Implication of inclusion complexation of glimepiride in cyclodextrin–polymer systems on its dissolution, stability and therapeutic efficacy

Ammar, H. O.; Salama, H. A.; Ghorab, Mahmoud M.; Mahmoud, Azza A.

doi:10.1016/j.ijpharm.2006.04.002

Cited by 52 publications

(29 citation statements)

References 14 publications

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“…The dissolution rate of glimeperide-β-cyclodextrin was improved by incorporation of 20% w/w of PVP. These results indicated the effectiveness of hydrophilic polymers on improving dissolution rate of the complex (18).…”

Section: Discussionmentioning

confidence: 64%

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: Discussionmentioning

confidence: 64%

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

2009

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“…It has been described in some past publications that the formation of ternary complexes is hard to be determined by either of the spectroscopic techniques due to the overlapping spectral readings [6,31,32]. Only the existence of the Eze-CD complex in all the systems may be inferred.…”

Section: Discussionmentioning

confidence: 99%

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances

Srivalli

Mishra

2015

AAPS PharmSciTech

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Abstract. The purpose of this study was to improve the aqueous solubility, dissolution, and pharmacodynamic properties of a BCS class II drug, ezetimibe (Eze) by preparing ternary cyclodextrin complex systems. We investigated the potential synergistic effect of two novel hydrophilic auxiliary substances, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) and L-ascorbic acid-2-glucoside (AA2G) on hydroxypropyl-β-cyclodextrin (HPBCD) solubilization of poorly water-soluble hypocholesterolemic drug, Eze. In solution state, the binary and ternary systems were analyzed by phase solubility studies and Job's plot. The solid complexes prepared by freeze-drying were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), nuclear magnetic resonance (NMR), and scanning electron microscopy (SEM). The log P values, aqueous solubility, dissolution, and antihypercholesterolemic activity of all systems were studied. The analytical techniques confirmed the formation of inclusion complexes in the binary and ternary systems. HPBCD complexation significantly (p<0.05) reduced the log P and improved the solubility, dissolution, and hypocholesterolemic properties of Eze, and the addition of ternary component produced further significant improvement (p<0.05) even compared to binary system. The remarkable reduction in log P and enhancement in solubility, dissolution, and antihypercholesterolemic activity due to the addition of TPGS or AA2G may be attributed to enhanced wetting, dispersibility, and complete amorphization. The use of TPGS or AA2G as ternary hydrophilic auxiliary substances improved the HPBCD solubilization and antihypercholesterolemic activity of Eze.

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“…In order to investigate the statistical significance difference (if any) in the characterized parameters, one-way ANOVA was employed by using the GraphPad Prism 5 Statistical Software (GraphPad Prism Version 5.01). (20,21). Figure 1 displays the FTIR spectra of (A) glimepiride and the formulated (B) buccoadhesive film.…”

Section: Discussionmentioning

confidence: 99%

Cellulose Buccoadhesive Film Bearing Glimepiride: Physicomechanical Characterization and Biophysics of Buccoadhesion

Meher

Tarai

Patnaik³

et al. 2015

AAPS PharmSciTech

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Abstract. The present study aimed to develop buccoadhesive film of glimepiride with unique combination of polymers and to investigate its effect(s) on physicomechanical parameters, drug-release, and permeation of films. Drug-polymer interaction was examined by FTIR and DSC analysis. Films were prepared by solvent casting technique and characterized for film strength (320 ± 8.5 g, 28.98 ± 2.00 mJ), buccoadhesive strength (28.8±1.37 g, 3.04±0.32 mJ), and tensile strength (260±6.88 g, 18.00±0.44 mJ) by new instrumental techniques. Increase in polymer concentration augmented zeta potential of polymeric matrix-mucin mixture and exhibited strong buccoadhesion (electrical theory). Buccoadhesion was also influenced by particle size (adsorption theory) and swelling (wetting theory). Erosion behavior of films was observed in swelling and SEM studies. Film GM4 exhibited 98±2% in vitro drug release and 85±8% ex vivo drug permeation in 12 h with controlled diffusion mechanism. Films were compatible with oral probiotic microorganisms. Stability studies revealed no significant (P < 0.05) variation in physicomechanical characteristics.

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Implication of inclusion complexation of glimepiride in cyclodextrin–polymer systems on its dissolution, stability and therapeutic efficacy

Cited by 52 publications

References 14 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

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances

Cellulose Buccoadhesive Film Bearing Glimepiride: Physicomechanical Characterization and Biophysics of Buccoadhesion

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