Sustained Release of Flufenamic Acid from a Drug-Triacetyl-β-Cyclodextrin Complex
スポンサーリンク
概要
- 論文の詳細を見る
Triacetyl-β-cyclodextrin (TA-β-CyD), a hydrophobic cyclodextrin derivative that is insoluble in water, was used to form a complex with flufenamic acid (FA). Complexes of FA with TA-β-CyD (FA-TA-β-CyD) at various molar ratios (1 : 1,1 : 2,1 : 3) were prepared by a kneading method, using ethanol as a solvent. FA-TA-β-CyD complex formation was demonstrated by differential scanning calorimetry and powder X-ray diffractometry. The release rate of FA from the FA-TA-β-CyD complexes was measured in both the Japanese Pharmacopoeia XII 1st fluid pH 1.2 and isotonic phosphate buffer pH 6.8. The release rate of FA from the FA-TA-β-CyD complexes in the isotonic phosphate buffer pH 6.8 was significantly retarded compared to the release rate of FA from the FA-glucose mixture. After 1 h, 100% of the drug was released from the FA-glucose mixture and 10-25% was released from the complexes. When either the powder of the FA-glucose mixture or the FA-TA-β-CyD mixture was administered directly into the intraduodenal lumen in rats, the plasma concentration of FA reached a maximum level within 40 min after administration. On the other hand, when the FA-TA-β-CyD complexes were administered into the intraduodenal lumen, the plasma concentration of FA did not show a sharp peak, but remained at a plateau level (10-18 μg/ml) for 6-8 h. An increased mean residence time of FA following FA-TA-β-CyD complexes administration was observed; however, the AUC_<0-10> for the FA-TA-β-CyD complexes showed no significant difference from that for the FA-TA-β-CyD mixture. These results indicate that TA-β-CyD may serve as a hydrophobic carrier in sustained-release preparations of FA.The drug-TA-β-CyD complexes may therefore be useful in oral administration to achieve prolonged action and reduced side effects.
- 公益社団法人日本薬学会の論文
- 1997-01-15
著者
-
NADAI Tanekazu
Faculty of Pharmaceutical Sciences, Setsunan University
-
NAKANISHI KUNIO
Faculty of Pharmaceutical Sciences, Setsunan University
-
MASUKAWA TOHRU
Faculty of Pharmaceutical Sciences, Osaka University
-
OKADA Satoshi
National Institute of Health Sciences
-
Nadai Tanekazu
Faculty Of Pharmaceutical Sciences Setsunan University
-
Nadai Tanekazu
Faculty Of Pharmaceutical Sciences Josai University
-
Masukawa T
Setsunan Univ. Osaka Jpn
-
Nakanishi Kunio
Faculty Of Pharmaceutical Sciences Setsunan University
-
YOSHII Kimihiko
National Institute of Hygienic Sciences, Osaka Branch
-
MIYAJIMA Kouichiro
Faculty of Pharmaceutical Sciences, Kyoto University
-
Yoshii Kimihiko
National Institute Of Hygienic Sciences Osaka Branch
-
Miyajima Kouichiro
Faculty Of Pharmaceutical Sciences Kyoto University
-
Nakanishi Kunio
Faculty of Pharmaceutical Science, Setsunan University
関連論文
- EVALUATION OF DRUG DISPOSITION IN BRAIN BY MOMENT ANALYSIS (II)
- ELECTROPHYSIOLOGICAL INVERSTIGATIONS ON THE DRUG PERMEATION ACROSS STRATUM CORNEUM (I)
- Effects of Sodium or Glucose Exclusion from the Incubation Medium on Drug Transfer across Rat Jejunal Membrane in Vitro : An Electrophysiological Study(Pharmaceutical)
- EFFECTS OF ABSORPTION PROMOTERS ON THE SELECTIVE PERMEABILITY OF RAT INTESTINAL MEMBRANE TO IONS : ANALYSIS OF PERMEABILITY ENHANCING MECHANISMS BY USING DIFFUSION POTENTIALS
- INVESTIGATIONS OF INFLUX AND ACCUMULATION PROCESSES OF β-LACTAM ANTIBIOTICS AND THEIR ROLE IN THE TRANSMURAL TRANSFER ACROSS RAT JEJUNUM
- FURTHER INVESTIGATIONS ON THE TRANSPORT MECHANISM OF CEPHALEXIN AND AMPICILLIN ACROSS RAT JEJUNUM
- EFFECT OF PHARMACEUTICAL ADJUVANTS ON THE RECTAL PERMEABILITY OF DRUGS
- Quantitative Evaluation of the Gastrointestinal Absorption of Protein into the Blood and Lymph Circulation
- INFLUENCE OF DIETHYLMALEATE ON THE FORMATION OF BIS(METHYLMERCURIC)SELENIDE AND METHYLMERCURY DISTRIBUTION IN RATS
- Hyaluronate Depolymerization Following Thermal Decomposition of Oxytetracycline
- DRUG-CARRIER PROPERTY OF ALBUMIN MICROSPHERES IN CHEMOTHERAPY. III. EFFECT OF MICROSPHERE-ENTRAPPED 5-FLUOROURACIL ON EHRLICH ASCITES CARCINOMA IN MICE
- Prediction of Measurement Precision by Chemometric Invalidation of Flow Pulsation in Refractive Index Detection of Liquid Chromatography
- Discrimination limit for purity test of human insulin by capillary electrophoresis
- Improvement by Adjuvants on the Rectal Bioavailability of Non-absorbable Drugs Following Administration of Suppository
- A New Technique for in Vivo Percutaneous Absorption(Pharmaceutical)
- Determination of Fenoxaprop-Ethyl in Agricultural Products by HPLC with Photometric Detection and Mass Spectrometry
- Sustained Release of Flufenamic Acid from a Drug-Triacetyl-β-Cyclodextrin Complex
- Phthalates, Adipates, Citrate and Some of the Other Plasticizers Detected in Japanese Retail Foods : a Survey
- Simultaneous Determination of Azimsulfuron, Flazasulfuron and Halosulfuron-methyl in Grains, Seeds, Vegetables and Fruits by HPLC
- Multiresidue Analysis of Pesticides in Fresh Fruits and Vegetables by Supercritical Fluid Extraction and HPLC
- EFFECT OF CHOLESTEROL ON THE FORMATION OF INTERDIGITATED GEL PHASE IN LECITHIN MEMBRANES
- Intravenously Administered 2'-Deoxycytidine Suppresses Mouse Myeloma Tumor Growth
- Reduction of Enhanced Rabbit Intraocular Pressure by Instillation of Pyroglutamic Acid Eye Drops