Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with β-cyclodextrin and its sulfobutyl ether derivative in solution and solid state

Ribeiro, Laura; Ferreira, Domingos; Veiga, Francisco

doi:10.1016/s0928-0987(03)00199-4

Cited by 78 publications

(46 citation statements)

References 22 publications

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“…Due to complex formation, it could result in inclusion of tetrazole moiety into the hydrophobic cavity of βCD. These findings were in full agreement with earlier author Veiga et al (11), who reported similar behavior for vinpocetine-βCD complex. The shift in characteristic bands of IRB in ternary systems was similar to that of binary system, indicating that water-soluble polymers played no role in interaction involved in complex formation.…”

Section: Discussionsupporting

confidence: 93%

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Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility

2009

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Abstract. The effect of complexation of irbesartan (IRB), a practically water-insoluble drug, with cyclodextrins in presence of different concentrations of water-soluble polymers (PEG 4000 and PVP K-90) on the dissolution rate of the drug has been investigated. Phase solubility studies were carried out to evaluate the solubilizing power of βCD in association with water-soluble polymers towards IRB and to determine the apparent stability constant (K S ) of the complexes. Improvement in K S value for ternary complexes (IRB-βCD-polymers) clearly proved the benefit on the addition of water-soluble polymer to increase complexation efficiency. The dissolution rate of the drug from ternary systems containing PEG 4000 and PVP K-90 was higher as compared to the binary system. An optimum increase in the dissolution rate of the drug was observed at a polymer concentration of 5% w/w for PVP K-90 and 10% w/w for PEG 4000. DSC, FTIR, SEM, and XRD studies were carried out to characterize the complexes.

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Section: Discussionsupporting

confidence: 93%

“…The suspensions were further sonicated. The clear solution was subjected to coevaporation (11,12) at temperature 50-70°C on a magnetic stirrer till all the solvent got evaporated. The complex obtained was dried at 50°C and kept under vacuum overnight.…”

Section: Coevaporation Methodsmentioning

confidence: 99%

Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility

2009

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“…5 a and b, respectively. Similar observations have been reported by other authors [37][38][39]. As shown in Fig.…”

Section: X-ray Diffractometrysupporting

confidence: 93%

“…The diffractogram of the physical mixture ND-SBE-β-CD shows a higher reduction in peak intensities: 332, 399, and 286, respectively, whereas the ND-HPBCD PM diffractograms presents the typical ND peaks at ∼20.3°, 17.3°, and 12.8°with decreased intensities of 586, 310, and 745, respectively. This could be explained by the particle size reduction during physical mixing [37] and some interaction between ND and SBE-β-CD/HP-β-CD resulting in reduction in crystalline nature of ND [40]. As presented in Fig.…”

Section: X-ray Diffractometrymentioning

confidence: 90%

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

et al. 2014

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Abstract. The aims of this study were to enhance the solubility and dissolution rate of nimodipine (ND) by preparing the inclusion complexes of ND with sulfobutylether-b-cyclodextrin (SBE-β-CD) and 2-hydroxypropyl-b-cyclodextrin (HP-β-CD) and to study the effect of the preparation method on the in vitro dissolution profile in different media (0.1 N HCl pH 1.2, phosphate buffer pH 7.4, and distilled water). Thus, the inclusion complexes were prepared by kneading, coprecipitation, and freeze-drying methods. Phase solubility studies were conducted to characterize the complexes in the liquid state. The inclusion complexes in the solid state were investigated with differential scanning calorimetry (DSC), Xray diffractometry (X-RD), and Fourier transform infrared spectroscopy (FT-IR). Stable complexes of ND/SBE-β-CD and ND/HP-β-CD were formed in distilled water in a 1:1 stoichiometric inclusion complex as indicated by an A L -type diagram. The apparent stability constants (Ks) were 1334.4 and 464.1 M −1 for ND/SBE-β-CD and ND/HP-β-CD, respectively. The water-solubility of ND was significantly increased in an average of 22-and 8-fold for SBE-β-CD and HP-β-CD, respectively. DSC results showed the formation of true inclusion complexes between the drug and both SBE-β-CD and HP-β-CD prepared by the kneading method. In contrast, crystalline drug was detectable in all other products. The dissolution studies showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products.

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“…Although the mechanism involved in increasing the complexation efficiency is not fully understood, however, it is believed that the addition of a ternary component to the binary complex leads to improved macromolecular self-assembly [15][16][17][18][19][20][21][22].…”

Section: Introductionmentioning

confidence: 99%

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

Arora¹,

Singh²,

Chadha

2017

Int J Pharm Pharm Sci

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Objective: The present work was aimed to study the effect of the ternary component on complexation efficiency of cyclodextrins towards telmisartan which is a poorly soluble anti-hypertensive agent. Methods:The elucidation of inclusion complexation of telmisartan (TEL) with hydroxypropyl-β-cyclodextrin (HP-β-CD) in the presence and absence of tween 80 was done by investigating their interactions in solid and solution state. The solid state characterization was performed using differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD) fourier transform infra-red spectroscopy (FTIR) studies. The host guest stoichiometry was confirmed in solution state by proton nuclear magnetic resonance ( 1 HNMR) and solution calorimetry studies. The improvement in solubility was evaluated through dissolution studies, which was further confirmed by in vivo studies. Results:In solution state, the phase solubility studies indicated 1:1 stoichiometry between TEL and HP-β-CD both in presence and absence of tween 80. The NMR and molecular modelling studies indicated the insertion of N-methyl benzimidazole and biphenyl carboxylate regions of TEL into HP-β-CD cavity suggesting the coexistence of two 1:1 complexes in equilibrium with each other. The stability constants, K1 (imidazole region of TEL-CD) and K2 (biphenyl acetic acid region of TEL-CD), were enhanced in the presence of tween 80 as evident by the higher value of stability constants. Efficacy of ternary complex was established by a significant decrease in the systolic blood pressure of deoxycorticosterone acetate (DOCA) induced hypertensive rats. Conclusion:It can be concluded that solubility of TEL was increased by encapsulation with HP-β-CD. Tween 80 further increased the complexation efficiency and decreased the bulk of cyclodextrin.

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Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with β-cyclodextrin and its sulfobutyl ether derivative in solution and solid state

Cited by 78 publications

References 22 publications

Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility

Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

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