Evidence for Solid- and Liquid-State Interactions in a Furosemide-Polyvinylpyrrolidone Solid Dispersion

Doherty, Chris; York, Peter

doi:10.1002/jps.2600760912

Cited by 67 publications

(36 citation statements)

References 13 publications

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“…The interaction mechanisms between the drug and the carrier in solid dispersions have been studied. 8,9) Previous studies of naproxen-a-lactose monohydrate solid dispersions, 10,11) prepared using melting methods, supported the existence of a high-energy amorphous drug phase in systems containing more than 50% a-lactose monohydrate. The dissolution data suggested that the dissolution rate of this phase was 7-20-fold greater than the crystalline drug.…”

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confidence: 96%

Acetaminophen Particle Design Using Chitosan and a Spray-Drying Technique

et al. 2005

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Previous studies have shown that coprecipitation with polyvinylpyrrolidone (PVP) can markedly enhance the dissolution of poorly water-soluble drugs.1,2) The mechanism responsible for such enhanced dissolution has been the subject of debate. Some authors have proposed that the increased drug dissolution rate is due to the formation of a high-energy amorphous drug phase.3,4) Several water-soluble polymer carrier systems, such as polyethylene glycol (PEG), PVP, and hydroxypropylcellulose (HPC), [5][6][7] have been used in fast-release preparations. The interaction mechanisms between the drug and the carrier in solid dispersions have been studied. 8,9) Previous studies of naproxen-a-lactose monohydrate solid dispersions, 10,11) prepared using melting methods, supported the existence of a high-energy amorphous drug phase in systems containing more than 50% a-lactose monohydrate. The dissolution data suggested that the dissolution rate of this phase was 7-20-fold greater than the crystalline drug.Recently, a spray-drying technique has yielded an amorphous form of such crystalline drugs as cimeditine that becomes amorphous when spray-dried with chitosan, as reported by He et al. 12) This indicates that a solid dispersion was formed when cimeditine was dispersed in the chitosan molecules by spray drying. Corrigan et al. 13) tried to make an amorphous drug by spray drying using PVP as a carrier. Generally, the dissolution rate of a drug increases when a solid dispersion is formed using a polymer as a carrier, as described above. However, only a few studies have investigated the slow release of a drug after the formation of a solid dispersion using spray-drying. Shaikh et al. 14) performed spraydrying using acetaminophen (Act) and ethylcellulose (EC) and tried to achieve a sustained release of Act. Their results demonstrated that it is possible to form a solid dispersion by dispersing Act using a spray-drying technique with EC molecules in a molecular state. They concluded that the sustained release of Act from this solid dispersion was caused by an increase in the viscosity of EC.In this study, we designed matrix particles to slowly release Act by changing the mixture ratio of chitosan and Act. Slow release in the digestive tract is attempted in this formation by using chitosan powder (Cht) as a carrier and the solid dispersion in Cht and between drugs. As expected, the absorbability of the drug from the mucosa increased, because Cht easily harmonizes with biological membrane. In addition, the dosage form design of the administration to the lung is also possible, because fine particles are prepared by a spray-drying technique. Then, the design of the particles for the slow release of the drug was tried by forming a solid dispersion by a spray-drying technique that used chitosan as the carrier. ExperimentalMaterials The acetaminophen (model drug) was supplied by Fujisawa Astor Co., Ltd., Chitosan (carrier), whose degree of deacetylation was calculated at 89.0% by amino group content with a coefficient viscosity of 7...

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Acetaminophen Particle Design Using Chitosan and a Spray-Drying Technique

et al. 2005

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“…For instance, Form I unit cell was shown to possess an intermolecular hydrogen bond network involving sulphonamide groups. 21 The IR data for the furosemide II crystalline form suggests that there is an alteration in the hydrogen bond sequence within the crystal. 22 From the above results, it can be concluded that the THz spectra differences of the polymorphic forms of furosemide are not intramolecular interactions, possibly due to the crystalline phonon and the hydrogen-bonding vibrations.…”

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Polymorphic Forms of Furosemide Characterized by THz Time Domain Spectroscopy

Min¹,

Ma²,

Wang³

2009

Bulletin of the Korean Chemical Society

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Terahertz time domain spectroscopy (THz-TDS) is applied in transmission to identify the five forms of modifications of furosemide and one commercial product from 0.3 THz to 1.6 THz at room temperature. The different absorption spectra of the different forms are sensitive to crystal structures. Density function theory (DFT) calculation was used to understand the vibrational modes of furosemide in the THz region. X-ray powder diffractometry (XRPD) was applied to confirm the different forms of modifications. The results demonstrate that THz-TDS is a potential analytical technique in investigating polymorphic forms in the pharmaceutical fields.

