42 results about "Flumazenil" patented technology

A method and related compositions, including the use of N-acyl derivatives of sarcosine, provide for the delivery of bioactive agents through tissue surfaces such as the skin. The method and composition are particularly well suited for hydrophobic active agents such as serotonin (5HT3) receptor antagonists (e.g., ondansetron), antipsychotic agents (e.g., risperidone), benzodiazepines (e.g., flumazenil), and progestins (e.g., levonorgestrel).

The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective quantity is administered to treat alcohol dependence.

Soluble complexes of flumazenil, methods for the preparation thereof, pharmaceutical compositions including same and use of the compositions for alleviating or counteracting the various types of hypersomnia, drowsiness, residual effects associated with the administration of sleep / hypnotic drugs, alcohol intoxication or hepatic encephalopathy.

The invention discloses a flumazenil liposome injection and a preparation method thereof. The liposome injection is prepared from flumazenil, cholesterol, phosphatidyl ethanolamine, soyasterol, tween 80, trehalose and polyvinylpyrrolidone in specific proportions by weight. The liposome injection disclosed by the invention has favorable preparation stability, the liposome can not be ruptured due to fusion, ice crystal and the like in the freezing process, and the liposome keeps the same favorable entrapment rate after long-term storage. The flumazenil liposome injection disclosed by the invention improves the solubility of flumazenil, improves the quality of the preparation product, reduces the toxic side effect, increases the retention time of the medicament in systemic circulation, improves the bioavailability of the medicament, obviously improves the curative effect, has a simple preparation method and is suitable for industrialized big production.

The present invention provides pharmaceutical compositions comprising a flumazenil, and methods of alleviating or counteracting residual effects (e.g. drowsiness) associated with the administration of sleep / hypnotic drugs or alleviating effects of alcohol intoxication, using self administration modes of delivery.

The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABAA chloride channel activity to treat alcohol and / or stimulant substance abuse. The present invention also relates to methods of, and protocols for, relieving symptoms associated with alcohol and / or stimulant substance abuse in a comprehensive treatment plan. More specifically, the present invention relates to the use of a selective chloride channel modulator, such as flumazenil, to treat alcohol and / or psychostimulant dependency, the withdrawal symptoms associated therewith, and the cravings associated therewith.

The invention discloses a compound antagonist of an animal anesthetic and an application of the compound antagonist, belonging to a medicine composition in the field of veterinarian. Each ml of compound antagonist comprises active ingredients of 0.5-2.0mg of Yohimbine hydrochloride and 0.1-0.4mg of flumazenil hydrochloride. The compound antagonist of the animal anesthetic has a remarkable awakening effect to an anesthetized animal, better effect compared with the single use of the Yohimbine hydrochloride or the flumazenil hydrochloride, is rapid in awakening, has no any adverse effect, is stable in recovery of circulating and breathing mechanisms, and has large safety factor and clinical application safety.

The invention relates to the technical field of medicament preparations, and in particular discloses a flumazenil injection and a preparation method thereof. The flumazenil injection contains flumazenil, osmotic pressure regulator, stabilizer, pH regulator and the like, wherein the osmotic pressure regulator is sodium chloride, the stabilizer is ethylene diamine tetraacetic acid disodium, and the pH regulator is acetic acid. By improving the formula and the preparation process, the stability of the physical and chemical properties of the flumazenil injection is improved, and the flumazenil injection has very high application value.

The invention provides a preparation method of a flumazenil compound, and the preparation method comprises the following steps of: carrying out hydrolysis reaction to obtain a flumazenil precursor intermediate, purifying the flumazenil precursor intermediate by activated carbon adsorption, and then carrying out esterification reaction to obtain flumazenil. The preparation method provided by the invention has the advantages of simple reaction steps, high product yield, high product purity and low cost, and is suitable for industrial mass production; and the quality of a preparation product prepared by the method is improved, and the toxic and side effects of the flumazenil compound used as benzodiazepine selective antagonist drugs can be reduced.

The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective quantity is administered to treat alcohol dependence.

