Enhanced solubility and dissolution rate of amiodarone by complexation with β-cyclodextrin through different methods

“…26 For furosemide, both 1:1 and 2:1 stoichiometries were described 27 ; for amiodarone and tamoxifen, the 1:1 complex with $-CD was published. 28,29 By dissolving amiodarone in water, a yellowish colloidal solution is obtained even at low (3 mg/mL) concentrations. 30 The solubility is less than 0.1 mg/mL.…”

Section: Discussionmentioning

confidence: 99%

Methyl-Beta-Cyclodextrins: The Role of Number and Types of Substituents in Solubilizing Power

Fenyvesi

Szemán

Csabai

et al. 2014

Journal of Pharmaceutical Sciences

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“…As compared to a-CD and g-CD, b-CD is mostly preferred and widely used for complexation in pharmaceuticals 9 . The unique hollow truncated cone like structure of CDs with a hydrophobic cavity and hydrophilic wall make them capable of forming non-covalent inclusion complexes with guest molecules having suitable polarity and dimension 10,11 . Besides, parent b-CD, its hydrophilic derivatives hydroxypropyl-b-cyclodextrin and epichlorohydrinb-cyclodextrin (HP-b-CD and Epi-b-CD) are more effective in complexation.…”

Section: Introductionmentioning

confidence: 99%

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gidwani

Vyas

2015

Drug Development and Industrial Pharmacy

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The objective of the present work was to investigate the inclusion behavior of bendamustine (BM) with β-cyclodextrin and its hydrophilic derivatives (HP-β-CD and Epi-β-CD) for the enhancement of aqueous solubility, dissolution and bioavailability. The supramolecular binary complexes were prepared by three different methods, viz. physical mixture (PM), kneading (KND) and co-evaporation (COE). Phase-solubility study revealed the higher solubilizing and complexing ability of polymerized cyclodextrin (Ks = 645 M(-1)) than parent cyclodextrin (Ks = 43 M(-1)) and chemically derived cyclodextrin (Ks = 100 M(-1)). Meanwhile, the solubility of BM was significantly enhanced in phosphate buffer of pH 6.8, which was 24.5 folds greater compared with the phosphate buffer pH 4.5 and four times greater than aqueous medium. The dissolution efficiency was found to be highest for BM: Epi-β-CD complex (87%) compared to BM: HP-β-CD complex (84%), BM: β-CD (79%) and pure drug (20%). In-vivo pharmacokinetic study revealed that the bioavailability of BM was enhanced 2.55 times on complexation with Epi-β-CD using KND method. The t1/2 of BM was increased from 34.2 min to approximately 75.7 min, allowing the absorption for longer time. The order of increase in solubility, dissolution and bioavailability of BM was KND > COE > PM > pure drug. Thus, the strategy of host-guest inclusion was very effective and could be successfully used in the development of suitable pharmaceutical dosage form with enhanced therapeutic activity.

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“…Different techniques have been used to improve the solubility and dissolution rate of the poorly soluble drugs, and in middle of the alternatives, the use of CD complexation presented a great interest [8] in recent years. CDs are cyclic oligosaccharides composed of glucopyranose units and can be represented as a truncated cone structure with a hydrophobic cavity.…”

Section: Introductionmentioning

confidence: 99%

INCLUSION STUDIES ON Α-Cyclodextrin COMPLEXES OF GLIPIZIDE AND GLICLAZIDE WITH EFFECT OF PH

Simon

Kumari²

2016

Asian J Pharm Clin Res

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Objective: To synthesize inclusion complexes of oral antidiabetic drugs, i.e., Glipizide (GP) and Gliclazide (Glc) with a-cyclodextrin (α-CD) and varying the pH which will enhance the solubility and thereby oral bioavailability of the drugs.Methods: Liquid inclusion complexes were prepared and characterized by ultraviolet-visible (UV-VIS) spectroscopic studies, and fluorescent studies solid inclusion complexes of GP and Glc with α-CD were prepared by co-evaporation method and characterized by differential scanning calorimetric studies (DSC) and 1 H nuclear magnetic resonance spectroscopic studies ( 1 H NMR). Results:The inclusion complexes of both GP and Glc with α-CD showed high binding constant values for pH 2 from the UV-VIS spectroscopy studies and fluorescent studies. DSC and 1 H NMR spectroscopic studies confirmed the inclusion of GP and Glc inside the α-CD cavity. Conclusion:Formed with more stable inclusion complexes, with α-CD are GP and Glc at pH 2, along with pH modulation could be a suitable strategy to enhance the solubility and oral bioavailability of both the drugs.

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Enhanced solubility and dissolution rate of amiodarone by complexation with β-cyclodextrin through different methods

Cited by 44 publications

References 24 publications

Methyl-Beta-Cyclodextrins: The Role of Number and Types of Substituents in Solubilizing Power

Methyl-Beta-Cyclodextrins: The Role of Number and Types of Substituents in Solubilizing Power

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

INCLUSION STUDIES ON Α-Cyclodextrin COMPLEXES OF GLIPIZIDE AND GLICLAZIDE WITH EFFECT OF PH

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