Amorphous spray-dried hydroflumethiazide-polyvinylpyrrolidone systems: Physicochemical properties

Corrigan, Owen I.; Holohan, Edmond

doi:10.1111/j.2042-7158.1984.tb04353.x

Cited by 63 publications

(22 citation statements)

References 14 publications

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“…Several methods are traditionally used to produce amorphous dispersions such as melt quenching (6), hot melt extrusion (12,13), spray drying (10,14,15) and freeze drying (16,17). Milling is a technique widely used to reduce particle size (18) but is not commonly used for making amorphous dispersions, although it has been shown to be suitable to amorphise pharmaceutical compounds and to produce glassy solutions (10,(19)(20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%

Amorphous Solid Dispersions of Sulfonamide/Soluplus® and Sulfonamide/PVP Prepared by Ball Milling

Caron

Tajber

et al. 2013

AAPS PharmSciTech

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Abstract. The aim of this paper is to investigate the physicochemical properties of binary amorphous dispersions of poorly soluble sulfonamide/polymeric excipient prepared by ball milling. The sulfonamides selected were sulfathiazole (STZ), sulfadimidine (SDM), sulfamerazine (SMZ) and sulfadiazine (SDZ). The excipients were polyvinylpyrrolidone (PVP) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer, commercially known as Soluplus®. Co-milled systems were characterised by powder X-ray diffraction and differential scanning calorimetry. PVP was shown to form amorphous dispersions over a wider composition range than Soluplus® for the four sulfonamides tested. Moreover, amorphous dispersions made with PVP were homogeneous [single glass transition (Tg)], while amorphous dispersions made from Soluplus® were heterogeneous (two Tgs). This behaviour is consistent with the fact that all the sulfonamides tested presented a lower solubility in Soluplus® than in PVP, as evidenced by Flory-Huggins parameters determined. Amorphous dispersions of SDM with Soluplus® could be produced even though SDM does not amorphise alone upon milling and Soluplus® presents Tg at a lower temperature than SDM. Amorphous dispersions of SMZ could be prepared with a lower excipient concentration compared to STZ, SDM and SDZ, which may reflect the one-dimensional H-bonding network in SMZ compared to the 2D or 3D Hbonding network found in the other sulfonamides. Stability tests (60% RH/25°C) revealed that dispersions made with Soluplus® remained dry and powdery compared to those made with PVP that formed a sticky paste in less than 2 weeks, indicating a possible advantage of using Soluplus® in terms of increased physical stability under high humidity storage conditions.

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Section: Introductionmentioning

confidence: 99%

Amorphous Solid Dispersions of Sulfonamide/Soluplus® and Sulfonamide/PVP Prepared by Ball Milling

Caron

Tajber

et al. 2013

AAPS PharmSciTech

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“…The background bump in the XRD pattern corresponding to amorphousness of the compound was found to be gradually increasing from neat CBZ, physical mixture of CBZ, and PS to CBZ-PS system. The amorphous systems contain more free energy which often serves as a driving potential for solubility; therefore, these systems are more soluble as compared to that of their crystalline counterpart (30) (Fig. 7).…”

Section: Ftir Spectroscopymentioning

confidence: 99%

Porous Starch: a Novel Carrier for Solubility Enhancement of Carbamazepine

et al. 2013

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Abstract. To circumvent the solubility-related issues associated with Biopharmaceutics Classification System class II drugs, a novel porous carrier has been developed. In the present study, a process for preparation of porous starch (PS) is demonstrated. The process briefly comprises of translucent gel preparation followed by solvent replacement, drying, and sizing. Carbamazepine (CBZ) was used as a drug candidate to exhibit solubility enhancement potential of PS. PS and CBZ-loaded PS (CBZ-PS) systems were characterized with respect to IR, DSC, XRD, SEM, and dissolution kinetic studies. PS-CBZ was found to follow a Fickian behavior during dissolution. In vivo studies conducted in mice displayed a superior performance of CBZ-PS as compared to neat CBZ.

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“…Solubility is improved by distributing the medicine in molecular form in the carrier under high-energy conditions to form an amorphous solid. 12,13) Most studies in this field have concentrated on improving the dissolution of poorly water-soluble drugs. Emara et al 14) improved the dissolution of nifedipine prepared with the fusion method.…”

mentioning

confidence: 99%

Preparation of Functional Composite Particles of Salbutamol Sulfate Using a 4-Fluid Nozzle Spray-Drying Technique

Chen

Okamoto

Danjo

2008

CHEMICAL & PHARMACEUTICAL BULLETIN

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A previous study on spray-drying demonstrated that it could promote the solubility of poorly water-soluble drugs using water-soluble polymers. Here, the preparation of composite particles of salbutamol sulfate (Sb) with water-insoluble polymers, such as Eudragit ® RS (RS) or Eudragit ® RL (RL) as a carrier, was examined. Despite the water insolubility of both polymers, the permeability of water was low in the former but high in the latter. We attempted to prepare controlled release composite particles by exploiting the characteristics of these carriers. The composite particles of the three components (Sb, RS, and RL) were prepared using a 4-fluid nozzle spraydryer, and their physico-chemical and dissolution properties were compared with physical mixtures. Examination of particle morphology by scanning electron microscopy (SEM) revealed that the particles from the spraydrying process had atomized to several microns and were spherical. Analysis by X-ray diffraction and differential scanning calorimetry revealed that diffraction peaks and heat of fusion of Sb in the spray-dried samples decreased, indicating that the drug was amorphous and formed a solid dispersion. FT-IR analysis suggested that the amino group of Sb and a carbonyl group of the polymers formed a hydrogen bond. A dissolution test of Sb-RS-RL particles prepared using the 4-fluid nozzle spray-drying method showed that release rates were depressed significantly compared to the physical mixture at pH 1.2 and 6.8, and the depression was greater when RS was used instead of RL, presumably because of the permeability difference. The compression of these particles into tablets revealed that desirable controlled released dosage forms could be prepared. In addition, Sb was used to simulate an anti-asthmatic drug. For this an Andersen cascade impactor for dry powder inhalers was used to investigate delivery to the lungs.

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Amorphous spray-dried hydroflumethiazide-polyvinylpyrrolidone systems: Physicochemical properties

Cited by 63 publications

References 14 publications

Amorphous Solid Dispersions of Sulfonamide/Soluplus® and Sulfonamide/PVP Prepared by Ball Milling

Amorphous Solid Dispersions of Sulfonamide/Soluplus® and Sulfonamide/PVP Prepared by Ball Milling

Porous Starch: a Novel Carrier for Solubility Enhancement of Carbamazepine

Preparation of Functional Composite Particles of Salbutamol Sulfate Using a 4-Fluid Nozzle Spray-Drying Technique

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