Enhancement of dissolution rate of poorly-soluble active ingredients by supercritical fluid processes

Perrut, M.; Jung, Jennifer; Leboeuf, Francis

doi:10.1016/j.ijpharm.2004.09.007

Cited by 192 publications

(79 citation statements)

References 8 publications

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“…2,4,8,9) Recently, Perrut and colleagues reported that in some cases, after a supercritical fluid process, the dissolution rates of poorly water-soluble APIs remained in the same order of magnitude, due to re-agglomeration and wetting problems, despite a reduction in particle size and increase in surface area. 10) They emphasized the use of hydrophilic pharmaceutical excipients to enhance wettability. 11) Various hydrophilic additives, such as poloxamers, hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP), have been used to enhance dissolution properties of poorly water-soluble APIs.…”

mentioning

confidence: 99%

Enhancement of Wettability and Dissolution Properties of Cilostazol Using the Supercritical Antisolvent Process: Effect of Various Additives

Kim

Hwang

2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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confidence: 99%

Enhancement of Wettability and Dissolution Properties of Cilostazol Using the Supercritical Antisolvent Process: Effect of Various Additives

Kim

Hwang

2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Chitosan dissolves readily in most of the acid solutions and upon dissolution, amine groups of the polymer become protonated, resulting in a positively charged polysaccharide (RNH3+) and chitosan salts (chloride, 24 glutamate, etc.) that are soluble in water .The earlier literature reveals that dissolution rate not only depends on the surface area and particle size of the processed powder, but is 25 greatly affected by crystal morphology and wettability . So increased wettability of the drug by the adsorption of chitosan and chitosan chlorhydrate onto the hydrophobic surface of the drug is the first reason.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

Design and Evaluation of Rapidly Disintegrating Tablets of Racecadotril with Enhanced in-vitro Dissolution Achieved by Solid Dispersion Technique

Singhvi¹,

Gampa²,

Yadav³

et al. 2013

IJPER

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The objectives of present investigations were to enhance dissolution rate of irbesartan by using chitosan and chitosan chlorhydrate and optimize an effective concentrations of both.Cocrystals of irbesartan (IB) were prepared by solvent change technique.Chitosan solution was prepared by soaking chitosan and chitosan chlorhydrate in glacial acetic acid. A weighed amount of drug was dispersed in chitosan solution by stirring. The dispersion was added to sodium citrate solution to precipitate 0 chitosan on drug crystals. The precipitate obtained was filtered through Whatmann No. 1 filter paper using vacuum filtration unit and dried at 45 C for 24 h. The prepared cocrystals were characterized in terms of saturation solubility, drug content, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), in vitro dissolution studies and stability studies. The considerable improvement in the dissolution rate of drug from optimized co-crystal formulation was attributed to the decreased drug crystallinity, altered surface morphology and reduction in particle size. The 0.2% chitosan and 0.4% chitosan chlorhydrate were found to be optimized concentrations for enhancement of dissolution rate of irbesartan. The technique is scalable and may prove valuable in manufacturing process in future for enhancement of dissolution of poorly water soluble drugs.

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“…15,16) However, some types of drugs grow very fast in anti-solvent, and thus, it was difficult to produce nano-sized drug particles in the beaker using the anti-solvent method alone. In such a case, the spray nozzle that we developed could be more effective because these suspensions were spray-dried immediately and produced microparticles before crystallization began.…”

Section: Preparation Of Ec/man Microspheres Using a Two-solution Miximentioning

confidence: 99%

Development of a Novel and Customizable Two-Solution Mixing Type Spray Nozzle for One-Step Preparation of Nanoparticle-Containing Microparticles

Ozeki

Akiyama

Takahashi

et al. 2012

Biological & Pharmaceutical Bulletin

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Production of drug nanoparticles is an effective strategy to enhance solubility and oral absorption of water-insoluble drugs. The handling of drug nanoparticles has been an important issue in drug formulation because nanoparticles easily aggregate each other and redispersion of these particles is very difficult. In the present study, we developed a unique two-solution mixing type spray nozzle that can prepare drug nanoparticles in microparticles in one step without any common solvent and surfactant, and then, the prepared formulation were evaluated. Ethylcellulose (EC) and mannitol (MAN) were used as a model polymer of water-insoluble compound and a water-soluble carrier, respectively. We characterized the EC/MAN microparticles produced by the novel spray nozzle when customizing the nozzle parts to mix EC and MAN solution. Relatively smaller EC nanoparticles (<110 nm) in MAN microparticles (approximately 3 µm) were obtained by changing the customizable parts in the nozzle. In addition, the core of EC nanoparticles (<50 nm) was also observed by atomic force microscopy. We also found that the mixing time in the nozzle parts affected the size and the standard deviation of EC nanoparticles. These results suggest that the size of EC nanoparticles in MAN microparticles is controllable by using this unique nozzle. After all, we could prepare MAN microparticles containing EC nanoparticles in one step by using the novel nozzle. The drug/MAN microparticles formulation produced by the nozzle may be useful for the handling of drug nanoparticles.Key words two-solution mixing type nozzle; spray drier; composite particle; anti-solvent effect; one-step preparation Improvement of water-insoluble drugs has been an important issue as increasing the promising drug candidates. The use of nano-sized drugs is an effective strategy to enhance drug solubility.1-5) Several methods have been extensively employed to prepare smaller particles from large drug particles, such as the use of ball and jet mills, crystallization by evaporating the drug in an organic solvent, and preparation of emulsions and liposomes. Although these methods have advantages and disadvantages, the handling of nano-sized drug powders has been an important factor. Nanoparticles can easily aggregate with each other because of their great surface energy; hence, redispersion of these aggregates is very difficult and the effective properties derived from nanoparticles are lost. Therefore, technologies to preserve nanoparticles have been pursued.In a previous study, we developed a four-fluid nozzle spray dryer to produce microparticles containing nano-sized drug particles.6-11) This nozzle has two liquid and two gas passages that allow two compounds (e.g., a water-insoluble drug in organic solvent and a water-soluble carrier in aqueous solution) to be dissolved in separate solvents, thereby overcoming the problems of finding and using a common solvent. Although the detailed mechanism of the production of drug nanoparticles/water-soluble carrier microparticles by using the...

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Enhancement of dissolution rate of poorly-soluble active ingredients by supercritical fluid processes

Cited by 192 publications

References 8 publications

Enhancement of Wettability and Dissolution Properties of Cilostazol Using the Supercritical Antisolvent Process: Effect of Various Additives

Enhancement of Wettability and Dissolution Properties of Cilostazol Using the Supercritical Antisolvent Process: Effect of Various Additives

Design and Evaluation of Rapidly Disintegrating Tablets of Racecadotril with Enhanced in-vitro Dissolution Achieved by Solid Dispersion Technique

Development of a Novel and Customizable Two-Solution Mixing Type Spray Nozzle for One-Step Preparation of Nanoparticle-Containing Microparticles

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