The Preparation and Stability of Fast Release Furosemide – PVP Solid Dispersion

Akbuğa, Jülide; Gürsoy, Aylâ; Kendi, E.

doi:10.3109/03639048809151942

Cited by 24 publications

(14 citation statements)

References 13 publications

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“…23 PVP is selected because it is an amorphous excipient, tolerated physiologically, widely used as a carrier for solid dispersions to increase the dissolution rate while suppressing recrystallization. [24][25][26][27][28] Several methods have been used to assess amorphous content such as XPRD. Differential Scanning Calorimetry (DSC) with limits of detectability down to 5% and dynamic vapor sorption (DVS) which can detect extent of disorders as low as 0.5%.…”

Section: Introductionmentioning

confidence: 99%

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

Balani

Tan

et al. 2010

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 99%

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

Balani

Tan

et al. 2010

Journal of Pharmaceutical Sciences

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“…Besides cellulose based polymers, such as HPMC, poly(vinyl pyrrolidone) (PVP) is also widely utilised to prepare solid dispersions (and especially glass solution) (Alves et al, 2014;Newman et al, 2011). PVP is a hydrophilic polymer and is known to inhibit crystal growth and phase transformation (Akbuga et al, 1988;Paudel et al, 2013). Every drug will have different affinity to different polymers, and PVP has shown to have a strong hydrogen bonding capacity for example to felodipine , but is also reported to be a useful component in solid dispersions with furosemide (Doherty and York, 1987).…”

Section: Introductionmentioning

confidence: 99%

“…Every drug will have different affinity to different polymers, and PVP has shown to have a strong hydrogen bonding capacity for example to felodipine , but is also reported to be a useful component in solid dispersions with furosemide (Doherty and York, 1987). Furthermore, it is reported in the literature that the chain length of PVP significantly influences the dissolution rate of furosemide with PVP K30 providing the fastest dissolution rate compared to other PVP types (Akbuga et al, 1988). PVP K30 has also been shown to increase the physical stability of amorphous efavirenz (Alves et al, 2014), and it was also reported that solid dispersions with celecoxib and PVP K30 led to increased dissolution rate (Homayouni et al, 2014) and in addition a higher oral bioavailability compared to the pure drug .…”

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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“…PVP-K30 is well tolerated physiologically, is readily soluble in water, and is used for increasing the dissolution and oral absorption of many water-insoluble drugs (7,8). A previous study on enhancement of the dissolution and permeation profile of meloxicam, a poorly water-soluble drug, has shown some successful results using PVP-K30 (9).…”

Section: Introductionmentioning

confidence: 99%

Permeation Kinetics Studies of Physical Mixtures of Artemisinin in Polyvinylpyrrolidone

Shah¹,

Shahzad²,

Ansari³

et al. 2012

Dissolution Technol.

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Artemisinin (ART), the parent compound of a novel family of antimalarial drugs, was used as a model drug that is lipophilic and has low bioavailability (32%) after oral delivery. The primary objective was to study the effect of polyvinylpyrrolidone (PVP) on the permeation enhancement and solubility of physical mixtures (PM) of ART in PVP-K30 in various solvent systems (i.e., distilled water, phosphate buffered saline [PBS], and methanol). PMs of drug-PVP in 1:0.5, 1:1, 1:2, 1:4, and 1:9 ratios were prepared by simple mixing in a mortar and pestle. Fourier transform infrared (FTIR) spectrophotometry and X-ray powder diffraction (XRPD) were applied to characterize the PMs. The solubility of ART was investigated at 37 ± 0.5 °C in three solvents. Permeation of ART-saturated solutions across a silicone membrane in Franz diffusion cells was studied using Fick's law of diffusion. FTIR and XRPD studies have shown some interactions, and there was a phase change of artemisinin from crystalline to amorphous form as the concentration of PVP-K30 in PM ratios increased. Solubility order increased with an increase in PVP-K30 concentration for the water-PBS solvent system, while in methanol, it was erratic. Flux rate and permeability coefficient were enhanced with an increase in PVP-K30 concentration. In less permeable solvents like water and PBS, the enhancement ratio was high, while the enhancement ratio was low in a highly permeable solvent like methanol. In conclusion, with an increase in concentration of PVP, the permeation rate and solubility of ART increased.

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The Preparation and Stability of Fast Release Furosemide – PVP Solid Dispersion

Cited by 24 publications

References 13 publications

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

Permeation Kinetics Studies of Physical Mixtures of Artemisinin in Polyvinylpyrrolidone

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