Potential of carrageenans to protect drugs from polymorphic transformation

Schmidt, Andrea G.; Wartewig, S.; Picker, Katharina M.

doi:10.1016/s0939-6411(03)00037-7

Cited by 51 publications

(26 citation statements)

References 30 publications

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“…11 In a previous paper, we showed that they also reduce the recrystallization of amorphous indomethacin due to tableting. 12 This special ability can be attributed to their high elasticity during tableting and also to their high elastic recovery after decompression, as already described. 13 -15 In this study, polyethylene oxides (PEOs) were tested to establish whether they are able to prevent or reduce polymorphic transitions.…”

Section: Introductionmentioning

confidence: 70%

“…The method was developed by Kontoyannis et al 27 for calcium oxalate hydrate and was used for indomethacin by Taylor and Zografi. 28 It was used in previous work 12 to study polymorphic transformations in mixtures with carrageenans.…”

Section: Spectroscopic Characterizationmentioning

confidence: 99%

“…For this reason, as in the previous study, only the results on the day of production and after 1 day of storage were chosen for interpretation. 12 This procedure is suitable for the MCCs and HPMC: the influence of pressure outweighs the influence of moisture at the first 2 days. For PEO, similarly to pure theophylline, even after 1 day of storage the dehydration of theophylline monohydrate is highly influenced by the moisture in the powder mixture.…”

Section: Dehydration Of Theophylline Monohydrate In Mixture With Excimentioning

confidence: 99%

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Polyethylene oxides: protection potential against polymorphic transitions of drugs?

Schmidt

Wartewig

Picker

2004

J Raman Spectroscopy

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Polyethylene oxides (PEOs) were analysed in mixtures with polymorphic drugs to test their potential in order to prevent polymorphic or pseudopolymorphic transitions, which are induced by the tableting process. Five PEOs with different molecular weights were tested in comparison with the wellknown tableting excipients microcrystalline cellulose (MCC), hydroxypropylmethylcellulose (HPMC) and dicalcium phosphate dihydrate (DCPD). Amorphous indomethacin was chosen as the model drug. Its recrystallization behaviour is well known and can be mechanically stimulated. Theophylline monohydrate was also used; its dehydration is induced by tableting. Pure materials and mixtures containing 20% (w/w) of drug were compressed at different maximum relative densities. The tablets were broken in order to determine the degree of transformation inside by FT-Raman spectroscopy. For quantitative interpretation, the intensities of representative Raman bands were used. Differential scanning calorimetry (DSC) was applied additionally. In tablets and mixtures of amorphous indomethacin and PEOs, recrystallization was dramatically lowered in comparison with the other excipients. The molecular weights of the various PEOs seem to have no influence. The Raman spectra indicate chemical interactions as the reason. Thus, PEO can stabilize amorphous indomethacin. DSC investigations verified these results. For theophylline monohydrate, no interactions could be detected and DCPD showed the best protection properties. Hence the results concerning indomethacin cannot be generalized, but blending with PEO could be a simple method to stabilize amorphous indomethacin.

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Section: Introductionmentioning

confidence: 70%

Section: Spectroscopic Characterizationmentioning

confidence: 99%

Section: Dehydration Of Theophylline Monohydrate In Mixture With Excimentioning

confidence: 99%

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Polyethylene oxides: protection potential against polymorphic transitions of drugs?

