Dissolution and solid state behaviours of carbamazepine-gluconolactone solid dispersion powders: The potential use of gluconolactone as dissolution enhancer

Nokhodchi, Ali; Al-Hamidi, Hiba; Antonijević, Milan D.; Owusu-Ware, Samuel K.; Kaialy, Waseem

doi:10.1016/j.cherd.2015.04.018

Cited by 11 publications

(11 citation statements)

References 25 publications

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“…The drug’s peak intensities reacted in inverse proportion to the concentration of the excipients, and proportionally to a mount of the drug, i.e., for higher drug-excipient ratios, the amount of drug was less, therefore, the drug peak intensities were reduced. A similar phenomenon occurred in the literature, supporting the explanation that, when the concentration of carriers in solid dispersion formulations of carbamazepine-gluconolactone increased to 1:4, the intensity of the drug peak significantly reduced, and it was similarly explained that this could be due to the presence of less carbamazepine in these samples [ 29 ]. Dissolution studies supported this phenomenon as the dissolution rate was higher when the excipients ratio was increased.…”

Section: Resultssupporting

confidence: 83%

“…All drug vehicles formulas showed more than 55% release within 30 min and by the end of this test, after 90 min the dissolution extents were as follows: (drug-cyclodextrin 1:5 (99.79%)), (drug: trehalose 1:2 (99.69%)), (drug: gluconolactone 1:2 (97.85%)). Gluconolactone has been used to be a potential hydrophilic carrier to improve the dissolution rate of a hydrophobic drug such as carbamazepine, using physical mixtures and solid dispersion formulations [ 29 ]. Moreover, gluconolactone improved the dissolution rate of a poorly water soluble piroxicam [ 32 ].…”

Section: Resultsmentioning

confidence: 99%

“…Gluconolactone is a polyhydroxy acid, lactone or oxidized derivative of glucose, a white odourless crystalline powder, freely soluble in water. It was utilized as a potential carrier to improve the dissolution rate of carbamazepine from physical mixtures and solid dispersion formulations [ 29 ].…”

Section: Introductionmentioning

confidence: 99%

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Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

et al. 2018

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Purpose: Hydrophobic drugs are facing a major challenge in dissolution rate enhancement and solubility in aqueous solutions; therefore, a variety of methods have been used to improve dissolution rate and/or solubility of bendroflumethiazide as a model hydrophobic drug. Methods: In this study, two main methods (physical mixing and lyophilisation) were used with gluconolactone, hydroxyl propyl γ-ccyclodextrin, and trehalose to explore this challenge. Bendroflumethiazide, practically insoluble in water, was mixed with one of the three excipients gluconolactone, hydroxyl propyl γ-cyclodextrin, and trehalose in three different ratios 1:1, 1:2, 1:5. To the best of our knowledge, the dissolution of the drug has not been previously enhanced by using either these methods or any of the used excipients. Samples containing drug and each of the excipients were characterized via dissolution testing, Fourier Transform infra-red spectroscopy, differential scanning calorimetry, and scanning electron microscopy. Results: The used methods showed a significant enhancement in dug dissolution rate; physical mixing significantly, p < 0.05, increased the percentage of the drug released with time; for example, bendroflumethiazide dissolution in distilled water was improved from less than 20% to 99.79% within 90 min for physically mixed drug-cyclodextrin 1:5. The lyophilisation process was enhanced and the drug dissolution rate and the highest drug dissolution was achieved for (drug-gluconolactone 1:1) with 98.98% drug release within 90 min. Conclusions: the physical mixing and freeze drying processes significantly increased the percentage of drug release with time.

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Section: Resultssupporting

confidence: 83%

Section: Resultsmentioning

confidence: 99%

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Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

et al. 2018

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“…This suggested that the long grinding time (60 min) induced some degree of polymorphism in the sample (Figure 6a). Pure CBZ displayed a melting peak at 176 ºC, followed by an exothermic peak at 179 ºC (an indication of solid-solid transformation of polymorphic form III to I) and then a sharp endothermic peak at 192 ºC (melting of form I) [38]. These processes were also evident in the ground samples.…”

