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Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator.
Int J Pharm. 2018 Apr 25; 541(1-2):246-252.IJ

Abstract

Water-soluble polymers with high viscosity are frequently used in the design of sustained-release formulations of poorly water-soluble drugs to enable complete release of the drug in the gastrointestinal tract. Tablets containing matrix granules with a water-soluble polymer are preferred because tablets are easier to handle and the multiple drug-release units of the matrix granules decreases the influences of the physiological environment on the drug. However, matrix granules with a particle size of over 800 μm sometimes cause a content uniformity problem in the tableting process because of the large particle size. An effective method of manufacturing controlled-release matrix granules with a smaller particle size is desired. The aim of this study was to develop tablets containing matrix granules with a smaller size and good controlled-release properties, using phenytoin as a model poorly water-soluble drug. We adapted the recently developed hollow spherical granule granulation technology, using water-soluble polymers with different viscosities. The prepared granules had an average particle size of 300 μm and sharp particle size distribution (relative width: 0.52-0.64). The values for the particle strength of the granules were 1.86-1.97 N/mm2, and the dissolution profiles of the granules were not affected by the tableting process. The dissolution profiles and the blood concentration levels of drug released from the granules depended on the viscosity of the polymer contained in the granules. We succeeded in developing the desired controlled-release granules, and this study should be valuable in the development of sustained-release formulations of poorly water-soluble drugs.

Authors+Show Affiliations

Sumitomo Dainippon Pharma Co., Ltd., 3-45 Kurakakiuchi 1-chome, Ibaraki-shi, Osaka 567-0878, Japan. Electronic address: takumi-asada@ds-pharma.co.jp.School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.Sumitomo Dainippon Pharma Co., Ltd., 3-45 Kurakakiuchi 1-chome, Ibaraki-shi, Osaka 567-0878, Japan.School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29496456

Citation

Asada, Takumi, et al. "Formulation of a Poorly Water-soluble Drug in Sustained-release Hollow Granules With a High Viscosity Water-soluble Polymer Using a Fluidized Bed Rotor Granulator." International Journal of Pharmaceutics, vol. 541, no. 1-2, 2018, pp. 246-252.
Asada T, Yoshihara N, Ochiai Y, et al. Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator. Int J Pharm. 2018;541(1-2):246-252.
Asada, T., Yoshihara, N., Ochiai, Y., Kimura, S. I., Iwao, Y., & Itai, S. (2018). Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator. International Journal of Pharmaceutics, 541(1-2), 246-252. https://doi.org/10.1016/j.ijpharm.2018.02.043
Asada T, et al. Formulation of a Poorly Water-soluble Drug in Sustained-release Hollow Granules With a High Viscosity Water-soluble Polymer Using a Fluidized Bed Rotor Granulator. Int J Pharm. 2018 Apr 25;541(1-2):246-252. PubMed PMID: 29496456.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator. AU - Asada,Takumi, AU - Yoshihara,Naoki, AU - Ochiai,Yasushi, AU - Kimura,Shin-Ichiro, AU - Iwao,Yasunori, AU - Itai,Shigeru, Y1 - 2018/02/27/ PY - 2017/10/31/received PY - 2018/02/21/revised PY - 2018/02/25/accepted PY - 2018/3/3/pubmed PY - 2018/9/8/medline PY - 2018/3/3/entrez KW - Controlled release KW - Granulation KW - High drug-loaded granule KW - Hollow spherical particle KW - Rotary fluidized bed granulator KW - Tablet SP - 246 EP - 252 JF - International journal of pharmaceutics JO - Int J Pharm VL - 541 IS - 1-2 N2 - Water-soluble polymers with high viscosity are frequently used in the design of sustained-release formulations of poorly water-soluble drugs to enable complete release of the drug in the gastrointestinal tract. Tablets containing matrix granules with a water-soluble polymer are preferred because tablets are easier to handle and the multiple drug-release units of the matrix granules decreases the influences of the physiological environment on the drug. However, matrix granules with a particle size of over 800 μm sometimes cause a content uniformity problem in the tableting process because of the large particle size. An effective method of manufacturing controlled-release matrix granules with a smaller particle size is desired. The aim of this study was to develop tablets containing matrix granules with a smaller size and good controlled-release properties, using phenytoin as a model poorly water-soluble drug. We adapted the recently developed hollow spherical granule granulation technology, using water-soluble polymers with different viscosities. The prepared granules had an average particle size of 300 μm and sharp particle size distribution (relative width: 0.52-0.64). The values for the particle strength of the granules were 1.86-1.97 N/mm2, and the dissolution profiles of the granules were not affected by the tableting process. The dissolution profiles and the blood concentration levels of drug released from the granules depended on the viscosity of the polymer contained in the granules. We succeeded in developing the desired controlled-release granules, and this study should be valuable in the development of sustained-release formulations of poorly water-soluble drugs. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/29496456/Formulation_of_a_poorly_water_soluble_drug_in_sustained_release_hollow_granules_with_a_high_viscosity_water_soluble_polymer_using_a_fluidized_bed_rotor_granulator_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(18)30124-8 DB - PRIME DP - Unbound Medicine ER -