOI. Il ne confirme ni la méthode ni les conclusions de l’étude, et il ne compte pas comme une seconde source scientifique indépendante.
Où se fait cette recherche
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Inc. Merck & Co. pays non établi dans la noticeEntreprise
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United States Military Academy pays non établi dans la noticeUniversité ou école supérieure
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Purdue University West Lafayette Department of Industrial and Physical Pharmacy pays non établi dans la noticeUniversité ou école supérieure
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University of Sheffield Department of Chemical and Biological Engineering pays non établi dans la noticeUniversité ou école supérieure
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† School of Chemical Engineering and ∇ Department of Industrial and Physical Pharmacy pays non établi dans la noticeUniversité ou école supérieure
Merck & Co. — Inc., United States Military Academy et Department of Industrial and Physical Pharmacy — Purdue University West Lafayette, avec 2 autres affiliations.
Une affiliation ne permet pas de déduire la nationalité d’un auteur.