Cyclodextrins in the Pharmaceutical Field

Bekers, Otto; Uijtendaal, Esther V.; Beijnen, Jos H.; Bult, A.; Underberg, W.J.M.

doi:10.3109/03639049109026630

Cited by 203 publications

(110 citation statements)

References 187 publications

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“…These inclusion complexes have been shown to improve the stability, solubility, dissolution rate, and bioavailability of the drugs [2]. The hydroxypropyl-β-cyclodextrin (HPβCD) is highly watersoluble due to both its chemical nature and amorphous property, and does not have limitations such as the renal toxicity associated with β-cyclodextrins (βCD) or other chemically modified cyclodextrins [3,4].…”

Section: Introductionmentioning

confidence: 99%

Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating ist Inclusion Complex with Hydroxypropyl-β-Cyclodextrin

Dahiya

Kaushik²,

Pathak

2015

Sci. Pharm.

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The present investigation reports the various pharmacokinetic parameters of immediate release aceclofenac tablets incorporating its inclusion complex with hydroxypropyl-β-cyclodextrin. The tablets were prepared using aceclofenac: hydroxypropyl-β-cyclodextrin in a 1:1 molar ratio by the direct compression method (TKN). The results were compared with those of the marketed brand (MKT) and pure drug (TAC). The P-values indicated that mean plasma concentrations were significantly different among all three formulations administered (P<0.05, P<0.01). TKN showed significantly higher plasma levels when compared to the pure drug (P<0.01). The C max and AUC (0-∞) of TKN were significantly higher (P<0.05) compared to the pure drug and marketed formulation. Furthermore, the first-order overall elimination rate constant (K el ) of TKN was also significantly higher (P<0.05) compared to the pure drug and its marketed formulation. These results suggested that tablets prepared by incorporating the AC-HPβCD inclusion complex (TKN) would provide a more rapid onset of pharmacological effects in comparison to the marketed formulation and pure drug.

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Section: Introductionmentioning

confidence: 99%

Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating ist Inclusion Complex with Hydroxypropyl-β-Cyclodextrin

Dahiya

Kaushik²,

Pathak

2015

Sci. Pharm.

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“…In general, cyclodextrins are well-known for their ability to form inclusion complexes with hydrophobic drugs (15). Drug/p-CD inclusion complex and p-CD itself do not penetrate across biological membranes largely due to the hydrophilic character of CDs (27,28).…”

Section: Discussionmentioning

confidence: 99%

“…Inclusion complex formation between drug and CD may improve drug solubility and/or stability (10)(11)(12) as well as bioavailability of the drug (13,14). The use of CDs has been studied extensively in parenteral, oral, rectal and dermal formulations (15)(16)(17), however, the effects of CDs on ocular delivery of topically applied drugs are poorly understood. It has been reported that coadministration of hydroxypropyl-p. CD increases the intraocular pressure lowering effect of prostaglandins (18) and ocular absorption of dexamethasone, dexamethasone acetate (19), and pilocarpine (20).…”

Section: Introductionmentioning

confidence: 99%

Sulfobutyl Ether β-Cyclodextrin (SBE-β-CD) in Eyedrops Improves the Tolerability of a Topically Applied Pilocarpine Prodrug in Rabbits

Järvinen¹,

Järvinen²,

Urtti³

et al. 1995

Journal of Ocular Pharmacology and Therapeutics

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The effects of a novel, modified p-cyclodextrin (SBE4-p-CD; a variably substituted sulfobutyl ether with an average degree of substitution of four) on eye irritation and miotic response of an ophthalmically applied pilocarpine prodrug, 0,0'-dipropionyl-(l,4-xylylene) bispilocarpate, in albino rabbits were studied. Compared to the commercial pilocarpine eyedrop solution (163 mM, equivalent to 3.4% pilocarpine), 12-24 mM pilocarpine prodrug solutions (equivalent to 0.5 -1.0% pilocarpine, respectively) decreased peak miotic intensity (I max ) and increased the time to reach peak (t max ), but did not significantly affect values for the area under the miosis versus time curves (AUC), i.e. 12 -24 mM pilocarpine prodrug appeared to be equivalent to 163 mM pilocarpine. Ocularly applied 12-24 mM pilocarpine prodrug solutions, however, were more irritating than a commercial pilocarpine eyedrop solution. Coadministered SBE4-p-CD significantly decreased the eye irritation of the pilocarpine prodrug solutions. Coadministered SBE4-P-CD did not affect the miotic response of prodrug solution when the molar ratio of SBE4-p-CD to prodrug was low. However, increasing the molar ratio of SBE4-p-CD to prodrug decreased the I max and AUC values. The results show that eye irritation of the pilocarpine prodrug is prevented by levels of SBE4-P-CD that do not affect the apparent ocular absorption of the prodrug.

