Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method

›› 2009, Vol. 17 ›› Issue (2): 318-323.

Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method

赵宏¹, 王洁欣¹, 张海霞¹, 沈志刚^1,2, 甄崇礼², 陈建峰¹

1. Sin-China Nano Technology Center, Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing 10029, China;
2. Nanomaterials Technology Pte. Ltd., Singapore

收稿日期:2008-09-03 修回日期:2008-11-11 出版日期:2009-04-28 发布日期:2009-04-28
通讯作者: CHEN Jianfeng,E-mail:chenjf@mail.buct.edu.cn
基金资助:
Supported by the National High Technology Research and Development Program of China (2006AA030202);the Talent Training Program of Beijing (2007B022)

Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method

ZHAO Hong¹, WANG Jiexin¹, ZHANG Haixia¹, SHEN Zhigang^1,2, Jimmy Yun², CHEN Jianfeng¹

1. Sin-China Nano Technology Center, Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing 10029, China;
2. Nanomaterials Technology Pte. Ltd., Singapore

Received:2008-09-03 Revised:2008-11-11 Online:2009-04-28 Published:2009-04-28
Supported by:
Supported by the National High Technology Research and Development Program of China (2006AA030202);the Talent Training Program of Beijing (2007B022)

摘要/Abstract

摘要： The nanoparticles of the hydrophobic drug of danazol with narrow size distribution are facilely prepared by controlled high-gravity anti-solvent precipitation(HGAP) process.Intensified micromixing and uniform nucleation environment are created by the high-gravity equipment(rotating packed bed) in carrying out the anti-solvent precipitation process to produce nanoparticles.The average particle size decreases from 55 μm of the raw danazol to 190 nm of the nanoparticles.The Brunauer-Emmett-Teller(BET) surface area sharply increases from 0.66 m²·g^-1 to 15.08 m²·g^-1.Accordingly,the dissolution rate is greatly improved.The molecular state,chemical composition,and crystal form of the danazol nanoparticles remains unchanged after processing according to Fourier transform infrared(FTIR) and X-ray diffraction(XRD).The high recovery ratio and continuous production capacity are highly appreciated in industry.Therefore,the HGAP method might offer a general and facile platform for mass production of hydrophobic pharmaceutical danazol particles in nanometer range.

关键词: high-gravity antisolvent precipitation,rotating packed bed, danazol,nanoparticles,dissolution rate

Abstract: The nanoparticles of the hydrophobic drug of danazol with narrow size distribution are facilely prepared by controlled high-gravity anti-solvent precipitation(HGAP) process.Intensified micromixing and uniform nucleation environment are created by the high-gravity equipment(rotating packed bed) in carrying out the anti-solvent precipitation process to produce nanoparticles.The average particle size decreases from 55 μm of the raw danazol to 190 nm of the nanoparticles.The Brunauer-Emmett-Teller(BET) surface area sharply increases from 0.66 m²·g^-1 to 15.08 m²·g^-1.Accordingly,the dissolution rate is greatly improved.The molecular state,chemical composition,and crystal form of the danazol nanoparticles remains unchanged after processing according to Fourier transform infrared(FTIR) and X-ray diffraction(XRD).The high recovery ratio and continuous production capacity are highly appreciated in industry.Therefore,the HGAP method might offer a general and facile platform for mass production of hydrophobic pharmaceutical danazol particles in nanometer range.

Key words: high-gravity antisolvent precipitation,rotating packed bed, danazol,nanoparticles,dissolution rate

赵宏, 王洁欣, 张海霞, 沈志刚, 甄崇礼, 陈建峰. Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method[J]. , 2009, 17(2): 318-323.

ZHAO Hong, WANG Jiexin, ZHANG Haixia, SHEN Zhigang, Jimmy Yun, CHEN Jianfeng. Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method[J]. , 2009, 17(2): 318-323.

