The Acid-Base Equilibrium Reaction of Benzodiazepinooxazoles
スポンサーリンク
概要
- 論文の詳細を見る
The acid-base equilibrium reactions of oxazolam (10-chloro-2,3,5,6,7,11b-hexahydro-2-methyl-11b-phenylbenzo [6,7]-1,4-diazepino [5,4-b] oxazol-6-one) and thirteen other derivatives of 1,4-benzodiazepinooxazole (BDOZ) were studied. Ultraviolet absorption and fluorescence spectroscopies were employed to obtain the equilibrium constants. In most BDOZs the protonated species were promptly cleaved at the oxazolidine ring fused to the diazepine nucleus, and equilibrated with the original species. A few exceptional compounds required an appreciable time lag for the equilibration. The effects of substituents on the pK_a value are discussed from the viewpoint of physical organic chemistry.
- 公益社団法人日本薬学会の論文
- 1982-10-25
著者
-
永井 恒司
Department of Pharmaceutics, Hoshi University
-
永井 恒司
Research Center Taisho Pharmaceutical Co. Ltd.
-
永井 恒司
Hoshi Institute of Pharmaceutical Sciences
-
池田 勝
Product Development Laboratories Sankyo Co. Ltd.
関連論文
- Evaluation of New Paty-Type Implantable Devices Consisting of Poly(ε-caprolactone/δ-valerolactone) and Estracyt or Estramustine
- Morphologic Examination of Rabbit Nasal Mucosa after the Nasal Administration of Insulin Peanut Oil Suspension and a Powder Dosage Form with Soybean-Derived Sterylglucoside
- Permeation of Diclofenac Salts through Silicone Membrane : a Mechanistic Study of Percutaneous Absorption of Ionizable Drugs
- Permeability of Insulin Entrapped in Liposome through the Nasal Mucosa of Rabbits
- Effects of Orally Administered Liposomes with Soybean-Derived Sterols and Their Glucosides on Rat Body Weight
- Effects of Dose, pH and Osmolarity on Intranasal Absorption of Recombinant Human Erythropoietin in Rats
- Evaluation of Liposomal Erythropoietin Prepared with Reverse-Phase Evaporation Vesicle Method by Subcutaneous Administration in Rats
- Comparative Bioavailability Study of Acetaminophen Solutions Used in Hospital Formulary
- Preparation and Evaluation of Free Oxygen Absorber in Pharmaceutical Preparations
- Pharmacokinetic Characteristics and Antitumor Activity of the N-Succinyl-chitosan-Mitomycin C Conjugate and the Carboxymethyl-chitin-Mitomycin C Conjugate
- Synthesis and Drug-Release Characteristics of the Conjugates of Mitomycin C with N-Succinyl-chitosan and Carboxymethyl-chitin
- Accelerated Degradation of Non-steroid Anti-inflammatory Drugs at Carbon Black/Water Interface
- Adsorption from Solution, Permeation through Cellulose Membrane, Partition Coefficient and Surface Tension of Several Antidepressants and Phenothiazines
- Adsorption of Phenothiazines from Aqueous Solution by Aerosil
- Preparation and Phase II Clinical Examination of Topical Dosage Form for Treatment of Carcinoma Colli Containing Bleomycin with Hydroxypropyl Cellulose
- In Vitro pH-Dependent Drug Release from N^4-(4-Carboxybutyryl)-1-β-D-arabinofuranosylcytosine and Its Conjugate with Poly-L-lysine or Decylenediamine-dextran T70
- Novel Preparation of Decylenediamine-dextran T70 and Inhibitory Activity toward Dihydrofolate Reductase of Decylenediamine-dextran T70-Methotrexate Conjugate(Pharmaceutical)
- Preparation of Dextran T70-Methotrexate Conjugate and Dextran T70-Mycophenolic Acid Conjugate, and in Vitro Effect of Dextran T70-Methotrexate on Dihydrofolate Reductase
- Effect of Pretreatment of Skin with Cyclic Monoterpenes on Permeation of Diclofenac in Hairless Rat
- Dissolution Behavior of Flufenamic Acid dispersed in Cross-linked Insoluble Polyvinylpyrrolidone : Effect of Water-soluble Polymers added as the Third Component
- Stability and Several Physical Properties of Amorphous and Crystalline Forms of Indomethacin
- Nuclear Magnetic Resonance Study of the Binding of Tolbutamide and Chlorpropamide to Bovine Serum Albumin
- Adsorption of Benzoic Acid Derivatives by Carbon Black from Aqueous Solution and Related Phenomena