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“…1,2) The formation of solid dispersion using a carrier is one such method. Some researchers have proposed that increased drug dissolution rates reflect the formation of a high-energy amorphous drug phase.3) Several water-soluble polymer carrier systems, such as polyethylene glycol (PEG), [4][5][6] polyvinylpyrrolidone (PVP), 7) and hydroxypropylcellulose (HPC), 8) have been used in fast-release preparations. The mechanisms of interaction between drug and carrier in solid dispersions have also been studied.…”

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confidence: 99%

“…3) Several water-soluble polymer carrier systems, such as polyethylene glycol (PEG), [4][5][6] polyvinylpyrrolidone (PVP), 7) and hydroxypropylcellulose (HPC), 8) have been used in fast-release preparations. The mechanisms of interaction between drug and carrier in solid dispersions have also been studied.…”

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Particle Design of Three-Component System for Sustained Release Using a 4-Fluid Nozzle Spray-Drying Technique

Chen

Takahashi

Okamoto

et al. 2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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Various methods to improve the dissolution of poor watersoluble drugs have been reported. 1,2) The formation of solid dispersion using a carrier is one such method. Some researchers have proposed that increased drug dissolution rates reflect the formation of a high-energy amorphous drug phase.3) Several water-soluble polymer carrier systems, such as polyethylene glycol (PEG), [4][5][6] polyvinylpyrrolidone (PVP), 7) and hydroxypropylcellulose (HPC), 8) have been used in fast-release preparations. The mechanisms of interaction between drug and carrier in solid dispersions have also been studied. Solid dispersions of nifedipine and a carrier polymer such as hydroxypropylmethylcellulose acetate succinate (HPMCAS) were prepared by a solvent method. 9) Emara et al. 10) improved the dissolution of nifedipine prepared by a fusion method. Yamashita et al. 11) prepared the solid dispersion of tacrolimus using PEG, PVP, and hydroxypropylmethylcellulose (HPMC). We reported that naproxen-a-lactose monohydrate solid dispersions, 12,13) prepared using melting methods, supported the existence of a high-energy amorphous drug phase in systems containing more than 50% alactose monohydrate. The dissolution data suggested that the dissolution rate of this phase was 7-20-fold greater than the crystalline drug.Recently, a spray-drying technique yielded an amorphous form of crystalline drugs, such as cimetidine, that becomes amorphous when spray-dried with Cht, as reported by He et al. 14) This indicates that solid dispersion was formed when cimetidine was dispersed in Cht molecules by spray-drying. Corrigan et al. 15) tried to make an amorphous drug by spraydrying using PVP as a carrier. The dissolution rate of the drug commonly quickens when a solid dispersion is formed by using a polymer as a carrier. However, few studies have investigated the slow release of the drug after the formation of a solid dispersion using spray-drying. Shaikh et al. 16) performed a spray-drying technique using Act and ethylcellulose (EC) and tried to achieve a sustained release of Act. Their results demonstrated the possibility of forming solid dispersion by dispersing Act with a spray-drying technique with EC molecules in a molecular state. They concluded that the sustained release of Act in this solid dispersion was caused by an increase in EC viscosity.In this study, we designed composite particles to the sustained release of Act by changing the mixture ratio of Act and carriers (Cht and HPMCP). Sustained release in the digestive tract was attempted in this formation by using Cht and HPMCP as carriers and solid dispersions between the carriers and drugs. Cht dissolved after it formed a gel 17,18) in the acid solution, and HPMCP was insoluble in the acid solution. However, HPMCP dissolved in the alkaline solution, and Cht was insoluble. Sustained release of the drug was tried using such dissolution properties as the pH of the carrier. Then the particle design of a three-component system for the sustained release of the drug was tried by forming s...

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Evidence for Solid- and Liquid-State Interactions in a Furosemide-Polyvinylpyrrolidone Solid Dispersion

Cited by 67 publications

References 13 publications

Acetaminophen Particle Design Using Chitosan and a Spray-Drying Technique

Acetaminophen Particle Design Using Chitosan and a Spray-Drying Technique

Polymorphic Forms of Furosemide Characterized by THz Time Domain Spectroscopy

Particle Design of Three-Component System for Sustained Release Using a 4-Fluid Nozzle Spray-Drying Technique

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