Novel polyvinylpyrrolidones to improve delivery of poorly-water soluble drugs; from design to synthesis and evaluation
Data(s) |
27/06/2012
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Resumo |
Polyvinylpyrrolidone is a widely used in tablet formulations with the linear form acting as a wetting agent and disintegrant whereas the cross-linked form is a super-disintegrant. 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 which have then be polymerized with vinylpyrrolidone to generate a suite of novel excipients with enhanced hydrogen-bonding capabilities. The polymers have a porous surface and swell in most common solvents and in water; properties which 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 storage. |
Formato |
text |
Identificador |
http://centaur.reading.ac.uk/28994/1/Mol%20Pharm%20manuscript%20for%20Centaur%20aug%202012.pdf Niemczyk, A. I., Williams, A. C. <http://centaur.reading.ac.uk/view/creators/90000834.html>, Rawlinson-Malone, C. F. <http://centaur.reading.ac.uk/view/creators/90000579.html>, Hayes, W. <http://centaur.reading.ac.uk/view/creators/90000315.html>, Greenland, B. <http://centaur.reading.ac.uk/view/creators/90000619.html>, Chappell, D. <http://centaur.reading.ac.uk/view/creators/90000971.html> and Khutoryanskaya, O. <http://centaur.reading.ac.uk/view/creators/90004478.html> (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 1543-8392 doi: 10.1021/mp300079x <http://dx.doi.org/10.1021/mp300079x> |
Idioma(s) |
en |
Publicador |
American Chemical Society |
Relação |
http://centaur.reading.ac.uk/28994/ creatorInternal Williams, Adrian C creatorInternal Rawlinson-Malone, Clare Frances creatorInternal Hayes, Wayne creatorInternal Greenland, Barny creatorInternal Chappell, David creatorInternal Khutoryanskaya, Olga 10.1021/mp300079x |
Tipo |
Article PeerReviewed |