Solid-state characterization of nifedipine solid dispersions

Vippagunta, Sudha R.; Maul, Karin A.; Tallavajhala, Siva; Grant, David J.W.

doi:10.1016/s0378-5173(02)00019-4

Cited by 164 publications

(93 citation statements)

References 24 publications

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“…This effect suggests that on heating the physical mixture in DSC, the drug progressively interacts with the Pluronic which melts at lower temperature. Similar suggestion was recorded for the interaction of nifedipine with Pluoronic and/or Gelucire [23]. Fig.…”

Section: Tabsupporting

confidence: 85%

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Maghraby

2009

Sci. Pharm.

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Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on the dissolution rate of itraconazole. Binary solid dispersions with HPMC, reduced the drug crystallinity, increased the equilibrium solubility but showed slow dissolution. Binary dispersions with Pluronic produced eutectic systems but the increase in solubility and dissolution was lower than that of HPMC systems. Ternary system comprising optimum proportions of drug with Pluronic and HPMC enhanced the dissolution rate showing dissolution efficiency comparable to that obtained with the marketed product of itraconazole. The study thus presented a system capable of increasing the dissolution rate of itraconazole with a potential for increased oral bioavailability by inhibiting its pre-systemic metabolism as well.

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Section: Tabsupporting

confidence: 85%

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Maghraby

2009

Sci. Pharm.

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“…The solubility of the incorporated PZQ in water was determined by dispersing aliquots of hydrogels containing 10 mg of PZQ in 10 mL of water, according to the approach adapted from work carried out by Nepal et al (2010) and Vippagunta et al (2002). These samples were stirred for 24 h, then centrifuged at 3400 rpm for 10 min and the amount of dissolved PZQ determined by UV spectrophotometry at 263 nm.…”

Section: Solubility Assaysmentioning

confidence: 99%

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Campos

Cassimiro

Crespi

et al. 2013

Braz. J. Pharm. Sci.

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A hydrogel was developed from 70 kDa dextran (DEX-70) and praziquantel (PZQ) incorporated as a model drug. Biopharmaceutical properties, such as solubility and dissolution rate, were analysed in the design of the hydrogel. Furthermore, the hydrogel was also characterized by IR spectroscopy and DSC. Tests of the swelling rate showed that the hydrogel swelled slowly, albeit faster than the rate for the free polymer. In dissolution tests, the hydrogel released the drug slowly and continuously. This slow release was similar to that observed in the swelling tests and resulted in controlled release of the drug. Thus, this dextran is a suitable polymer for the development of hydrogels as vehicles for the controlled release of drugs.Uniterms: Hydrogel/development. Hydrogel/biopharmaceutical properties. Dextran/hydrogel development. Praziquantel/controlled release. Hydrogel/swelling test.Um hidrogel foi desenvolvido a partir de dextrano 70 kDa (DEX-70) e praziquantel incorporado (PZQ) como fármaco modelo. Propriedades biofarmacêuticas, como solubilidade e velocidade de dissolução, foram analisadas no desenvolvimento do hidrogel. Além disso, o hidrogel também foi caracterizado por espectroscopia na região do infravermelho e calorimetria diferencial exploratória (DSC). Testes da taxa de intumescimento mostraram que o hidrogel intumesce lentamente, embora tenha sido mais rápido do que a taxa do polímero livre. Nos testes de dissolução, o hidrogel liberou o fármaco lenta e continuamente. Esta liberação lenta foi semelhante a observada nos testes de intumescimento e resultou em uma liberação controlada do fármaco. Assim, o dextrano 70 kDa é um polímero adequado para o desenvolvimento de hidrogéis como veículos para a liberação controlada de fármacos.Unitermos: Hidrogel/desenvolvimento. Hidrogel/propriedades biofarmacêuticas. Dextrano/ desenvolvimento de hidrogel. Praziquantel/liberação controlada. Hidrogel/teste de intumescimento.

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“…However, in coground mixture, similar diffraction peaks were obtained at 2θ of 8.3, 10.4, 14.7, 15.1, 16.3, 18.8, 20.2, 20.8, 22.2, 24.8, 25.2 and 28.1. These peaks were broadened and reduced in intensity in comparison to diffraction peaks of corresponding physical mixture (Figure 2c, 2d, 2e), suggesting that either the crystal quality is reduced or change is induced in the crystal orientation or only some of drug is still present in the crystalline form (Vippangunta et al, 2002;Valizadeh et al, 2004;Betageri et al, 1995). PAL therefore existed in a very less crystalline state in co-ground mixture with Plasdone S630.…”

Section: X-ray Diffraction (Xrd)mentioning

confidence: 96%

Dissolution rate and bioavailability enhancement of co-ground mixtures of paliperidone, with different hydrophilic carriers

Pandey¹,

Rath²,

Dwivedi³

2013

Int Curr Pharm J

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Co-ground mixtures of poorly water soluble drug Paliperidone (PAL) with different hydrophilic carriers [Polyvinylpyrrolidine (Plasdone K-25 and Plasdone S-630), Hydroxypropyl methyl cellulose (HPMC), Hydroxypropylcellulose (HPC) and Sodium alginate were prepared to improve the dissolution rate of PAL. Co-grinding with PVP, especially with PVP- S630 (Vinyl pyrrolidone/ vinyl acetate co-polymer), was more effective in reduction of particle size than milling of drug alone. DSC studies indicated that crystalline nature of drug was reduced after co-grinding with PVP grades as compared to their corresponding physical mixtures. The hydrophilic carriers other than PVP did not reduce the crystalline nature of the drug significantly. X-ray diffraction (XRD) was carried out for selected batches to confirm DSC results. Significant enhancement in dissolution rate as well as extent was observed with co-ground mixtures of drug and PVP. Among all the prepared batches in this study, co-ground mixture of PAL and Plasdone S-630 in 1:1 ratio showed best results in terms of extent of dissolution as well as dissolution rate in water. This effect was not only due to particle size reduction, but also loss of crystalline nature of the drug during co-grinding. PVP was found to be a better carrier among the different hydrophilic carriers used in the study for improving the dissolution characteristics of PAL. The extent of the mean plasma exposures of PAL was 7-fold higher in animals treated with co-ground mixture of PAL, Plasdone S630 (1:1) compared to animals treated with Pure PAL.DOI: http://dx.doi.org/10.3329/icpj.v2i3.13632 International Current Pharmaceutical Journal, February 2013, 2(3): 70-77

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Solid-state characterization of nifedipine solid dispersions

Cited by 164 publications

References 24 publications

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Dissolution rate and bioavailability enhancement of co-ground mixtures of paliperidone, with different hydrophilic carriers

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