Cyclodextrins in Pharmacy

Frömming, K.‐H.; Szejtli, J.

doi:10.1007/978-94-015-8277-3

Cited by 443 publications

(303 citation statements)

References 15 publications

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“…The values of βCD are largely in line with those presented in the literature (0.42-0.49 and 0.74-0.76 g/cm 3 for the bulk and tapped densities, respectively) [24]. Looking at the powders processed, the formulations with a high interparticle porosity were observed for powders prepared by FD followed by AS and SD.…”

Section: Properties Of the Powders And References Mixturessupporting

confidence: 89%

“…The Carr's index and angle of repose observations were confirmed on the preparation of the minitablets and capsules: would their preparation had been different from manual and a glidant had to be added to the formulations. This was particularly relevant for the powders produced by spray or freeze-drying, which are described as amorphous with small and porous particles [24,25]. Looking at the true densities (expected and measured) the values for the raw materials are in agreement with the literature [19,26].…”

Section: Properties Of the Powders And References Mixturessupporting

confidence: 71%

“…The results have also shown that different drying techniques yielded different products with different moisture contents ( Table 2, lower part). This should be taken into consideration because the residual water may affect the formation of the complex and tabletting of the mixtures of materials, as shown by Frӧmming and Szejtli [24] who identified the optimal βCD compressibility for a moisture content around 14% and suggested that this water can be regarded as little bounded to the solid raw materials. As discussed elsewhere, freeze-and spray-drying techniques were more efficient on drying than the others, but the residual water seems to be useful to improve the powders flow ability and compressibility ( Table 2, IC r and angle repose).…”

Section: Properties Of the Powders And References Mixturesmentioning

confidence: 99%

See 2 more Smart Citations

Comparison of ibuprofen release from minitablets and capsules containing ibuprofen: β-Cyclodextrin complex

Salústio¹,

Cabral-Marques²,

Costa³

et al. 2011

European Journal of Pharmaceutics and Biopharmaceutics

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Mixtures containing ibuprofen (IB) complexed with β-cyclodextrin (βCD) obtained by two complexation methods [suspension/solution (with water removed by air stream, spray-and freezedrying) and kneading technique] were processed into pharmaceutical dosage forms (minitablets and capsules). Powders (IB, βCD and IBβCD) were characterized for moisture content, densities (true and bulk), angle of repose and Carr's index, X-ray and NMR. 2.5 mm diameter minitablets and capsules were prepared from physical mixtures and IBβCD complexes without other excipients. Minitablets were characterized for the energy of compaction, tensile strength, friability, density and IB release (at pH 1.0 and 7.2), whereby capsules were characterized for IB release. The results from the release of IB were analyzed using different parameters, namely, the similarity factor (f 2 ), the dissolution efficiency (DE) and the amounts released at a certain time (30, 60 and 180 min) and compared statistically (α = 0.05). The release of IB from the minitablets showed no dependency on the amount of water used in the formation of the complexes. Differences were due to the compaction force used or the presence of a shell, for the capsules. The differences observed were mostly due to the characteristics of the particles (dependent on the method considered on the formation of the complexes) and neither to the dosage form nor to the complex of the IB.

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Section: Properties Of the Powders And References Mixturessupporting

confidence: 89%

Section: Properties Of the Powders And References Mixturessupporting

confidence: 71%

Section: Properties Of the Powders And References Mixturesmentioning

confidence: 99%

See 1 more Smart Citation

Comparison of ibuprofen release from minitablets and capsules containing ibuprofen: β-Cyclodextrin complex

Salústio¹,

Cabral-Marques²,

Costa³

et al. 2011

European Journal of Pharmaceutics and Biopharmaceutics

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“…A major obstacle to the widespread use of pulmonary drug delivery is the relative impermeability of the lung to many of these peptide and macromolecular drugs when they are administered without an absorption enhancer. Cyclodextrins (CDs) have been reported as potential absorption enhancer in pulmonary protein delivery [3],…”

Section: Introductionmentioning

confidence: 99%

Cyclodextrins as a potential carrier in drug nebulization

Évrard

Bertholet

Guéders

et al. 2004

Journal of Controlled Release

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The inhalation route is widely studied for many drug applications focusing on either local or systemic distributions. One matter of concern is the solubilization of hydrophobic drugs.We have studied the feasibility of using different cyclodextrins (CDs) to elaborate pharmaceutical formulations for the inhalation route and tested the short-term toxicity of such formulations administered by inhalation to C57BL/6 mice.We have shown that HP-β-CD, γ-CD, as well as RAMEB aqueous solutions can undergo aerosolization and that the resulting droplet-size ranges are compatible with pulmonary deposition. In vivo, we have demonstrated that short-term exposure to inhaled HP-β-CD, γ-CD and RAMEB solutions are non-toxic after assessing bronchoalveolar lavage (BAL), lung and kidney histology, bronchial responsiveness to methacholine and blood urea. The only change noted is a slight increase in lymphocyte count in the BAL after HP-β-CD and γ-CD inhalation.We conclude that CDs are useful in significantly enhancing the solubility of apolar drugs with a view to inhalation therapy although an increase in lymphocyte counts in the BAL after CDs inhalations needs further investigations.

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“…By exchange with the water molecules present in their cavity in the crystalline state, cyclodextrins are able to include large organic molecules by noncovalent interactions forces (Frömming and Szejtli, 1994) leading to an increase of aqueous solubility and stability of these molecules (Loftsson and Brewster, 1996). However, this phenomenon is not always verified for all the substances; in fact the complexation ability depends on the geometry of the guest molecule inside the CD cavity and also its charge and polarity criteria (Frömming and Szejtli, 1994).…”

Section: Introductionmentioning

confidence: 99%

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

Zimé-Diawara¹,

Gbaguidi²,

Semdé³

et al. 2014

Int. J. Bio. Chem. Sci

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Artemisinin is extracted from the Asian plant Artemisia annua L. It has been proven to be, with its derivatives, the molecules that have shown so far the most powerful activity on malaria, even in its complicated forms and resistance cases. To resolve the problem of low aqueous solubility of this molecule, the use of cyclodextrins (CDs) was envisaged and gave good results in this topic. However, the impact on its stability and in vitro dissolution, important parameters for drug formulation and evaluation, was not evaluated. In this study, stability in accelerated degradation conditions and in vitro dissolution analysis of artemisinin were performed in comparison with complexes of artemisinin and cyclodextrins. The findings of this work allowed us to suggest that CDs improve the stability of artemisinin, especially when it's in aqueous solution. We also demonstrated the beneficial impact of cyclodextrins on the in vitro dissolution of artemisinin from capsules prepared with rough extracts of A. annua.

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Cyclodextrins in Pharmacy

Cited by 443 publications

References 15 publications

Comparison of ibuprofen release from minitablets and capsules containing ibuprofen: β-Cyclodextrin complex

Comparison of ibuprofen release from minitablets and capsules containing ibuprofen: β-Cyclodextrin complex

Cyclodextrins as a potential carrier in drug nebulization

Effect of cyclodextrins on artemisinin stability and <i>in vitro</i> dissolution

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