参考文献

1 Lipinski, C., “Poor aqueous solubility-An industry wide problem in drug delivery”, Am. Pharm. Rev., 5, 82-85 (2002).
2 Radtke, M., “Pure drug nanoparticles for the formulation of poorly soluble drugs”, New Drugs, 3, 62-68 (2001).
3 Liversidge, G.G., Cundy, K.C., “Particle size reduction for improvement of oral bioavailability of hydrophobic drygs:I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs”, Int. J. Pharm., 125, 91-97 (1995).
4 Rawlings, E.A., Tindall, B., Bentley's Textbook of Pharmaceutics, Baillière Tindall London (1977).
5 Hu, J.H., Rogers, T.L., Brown, J., Young, T., Johnston, K.P., Williams, R.O., “Improvement of dissolution rates of poorly water soluble APIs using novel spray freezing into liquid technology”, Pharm. Res., 19, 1278-1284 (2002).
6 Rasenack, N., Müller, B.W., “Dissolution rate enhancement by in situ micronization of poorly water-soluble drugs”, Pharm. Res., 19, 1894-900 (2002).
7 Ripple, E.G., Powders:Remington's Pharmaceutical Sciences, 17th Edition, Gennaro, A.R., eds., Mack Publishing Co., Easton, PA (1985).
8 Liversidge, G.G., Conzentino, P., “Drug particle size reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats”, Int. J. Pharm., 125, 309-313 (1995).
9 Vivek, K., Meenakshi, B., Harish, D., Deepak, K., “Nanoparticle technology for the delivery of poorly water-soluble drugs”, Pharm. Tech., 30 (2), 82-92 (2006).
10 Esclisa-Díaz, M.T., Guimaraens-Méndez, M., Pérez-Marcos, M.B., Vila-Jato, J.L., Torres-Labandeira, J.J., “Characterization and in vitro dissolution behaviour of ketoconazole/βand 2-hydroxypropyl-βcyclodextrin inclusion compounds”, Int. J. Pharm., 143, 203-210 (1996).
11 Elversson, J., Millqvist-Fureby, A., Alderborn, G., Elofsson, U., “Droplet and particle size relationship and shell thickness of inhalable lactose particles during spray drying”, J. Pharm. Sci., 92, 900-910 (2003).
12 Domingo, C., Berends, E., van Rosmalen, G.M., “Precipitation of ultrafine organic crystals from the rapid expansion of supercritical solutions over a capillary and a frit nozzle”, J. Supercrit. Fluids, 10, 39-55 (1997).
13 Reverchon, E., Porta, G.D., “Production of antibiotic microand nano-particles by supercritical anti-solvent precipitation”, Powder Tech., 106, 23-29 (1999).
14 Chattopadhyay, P., Gupta, R.B., “Production of griseofulvin nanoparticles using supercritical CO₂ antisolvent with enhanced mass transfer”, Int. J. Pharm., 228, 19-31 (2001).
15 Violanto, M.R., Fischer, H.W., “Method for making uniformly sized particles from water-insoluble organic compounds”, US Pat., 4826689 (1989).
16 Ruch, F., Matijevi , E., “Preparation of micrometer size Budesonide particles by precipitation”, J. Colloid and Interf. Sci., 229, 207-211 (2000).
17 Cushing, B.L., Kolesnichenko, V.L., O'Connor, C.J., “Recent advances in the liquid-phase syntheses of inorganic nanoparticles”, Chem. Rev., 104, 3893-3946 (2004).
18 Mersmann, A., “Crystallization and precipitation”, Chem. Eng. & Process., 38, 345-353 (1999).
19 Grenman, H., Murzina, E., Ronnholm, M., Eranen, K., Mikkola, J.P., Lahtinen, M., Salmi, T., Murzin, D.Y., “Enhancement of solid dissolution by ultrasound”, Chem. Eng. & Process., 46, 862-869 (2007).
20 Rao, D.P., Bhowal, A., Goswami, P.S., “Process intensification in rotating packed beds (higee):An appraisal”, Ind. & Eng. Chem. Res., 43, 1150-1162 (2004).
21 Akay, G., Tong, L., Addleman, R., “Process intensification in particle technology:intensive granulation of powders by thermomechanically induced melt fracture”, Ind. & Eng. Chem. Res., 41, 5436-5446 (2002).
22 Chen, J.F., Wang, Y.H., Guo, F., Wang, X.M., Zheng, C., “Synthesis of nanoparticles with novel technology:high gravity reactive precipitation”, Ind. Eng. Chem. Res., 39, 948-954 (2000).
23 Hessel, V., Lowe, H., Schonfeld, F., “Micromixers-A review on passive and active mixing principles”, Chem. Eng. Sci., 60, 2479-2501 (2005).
24 Chen, J.F., Shao, L., “Mass production of nanoparticles by high gravity reactive precipitation technology with low cost”, China Particuology, 1, 64-69 (2003).
25 Chen, J.F., Zhou, M.Y., Shao, L., Wang, Y.Y., Yun, J., Chew, N.Y., Chan, H.K., “Feasibility of preparing nanodrugs by high-gravity reactive precipitation”, Int. J. Pharm., 269, 267-274 (2004).
26 Hu, T.T., Wang, J.X., Shen, Z.G., Chen, J.F., “Engineering of drug nanoparticles by HGCP for pharmaceutical applications”, Particuology, 6, 239-251 (2008).
27 Yang, H.J., Chu, G.W., Zhang, J.W., Shen, Z.G., Chen, J.F., “Micromixing efficiency in a rotating packed bed:Experiments and simulation”, Ind. Eng. Chem. Res., 44, 7730-7737 (2005).
28 Kucher, M., Babic, D., Kind, M., “Precipitation of barium sulfate:Experimental investigation about the influence of supersaturation and free lattice ion ratio on particle formation”, Chem. Eng. & Process., 45, 900-907 (2006).
29 Horn, D., Rieger, J., “Organic nanoparticles in the aqueous phase-theory, experiment, and use”, Angew. Chem. Int. Ed. Engl., 40, 4330-4361 (2001).
30 Dirksen, J.A., Ring, T.A., “Fundamentals of crystallization:kinetic effects on particle size distributions and morphology”, Chem. Eng. Sci., 46, 2389-2427 (1991).
31 Lobenberg, R., Amidon, G.L., Modern bioavailability, “bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards”, Eur. J. Pharm. Biopharm., 50, 3-12 (2000).

Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method

Facile Preparation of Danazol Nanoparticles by High-Gravity Anti-solvent Precipitation(HGAP) Method

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