Interactions of Griseofulvin with Cyclodextrins in Solid Binary Systems

Veiga, María-Dolores; Díaz, Paloma J.; Ahsan, Fakhrul

doi:10.1021/js970233x

Cited by 66 publications

(25 citation statements)

References 12 publications

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“…The thermogram of HP-β-CD (Fig. 4D) showed a very broad endothermic peak in the range of 90.03 º C due to elimination of water of crystallization, as reported by many authors [13,14]. The endothermic peak of the drug was retained at 150.9 º C in the case of the physical mixture (Fig.…”

Section: Dsc Analysissupporting

confidence: 73%

Inter-molecular physiochemical characterization for etodolac-hydroxypropyl-β-cyclodextrin polymeric systems in solid and liquid state

et al. 2010

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Abstract:The purpose of this study was to explore the utility of hydroxypropyl-β-cyclodextrin (HP-β-CD) systems in forming inclusion complexes with the anti-rheumatic or anti-arthritic drug, etodolac (EDC), in order to overcome the limitation of its poor aqueous solubility. This inclusion system achieved high solubility for the hydrophobic molecule. The physical and chemical properties of each inclusion compound were investigated. Complexes of EDC with HP-β-CD were obtained using the kneading and co-evaporation techniques. Solid state characterization of the products was carried out using Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and Scanning electron microscopy (SEM). Studies in the solution state were performed using UV-Vis spectrophotometry and 1 H-NMR spectroscopy. Phase solubility profiles with HP-β-CD employed was found to be A L type. Stability constants (K c ) from the phase solubility diagrams were calculated indicating the formation of 1:1 inclusion complex. Stability studies in the solid state and in liquid state were performed; the possible degradation by RP-HPLC was monitored. The dissolution studies revealed that EDC dissolution rate was improved by the formation of inclusion complexes.

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Section: Dsc Analysissupporting

confidence: 73%

Inter-molecular physiochemical characterization for etodolac-hydroxypropyl-β-cyclodextrin polymeric systems in solid and liquid state

et al. 2010

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“…The relation used to calculate the crystallinity was the degree of relative crystallinity (DRC)=I SA /I REF , where I SA is the height of the peak of sample under investigation and I REF , the height of the benchmark peak for the same angle, with the highest intensity. The LPSF/FZ4 was used as a benchmark for calculating the DRC values in solid dispersions (12,13).…”

Section: X-ray Diffractionmentioning

confidence: 99%

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Guedes¹,

Oliveira²,

Hernandes³

et al. 2011

AAPS PharmSciTech

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Abstract. Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble drugs. The increase of the dissolution rate presented by (5Z)-3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (LPSF/FZ4) from the solid dispersions is related to the existence of intermolecular interactions of hydrogen bond type (>N-H ... O<) between the amide group (>N-H) of the LPSF/FZ4 and the ether group (-O-) of the polyethyleneglycol polymer, or the carbonyl (C=O) of the polyvinylpyrrolidone polymer (PVP). The intensity of these interactions is directly reflected in the morphology acquired by LPSF/FZ4 in these systems, where a new solid phase, in the form of amorphous aggregates of irregular size, was identified through scanning electron microscopy and confirmed in the characterizations achieved using X-ray diffraction and thermal analysis of DSC. The solid dispersions with the polymer PVP, in higher concentrations, were revealed to be the best option to be used in the formulations of LPSF/FZ4 in both theoretical and experimental studies.

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“…The formation of mixed crystalline particles during the desiccation process might be the reason for the high RDC-values for the drug: HPbCD complexes in 1:1 and 1:4 molar ratio compared to their corresponding physical mixtures [49].…”

Section: X-ray Diffractometry (Xrd)mentioning

confidence: 99%

Topical liquid crystalline gel containing lornoxicam/cyclodextrin complex

Ammar

Ghorab

Mahmoud

et al. 2011

J Incl Phenom Macrocycl Chem

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Lornoxicam is a potent analgesic non-steroidal anti-inflammatory drug that can be used topically to relieve pain and to reduce inflammation. The objectives of this study were to improve the therapeutic efficacy of lornoxicam by complexation with cyclodextrins and to formulate it in liquid crystalline gel. Lornoxicam and b-cyclodextrin (bCD) or hydroxypropyl-b-cyclodextrin (HPbCD) complexes were prepared using the kneaded method in 1:1, 1:2, 1:3 and 1:4 drug:CD molar ratios. Inclusion complexation in aqueous solution and solid state was evaluated by the ultraviolet, phase solubility diagram, differential scanning calorimetry, X-ray diffractometry and Fourier-transform infrared spectroscopy. The stoichiometry for the inclusion complex was found to be 1:2 drug:CD molar ratio as determined from Job's plot. This result was confirmed by the in vitro dissolution studies for the prepared complexes. Among all the prepared complexes, the complex prepared with bCD in 1:2 drug:CD molar ratio showed highest improvement in drug dissolution and was chosen to be formulated in a topical preparation. For developing liquid crystalline gel, different ratios of Brij 97, glycerol and oils (liquid paraffin, isopropyl myristate and Miglyol Ò 812) were prepared. The formula composed of Brij 97 and glycerol in 3:1 weight ratio, 10% Miglyol Ò 812 and 40% water showed higher drug release compared to the other prepared gels. Moreover, this formula showed low ex vivo permeation on excised pigskin thus it could offer high topical effect with low systematic side effects. This formula showed superior anti-inflammatory activity when applied topically on rats' skin after induction of burn compared to that of Feldene Ò gel.

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Interactions of Griseofulvin with Cyclodextrins in Solid Binary Systems

Cited by 66 publications

References 12 publications

Inter-molecular physiochemical characterization for etodolac-hydroxypropyl-β-cyclodextrin polymeric systems in solid and liquid state

Inter-molecular physiochemical characterization for etodolac-hydroxypropyl-β-cyclodextrin polymeric systems in solid and liquid state

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Topical liquid crystalline gel containing lornoxicam/cyclodextrin complex

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