Dissolution, Solubility, XRD, and DSC Studies on Flurbiprofen-Nicotinamide Solid Dispersions

Varma, M. Mohan; Pandi, J. K.

doi:10.1080/03639040500214613

Cited by 29 publications

(12 citation statements)

References 15 publications

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“…This enhancement of valsartan dissolution from drug carrier systems can be ascribed to several factors. Lack of crystallinity (i.e., amorphization), increased wettability and dispersibility, and particle size reduction are considered important factors for dissolution rate enhancement (18). FTIR spectroscopy shows that individual peak characteristics are retained in the spectra of drug and hydrophilic carriers, indicating there is no interaction between the drug and the carriers.…”

Section: Discussionmentioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

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Solid dispersions (SDs) and physical mixtures (PMs) of valsartan in β-cyclodextrin (β-CD), hydroxypropyl β-cyclodextrin (HP β-CD), and polyvinyl pyrollidone (PVP K-30) were prepared to increase its solubility characteristics. The drug formulations were characterized in the solid state by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). By these physical determinations, drug-polymer interactions were found. Both the solubility and the dissolution rate of the drug in these formulations were increased. Drug contents were determined by UV spectrophotometry at a λ max of 249.5 nm. The phase solubility behavior of valsartan in various concentrations of β-CD, HP β-CD, and PVP K-30 (0.25-1.0% w/v) in distilled water was obtained at 37 ± 2 °C. The dissolution of valsartan is increased with increasing amounts of the hydrophilic carriers (i.e., β-CD, HP β-CD, and PVP K-30). Gibbs free energy (ΔG o tr ) values were all negative, indicating the spontaneous nature of valsartan solubilization. The SDs of valsartan with β-CD and HP β-CD were prepared at 1:1, 1:3, and 1:5 drug/carrier ratios by a kneading method, and PVP K-30 SDs were prepared at the same ratios (i.e., 1:1, 1:3 and 1:5 drug/carrier) by a lyophilization technique. The FTIR spectroscopic studies show the stability of valsartan and the absence of well-defined drug-polymer interaction. Compared with β-CD, HP β-CD showed better enhancement of dissolution rate; compared with HP β-CD, PVP K-30 showed better solubility and dissolution enhancement.

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Section: Discussionmentioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

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“…Solid dispersion of sulpiride and tartaric acid as the investigated carrier was prepared using an oil-in-water solvent evaporation technique (13). Accurately weighed quantities of sulpiride and tartaric acid with a drug to carrier ratio of 1:0.25 (w/w) were transferred into a flask.…”

Section: Preparation Of Solid Dispersions and Physical Mixturesmentioning

confidence: 99%

“…Solid residue was dried in a vacuum oven for 24 h at room temperature and then pulverized and sieved (14). Physical mixtures (PMs) were prepared by triturating the corresponding amounts of sulpiride and tartaric acid using a mortar and pestle and then transferred to a vacuum desiccator until use (13). The powder fractions of SD and PM that passed through a 355-μm sieve and retained on a 150-μm sieve were stored in sealed glass containers for further investigations.…”

Section: Preparation Of Solid Dispersions and Physical Mixturesmentioning

confidence: 99%

Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations

et al. 2014

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Abstract. Pharmaceutical development was adopted in the current study to propose a pediatric rectal formulation of sulpiride as a substitute to the available oral or parenteral formulations in the management of Tourette syndrome (TS). The goal was to formulate a product that is easy to use, stable, and highly bioavailable and to achieve a rapid clinical efficacy. Towards this aim, sulpiride solid dispersion (SD) with tartaric acid at a weight ratio of 1:0.25 was incorporated into different suppository bases, namely witepsol W25, witepsol H15, witepsol E75, suppocire NA, suppocire A, glycerogelatin, and polyethylene glycols. The formulae were evaluated in vitro using different pharmacotechnical methods such as visual, melting, weight and content uniformities, drug release, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and X-ray diffraction (XRD) analyses. In vivo bioavailability was also assessed in rabbits to compare the bioavailability of either raw sulpiride-incorporated or its SD-incorporated witepsol H15-based suppositories to its oral suspension (reference). Sulpiride SD-incorporated witepsol H15 formulation showed acceptable in vitro characteristics with a bioavailability of 117% relative to oral dosing, which excel that in humans (27% after dosing of oral product). In addition, the proposed formula not only passed the 6-month stability study but also proposed a promising scale-up approach. Hence, it showed a great potential for pediatric product development to manage TS in rural areas.

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“…This area of study is very important not only from the technological but also from the pharmacological point of view as different polymorphous forms can have different physical properties such as density, solubility, melting point and hence may be characterised by different bioavailability [7]. Many authors recommend this method for investigation of phase equilibria in multicomponent systems and for detection of inconsistencies between two biologically active substances [8] or between the therapeutic substance and emollients used in drug formulation technology [9][10][11][12]. The DSC method has been also appreciated by the authors working on evaluation of stability of therapeutic substances [13][14][15][16][17][18][19].…”

Section: Introductionmentioning

confidence: 99%

“…Differential scanning calorimetry (DSC) has been recently often used in analysis of medicaments [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19]. For many years it has been an important tool in the study of drug polymorphism [2][3][4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Thermal study of four irradiated imidazoline derivatives in solid state

Marciniec

Kozak

Naskrent

et al. 2007

J Therm Anal Calorim

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Four imidazoline derivatives: antazoline (AN), naphazoline (NN), tymazoline (TM), xylometazoline (XM), in the form of hydrochlorides in solid phase have been subjected to high energy e-beam irradiation from an accelerator (~10 MeV) at a dose varied from 25 to 200 kGy. The effects of the irradiation have been assessed by DSC, X-ray diffraction, FTIR, EPR and TLC.The standard sterilisation dose of 25 kGy has been found to produce changes in the properties of one derivative (XM), two other ones (AN and TM) have been found sensitive to doses >100 kGy, whereas NN has been resistant to irradiation in the whole range studied (25-200 kGy). EPR results indicated that the changes taking place in the therapeutic substances studied are related to radical formation. The irradiation induced changes in colour, a decrease or increase in the melting point, changes in the XRD pattern, small changes in the shape of FTIR peaks and the presence of radiolysis products. The XM compounds cannot be sterilised by irradiation because of the radiation induced changes in its physico-chemical properties.

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Dissolution, Solubility, XRD, and DSC Studies on Flurbiprofen-Nicotinamide Solid Dispersions

Cited by 29 publications

References 15 publications

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations

Thermal study of four irradiated imidazoline derivatives in solid state

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