Preparation and solid-state characterization of ball milled saquinavir mesylate for solubility enhancement

Branham, Michael L.; Moyo, T.; Govender, Thirumala

doi:10.1016/j.ejpb.2011.08.005

Cited by 56 publications

(29 citation statements)

References 42 publications

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“…High-Energy Milling (HEM hereafter) has been integrated to pharmaceutical development mainly to reduce particle size (Liversidge and Cundy, 1995). Indeed, an accurate control of granulometry of molecular compounds leads to an enhanced ability to dissolve, a facilitated tablet compression and an improved control of dosages (Brittain, 2002) (Branham et al, 2012). However, such downstream operations can induce changes in the physical state of the product, eg.…”

Section: Introductionmentioning

confidence: 99%

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Schammé

Couvrat

Malpeli³

et al. 2016

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Schammé

Couvrat

Malpeli³

et al. 2016

International Journal of Pharmaceutics

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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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“…For particle size reduction, dry (Branham et al, 2012) and wet milling (Afolabi et al, 2014) processes are commonly used. Wet milling requires less energy and time than dry milling.…”

Section: Introductionmentioning

confidence: 99%

Study of sodium hyaluronate-based intranasal formulations containing micro- or nanosized meloxicam particles

Bartos

Ambrus

Sipos

et al. 2015

International Journal of Pharmaceutics

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Preparation and solid-state characterization of ball milled saquinavir mesylate for solubility enhancement

Cited by 56 publications

References 42 publications

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

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

Study of sodium hyaluronate-based intranasal formulations containing micro- or nanosized meloxicam particles

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