- Chitosan Film Prepared on a Metal Plate Loaded with Electric Charge
- Dissolution Profile and Bioavailability of Sulfamonomethoxine/18-Crown-6 Complex in Comparison with Sulfamonomethoxine Anhydrate and Hydrate
- Apparent Oral Toxicity of 18-Crown-6 in Dogs
- Adsorption of Local Anesthetics from Aqueous Solution. Analysis of Factors Affecting the Nerve Blocking
- Particle Size Distribution Affects the Human Bioavailability of Phenytoin
- Dissolution and Bioavailability of Phenytoin in Phenytoin-Polyvinylpyrrolidone-Sodium Deoxycholate Coprecipitate
- Particle Size Dependency of Dissolution Rate and Human Bioavailability of Phenytoin in Powders and Phenytoin-Polyethylene Glycol Solid Dispersions
- Sustained-Release Formulation of Buformin Hydrochloride
- Analysis of Factors affecting Dissolution of Digoxin from Tablets
- Model Barrier Affecting Drug Transport
- Factors affecting the Adsorption of Chlorhexidine Gluconate by Hydroxyapatite
- Dissolution Kinetics of Polyvinylpyrrolidone of Various Molecular Weights
- Dissolution Kinetics of Polyvinylpyrrolidone
- Directly Compressed Tablets containing Water-insoluble Glucan and Microcrystalline Cellulose in Addition to Lactose
- Evaluation of Skin Damage of Cyclic Monoterpenes, Percutaneous Absorption Enhancers, by Using Cultured Human Skin Cells
- Investigation on Rectal Absorption of Indomethacin from Sustained-Release Hydrogel Suppositories Prepared with Water-Soluble Dietary Fibers, Xanthan Gum and Locust Bean Gum
- Factors Affecting Prednisolone Release from Hydrogels Prepared with Water-Soluble Dietary Fibers, Xanthan and Locust Bean Gums
- Relationship between Competitive Adsorption by Carbon Black from Aqueous Solution and Formation of Molecular Compounds in the Solid Phase for Aminopyrine and Barbituric Acid Derivatives
- Computer Optimization for the Formulation of Controlled-Release Theophylline Tablet Made of Micronized Low-Substituted Hydroxypropylcellulose and Methylcellulose
- Physicochemical Properties and Stability in the Acidic Solution of a New Macrolide Antibiotic, Clarithromycin, in Comparison with Erthyomycin
- Development of a Tablet Excipient from Bagasse(Pharmaceutical)
- Kinetic Approach to Determine the Generation Rate of Available Surface Area during the Dissolution Process
- Effect of Compression Pressure and Formulation on the Available Surface Area of Flufenamic Acid in Tablets
- Influence of Wetting Factors on the Dissolution Behavior of Flufenamic Acid
- Dissolution Profiles of Nalidixic Acid Powders Having Weibull Particle Size Distribution
- Prediction of Available Surface Area of Powdered Particles of Flufenamic Acid in Tablets
- Kinetics of Hydrolysis of Oxazolam in Aqueous Solution
- Properties of Cyclodextrin Polymer as a Tabletting Aid
- The Acid-Base Equilibrium Reaction of Benzodiazepinooxazoles
- Absorption of Salicylic Acid through the Oral Mucous Membrane of Hamster Cheek Pouch
- Permeation of Drug through a Model Membrane consisting of Millipore Filter with Oil
- Complexes of Polyethylene Oxide with Guanidine Hydrochloride and with Phenobarbital. Preliminary Structural Studies by Differential Scanning Calorimetry, Polarized Infrared Spectroscopy and X-Ray Fiber Photography
- Relationship between the Adsorption by Carbon Black from Aqueous Solution and the Biopharmaceutical Data of Sulfonamides
- Adsorption of Sulfonamides from Aqueous Solution
- Polymorphism of Phenylbutazone
- Preparation and Phase II Clinical Examination of Topical Dosage Forms for the Treatment of Carcinoma Colli Containing Bleomycin, Carboquone, or 5-Fluorouracil with Hydroxypropyl Cellulose
- Effect of Interpolymer Complex Formation on Bioadhesive Property and Drug Release Phenomenon of Compressed Tablet Consisting of Chitosan and Sodium Hyaluronate
- Solubility of Acetaminophen in Cosolvents
- percutaneous Absorption of Ketoprofen from Acrylic Gel patches Containing d-Limonene and Ethanol as Absorption Enhancers