Section: Solid State Characterization Co-ground Samples and Physical mentioning

confidence: 60%

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

et al. 2016

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An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine, Powder Technology (2016Technology ( ), doi: 10.1016Technology ( /j.powtec.2016 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.A C C E P T E D M A N U S C R I P T AbstractOne of strategies adopted to improve the dissolution rates of poorly soluble drugs is by co-grinding the drug with a hydrophilic carrier. However, the introduction of mechanical forces during th e grinding process can lead to changes in the physicochemical characteristics as well as an increase in the surface free energy of the ground particles, which causes an alteration in the electrostatic properties of these particles. The solid state characteristics of glucosamine hydrochloride (GLU) and carbamazepine (CBZ) and their co-ground mixtures were studied using DSC, XRPD and SEM.These revealed that polymorphic transformations occurred due to the grinding process. The influence of grinding time on the triboelectrification properties of the formulations was also studied.Both pure CBZ and GLU powders were predominantly electro-positively charged and their charging properties increased with increasing grinding time. CBZ:GLU physical mixtures exhibited complicated bipolar charging behaviour, however, when subjected to grinding, these mixtures demonstrated mainly electronegative charge properties. The influence of both grinding time and CBZ content within CBZ:GLU mixtures were examined. The value of net-electronegative-charge density of CBZ:GLU mixtures was shown to increase with grinding time and /or when increasing the percentage proportion of CBZ up to 30 % w:w. This study helps to provide information about the handling of these formulation and gives a formulator tools to ascertain appropriate ratios for handling and possible simultaneous dissolution improvements.

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“…Dissolution tests 22 for cilostazol-free base, cilostazol mesylate, and cilostazol besylate were carried out in triplicate at 37°C±0.5°C using the basket method in a dissolution tester (708-DS; Agilent Technologies, Santa Clara, CA, USA). Hard gelatin capsules, “5” size (Capsugel, Morristown, NJ, USA), were filled with the accurately weighed samples equivalent to 20.0 mg of cilostazol.…”

Section: Methodsmentioning

confidence: 99%

Improved oral absorption of cilostazol via sulfonate salt formation with mesylate and besylate

Seo¹,

Park²,

Choi³

et al. 2015

DDDT

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ObjectiveCilostazol is a Biopharmaceutical Classification System class II drug with low solubility and high permeability, so its oral absorption is variable and incomplete. The aim of this study was to prepare two sulfonate salts of cilostazol to increase the dissolution and hence the oral bioavailability of cilostazol.MethodsCilostazol mesylate and cilostazol besylate were synthesized from cilostazol by acid addition reaction with methane sulfonic acid and benzene sulfonic acid, respectively. The salt preparations were characterized by nuclear magnetic resonance spectroscopy. The water contents, hygroscopicity, stress stability, and photostability of the two cilostazol salts were also determined. The dissolution profiles in various pH conditions and pharmacokinetic studies in rats were compared with those of cilostazol-free base.ResultsThe two cilostazol salts exhibited good physicochemical properties, such as nonhygroscopicity, stress stability, and photostability, which make it suitable for the preparation of pharmaceutical formulations. Both cilostazol mesylate and cilostazol besylate showed significantly improved dissolution rate and extent of drug release in the pH range 1.2–6.8 compared to the cilostazol-free base. In addition, after oral administration to rats, cilostazol mesylate and cilostazol besylate showed increases in Cmax and AUCt of approximately 3.65- and 2.87-fold and 3.88- and 2.94-fold, respectively, compared to cilostazol-free base.ConclusionThis study showed that two novel salts of cilostazol, such as cilostazol mesylate and cilostazol besylate, could be used to enhance its oral absorption. The findings warrant further preclinical and clinical studies on cilostazol mesylate and cilostazol besylate at doses lower than the usually recommended dosage, so that it can be established as an alternative to the marketed cilostazol tablet.

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Dissolution and solid state behaviours of carbamazepine-gluconolactone solid dispersion powders: The potential use of gluconolactone as dissolution enhancer

Cited by 11 publications

References 25 publications

Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

Improved oral absorption of cilostazol via sulfonate salt formation with mesylate and besylate

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Dissolution and solid state behaviours of carbamazepine-gluconolactone solid dispersion powders: The potential use of gluconolactone as dissolution enhancer

Cited by 11 publications

References 25 publications

Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

Feasibility of Using Gluconolactone, Trehalose and Hydroxy-Propyl Gamma Cyclodextrin to Enhance Bendroflumethiazide Dissolution Using Lyophilisation and Physical Mixing Techniques

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

Improved oral absorption of cilostazol via sulfonate salt formation with mesylate and&nbsp;besylate

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Improved oral absorption of cilostazol via sulfonate salt formation with mesylate and besylate