47 results about "Narcotic Effects" patented technology

The invention provides N-diethylaminoacetyl-2,6-dimethylaniline derivatives, a preparation method and applications thereof. The structure of the derivatives is represented by the formula (I). The preparation method comprises the following steps: carrying out reactions between N-diethylaminoacetyl-2,6-dimethylaniline and halogenated compounds to obtain a corresponding quaternary ammonium salt intermediate, and then subjecting the quaternary ammonium salt intermediate to react with corresponding 2-methoxyl-4-subsituted phenol derivative raw material so as to obtain the N-diethylaminoacetyl-2,6-dimethylaniline derivatives. The derivatives can be used as a long-acting local anesthetic drug or a pain relieving drug capable of separating the motion and the feeling, can exert a reversible and lasting local anesthetic effect in organism bodies, do not affect motor function in a certain dosage range, and have an ideal retardant effect on separation of motion and feeling.

The invention relates to a preparation method of ropivacaine mesylate injection packed by a soda-lime glass bottle, which comprises the following processing steps of ingredient preparation, liquor preparation, soda-lime glass bottle and rubber plug cleaning, filling, capping, sterilization, lamp test, labeling, packing and finished product inspection. The injection is subject to a filtration sterilization processing step once and a flowing steam sterilization processing step once, wherein microorganisms larger than 0.22 microns in liquid medicine are removed by a filter method, microorganismssmaller than 0.22 microns are killed by flowing steam sterilization, and insoluble particles in the liquid medicine are removed during filtration sterilization simultaneously, thereby greatly reducingthe occurrence of phlebitis; and the invention is packed by the soda-lime glass bottle which has the advantages of heat resistance, acid and alkali resistance, large strength, and the like, thereby ensuring the stability of the medicine. Clinic comparison tests show that the ropivacaine mesylate injection packed by a soda-lime glass bottle has the advantages of quicker effect, long action time, reliable anesthetic effect, small toxicity to heart, separate blocking pf sensory and motor nerves, and the like, thereby being suitable for anesthesia in surgeries and postoperative analgesia.

The invention discloses an application of an N-acetanilide cationic compound in preparation of a local nerve blocking drug. The cationic compound is a quaternary ammonium salt compound and has a structure as shown in a formula (I), wherein X is a halogen atom. When used alone, the compound has the characteristics of good safety performance, strong nerve blocking effect and the like, can take a reversible and durable local anaesthesia effect in vivo and can be used as a local anaesthesia drug or an analgesic drug which is long-acting and / or capable of realizing selective blocking. Particularly, a composition composed of the compound and other local anaesthesia drugs has the remarkable characteristics of high effect taking speed, strong effect, long acting time, little nerve injury and the like when used for nerve blocking.

The invention relates to an N-substituted imidazolecarboxylic acid ester chiral compound containing an ether side chain, a preparation method and an application thereof. The structure of the compound is shown in the formula (I). The compound can produce rapid and reversible general anesthesia effect. Animal experiments show rapid and short-acting pharmacological characteristics of the compound, so that the compound can be used as a rapid and short-acting general anesthesia medicine, meanwhile, compared with etomidate, the compound can reduce the inhibition effect on synthesis of adrenal cortical hormone, recovery is rapid and thorough, and the compound has obvious advantages and good application prospect. The only chiral carbon in the structure of the compound must be of R type. An imidazole ring in the structure of the compound has acidifiable N atoms, so that the compound and medicinal salt molecules thereof can be applied to the preparation of central inhibitory medicines which can produce sedative and hypnotic and / or anesthetic effects on animals or persons through veins or paths outside veins.

The present invention relates to one kind of polycinnamic alcohol injection and its preparation. The polycinnamic alcohol injection is used mainly in treating esophagus varication hemorrhage and esophagus varication cirrhosis under endoscope. The polycinnamic alcohol injection contains in each 100 ml polycinnamic alcohol 1 g and alcohol 5 ml. Alcohol can dissolve polycinnamic alcohol easily and has slight narcosis, so that the polycinnamic alcohol injection has no pain caused, low viscosity for easy injecting, no side effect and less complication.

