Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques

Drooge, Dirk Jan van; Hinrichs, Wouter L. J.; Visser, Marinella R; Frijlink, Henderik W.

doi:10.1016/j.ijpharm.2005.12.007

Cited by 139 publications

(64 citation statements)

References 31 publications

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“…As shown in Fig. 7, all binary solid dispersions, ITSDs, and ETSDs showed an absence of the characteristic melting endotherm of sulfathiazole, confirming a solid solution of an amorphous form of sulfathiazole dispersed in the polymeric porous carrier matrix at the molecular level (25)(26)(27). While preparing the PM, a partial disorientation of the organized crystalline structure of sulfathiazole occurs due to the size reduction, which partially disrupts the crystalline structure (28,29).…”

Section: Modulated Differential Scanning Calorimetrymentioning

confidence: 76%

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel¹,

Dave²

2013

AAPS PharmSciTech

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Abstract. Colloidal solid dispersion is an innovative breakthrough in the pharmaceutical industry that overcomes the solubility-related issue of poorly soluble drugs by using an amorphous approach and also the stability-related issue by means of a complex formation phenomenon using different carrier materials. In the present study, a newly developed adsorption method is introduced to incorporate a high-energy sulfathiazole-polyvinylpyrrolidone (Plasdone® K-29/32) solid dispersion on porous silicon dioxide (Syloid® 244FP). Different ternary systems of sulfathiazole-Plasdone® K-29/32-Syloid® 244FP were prepared (1:1:2, 1:1:3, and 1:2:2) and categorized depending on the mechanism by which Syloid® 244FP was incorporated. Modulated differential scanning calorimetry (MDSC), X-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were conducted to characterize the ternary systems. The X-ray diffraction and MDSC data showed a lack of crystallinity in all internal and external ternary systems, suggesting a loss of the crystallinity of sulfathiazole compared to the physical mixtures. USP apparatus II was used to measure the in vitro dissolution rate of the prepared systems at 75 rpm in different media. The dissolution rate of the optimum ratio (1:2:2) containing an internal ternary solid dispersion system was found to be three times higher than that of the external and physical systems. Thus, the porous silicon dioxide incorporated into the conventional binary solid dispersion acted as a carrier to disperse the complex and increase the dissolution rate.

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Section: Modulated Differential Scanning Calorimetrymentioning

confidence: 76%

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel¹,

Dave²

2013

AAPS PharmSciTech

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“…The solid sample retained its amorphous nature as confirmed by the halo pattern of the PXRD and its non-birefringent behavior under polarized light. The low moisture uptake and the ability to retain the amorphous state can be attributed to the hydrophobic nature of the molecule [21]. This non-hygroscopic nature of amorphous IBS further strengthens its case as a good molecule for amorphous delivery.…”

Section: Hygroscopicity Studies Of Crystalline and Amorphous Ibsmentioning

confidence: 84%

Molecular Mobility and Physical Stability of Amorphous Irbesartan

Chawla

2009

Sci. Pharm.

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Amorphous systems have attracted considerable attention due to their favorable properties; however, their stability issues still pose a major challenge. The purpose of the present work was to investigate the role of molecular mobility and moisture in the physical stability of a selected pharmaceutical amorphous system. Irbesartan (IBS), a relatively stable glass, was chosen as the model drug, as it exhibits a good physical stability (resistance to crystallization) at temperatures below the glass transition (T g -50 K). The amorphous system was annealed at temperatures 298 K (25 °C) and 313 K (40 °C) at 0 and 75 % RH to study the effect of temperature and moisture on its relaxation behavior. Differential scanning calorimetry (DSC) was used to characterize both the crystalline and the freshly prepared glass, and to monitor the extent of relaxation at temperatures below glass transition (Tg) as well as heat capacity changes as a function of temperature. Molecular relaxation time constant (τ) decreased drastically from 302 years to 68 hours with the increase in annealing temperature as determined by Kohlrausch-William-Watts (KWW) equation. IBS was found to be 'relatively' stable in the amorphous state and presented a challenge for temporal measurements. Hence, at low annealing temperatures, (T g -50 K or below) initial relaxation time (τ 0 ) was estimated using the calorimetric based approach. Amorphous IBS was non-hygroscopic and retained its glassy nature under the accelerated stability conditions. The extent of relaxation in the amorphous drug in the presence of moisture was also estimated.

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“…The electrospun fibers exhibited a significantly improved dissolution due to the large surface area and the increased solubility of the amorphous form of SPIR evidenced by DSC and XRPD. Theoretically, fibers with higher loadings of a poorly water-soluble drug dissolve slower due to the hydrophobization effect of the drug on the hydrophilic carrier (Van Drooge et al, 2006). Despite that, HPMC-PEO+40%SPIR AC electrospun fibers dissolved almost two times faster than those of with 20% SPIR content.…”

Section: In Vitro Dissolution Of Drug-loaded Hpmc-based Fibersmentioning

confidence: 98%

AC and DC electrospinning of hydroxypropylmethylcellulose with polyethylene oxides as secondary polymer for improved drug dissolution

Balogh

Farkas

Verreck

et al. 2016

International Journal of Pharmaceutics

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Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques

Cited by 139 publications

References 31 publications

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Molecular Mobility and Physical Stability of Amorphous Irbesartan

AC and DC electrospinning of hydroxypropylmethylcellulose with polyethylene oxides as secondary polymer for improved drug dissolution

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