Drug mechanochemical activation

Colombo, I.; Grassi, Gabriele

doi:10.1002/jps.21733

Cited by 139 publications

(105 citation statements)

References 75 publications

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“…The removal of unimportant baseline (offset) 7 interferences and scattering effects and the accentuation of the spectral signals of interest were effected using several different pre-processing methods. The methods used for NIR data included multiplicative scatter correction (MSC), standard normal variate (SNV), first derivative, and second derivative calculations.…”

Section: Discussionmentioning

confidence: 99%

“…[1][2][3] When milling a crystalline active pharmaceutical ingredient (API), the mechanical stress during the milling process cannot only change the particle size, surface area and crystallinity of the API but can also induce polymorphic transformations. [3][4][5][6][7][8][9][10][11] Solid-state polymorphic transitions and amorphization induced by milling have been reported for many pharmaceutical products such as gabapentin, 3 famotidine, 9 ranitidine hydrochloride, 10 and Fananserine. 11 Cryo-milling (Cryogenic grinding) seeks to operate ball milling, a high energy process, at low temperatures with the aid of cryogenic media such as liquid nitrogen.…”

Section: Introductionmentioning

confidence: 99%

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Formation, Physical Stability, and Quantification of Process-Induced Disorder in Cryomilled Samples of a Model Polymorphic Drug

MacFhionnghaile

Caron

et al. 2013

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Formation, Physical Stability, and Quantification of Process-Induced Disorder in Cryomilled Samples of a Model Polymorphic Drug

MacFhionnghaile

Caron

et al. 2013

Journal of Pharmaceutical Sciences

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“…These changes clearly have the potential to lead to a significant change in the physicochemical properties of pharmaceutical products [2][3][4][5][6][7]. Since milling may affect the mechanical properties of pharmaceutical dosage forms an ability to control these transformations would be highly valuable.…”

Section: Introductionmentioning

confidence: 99%

Solid-State Transformations of Sulfathiazole Polymorphs: The Effects of Milling and Humidity

Erxleben

Hodnett

et al. 2013

Crystal Growth & Design

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The effect of milling on the solid-state transitions of sulfathiazole polymorphs in the absence and presence of solvent and excipients was monitored by X-ray powder diffraction (XRPD), attenuated total reflectance infrared (ATR-IR) and near-infrared (NIR) spectroscopy. Sulfathiazole forms FII-FV undergo a transformation toward the metastable FI, which involves an intermediate amorphous stage upon milling at ambient temperature. Milling FIII with catalytic amounts of solvent converts FIII to FIV or to mixtures of FI and FIV depending on the solvent used. Pure FIV can be easily prepared from FIII by this method. The physical stability of pure sulfathiazole forms in the presence of different levels of relative humidity (RH) was also investigated. At low RH all sulfathiazole forms are stable but at RH levels above 70% FII, FIII and FIV remain stable while FI and FV transform to mixtures of FII and FIV without any apparent change in the external form of the crystals. Co-milling FIII with a range of excipients gave results which depended on the excipient used and co-milling with cellulose gave samples which had an amorphous content that was stable at 10% RH for at least nine months at ambient temperature.

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“…The mechanical activation of drugs with the polymers is a well-known effective method for preparing powder systems which are characterized by an increased rate of dissolution and solubility of the drugs (Colombo et al 1998;Shakhtshneider & Boldyrev 1999). In our previous studies (Mikhailenko et al 2010;, the mechanocomposites of betulin with water-soluble synthetic polymers, polyvinylpyrrolidone and polyethylene glycol, were prepared that showed higher solubility of betulin and its gastroprotective properties.…”

Section: Introductionmentioning

confidence: 99%

New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents

Шахтшнейдер

Кузнецова

Zamay

et al. 2015

Natural Product Research

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Betulin and its esters are the natural compounds with high in vitro cytotoxicity toward many cancer cells. However, the poor water solubility of these compounds has limited their applications. We prepared new composites of betulin esters using two methods, namely ball milling of the mixtures of betulin esters with arabinogalactan and preparation of thin films of these mixtures by evaporating the aqueous solutions. These composites revealed higher water solubility as compared to the initial substances without losing the structural integrity and functionality of these compounds. As a result, the new composites have shown much higher inhibitory effects against different cancer cell lines such as Ehrlich ascite carcinoma cells and lung carcinoma cells (A549) in comparison with the initial substances. The cell viability studies based on Annexin V and Propidium iodide probes have confirmed the high proapoptotic effect of betulin esters derivatives against cancer cells.

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Drug mechanochemical activation

Cited by 139 publications

References 75 publications

Formation, Physical Stability, and Quantification of Process-Induced Disorder in Cryomilled Samples of a Model Polymorphic Drug

Formation, Physical Stability, and Quantification of Process-Induced Disorder in Cryomilled Samples of a Model Polymorphic Drug

Solid-State Transformations of Sulfathiazole Polymorphs: The Effects of Milling and Humidity

New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents

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