Influence of Particle Design on Oral Absorption of Poorly Water-Soluble Drug in a Silica Particle–Supercritical Fluid System
スポンサーリンク
概要
- 論文の詳細を見る
The physicochemical characteristics and oral absorption of a poorly water-soluble drug, K-832, adsorbed onto porous silica (Sylysia 350), were compared with those of K-832 adsorbed onto non-porous silica (Aerosil 200). K-832 and silica were treated with supercritical CO2 (scCO2) to produce K-832-Sylysia 350 and K-832-Aerosil 200 formulations. Scanning electron microscopy, polarizing microscopy, powder X-ray diffraction, and differential scanning calorimetry results suggested that K-832 mainly existed in an amorphous state in both formulations. The specific surface area of both formulations was much larger than that of pure K-832 crystals. The dissolution rate of K-832 from both formulations was considerably greater than that from corresponding physical mixtures due to rapid wetting of the hydrophilic carrier surfaces and amorphous state, the dissolution from the K-832-Sylysia 350 formulation being the fastest. In vivo absorption tests on the two formulations indicated no significant differences in their peak concentration (Cmax) and the area under their plasma concentration–time curve (AUC), while the concentrations of K-832 in the K-832-Sylysia 350 formulation were significantly higher than those in the K-832-Aerosil 200 formulation 1 h and 1.5 h after administration of these formulations (p<0.05). This could be attributed to the different dispersion states of K-832 in the formulations due to their different three-dimensional structures (porous and non-porous). In physical stability tests, the amorphous drugs in both formulations were stable at room temperature for at least 14 months. Thus, the absorption of poorly water-soluble drugs could be greatly improved by adsorption onto porous silica using scCO2.
- 公益社団法人 日本薬学会の論文
著者
-
TERADA Katsuhide
Faculty of Pharmaceutical Sciences, Toho University
-
Terada Katsuhide
Faculty Of Pharmaceutical Sciences Chiba University
-
KANEBAKO Makoto
Fuji Research Laboratories, Pharmaceutical Division, Kowa Company, LTD.
-
INAGI Toshio
Fuji Research Laboratories, Pharmaceutical Division, Kowa Company, LTD.
-
Miura Hiroshi
Fuji Research Laboratories, Pharmaceutical Division, Kowa Co., Ltd.
-
Shirai Hiroyuki
Fuji Research Laboratories, Pharmaceutical Division, Kowa Co., Ltd.
-
Nakao Hiroshi
Fuji Research Laboratories, Pharmaceutical Division, Kowa Co., Ltd.
-
Kanebako Makoto
Fuji Research Laboratories, Pharmaceutical Division, Kowa Co., Ltd.
-
Inagi Toshio
Fuji Research Laboratories, Pharmaceutical Division, Kowa Co., Ltd.
関連論文
- Development of Fast Disintegrating Compressed Tablets Using Amino Acid as Disintegratation Accelerator : Evaluation of Wetting and Disintegration of Tablet on the Basis of Surface Free Energy
- STUDY OF FREEZE-DRYING IN DRUG-ADDITIVE BINARY SYSTEM
- POSSIBLE MECHANISM BEHIND THE INTERACTIONS BETWEEN POROUS POWDER AND CRYSTALLINE MEDICINALS
- Evaluation of Skin Barrier Function Using Direct Current II : Effects of Duty Cycle, Waveform, Frequency and Mode
- Evaluation of Skin Barrier Function Using Direct Current I : Effects of Conductivity, Voltage, Distance between Electrodes and Electrode Area
- Transdermal Delivery of Indomethacin by lontophoresis
- Evaluation of Skin Barrier Function Using Direct Current III: Effects of Electrode Distance, Boundary Length and Shape
- Application of Eudragit RS to Thermo-Sensitive Drug Delivery Systems. I. Thermo-Sensitive Drug Release from Acetaminophen Matrix Tablets Consisting of Eudragit RS/PEG 400 Blend Polymers
- POLYMORPHISM OF TEGAFUR
- Quantification of Pharmaceutical Polymorphs and Prediction of Dissolution Rate Using Theophylline Tablet by Terahertz Spectroscopy
- Freeze-Drying of Proteins in Glass Solids Formed by Basic Amino Acids and Dicarboxylic Acids
- Stabilization of Protein Structure in Freeze-Dried Amorphous Organic Acid Buffer Salts
- Glass-State Amorphous Salt Solids Formed by Freeze-Drying of Amines and Hydroxy Carboxylic Acids : Effect of Hydrogen-Bonding and Electrostatic Interactions
- Influence of Particle Design on Oral Absorption of Poorly Water-Soluble Drug in a Silica Particle–Supercritical Fluid System
- BEHAVIOUR OF MEDICINAL MOLECULES IN THE INCLUSION COMPOUNDS OR GROUND MIXTURES WITH CYCLODEXTRINS
- PHYSICOCHEMICAL PROPERTIES OF TRI-O-METHYL-β-CYCLODEXTRIN AND ITS INTERACTIONS WITH DRUGS
- Application and Mechanism of Inhalation Profile Improvement of DPI Formulations by Mechanofusion with Magnesium Stearate
- Novel Approach to DPI Carrier Lactose with Mechanofusion Process with Additives and Evaluation by IGC
- Chemical Mapping of Hydration and Dehydration Process of Theophylline in Tablets Using Terahertz Pulsed Imaging
- Component Crystallization and Physical Collapse during Freeze-Drying of L-Arginine–Citric Acid Mixtures
- Do Amorphous Troglitazones Prepared from Two Diastereomer-Pairs Have the Same Molecular Mobility and Crystallization Rate at the Surface?
- Freeze-Drying of Proteins in Glass Solids Formed by Basic Amino Acids and Dicarboxylic Acids
- Using Terahertz Reflectance Spectroscopy to Quantify Drug Substance in Tablets
- Practical Approach for Measuring Heat Capacity of Pharmaceutical Crystals/Glasses by Modulated-Temperature Differential Scanning Calorimetry
- Effects of Phosphate Buffer in Parenteral Drugs on Particle Formation from Glass Vials