Influence of the preparation method on the physical–chemical properties of ketoprofen–cyclodextrin–phosphatidylcholine ternary systems

Cirri, Marzia; Maestrelli, Francesca; Mennini, Natascia; Mura, Paola

doi:10.1016/j.jpba.2008.11.002

Cited by 32 publications

(9 citation statements)

References 25 publications

(30 reference statements)

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“…Grinding of a drug/CD mixture often produces amorphous products [31,32,33,34,47,51,54,55,56,57,58,59,60,61,62,63,64,65] or products containing only traces of crystalline drug [33,37,53,66,67,68,69,70,71,72,73,74,75,76], depending on the time and intensity of grinding and on the physicochemical properties of both drug and CD subjected to grinding. Several authors have demonstrated, by the use of 13 C MAS CP/TOSS NMR spectroscopy, the actual inclusion complex formation in amorphous drug/CD products obtained by co-grinding; examples from the literature included two thiadiazole-based anti-Alzheimer drug candidates co-ground with βCD and HPβCD [27,37], a fentanyl/βCD [59], and a bisacodyl/βCD [54] co-ground system.…”

Section: Mechanism Of the Inclusion Complex Formation In The Solidmentioning

confidence: 99%

“…However, such a method often results in only partial drug/CD complexation [14]. Methods in the solid state , where CD complexation is achieved by microwave irradiation (MWI) [33] or by gentle heating at temperatures below the fusion point of the compounds in a sealed container, eventually in the presence of a minimum water amount, according to the so-called “sealed-heating” method (SH) [34,35] or by mechanochemical activation through grinding (GR) with different types of mills [36,37] of the drug/cyclodextrin physical mixture. The drawback of both MW and SH technologies is in the possibility of drug degradation during microwave irradiation or heating [38].…”

Section: Introductionmentioning

confidence: 99%

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Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Jug

Mura

2018

Pharmaceutics

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Among the different techniques proposed for preparing cyclodextrin inclusion complex in the solid state, mechanochemical activation by grinding appears as a fast, highly efficient, convenient, versatile, sustainable, and eco-friendly solvent-free method. This review is intended to give a systematic overview of the currently available data in this field, highlighting both the advantages as well as the shortcomings of such an approach. The possible mechanisms involved in the inclusion complex formation in the solid state, by grinding, have been illustrated. For each type of applied milling device, the respective process variables have been examined and discussed, together with the characteristics of the obtained products, also in relation with the physicochemical characteristics of both the drug and cyclodextrin subjected to grinding. The critical process parameters were evidenced in order to provide a useful guide for a rational selection of the most suitable conditions for an efficient inclusion complex preparation by grinding, with the final purpose of promoting a wider use of this effective solvent-free cyclodextrin inclusion complex preparation method in the solid state.

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Section: Mechanism Of the Inclusion Complex Formation In The Solidmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Jug

Mura

2018

Pharmaceutics

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“…Every determination at each time point was performed in triplicate and the error bars on the graphs represented the standard deviation. DE was calculated from the area under the dissolution curve at time t and expressed as a percentage of the area of the rectangle described by 100% dissolution in the same time 14,15…”

Section: Methodsmentioning

confidence: 99%

“…In our opinion, this same method without sodium lauryl sulfate might be more appropriate to calculate various dissolution parameters such as drug percent (DP) dissolved and dissolution efficiency (DE) of the raw material and MBZ microparticles 14,15…”

Section: Introductionmentioning

confidence: 99%

Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose

Torre-Iglesias¹,

García-Rodríguez²,

Pena-Fernandez³

et al. 2014

DDDT

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BackgroundMebendazole (MBZ) is an extremely insoluble and therefore poorly absorbed drug and the variable clinical results may correlate with blood concentrations. The necessity of a prolonged high dose treatment of this drug increases the risk of adverse effects.MethodsIn the present study we prepared redispersible microparticles (RDM) containing MBZ, an oral, poorly water-soluble drug, in different proportions of low-substituted hydroxypropylcellulose (L-HPC). We investigated the microparticulate structures that emerge spontaneously upon dispersion of an RDM in aqueous medium and elucidated their influence on dissolution, and also on their oral bioavailability and therapeutic efficiency using a murine model of infection with the nematode parasite Trichinella spiralis.ResultsElevated percentages of dissolved drug were obtained with RDM at 1:2.5 and 1:5 ratios of MBZ: L-HPC. Thermal analysis showed an amorphization of MBZ in the RDM by the absence of a clear MBZ melting peak in formulations. The rapid dissolution behavior could be due to the decreased drug crystallinity, the fast dissolution time of carriers as L-HPC, together with its superior dispersibility and excellent wetting properties. RDM-1:2.5 and RDM-1:5 resulted in increased maximum plasma concentration and area(s) under the curve (AUC)0-∞ values. Likewise, after oral administration of the RDM-1:2.5 and RDM-1:5 the AUC0-∞ were 2.67- and 2.97-fold higher, respectively, compared to those of pure MBZ. Therapeutic activity, assessed on the Trichinella spiralis life cycle, showed that RDM-1:5 was the most effective in reducing the number of parasites (4.56-fold) as compared to pure MBZ, on the encysted stage.ConclusionThe MBZ: L-HPC RDM might be an effective way of improving oral bioavailability and therapeutic activity using low doses of MBZ (5 mg/kg), which implies a low degree of toxicity for humans.

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“…There are a number of US FDA (U.S. Food and Drug Administration) approved products of water insoluble drugs which utilize cyclodextrin inclusion technology. In addition to improving the solubility and taste masking of drugs [11], CD also improve their physical and chemical stability [12], absorption [13] and bioavailability [10].…”

Section: Introductionmentioning

confidence: 99%

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

Desai

Poddar

Sawant

2016

Materials Science and Engineering: C

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Influence of the preparation method on the physical–chemical properties of ketoprofen–cyclodextrin–phosphatidylcholine ternary systems

Cited by 32 publications

References 25 publications

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

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