Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs

Vasconcelos, Teófilo; Sarmento, Bruno; Costa, Paulo

doi:10.1016/j.drudis.2007.09.005

Cited by 1,317 publications

(871 citation statements)

References 83 publications

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“…Among other physical approaches such as nanosuspensions (Müller et al, 2001), crystallization techniques (Fages et al, 2004;Rasenack and Müller, 2002) and the use of solubilizers (e.g., surfactants (Lawrence and Rees, 2000;Pouton, 1997) and cyclodextrins (Brewster and Loftsson, 2007)), polymerbased solid dispersions has received a great deal of attention to overcome the hurdle of limited solubility (Vasconcelos et al, 2007). Amorphous solid dispersion of a drug in an inert water-soluble matrix (most often a polymer) ensure improved dissolution owing to three reasons: on the one hand higher solubility of the amorphous drug, on the other hand the wellsoluble hydrophilic carrier used, thirdly an increased surface area can be obtained depending on the preparation method (Nagy et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

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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Section: Introductionmentioning

confidence: 99%

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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“…The solubility of recently discovered APIs is often very poor (Macarron, 2006;Vasconcelos et al, 2007) in the gastrointestinal fluids, resulting in low oral bioavailability (Wong et al, 2006). Methods that are available to eliminate the solubility problem (Fahr and Liu, 2007;Sarode et al, 2014) are either costly or their industrial applicability is limited .…”

Section: Introductionmentioning

confidence: 99%

Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

Sóti

Bocz

Pataki

et al. 2015

International Journal of Pharmaceutics

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Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state.

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“…The drug is dispersed in a polymer on a molecular level and a single homogeneous amorphous solid is formed, in many cases aided by drug-polymer intermolecular interactions (e.g. the formation of hydrogen bonds between the drug and polymer) (Patterson et al, 2005;Vasconcelos et al, 2007). The capability of the polymer to inhibit crystallisation of the amorphous form has been reported to be possible also at low polymer concentrations (Van den Mooter et al, 2001), and nucleation and crystal growth of the amorphous drug is inhibited by the intermolecular interactions.…”

Section: Introductionmentioning

confidence: 99%

Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

Nielsen

Rades

2015

International Journal of Pharmaceutics

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A glass solution of the amorphous sodium salt of furosemide (ASSF) and polyvinylpyrrolidone (PVP) (80:20 w/w%) was prepared by spray drying. It was investigated if PVP was able to stabilise ASSF during storage and dissolution and whether this influenced the in vivo performance of the glass solution after oral dosing to rats. The glass solution had a glass transition temperature of 121.3±0.5°C, which was significantly higher than that of the pure drug (101.2°C). ASSF in the glass solution was stable for at least 168 days when stored at 20°C and 0% relative humidity. The glass solution exhibited fast dissolution in simulated intestinal medium, pH 6.5; the intrinsic dissolution rate was found to be 10.1±0.6 mg/cm 2 /min, which was significantly faster than the pure ASSF. When investigating the stability during dissolution in stimulated intestinal medium at pH 6.5, the ASSF in the glass solution showed signs of crystallinity after 1 min of dissolution, but crystallised to a lesser extent than pure ASSF. The stabilising effect of PVP on ASSF, led to improved relative oral bioavailability in rats of 263%, when compared to the pure ASSF.

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Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs

Cited by 1,317 publications

References 83 publications

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

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

Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

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