Effect of Hydroxypropyl-β-Cyclodextrin on the Solubility of an Antiarrhythmic Agent

Paduraru, Oana Maria; Bosînceanu, Andreea; Ţântaru, Gladiola; Vasile, Cornelia

doi:10.1021/ie303440w

Cited by 13 publications

(16 citation statements)

References 20 publications

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“…The DSC curve shows that AMH has a sharp melting endothermic peak at about 163.47 ºC, indicating a typical behavior of the anhydrous crystalline state. This DSC curve was similar to those in other studies (Paduraru et al, 2013, Riekes et al, 2010. During the DSC analysis the thermogram of HP-β-CD showed a very broad endothermic peak between 60 ºC and 110 ºC.…”

Section: Thermal Analysissupporting

confidence: 88%

“…Similar results were observed with Methyl-β-CD and HP-β-CD by spray-drying and freeze-drying methods. This solid state form transition was also observed by Bankar and Mahatma (2012), Paduraru et al (2013) and Riekes et al (2010), when the amorphization of the compounds after complexation with cyclodextrins was demonstrated.…”

Section: X-ray Powder Diffraction Analysissupporting

confidence: 80%

“…Pure AMH shows about 22.20% dissolution in water, 7.83%, 18.31% and 4.82% dissolution in acid buffer pH 1.2, acetate buffer pH 4.5 and phosphate buffer pH 6.8, respectively after 60 minutes of study. As expected, AMH is a drug that depends on the pH value due to the presence of a tert-amine ionizable in different fluids (Paduraru et al, 2013).…”

Section: Dissolution Rate Studiessupporting

confidence: 72%

“…In solutions with low pH the AMH has appreciable solubility due to its basic nature and ionization (6.56 ± 0.06). On the other hand it is obvious that AMH shows low solubility in a higher pH solution in which it remains in a unionized form (Lamprecht, Bouligand, Benoit, 2002;Paduraru et al, 2013).…”

Section: Ph-dependent Solubility and Phase Solubility Studiesmentioning

confidence: 99%

See 3 more Smart Citations

Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Rubim

Rubenick

Maurer

et al. 2017

Braz. J. Pharm. Sci.

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This study aimed to improve the water solubility of amiodarone hydrochloride (AMH) via inclusion complexes with β-cyclodextrin, methyl-β-cyclodextrin and 2-hydroxypropyl-β-cyclodextrin. Inclusion complexes were developed by physical mixture, coevaporation, spray-drying and freeze-drying. Solid state analysis was performed using X-ray powder diffraction, differential scanning calorimetry and scanning electronic microscopy. Thermodynamic studies demonstrate that the inclusion complexes of drug into different cyclodextrins were an exothermic process that occurred spontaneously. Water solubility and drug dissolution rates were significantly increased after the formation of inclusion complexes with the cyclodextrins evaluated in relation to the physical mixture and pure drug. The present study provides useful information for the potential application of complexation with amiodarone HCl. This may be a good strategy for the development of solid pharmaceutical dosage forms.

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Section: Thermal Analysissupporting

confidence: 88%

Section: X-ray Powder Diffraction Analysissupporting

confidence: 80%

Section: Dissolution Rate Studiessupporting

confidence: 72%

Section: Ph-dependent Solubility and Phase Solubility Studiesmentioning

confidence: 99%

See 2 more Smart Citations

Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Rubim

Rubenick

Maurer

et al. 2017

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

show abstract

“…Few studies were shown in the literature about the improvement of aqueous solubility and absorption of AMH including Elhasi, Astaneh, Lavasanifar(2007); Jouyban, Eghrary, Zarghami (2013);Martín-Algarra et al(1995); Paduraru et al (2013) and Riekes et al (2010).…”

Section: Introductionmentioning

confidence: 99%

Amiodarone hydrochloride: enhancement of solubility and dissolution rate by solid dispersion technique

Rubim

Rubenick

Gregolin

et al. 2015

Braz. J. Pharm. Sci.

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Amiodarone HCl is an antiarrhythmic agent, which has low aqueous solubility and presents absorption problems. This study aimed to develop inclusion complexes containing hydrophilic carriers PEG 1500, 4000 and 6000 by fusion and kneading methods in order to evaluate the increase in solubility and dissolution rate of amiodarone HCl. The solid dispersion and physical mixtures were characterized by X-ray diffraction, FT-IR spectra, water solubility and dissolution profiles. Both methods and carriers increased the solubility of drug, however PEG 6000 enhanced the drug solubility in solid dispersion better than other carriers. Different media were evaluated for the solubility study, including distilled water, acid buffer pH 1.2, acetate buffer pH 4.5 and phosphate buffer pH 6.8 at 37 ºC. Based on the evaluation of the results obtained in the study phase solubility carriers PEG 4000 and PEG 6000 were selected for the preparation of the physical mixture and solid dispersion. All formulations were prepared at drug-carrier ratios of 1:1 to 1:10(w/w). The results of in vitro release studies indicated that the solid dispersion technique by fusion method in proportion of 1:10 (w/w) increased significantly the dissolution rate of the drug. X-ray diffraction studies showed reduced drug crystallinity in the solid dispersions. FT-IR demonstrated interactions between the drug and polymers.

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Super porous α‐, β‐, γ‐cyclodextrin cryogels with high active agent loading and controllable release profiles

Yilmaz,

Sahiner

2023

J of Applied Polymer Sci

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Cyclodextrins (CDs) are truncated cone‐like structures that are natural cyclic oligosaccharides. Here, a simple preparation method for super porous poly(α‐CD), poly(β‐CD), and poly(γ‐CD) cryogels crosslinking with divinyl sulfone at 150%, 100% and 125% mole ratios with respect to the α‐CD, β‐CD, and γ‐CD molecules, respectively, under cryogenic conditions, is reported. The interconnected homogeneous pore distribution of CD‐based cryogels with pore sizes in the range of 5–100 μm is confirmed by SEM analysis. The CD‐based cryogels weighing 10 mg are determined as hemocompatible with <1% hemolysis ratios and >79% blood clotting indexes; whereas the same materials weighing 1 mg are biocompatible with >75% cell viability on L929 fibroblasts. Additionally, active agent adsorption/delivery efficiencies of CD‐based cryogels utilizing two active agents, Bisphenol A (BPA, a carcinogenic compound) and Curcumin (CUR, a polyphenolic compound), are individually evaluated. It was revealed that p(γ‐CD) cryogels exhibited the highest active agent loading capacity for BPA, 87 ± 13 mg/g, whereas p(α‐CD) cryogels showed the highest loading capacity for CUR, 136 ± 4 mg/g. Moreover, the active agent release from p(α‐CD), p(β‐CD), and p(γ‐CD) cryogel networks at pH 7.4 and 37°C were determined as 40.6 ± 2, 35.3 ± 2, and 34 ± 1 mg/g for BPA, and 1.07 ± 0.2, 1.27 ± 0.1, and 1.37 ± 0.1 mg/g for CUR, respectively, within 96 h.

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Effect of Hydroxypropyl-β-Cyclodextrin on the Solubility of an Antiarrhythmic Agent

Cited by 13 publications

References 20 publications

Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Amiodarone hydrochloride: enhancement of solubility and dissolution rate by solid dispersion technique

Super porous α‐, β‐, γ‐cyclodextrin cryogels with high active agent loading and controllable release profiles

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