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Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation.
Chem Pharm Bull (Tokyo). 2015; 63(12):1070-5.CP

Abstract

The effect of some drug properties (wettability and particle size distribution) on granule properties (mean particle size, particle size distribution, sphericity, and granule strength) were investigated in a high (>97%) drug-loading formulation using fluidized bed rotor granulation. Three drugs: acetaminophen (APAP); ibuprofen (IBU); and ethenzamide (ETZ) were used as model drugs based on their differences in wettability and particle size distribution. Granules with mean particle sizes of 100-200 µm and a narrow particle size distribution (PSD) could be prepared regardless of the drug used. IBU and ETZ granules showed a higher sphericity than APAP granules, while APAP and ETZ granules exhibited higher granule strength than IBU. The relationship between drug and granule properties suggested that the wettability and the PSD of the drugs were critical parameters affecting sphericity and granule strength, respectively. Furthermore, the dissolution profiles of granules prepared with poorly water-soluble drugs (IBU and ETZ) showed a rapid release (80% release in 20 min) because of the improved wettability with granulation. The present study demonstrated for the first time that fluidized bed rotor granulation can prepare high drug-loaded (>97%) globular granules with a mean particle size of less than 200 µm and the relationship between physicochemical drug properties and the properties of the granules obtained could be readily determined, indicating the potential for further application of this methodology to various drugs.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Mise R
Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka.
Iwao Y
No affiliation info available
Kimura S
No affiliation info available
Osugi Y
No affiliation info available
Noguchi S
No affiliation info available
Itai S
No affiliation info available

MeSH

AcetaminophenChemistry, PhysicalIbuprofenParticle SizeSalicylamidesWettability

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26633029

Citation

Mise, Ryohei, et al. "Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation." Chemical & Pharmaceutical Bulletin, vol. 63, no. 12, 2015, pp. 1070-5.
Mise R, Iwao Y, Kimura S, et al. Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation. Chem Pharm Bull (Tokyo). 2015;63(12):1070-5.
Mise, R., Iwao, Y., Kimura, S., Osugi, Y., Noguchi, S., & Itai, S. (2015). Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation. Chemical & Pharmaceutical Bulletin, 63(12), 1070-5. https://doi.org/10.1248/cpb.c15-00491
Mise R, et al. Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation. Chem Pharm Bull (Tokyo). 2015;63(12):1070-5. PubMed PMID: 26633029.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Investigation of Physicochemical Drug Properties to Prepare Fine Globular Granules Composed of Only Drug Substance in Fluidized Bed Rotor Granulation. AU - Mise,Ryohei, AU - Iwao,Yasunori, AU - Kimura,Shin-Ichiro, AU - Osugi,Yukiko, AU - Noguchi,Shuji, AU - Itai,Shigeru, PY - 2015/12/4/entrez PY - 2015/12/4/pubmed PY - 2016/7/13/medline SP - 1070 EP - 5 JF - Chemical & pharmaceutical bulletin JO - Chem Pharm Bull (Tokyo) VL - 63 IS - 12 N2 - The effect of some drug properties (wettability and particle size distribution) on granule properties (mean particle size, particle size distribution, sphericity, and granule strength) were investigated in a high (>97%) drug-loading formulation using fluidized bed rotor granulation. Three drugs: acetaminophen (APAP); ibuprofen (IBU); and ethenzamide (ETZ) were used as model drugs based on their differences in wettability and particle size distribution. Granules with mean particle sizes of 100-200 µm and a narrow particle size distribution (PSD) could be prepared regardless of the drug used. IBU and ETZ granules showed a higher sphericity than APAP granules, while APAP and ETZ granules exhibited higher granule strength than IBU. The relationship between drug and granule properties suggested that the wettability and the PSD of the drugs were critical parameters affecting sphericity and granule strength, respectively. Furthermore, the dissolution profiles of granules prepared with poorly water-soluble drugs (IBU and ETZ) showed a rapid release (80% release in 20 min) because of the improved wettability with granulation. The present study demonstrated for the first time that fluidized bed rotor granulation can prepare high drug-loaded (>97%) globular granules with a mean particle size of less than 200 µm and the relationship between physicochemical drug properties and the properties of the granules obtained could be readily determined, indicating the potential for further application of this methodology to various drugs. SN - 1347-5223 UR - https://www.unboundmedicine.com/medline/citation/26633029/Investigation_of_Physicochemical_Drug_Properties_to_Prepare_Fine_Globular_Granules_Composed_of_Only_Drug_Substance_in_Fluidized_Bed_Rotor_Granulation_ DB - PRIME DP - Unbound Medicine ER -