Schmidt

Wartewig

Picker

2004

J Raman Spectroscopy

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“…It has been used for predicting content [14][15][16][17] , polymorphic transformations 18,19 , coating thickness 20 , and hydration state. 21 However in the current study, Raman spectroscopy was used to predict the porosity of tablets.…”

Section: Raman Analysismentioning

confidence: 99%

Process Analytical Technology: Chemometric Analysis of Raman and Near Infra-Red Spectroscopic Data for Predicting Physical Properties of Extended Release Matrix Tablets

Shah

Tawakkul

Khan

2007

Journal of Pharmaceutical Sciences

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“…It was found to be superior to microcrystalline cellulose, the effect was attributed to the high elasticity of carrageenan during tableting. [5][6][7] Schmidt et al 8) have reported the potential of polyethylene oxides for protection of amorphous indomethacin due to tableting. Similarly, heterogeneous system containing lipids has been reported for enzyme stabilization in the tablet form.…”

mentioning

confidence: 99%

Application of Polyglycolized Glycerides in Protection of Amorphous Form of Etoricoxib during Compression

Shimpi

Mahadik

Takada

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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Amorphous form of poorly water-soluble drugs lead to marked improvement in their dissolution and thus their relative bioavailability. Many reports on preparation and stabilization of amorphous form have been documented in the literature. Solid dispersion of itraconazole, prepared by spraying the drug and hydroxypropyl methyl cellulose (HPMC) on neutral pellets using organic solvent, is marketed in the trade name of Sporanox ® . Similarly solid dispersion of griseofulvin in PEG (Gris-PEG, Novartis) and Nobilon in povidone (Cesamet, Lilly) was marketed.Despite of this its commercial potential has been limited because of problem in processing of solid dispersions in the suitable dosage form like tablet. Development of solid dispersion into convenient dosage form for their clinical use and successful commercialization is a major challenge for pharmaceutical scientists. Amorphous drug prepared by super critical fluid precipitation has been formulated in the inhalers/spray. Akbuga et al. reported tablets of furosemide-PVP solid dispersion but it has limitations like large amount of disintegrants were required for disintegration of tablet 2) compression difficulties were encountered due to sticking to punches and dies.3) Pirttimaki et al. reported the polymorphic transformation of caffeine in the tableting, 4) because during tableting material obtains energy from mechanical pharmaceutical operations like mixing, grinding, granulation, drying and tableting necessary for transformation.In an effort to prevent polymorphic transformation of amorphous indomethacin and stabilization of enzymes, Picker et al. has evaluated carrageenan, a polymer with high viscoelastic property. It was found to be superior to microcrystalline cellulose, the effect was attributed to the high elasticity of carrageenan during tableting.5-7) Schmidt et al. 8) have reported the potential of polyethylene oxides for protection of amorphous indomethacin due to tableting. Similarly, heterogeneous system containing lipids has been reported for enzyme stabilization in the tablet form. 9) Recently, Shimpi et al. 10) have reported stabilization of amorphous form of etoricoxib in the melt granules with low amount of polyglycolized glycerides (Gelucire) 50/13. The stabilization has been attributed to H-bonding between Gelucire and drug and immobilization of the molecule in the matrix.In the present study it is hypothesized that Gelucires can offer elasticity and protects amorphous form during compression and shelf life. Aim of the present study was to evaluate the effect of compression on the stability of amorphous etoricoxib. Our earlier study on the melt granules revealed that Gelucire 50/13 has the stabilizing ability for amorphous etoricoxib in the ratio of 1 : 0.5 w/w. ExperimentalMaterials Etoricoxib (ET) was obtained as a gift sample from Unichem Laboratories Ltd. (Mumbai, India). Gelucire ® 50/13 (Stearoyl Macrogoglycerides EP, Gattefosse, France) and Avicel PH 102 (microcrystalline cellulose) were supplied by Colorcon India (Mumbai, India) and ...

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Potential of carrageenans to protect drugs from polymorphic transformation

Cited by 51 publications

References 30 publications

Polyethylene oxides: protection potential against polymorphic transitions of drugs?

Polyethylene oxides: protection potential against polymorphic transitions of drugs?

Process Analytical Technology: Chemometric Analysis of Raman and Near Infra-Red Spectroscopic Data for Predicting Physical Properties of Extended Release Matrix Tablets

Application of Polyglycolized Glycerides in Protection of Amorphous Form of Etoricoxib during Compression

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