Preparation of griseofulvin microparticles by supercritical fluid expansion depressurization process

Li, Zhiyi; Jiang, Jingzhi; Liu, Xuewu; Shunxuan, Zhao; Yuanjing, Xia; Wang, Jian

doi:10.1016/j.powtec.2007.07.016

Cited by 13 publications

(5 citation statements)

References 8 publications

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“…In this work, griseofulvin (GF), an antifungal agent, was chosen as a poorly water-soluble, highly hydrophobic model drug having a solubility of about 12 ppm . Micronization of GF has been attempted by many researchers, − mainly using various supercritical fluid techniques (see Table ), and often, long bipyramidal needle-shaped particles with sizes up to several micrometers have been precipitated. The LAS process has also been used to precipitate GF particles, with chloroform as the solvent and hexane and HFE-7100 as antisolvents.…”

Section: Introductionmentioning

confidence: 99%

Controlling Particle Size of a Poorly Water-Soluble Drug Using Ultrasound and Stabilizers in Antisolvent Precipitation

Dalvi

Davé

2009

Ind. Eng. Chem. Res.

198

124

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The objective of this work was to develop a better understanding of a potentially scalable, liquid antisolvent (LAS) precipitation process, for the preparation of stable aqueous suspensions of ultrafine particles of poorly watersoluble active pharmaceutical ingredients (APIs). A novel combination of jets, ultrasound, polymers, and surfactants was used for the precipitation and stabilization of ultrafine particles of griseofulvin (GF). Use of ultrasound and high stream velocities enhances micromixing, whereas addition of polymers/surfactants inhibits/lowers the particle growth. A combination of ultrasound, high jet velocities, and stabilizers decreased the GF particle size to 1.04 µm ((0.46 µm) from 30.8 µm ((14.2 µm), when none of the treatments were used. A rational understanding was developed for predicting process performance and selecting suitable particle growth inhibitors/stabilizers. Favorable process conditions and combinations of polymer and surfactants were also identified experimentally for the precipitation of ultrafine particles of GF with a narrow particle size distribution (PSD).

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Section: Introductionmentioning

confidence: 99%

Controlling Particle Size of a Poorly Water-Soluble Drug Using Ultrasound and Stabilizers in Antisolvent Precipitation

Dalvi

Davé

2009

Ind. Eng. Chem. Res.

198

124

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“…-Particle generation and co-precipitation: In the pharmaceutical industry, fine particles (μm or nm) with uniform narrow size range are of particular interest. Various supercritical (SCF) processes for particle formation include: i) Rapid expansion of supercritical solutions (RESS): involves a fast depressurization of saturated supercritical fluid-drug solution through a heated nozzle into a low pressure vessel that produces a rapid nucleation of the substrate in form of very small particles 113 .…”

Section: Pharmaceuticalmentioning

confidence: 99%

Membrane Separation

Voutsas¹

2014

Food Engineering Handbook

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Supercritical fluid extraction (SFE) has become one of the most popular green extraction techniques nowadays since it has demonstrated many advantages compared to traditional or classical extraction processes. Aspects such as improved selectivity, higher extraction yields, better fractionation capabilities and lower environmental impacts have been crucialto the important growth of SFE. In this chapter, fundamentals of SFE are presented together with the most important variables that can affect the extraction process and how to tune them. Moreover, interesting and new applications in different areas such as food science, pharmaceutical and others like, for instance, heavy metals recovery are presented.

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“…Understanding the change in the morphology of precipitated GF particles due to changes in mixing conditions (ultrasound vs stirring) and the use of additives was the main focus of this work. Interestingly, as can be seen from Table , there are several reports available in the literature on precipitation of GF particles, ,,− ,− and the morphologies observed for GF range from spheres , to bipyramids , to needles. , However, formation of hyperbranched structures of GF and their mechanism thereof has not yet been reported. Therefore, in this work possible mechanisms for evolution of different hierarchical GF morphologies in the presence of different additives and use of ultrasound have been discussed.…”

Section: Introductionmentioning

confidence: 99%

Understanding Morphological Evolution of Griseofulvin Particles into Hierarchical Microstructures during Liquid Antisolvent Precipitation

Prasad

Dalvi

2019

Crystal Growth & Design

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Controlling morphology of active pharmaceutical ingredients (APIs) during crystallization/precipitation is essential for pharmaceutical development since the pharmaceutical powder properties such as solubility, flowability, and dissolution rates are morphology dependent. The objective of this work was to understand the morphological evolution of a poorly water-soluble antifungal drug, griseofulvin (GF), during liquid antisolvent (LAS) precipitation in the presence of ultrasound and additives. GF was found to precipitate as hierarchical structures in the presence of different additives and in the absence of ultrasound. An umbrella-like morphology was observed when hydroxypropyl methylcellulose was used, hexagonal particles elongated along the central axis were obtained in the presence of Tween 80, and the use of polyvinylpyrrolidone yielded long needle-like particles. The most fascinating morphology was observed in the case of bovine serum albumin and no ultrasound, where the GF particles precipitated as six-branched hierarchical structures. Interestingly, the morphology of 6-month-old GF particles reveals that the outline of the overall morphology of initial unfilled skeletons resembled the bipyramidal morphology that would form when particles are completely filled/fused due to Ostwald ripening. The size of GF particles typically varied from 30 to 50 μm when no ultrasound was used. Time-resolved scanning electron microscopy (SEM) studies imply that interesting morphologies of GF particles observed in the absence of ultrasound could be the result of aggregation and fusion of a large number of small particles formed in the beginning of the precipitation process. These smaller particles fuse to form primary bipyramidal particles which then undergo diffusion-limited growth through Ostwald ripening and secondary nucleation on specific particle faces due to selective adsorption of additives depending on the functional groups present on those particular faces. In contrast to the no ultrasound situation, the use of ultrasound along with the additives resulted in the formation of completely filled octahedron/bipyramidal GF particles irrespective of the additive used. These particles were significantly smaller with sizes ranging from 4 to 6 μm. Use of ultrasound improves micromixing and alters the particle growth mechanism from diffusion limited to integration controlled resulting in smaller and well-formed GF particles.

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Preparation of griseofulvin microparticles by supercritical fluid expansion depressurization process

Cited by 13 publications

References 8 publications

Controlling Particle Size of a Poorly Water-Soluble Drug Using Ultrasound and Stabilizers in Antisolvent Precipitation

Controlling Particle Size of a Poorly Water-Soluble Drug Using Ultrasound and Stabilizers in Antisolvent Precipitation

Membrane Separation

Understanding Morphological Evolution of Griseofulvin Particles into Hierarchical Microstructures during Liquid Antisolvent Precipitation

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