- Factors Affecting Dissolution Rate of Cellulose Acetate Phthalate in Aqueous Solution
- Interaction of Phenothiazines with Pectin in the Solid State
- Interaction of Phenothiazines with Pectin in Aqueous Solution
- New Procedure for Assay of Lactobacilli using the Luciferin-Luciferase System
- Interaction of Several Nonsteroidal Antiinflammatory Drugs with Pectin in Aqueous Solution and in Solid State
- Influence of Inclusion of Nonsteroidal Antiinflammatory Drugs with β-Cyclodextrin on the Irritation to Stomach of Rats upon Oral Administration
- Bioavailability of Powdered Inclusion Compounds of Nonsteroidal Antiinflammatory Drugs with β-Cyclodextrin in Rabbits and Dogs
- Binding of 1-Anilino-8-naphthalenesulfonate to Polyvinylpyrrolidone, Poly-N-vinyl-2-oxazolidone, Poly-N-vinyl-5-methyl-2-oxazolidone and Polyethylene Glycol-20M in Aqueous Solution
- Mechanism of Adsorption of Phenols by Carbon Black from Aqueous Solution
- Analysis of Solubility Properties of L-Tryptophan in Aqueous Solution based on the Effects of Third Component on Optical Rotatory Dispersion and on Adsorption by Carbon Black
- Interactions of α- and β-Cyclodextrin with Several Non-Steroidal Antiinflammatory Drugs in Aqueous Solution
- Thermodynamic Properties of Polymorphs of Tolbutamide
- Solid-State Nuclear Magnetic Resonance Spectroscopy and Raman Spectroscopy of the Inclusion Compound of Tolbutamide with β-Cyclodextrin
- Permeation of Sulfonylureas through Cellulose and Dimethylpolysiloxane Membranes
- Adsorption of Benzothiadiazines by Carbon Black from Aqueous Solution, and Related Phenomena
- Nuclear Magnetic Resonance (NMR) Spectroscopy of Inclusion Compounds of Tolbutamide and Chlorpropamide with β-Cyclodextrin in Aqueous Solution
- Adsorption of Sulphonylureas by Carbon Black from Aqueous Solution
- Binding of 1-Anilinonaphthalene-8-sulfonate to Water Soluble Synthetic Polymers
- Combined Effect of d-Limonene Pretreatment and Temperature on the Rat Skin Permeation of Lipophilic and Hydrophilic Drugs
- Effect of d-Limonene on the Amounts of Ethanol and Indomethacin Penetrated from Aqueous Gel Ointments to Rat Skin
- Enhancement of Dissolution Properties of Griseofulvin from Ground Mixtures with Chitin or Chitosan
- Permeation of Drugs through Chitosan Membranes
- Directly Compressed Tablets containing Chitin or Chitosan in Addition to Lactose or Potato Starch
- Absorption of Insulin Using Water-in-Oil-in-Water Emulsion from an Enteral Loop in Rats
- Site-Dependent Effect of Aprotinin, Sodium Caprate, Na_2EDTA and Sodium Glycocholate on Intestinal Absorption of Insulin
- Formulation Optimization of Sustained-Release Tablet of Chlorpheniramine Maleate by Means of Extreme Vertices Design and Simultaneous Optimization Technique
- Factors Affecting the Dissolution of Ketoprofen from Solid Dispersions in Various Water-soluble Polymers
- Mucosal Dosage Form of Lidocaine for Toothache using Hydroxypropyl Cellulose and Carbopol
- Factors affecting the Dissolution of Indomethacin dispersed in Various Water-Soluble Polymers
- Analysis of Interfacial Transfer of Indomethacin following Dissolution of Indomethacin/Polyvinylpyrrolidone Coprecipitates
- Adsorption of Nicotinic and Isonicotinic Acid Derivatives by Hydroxyapatite from Aqueous Solutions
- New Mucosal Dosage Form of Insulin
- Microencapsulation and Bioavaliability in Beagle Dogs of Indomethacin
- Dissolution Kinetics for Coprecipitates of Indomethacin with Polyvinylpyrrolidone
- Ultraviolet Absorption Spectroscopy and Nuclear Magnetic Resonance Spectroscopy of Complexes of Sulfonamides with Cyclic Polyether 18-Crown-6
- Dissolution Kinetics of Complexes of Sulfamethoxazole and Sulfamonomethoxine with 18-Crown-6
- Interaction of Sulfonamides with Cyclic Polyether 18-Crown-6 in Solution and in Solid State
- Interaction of N-Methyl-2-pyrrolidone with Aminobenzoic Acids in Solution and in Solid State