Novel polyvinylpyrrolidones to improve delivery of poorly water- soluble drugs: from design to synthesis and evaluation

Niemczyk, Anna I, Williams, Adrian C, Rawlinson-Malone, Clare F, Hayes, Wayne, Greenland, Barnaby W, Chappell, David, Khutoryanskaya, Olga and Timmins, Peter (2012) Novel polyvinylpyrrolidones to improve delivery of poorly water- soluble drugs: from design to synthesis and evaluation. Molecular Pharmaceutics, 9 (8). pp. 2237-2247. ISSN 1543-8384

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Official URL: 10.1021/mp300079x

Abstract

Polyvinylpyrrolidone is widely used in tablet formulations with the linear form acting as a wetting agent and disintegrant, whereas the cross-linked form is a superdisintegrant. We have previously reported that simply mixing the commercial cross-linked polymer with ibuprofen disrupted drug crystallinity with consequent improvements in drug dissolution behavior. In this study, we have designed and synthesized novel cross-linking agents containing a range of oligoether moieties that have then been polymerized with vinylpyrrolidone to generate a suite of novel excipients with enhanced hydrogen-bonding capabilities. The polymers have a porous surface and swell in the most common solvents and in water, properties that suggest their value as disintegrants. The polymers were evaluated in simple physical mixtures with ibuprofen as a model poorly water-soluble drug. The results show that the novel PVPs induce the drug to become “X-ray amorphous”, which increased dissolution to a greater extent than that seen with commercial cross-linked PVP. The polymers stabilize the amorphous drug with no evidence for recrystallization seen after 20 weeks of storage.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Barnaby Greenland
Date Deposited: 12 Apr 2018 13:40
Last Modified: 12 Apr 2018 13:40
URI: http://sro.sussex.ac.uk/id/eprint/75050

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