The invention discloses a quaternary ammonium salt compound as well as a preparation method and application thereof, and belongs to the field of chemical medicines. The present invention provides a compound represented by a formula I, or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a prodrug, or a metabolite thereof. The compound takes effect fast, a long-time local anesthesia effect is achieved after single administration, the sensory nerve blocking time is longer than the motor nerve blocking time, the long-acting local anesthetic effect and the selective local anesthetic effect are achieved, and meanwhile, the side effect of the quaternary ammonium salt compound with the structural characteristics of a surfactant is obviously reduced. The compound has high safety, namely, the compound shown in the formula I and the pharmaceutically acceptable salt thereof can be used for preparing safe medicines with long-time local anesthesia and selective local anesthesia effects. The compound has the advantages of long local anesthesia action time, good local anesthesia selectivity and high safety.

A method for controlling a narcotic effect value of a mixture of at least two narcotic agents of a breathing gas is disclosed herein. The method includes setting a target value for a desired narcotic effect of narcotic agents and measuring a breathing gas concentration of each narcotic agent of the breathing gas. The method also includes converting measured breathing gas concentration of each narcotic agent to a narcotic effect value of the breathing gas and calculating a total narcotic effect value of the mixture of the at least two narcotic agents. The method also includes comparing the total narcotic effect value with the target value and determining whether or not to change the breathing gas concentration to meet the target value.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention relates to a propofol ester derivative containing an amino carboxylic acid amide structure, its preparation method and its purpose. The derivative has a following formula (I), in the formula, M is H, NH4 or pharmaceutically acceptable alkali metal element or alkali earth metal element, n=1-3, m=1-7, x=1 / 2-1. 2,6-diisopropyl phenol (II) is taken as a raw material, reacted with diacid or the corresponding anhydride to obtain a 2,6-diisopropyl phenol monoester intermediate, and continuously reacted with amino carboxylic acid to obtain the corresponding product (I). The propofol ester derivative can be used for preparing injection type central inhibition medicaments for generating effects of calmness, hypnosis and / or anaesthesia on animals and human, and is capable of improving the water-solubility of propofol, reducing the toxic and side effects of original drug and analogous prodrug, increasing the stability of profrug in vitro and increasing the application scope. The preparation method is simple which has industrial application value.

The invention discloses a compound shown as formula I in the specification, or a stereoisomer, or a pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. Belonging to the field of pharmaceutical chemistry, the compound is a polysubstituted triazole formate derivative with a novel structure. The invention also discloses application of thepolysubstituted triazole formate derivative in preparation of drugs with sedative, hypnotic and / or anesthetic effects, and application in preparation of drugs capable of controlling status epilepticus. The compound has good inhibition effect on the central nervous system, and provides a new choice for clinical screening and / or preparation of drugs with sedative, hypnotic and / or anesthetic effectsand status epilepticus controlling function.

The invention discloses a compound shown in a formula I, or a stereoisomer, or a pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative of the compound, and belongs to the field of medicinal chemistry. The compound is a substituted imidazolecarboxylate derivative with novel structure. The invention further discloses application of the substitutedimidazolecarboxylate derivative in preparation of drugs with effects of sedation, hypnosis and / or anesthesia and application of the substituted imidazolecarboxylate derivative in preparation of drugscapable of controlling status epilepticus, wherein the compound has good inhibition effects on the central nervous system, and a new choice is provided for clinically screening and / or preparing drugswith effects of sedation, hypnosis and / or anesthesia and drugs for controlling the status epilepticus.

