Effect of hydroxylpropyl-β-cyclodextrin on solubility of carvedilol

Shewale, BD; Sapkal, Nidhi; Raut, Nishikant A.; Gaikwad, NJ; Fursule, RA

doi:10.4103/0250-474x.41470

Cited by 30 publications

(19 citation statements)

References 8 publications

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“…Hydrochloride salt generated in situ in an acidic medium might be less soluble in this medium than the protonated carvedilol itself. At basic pH as the pH increases from 9.2 to 11 its solubility remains more or less constant [28]. In formulation of solid dispersions glacial acetic acid was used so acetic acid incorporates acidity to the formulation that’s why there might be possibility of enhancement of dissolution rate of carvediol [28].…”

Section: Resultsmentioning

confidence: 99%

Chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol

Shete

Yadav

Murthy³

2012

DARU J Pharm Sci

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Background and the purpose of the studyCarvedilol nonselective β-adrenoreceptor blocker, chemically (±)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxypHenoxy) ethyl] amino]-2-propanol, slightly soluble in ethyl ether; and practically insoluble in water, gastric fluid (simulated, TS, pH 1.1), and intestinal fluid (simulated, TS without pancreatin, pH 7.5) Compounds with aqueous solubility less than 1% W/V often represents dissolution rate limited absorption. There is need to enhance the dissolution rate of carvedilol. The objective of our present investigation was to compare chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol.MethodsThe different formulations were prepared by different methods like solvent change approach to prepare hydrosols, solvent evaporation technique to form solid dispersions and cogrind mixtures. The prepared formulations were characterized in terms of saturation solubility, drug content, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), electron microscopy, in vitro dissolution studies and stability studies.ResultsThe practical yield in case of hydrosols was ranged from 59.76 to 92.32%. The drug content was found to uniform among the different batches of hydrosols, cogrind mixture and solid dispersions ranged from 98.24 to 99.89%. There was significant improvement in dissolution rate of carvedilol with chitosan chlorhdyrate as compare to chitosan and explanation to this behavior was found in the differences in the wetting, solubilities and swelling capacity of the chitosan and chitosan salts, chitosan chlorhydrate rapidly wet and dissolve upon its incorporation into the dissolution medium, whereas the chitosan base, less water soluble, would take more time to dissolve.ConclusionThis technique is scalable and valuable in manufacturing process in future for enhancement of dissolution of poorly water soluble drugs.

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Section: Resultsmentioning

confidence: 99%

Chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol

Shete

Yadav

Murthy³

2012

DARU J Pharm Sci

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“…There have been several methods to prepare inclusion complexes of cyclodextrin and different class of drugs [8][9][10][11][12][13][14][15]. CDL with b-cyclodextrin inclusion complex was reported by Wen et al [16][17][18]. Liu et al conclude that the complexation ability of the calixarenes is largely driven by electrostatic interaction, rather than the hydrophobic interaction in the CDs complexation.…”

Section: Introductionmentioning

confidence: 94%

Evaluation and solubility improvement of Carvedilol: PSC[n]arene inclusion complexes with acute oral toxicity studies

Menon

Mistry

Joshi

et al. 2011

J Incl Phenom Macrocycl Chem

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The aqua phobic molecules that are practically insoluble in aqueous media demonstrate a staggeringly slow intrinsic dissolution rate. In this work, we exemplify the utility of calixarenes as a tool to form inclusion complexes with Carvedilol (CDL). It is poorly water soluble drug. CDL is a Biopharmaceutical Classification System (BCS) Class II drug and it is a nonselective b-adrenegenic blocking agent with a1-blocking activity. It is mainly used in the management of hypertension. The maximum complexation of the drug was accomplished after 48 h of stirring with para sulphonato calix[4]arene (PSC[4]arene) and para sulphonato calix[6]arene (PSC[6]arene) in water and evaporation of water to acquire solid complexes. The study includes characterisation of both the complexes-physical mixtures of drug and PSC[4]arene and PSC[6]arenes by different methods like Fourier-transform infra red spectroscopy, differential scanning calorimetry and powder X-ray diffraction, proton nuclear magnetic resonance. This studies shows that there is electrostatic interaction between drug and PSC[n]arenes. The complexation was determined by phase solubility study. The prepared complexes exhibited improved in vitro dissolution profile and decreased in vivo acute oral toxicity compared to the pure drug.

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“…[34] When the guest molecules are embedded in the cyclodextrin cavity, their melting point, boiling point or sublimation points generally shifted to a different temperature. [35] The thermograms of SV, PM, pure HPBCD and SD2 are shown in Figure 10.…”

Section: Kinetic Modelling Of Drug Release Profilesmentioning

confidence: 99%

Preparation and evaluation of mucoadhesive simvastatin microcapsules using orifice gelation technique

Bal¹,

Murthy²,

Sengupta³

2012

Asian J Pharm

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P reparation and characterization of Simvastatin/ Hydroxy propyl beta cyclodextrin (HPBCD) (SV/HPBCD) binary systems by co-grinding technique and formulating the binary system in oral mucoadhesive microcapsules by using hydrophilic sodium alginate (SA) and another plant seed mucilage dillenia (obtained from Dillenia indica, Family, Dilleniaceae) using orifice gelation technique and systematically evaluating in vitro by using scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometer (XRD). The microcapsules were smooth and elegant in appearance showed no visible cracks as confirmed by SEM; and extended drug release of 72.682% upto 12 hours in phosphate buffer of pH 6.8; showing particle size within the range of 371.5-457 µm, and less angle of repose, Hausner's ratio and Carr's consolidation index; and showed encapsulation efficiency of 63.068 ± 0.002 to 99.083 ± 0.017%. The in vitro release data of optimized batch of microcapsules were plotted in various kinetic equations to understand the mechanisms and kinetics of drug release, which followed zero order kinetics and value of "n," is calculated to be 0.505 and drug release was diffusion controlled. The in vivo antihyperlipidemic activity of formulations in mice was carried out developing hyperlipidemia in mice and then administering the optimized formulations orally, and the formulation showed promising results.

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Effect of hydroxylpropyl-β-cyclodextrin on solubility of carvedilol

Cited by 30 publications

References 8 publications

Chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol

Chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol

Evaluation and solubility improvement of Carvedilol: PSC[n]arene inclusion complexes with acute oral toxicity studies

Preparation and evaluation of mucoadhesive simvastatin microcapsules using orifice gelation technique

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