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Potential of carrageenans to protect drugs from polymorphic transformation.
Eur J Pharm Biopharm. 2003 Jul; 56(1):101-10.EJ

Abstract

Carrageenans were analysed in mixture with polymorphic drugs to test their potential for minimising polymorphic or pseudopolymorphic transitions, which are induced by the tableting process. The kappa-carrageenans Gelcarin GP-812 NF and Gelcarin GP-911 NF and the iota-carrageenan Gelcarin GP-379 NF were tested in comparison to the well-known tableting excipients microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), and dicalcium phosphate dihydrate (DCPD). Amorphous indomethacin was chosen as model drug since its well-known recrystallisation behaviour can be mechanically stimulated. Further on, theophylline monohydrate was used. Its dehydration is induced by tableting. Pure materials and mixtures containing 20% (w/w) drug were compressed up to different maximum relative densities. The data obtained during tableting were analysed by three-dimensional (3D) modelling. Afterwards tablets were broken and examined by Fourier transform Raman spectroscopy in order to determine the degree of transformation inside the tablet. For quantitative interpretation, the intensities of representative bands were used. Thermal analysis was used additionally. Using 3D modelling a decrease of plastic deformation can be noticed in the order HPMC>MCC>carrageenans, whereas DCPD represents an exception because of brittle fracture. Best hindrance of polymorphic transformation showed the carrageenans, the hindrance was slightly worse for HPMC. MCC and DCPD could not hinder transformation. A complete protection of the amorphous form could not be achieved. For theophylline monohydrate, the results were similar.

Authors+Show Affiliations

Schmidt AG
Institute of Pharmaceutical Technology and Biopharmacy, Martin-Luther-University Halle-Wittenberg, Halle, Germany.
Wartewig S
No affiliation info available
Picker KM
No affiliation info available

MeSH

CarrageenanCelluloseChemistry, PharmaceuticalCrystallizationExcipientsHypromellose DerivativesIndomethacinMethylcelluloseModels, ChemicalPowdersSpectrum Analysis, RamanTabletsTheophylline

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

12837488

Citation

Schmidt, Andrea G., et al. "Potential of Carrageenans to Protect Drugs From Polymorphic Transformation." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 56, no. 1, 2003, pp. 101-10.
Schmidt AG, Wartewig S, Picker KM. Potential of carrageenans to protect drugs from polymorphic transformation. Eur J Pharm Biopharm. 2003;56(1):101-10.
Schmidt, A. G., Wartewig, S., & Picker, K. M. (2003). Potential of carrageenans to protect drugs from polymorphic transformation. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 56(1), 101-10.
Schmidt AG, Wartewig S, Picker KM. Potential of Carrageenans to Protect Drugs From Polymorphic Transformation. Eur J Pharm Biopharm. 2003;56(1):101-10. PubMed PMID: 12837488.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Potential of carrageenans to protect drugs from polymorphic transformation. AU - Schmidt,Andrea G, AU - Wartewig,Siegfried, AU - Picker,Katharina M, PY - 2003/7/3/pubmed PY - 2004/2/26/medline PY - 2003/7/3/entrez SP - 101 EP - 10 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 56 IS - 1 N2 - Carrageenans were analysed in mixture with polymorphic drugs to test their potential for minimising polymorphic or pseudopolymorphic transitions, which are induced by the tableting process. The kappa-carrageenans Gelcarin GP-812 NF and Gelcarin GP-911 NF and the iota-carrageenan Gelcarin GP-379 NF were tested in comparison to the well-known tableting excipients microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), and dicalcium phosphate dihydrate (DCPD). Amorphous indomethacin was chosen as model drug since its well-known recrystallisation behaviour can be mechanically stimulated. Further on, theophylline monohydrate was used. Its dehydration is induced by tableting. Pure materials and mixtures containing 20% (w/w) drug were compressed up to different maximum relative densities. The data obtained during tableting were analysed by three-dimensional (3D) modelling. Afterwards tablets were broken and examined by Fourier transform Raman spectroscopy in order to determine the degree of transformation inside the tablet. For quantitative interpretation, the intensities of representative bands were used. Thermal analysis was used additionally. Using 3D modelling a decrease of plastic deformation can be noticed in the order HPMC>MCC>carrageenans, whereas DCPD represents an exception because of brittle fracture. Best hindrance of polymorphic transformation showed the carrageenans, the hindrance was slightly worse for HPMC. MCC and DCPD could not hinder transformation. A complete protection of the amorphous form could not be achieved. For theophylline monohydrate, the results were similar. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/12837488/Potential_of_carrageenans_to_protect_drugs_from_polymorphic_transformation_ DB - PRIME DP - Unbound Medicine ER -