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“…O estado de equilíbrio de um sistema formado pela CD e a molécula "convidada" (MC) com estequiometria de 1:1 pode ser dado pela equação da constante de associação, estabilidade ou formação do complexo (K) (Equação 2) 25,26 . A constante de afinidade do complexo é dependente da temperatura (o valor de K tende a diminuir rapidamente com o aumento da temperatura) devido à dissociação do complexo 27 . Dentre os métodos utilizados para determinação do valor de K estão as isotermas de solubilidade, onde a molécula "convidada", ao encontrar-se em um sistema composto por CD e água, pode mudar sua solubilidade.…”

Section: Isotermas De Solubilidadeunclassified

Caracterização físico-química de complexo de inclusão entre hidroximetilnitrofurazona e hidroxipropil-beta-ciclodextrina

Grillo¹,

Melo²,

Fraceto³

et al. 2008

Quím. Nova

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Recebido em 13/2/07; aceito em 13/7/07; publicado na web em 19/12/07 PHYSICO-CHEMICAL CHARACTERIZATION OF INCLUSION COMPLEX BETWEEN HYDROXYMETHYLNITRO-FURAZONE AND HYDROXYPROPYL-β-CYCLODEXTRIN. Hydroxymethylnitrofurazone (NFOH) is a prodrug that is active against Trypanosoma cruzi. It however presents low solubility and high toxicity. Hydroxypropyl-β-cyclodextrin (HP-β-CD) can be used as a drug-delivery system for NFOH modifying its physico-chemical properties. The aim of this work is to characterize the inclusion complex between NFOH and HP-β-CD. The rate of NFOH release decreases after complexation and thermodynamic parameters from the solubility isotherm studies revealed that a stable complex is formed (∆G o = -1.7 kJ/mol). This study focuses on the physico-chemical characterization of a drug-delivery formulation that comes out as a potentially new therapeutic option for Chagas disease treatment.Keywords: hydroxymethylnitrofurazone; cyclodextrin; inclusion complex. INTRODUÇÃOA tripanossomíase americana, também denominada doença de Chagas, é uma parasitose tecidual e hematológica causada pelo hemoflagelado Trypanosoma cruzi. A transmissão ao homem e a vários mamíferos ocorre por insetos pertencentes à subfamília Triatoma, que se caracterizam por picar a face das pessoas e são popularmente conhecidos como "barbeiros" 1 . A doença de Chagas apresenta-se em fases clínicas distintas. A fase aguda (inicial) leva, na ausência de tratamento específico, ao surgimento de sintomas característicos como febre e inchaço dos gânglios linfáticos, os quais persistem por cerca de dois meses. Esta fase pode ser fatal, 2 a 8% de óbito, em especial em crianças. Em seguida, a doença evolui à fase indeterminada ou à fase crônica. Na fase indeterminada, o indivíduo é portador do parasito, porém a doença é assintomática. Entretanto, cerca de 20 a 50% dos casos agudos evoluem à fase denominada crônica, caracterizada por baixa parasitemia e ausência do estado febril. A evolução da doença acarreta o comprometimento progressivo de órgãos, com destaque às formas cardíacas, seguidas por manifestações digestivas, através do desenvolvimento do megaesôfago e megacólon 2,3 . Em conseqüência de a evolução clínica coincidir com a fase economicamente produtiva (20 a 50 anos), a morbi-mortalidade manifestada é propriedade comum à doença e constitui-se em sério problema médico-social, agravado que é por sua incidência em países em desenvolvimento 4 . Compostos nitro-heterocíclicos constituem a principal classe dos fármacos empregados para o tratamento da tripanossomíase americana. Dois destes compostos representam as únicas opções terapêu-ticas na atualidade, nifurtimox e benznidazol. Entretanto, estudos diversos têm mostrado que a resposta a estes fármacos é dependente de uma série de fatores como a região geográfica, a idade do paciente, o período e dose utilizados e, em especial, da fase de desenvolvimento da doença. Estes fármacos apresentam efeito considerável na fase aguda e em infecções crônica recentes. Contudo, são pouco eficazes na fase c...

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Cyclodextrins in the Pharmaceutical Field

Cited by 203 publications

References 187 publications

Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating ist Inclusion Complex with Hydroxypropyl-β-Cyclodextrin

Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating ist Inclusion Complex with Hydroxypropyl-β-Cyclodextrin

Sulfobutyl Ether β-Cyclodextrin (SBE-β-CD) in Eyedrops Improves the Tolerability of a Topically Applied Pilocarpine Prodrug in Rabbits

Caracterização físico-química de complexo de inclusão entre hidroximetilnitrofurazona e hidroxipropil-beta-ciclodextrina

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