In some embodiments, the present invention may be directed to various pharmaceutical dosage units comprising at least one opioid analgesic in combination with a benzodiazepine blocker. In some embodiments, the present invention may be directed to various methods of treatment using such pharmaceutical dosage units. In some embodiments, these pharmaceutical dosage units may be used for treating: pain, chronic pain, sub-acute pain, chronic and sub-acute pain, anxiety, addiction in general, opiate addiction, and benzodiazepine addiction, opiate and benzodiazepine addiction; opiate dependence, benzodiazepine dependence; and for reducing a likelihood of overdose associated with concomitant use of opiates with benzodiazepines, and for mitigating against drug diversion. These pharmaceutical dosage units may be delivered by a variety of delivery methods and / or delivery systems, comprising one or more of: mucosal, sublingual, buccal, nasal inhalation, depot, implantable rod, transdermal patch, parenteral, intravenous, intrathecal, subcutaneous, intramuscular, and the like.

The invention discloses a flumazenil inclusion compound. The flumazenil inclusion compound contains flumazenil and beta-cyclodextrin or a derivative of the beta-cyclodextrin, wherein a molar mass ratio of the flumazenil to the beta-cyclodextrin or the derivative of the beta-cyclodextrin ranges from 1:1.5 to 1:4. A production method of the flumazenil inclusion compound is further disclosed. According to the flumazenil inclusion compound, production conditions are simple, the flumazenil inclusion compound is suitable for industrial mass production, the solubility of the flumazenil can be greatlyimproved, and development of novel dosage forms of flumazenil is facilitated, so that the flumazenil inclusion compound has wide application prospects.

A method for controlling or reversing the alcohol intake in the non-alcohol dependent individual both before or during their alcohol imbibing. This is accomplished by self-administering a spray directed into sensitive mucosal vein endings of the individual. There are at least three technologies to accomplish the above noted task. The first one is a nasal spray which is directed into the nasal passage. The second spray is directed into the mouth of the individual so that the medication can be absorbed by the buccal mucosal membrane in the mouth of the individual. The third medicated spray technology is pulmonary inhaler aerosolization which is absorbed in the tissues of the lung. All of the above noted sprays by-pass the liver and the intestines. The medication, Flumazenil, is the medication used in any of these sprays to accomplish the desired effect.

The present invention relates to the composition and methods of using a combination of a serotonin3 (5-HT3) receptor antagonist, such as ondansetron, and a selective chloride channel modulator, such as flumazenil, for treatment of patients with drug addiction or dependence. Examples of the drugs include prescription drugs as well as illegal drugs, such as, but not limited to, alcohol, cocaine, nicotine, marijuana, benzodiazepines and opiates. Furthermore, this combination can be used for treatment of patients suffering from central nervous system (CNS) disorders such as, but not limited to, depression, emotional and mood disorders and loss of memory.

A composition comprising two or more active agents in a micro-dose amount, such as a micro-dose of naltrexone in combination with a micro-dose of flumazenil, in the treatment of craving or anxiety resulting in rapid settling of the craving for substance use, smoking or an obsessional behaviour, preferably within minutes of administration of the composition.

The invention discloses a capsule preparation having a reverse pharmacological function and used for treating insomnia. The capsule preparation is prepared from, by weight, 4-6 parts of diazepam, 22-27 parts of flumazenil, 25-35 parts of caffeine, 100-150 parts of ethyl cellulose, 25-35 parts of starch, 18-22 parts of polyvinylpyrrolidone and 2-4 parts of magnesium stearate. The specific preparation process comprises the steps of uniformly mixing the diazepam and the starch, then adding distilled water to perform granulation, drying the mixture, then mixing the mixture and the magnesium stearate for size stabilization, using the ethyl cellulose as a capsule wall material for the flumazenil and the caffeine, adopting an emulsified solvent diffusion method to prepare micro-capsules, then mixing the micro-capsules with prepared diazepam granules, and charging the mixture into the capsules in a split mode to obtain the capsule preparation having the reverse pharmacological function and used for treating the insomnia. The capsule preparation can play the effect of promoting sleep at night and cannot affect the normal work of a user in the daytime.

A method of preventing a relapse in the abstinent substance dependent person. The method involves the use of the medication Flumazenil in a spray delivery device and to teach the person to self-administer the medication by spraying the medication into either the nasal passage, the buccal mucosol membranes or the pulmonary membranes, whenever the need and the urge to relapse arises, thereby preventing relapse.

