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Spray-dried solid dispersions of nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for compacted oral formulations.
Int J Pharm. 2015 Mar 15; 481(1-2):140-7.IJ

Abstract

The aim of this work was to investigate an alternative processing technology for a new polymeric solubilizer used mainly in hot melt extrusion. Poorly soluble nifedipine was co-processed through spray-drying with poly(vinyl caprolactam-co-vinyl acetate-co-ethylene glycol) (PVCVAEG) in different ratios. The resulting spray-dried powders were formulated and compacted into tablets forms. Spray drying produced reduced smooth spherical particles with PVCVAEG and more rough surfaces without PVCVAEG. Crystallinity of the co-processed nifedipine with the polymeric solubilizer was reduced. Plasticization of the polymeric solubilizer was observed with increasing drug content. Diffraction patterns in the small angle region as well as transmission electron microscopy showed results supporting phase separation throughout the spray dried particles of high drug content. Compaction with PVCVAEG improved cohesiveness of spray-dried compacts. Heckel modeling showed that deformation of PVCVAEG containing powders was more plastic compared than brittle nifedipine powders. Dissolution kinetics of all spray-dried samples was improved compared to original nifedipine crystals. Co-processed nifedipine with PVCVAEG did not show improved dissolution rate when compared to spray drying nifedipine alone. All though PVCVAEG is more commonly co-processed with drugs by hot melt extrusion to produce solid dispersions, the results show that it also can be processed by spray drying to produce solid dispersions. PVCVAEG improved compactibility of formulated spray dried powders.

Authors+Show Affiliations

Institut Charles Gerhardt - Equipe MACS, UMR 5253, Faculty of Pharmacy, University of Montpellier 1, 15 avenue Charles Flahault, 34093 Montpellier, France.Institut Charles Gerhardt - Equipe MACS, UMR 5253, Faculty of Pharmacy, University of Montpellier 1, 15 avenue Charles Flahault, 34093 Montpellier, France.Institut Charles Gerhardt - Equipe MACS, UMR 5253, Faculty of Pharmacy, University of Montpellier 1, 15 avenue Charles Flahault, 34093 Montpellier, France.Institut Charles Gerhardt - Equipe MACS, UMR 5253, Faculty of Pharmacy, University of Montpellier 1, 15 avenue Charles Flahault, 34093 Montpellier, France.Institut Charles Gerhardt - Equipe MACS, UMR 5253, Faculty of Pharmacy, University of Montpellier 1, 15 avenue Charles Flahault, 34093 Montpellier, France. Electronic address: tahmer.sharkawi@univ-montp1.fr.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25579869

Citation

Soulairol, Ian, et al. "Spray-dried Solid Dispersions of Nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for Compacted Oral Formulations." International Journal of Pharmaceutics, vol. 481, no. 1-2, 2015, pp. 140-7.
Soulairol I, Tarlier N, Bataille B, et al. Spray-dried solid dispersions of nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for compacted oral formulations. Int J Pharm. 2015;481(1-2):140-7.
Soulairol, I., Tarlier, N., Bataille, B., Cacciaguerra, T., & Sharkawi, T. (2015). Spray-dried solid dispersions of nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for compacted oral formulations. International Journal of Pharmaceutics, 481(1-2), 140-7. https://doi.org/10.1016/j.ijpharm.2015.01.012
Soulairol I, et al. Spray-dried Solid Dispersions of Nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for Compacted Oral Formulations. Int J Pharm. 2015 Mar 15;481(1-2):140-7. PubMed PMID: 25579869.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Spray-dried solid dispersions of nifedipine and vinylcaprolactam/vinylacetate/PEG₆₀₀₀ for compacted oral formulations. AU - Soulairol,Ian, AU - Tarlier,Nicolas, AU - Bataille,Bernard, AU - Cacciaguerra,Thomas, AU - Sharkawi,Tahmer, Y1 - 2015/01/08/ PY - 2014/11/10/received PY - 2015/01/03/revised PY - 2015/01/07/accepted PY - 2015/1/13/entrez PY - 2015/1/13/pubmed PY - 2015/12/15/medline KW - Compaction simulator KW - Drug solubility KW - Nifedipine KW - Solid dispersion KW - Soluplus(®) KW - Spray drying SP - 140 EP - 7 JF - International journal of pharmaceutics JO - Int J Pharm VL - 481 IS - 1-2 N2 - The aim of this work was to investigate an alternative processing technology for a new polymeric solubilizer used mainly in hot melt extrusion. Poorly soluble nifedipine was co-processed through spray-drying with poly(vinyl caprolactam-co-vinyl acetate-co-ethylene glycol) (PVCVAEG) in different ratios. The resulting spray-dried powders were formulated and compacted into tablets forms. Spray drying produced reduced smooth spherical particles with PVCVAEG and more rough surfaces without PVCVAEG. Crystallinity of the co-processed nifedipine with the polymeric solubilizer was reduced. Plasticization of the polymeric solubilizer was observed with increasing drug content. Diffraction patterns in the small angle region as well as transmission electron microscopy showed results supporting phase separation throughout the spray dried particles of high drug content. Compaction with PVCVAEG improved cohesiveness of spray-dried compacts. Heckel modeling showed that deformation of PVCVAEG containing powders was more plastic compared than brittle nifedipine powders. Dissolution kinetics of all spray-dried samples was improved compared to original nifedipine crystals. Co-processed nifedipine with PVCVAEG did not show improved dissolution rate when compared to spray drying nifedipine alone. All though PVCVAEG is more commonly co-processed with drugs by hot melt extrusion to produce solid dispersions, the results show that it also can be processed by spray drying to produce solid dispersions. PVCVAEG improved compactibility of formulated spray dried powders. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25579869/Spray_dried_solid_dispersions_of_nifedipine_and_vinylcaprolactam/vinylacetate/PEG₆₀₀₀_for_compacted_oral_formulations_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)00014-9 DB - PRIME DP - Unbound Medicine ER -