The invention discloses a method for detecting flumazenil in Chinese patent medicines and health food by liquid chromatography-mass spectrometry. The method comprises the following steps: (1) preparation of a reference substance: preparing the reference substance solution from a flumazenil reference substance and methanol; (2) preparation of a to-be-detected sample: extracting a Chinese materia medica preparation which improves memory in an assisted manner and health food with methanol, and purifying a solution obtained by extraction to obtain the to-be-detected sample solution; and (3) qualitatively and quantitatively measuring the flumazenil in a solution for testing product by using the reference substance solution and a liquid chromatograph / mass spectrometer on the to-be-detected sample solution. According to the method, detection is carried out by a multi-reaction monitoring mode; and the method is low in interference, high in sensitivity and accurate in detection result.

The invention provides application of pyrazinamide and flumazenil combination to preparation of anti-convulsion drugs. The application of pyrazinamide and flumazenil combination to preparation of anti-convulsion drugs is characterized in that based on a research in an experimental means, findings prove that after the pyrazinamide and the flumazenil are used together in a specific proportion, severe symptoms in a convulsion incidence process can be effectively alleviated. Based on that, a pharmacological action principle is explored, experimental findings prove that although drugs are used unilaterally, the pyrazinamide and flumazenil combination does not have an effect of affecting neurotransmitter; and under the condition of combined application of the pyrazinamide and the flumazenil, theactivity of AMPA (Aminomethyl Phosphonic Acid) receptor and the activity of NMDA (N-methyl-D-aspartic acid) receptor can be obviously inhibited, and the combination has exact effects on reduction ofexcitatory postsynaptic currents and alleviation of delayed lesion of nerve cells. Based on the above-mentioned beneficial findings, according to the pyrazinamide and flumazenil combination disclosedby the invention, new application of the pyrazinamide and flumazenil combination to preparation of the anti-convulsion drugs is determined, and thus, a selection range of the anti-convulsion drugs iswidened, the medicine application of both of the pyrazinamide and the flumazenil is widened, and the pyrazinamide and flumazenil combination has wide application prospects.

The invention provides a flumazenil injection. The flumazenil injection is prepared from the following drugs and excipient by weight: 1 part of flumazenil, 70 to 110 parts of sodium chloride, 0.5 to 2 parts of disodium edetate, 20 to 100 parts of mycose and 10 to 50 parts of lysine. The preparation method for the flumazenil injection comprises the following steps: weighting flumazenil, sodium chloride, disodium edetate, mycose and lysine; dissolving the above-mentioned components with a part of injection water and carrying out rough filtration; then adding the rest injection water and carrying out fine filtration; and carrying out filling, sealing and disinfection. Compared with the prior art, the invention has the following advantages: since mycose and lysine are added into the injection and cooperatively used with disodium edetate, stability of flumazenil is effectively improved, the quality of a preparation product is enhanced, and toxic and side effects are reduced; and the preparation method is simple, has low cost and is applicable to industrial large-scale production.

The invention relates to the use of flumazenil in the manufacture of a medicament for the treatment of depressive disorders, for example disorders including depressive symptoms, without psychotic alteration. The flumazenil can be administered sequentially in small quantities at short intervals until a quantity that is therapeutically effective for the treatment of the depressive disorder has been administered.

The invention discloses a preparation method of flumazenil, and belongs to the field of medicine synthesis. The method comprises the following steps: by taking 5-fluoro-2-nitrobenzoic acid as a raw material, carrying out condensation on 5-fluoro-2-nitrobenzoic acid and sarcosine ester, and then carrying out ring closing while reducing, so as to obtain 7-fluoro-3, 4-dihydro-4-methyl-1H-[1, 4] benzodiazepine-2, 5-diketone; and finally, carrying out halogenation and cycloaddition reaction to obtain flumazenil. According to the novel synthesis method of the flumazenil key intermediate 7-fluoro-3, 4-dihydro-4-methyl-1H-[1, 4] benzodiazepine-2, 5-diketone, provided by the invention, a green synthesis process is adopted, an intramolecular cyclization reaction is performed while a nitro group is reduced, and compared with a known flumazenil synthesis method, a strong oxidant, a highly toxic reagent (such as ethyl chloroformate) and the like are not needed, and the yield is higher.