The invention discloses a compound shown in a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt of the compound, or a solvate of the compound, or a prodrug of the compound, or a metabolite of the compound, or a deuterated derivative of the compound. The compound is a substituted pyrazole formate derivative with a novel structure and belongs to the field of pharmaceuticalchemistry. The invention also discloses an application of the substituted pyrazole formate derivative in preparing medicines with sedative, hypnotic and / or anaesthesia effects and in preparing medicines capable of controlling a continuous epilepsy state. The compound has a good inhibiting effect on central nervous system, and provides a new choice for clinically screening and / or preparing medicines which have sedative, hypnotic and / or anaesthesia effects and can control a continuous epilepsy state.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

N-diethylaminoacetyl-2,6-dimethylaniline derivative, preparation method and use. The structure of said derivative is shown in formula (I). During preparation, the corresponding quaternary ammonium salt intermediate compound can be prepared from N-diethylaminoacetyl-2,6-dimethylaniline and halogenated compounds first, and then the corresponding 2-methoxy-4-substituted phenol derivative It is obtained after the reaction of similar raw materials. The derivative can be used as a local anesthetic or analgesic drug with long-acting and motor-sensory separation, can exert a reversible and long-lasting local anesthetic effect in the living body, and has no effect on motor function within a certain dose range, and has ideal movement and sensation Detached blocking effect.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention relates to the field of medicines, and particularly relates to a pharmaceutical composition which has anesthetic action in operation. The composition is prepared from 1.0-3.0mg of bupivacaine, 1-5mu g of sufentanil, 15-30mu g of tetrahydropalmatine, 15-30 mu g of indometacin and 0.1-0.5mg of ropivacaine. The anesthetic composition is preferably prepared from 3.0mg of bupivacaine, 3mu g of sufentanil, 20mu g of tetrahydropalmatine, 20mu g of indometacin and 0.3mg of ropivacaine.

A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.

Disclosed are a propofol hydroxy acid ester compound with an ester constitutional terminal, a preparation method for the same and application thereof. As shown in the constitutional formula (I) of the compound, Y refers to a C1-4 linear carbon chain, and R refers to acetyl or propiono. The propofol hydroxy acid ester compound can be prepared by utilizing corresponding propofol hydroxy acid ester as raw materials and is obtained by means of esterification reaction with corresponding acid anhydride. As experiments show, the compound is stable in vitro but capable of quickly releasing propofol with sedation and hypnogenesis and / or narcotism in blood plasma. Since hydroxy in propofol hydroxy butyric ester molecules is protected by means of shielding, heat stability of the propofol hydroxy acid ester compound is improved, and self-decomposition of the propofol hydroxy acid ester compound caused by lactonization is reduced.

The invention discloses an alkyl-substituted phenol carboxylate derivative, and a preparation method and application thereof. The structure of the derivative is shown in the specification, wherein X in a formula is O, S and NR, and R is H or C1-5 alkyl; Y is CH2, CH2CH2 or CO; Z is OH, NH2, HSO4, H2PO4, N (CH3) 2, NHCH3, N < + > (CH3) 3, H2NPO3, OCH2COOH or H2NMePO3; L is isopropyl or A pharmaceutically acceptable salt of the alkyl-substituted phenol carboxylate derivative, such as sodium salt, amino acid salt, hydrochloride and the like. The invention also discloses a pharmaceutically acceptable solvate, such as a hydrate. The compound represented by formula (I) and the pharmaceutically acceptable salt or solvate thereof may have water solubility, are stable in aqueous solution, can rapidly release alkyl substituted phenol and non-toxic and low-toxicity metabolites with sedative-hypnotic and / or anesthetic effects under the action of enzyme after entering body, and are good in safety,so that the compound can be applied to the field of sedative-hypnotic and / or anesthetic drugs for intravenous or extravenous administration.

The invention relates to a propofol ester derivative containing an amino carboxylic acid amide structure, its preparation method and its purpose. The derivative has a following formula (I), in the formula, M is H, NH4 or pharmaceutically acceptable alkali metal element or alkali earth metal element, n=1-3, m=1-7, x=1 / 2-1. 2,6-diisopropyl phenol (II) is taken as a raw material, reacted with diacid or the corresponding anhydride to obtain a 2,6-diisopropyl phenol monoester intermediate, and continuously reacted with amino carboxylic acid to obtain the corresponding product (I). The propofol ester derivative can be used for preparing injection type central inhibition medicaments for generating effects of calmness, hypnosis and / or anaesthesia on animals and human, and is capable of improving the water-solubility of propofol, reducing the toxic and side effects of original drug and analogous prodrug, increasing the stability of profrug in vitro and increasing the application scope. The preparation method is simple which has industrial application value.

Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y═C14 straight carbon chain. The compound can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and / or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and / or anesthesia.

The invention discloses a ketone-substituted heterocyclic compound and its anesthetic effect. Specifically provided are compounds represented by formula I, or pharmaceutically acceptable salts thereof, or stereoisomers thereof, or deuterated derivatives thereof. The ketone-substituted heterocyclic compound provided by the present invention has a good inhibitory effect on the central nervous system, can produce sedative, hypnotic and / or general anesthesia, and can control status epilepticus; the ketone-substituted heterocyclic compound maintains excellent anesthetic activity At the same time, it also has the characteristics of rapid onset and rapid recovery; at the same time, the ketone-substituted heterocyclic compound has almost no inhibitory effect on the function of the adrenal cortex, and has little side effects, which solves the technical problems in this field. Or the preparation of drugs for sedation, hypnosis and / or general anesthesia and drugs for controlling status epilepticus provides a new option.

The invention discloses a quaternary ammonium salt compound, a preparation method and application thereof, and belongs to the field of chemical medicine. The present invention provides a compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a solvate thereof, or a prodrug thereof, or a metabolite thereof. The compound has quick onset, long-term local anesthesia effect after a single administration, sensory nerve block time longer than motor nerve block time, both long-acting local anesthesia effect and selective local anesthesia effect, and significantly reduces The side effects of the quaternary ammonium salt compound with surfactant structural characteristics have good safety, that is, the compound of formula I of the present invention and its pharmaceutically acceptable salt can be used to prepare safe, long-term local anesthesia and selective local Drugs with anesthesia effect have the advantages of long local anesthesia effect time, good local anesthesia selectivity and high safety.

Disclosed are a propofol hydroxy acid ester compound with an ester constitutional terminal, a preparation method for the same and application thereof. As shown in the constitutional formula (I) of the compound, Y refers to a C1-4 linear carbon chain, and R refers to acetyl or propiono. The propofol hydroxy acid ester compound can be prepared by utilizing corresponding propofol hydroxy acid ester as raw materials and is obtained by means of esterification reaction with corresponding acid anhydride. As experiments show, the compound is stable in vitro but capable of quickly releasing propofol with sedation and hypnogenesis and / or narcotism in blood plasma. Since hydroxy in propofol hydroxy butyric ester molecules is protected by means of shielding, heat stability of the propofol hydroxy acid ester compound is improved, and self-decomposition of the propofol hydroxy acid ester compound caused by lactonization is reduced.

The invention discloses a pure traditional Chinese medicine narcotic drug formula, and relates to the field of narcotic drugs; according to the pure traditional Chinese medicine narcotic drug formula, radix angelicae, ligusticum wallichii, raw radix aconite and galangal are used as raw materials; fresh ginger and honeysuckle are cooperatively used with the raw radix aconite, and mangnolia officinalis, angelica sinensis and cortex cassiae are cooperatively used with galangal, so the narcotic effect of the narcotic drug is effectively improved, the aching feeling of a user is alleviated, and the side effects are small.

The present invention describes a new propofol-containing anesthetic pharmaceutical composition for parenteral administration, in the form of an oil-in-water microemulsion in which the oily phase is constituted by propofol in the form of particles with size comprised between 1 and 100 nm using a single surfactant selected from the group consisting of polyethylene glycol stearates with general formula C17H35COO. (OCH2CH2)nH or C17H35COO. (OCH2CH2)n.COOC17H35. The anesthetic pharmaceutical composition of the present invention is more potent for induction of hypnosis and anesthesia, has a ready-to-use presentation and highly stable particle size, presenting improved physicochemical properties, and preventing the potential risks of undesirable effects encountered in the state-of-the-art propofol formulations.

A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and / or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and / or preparation of a drug with sedative, hypnotic and / or anesthetic effects and controlling the state of epilepsy.

The invention discloses a preoperative narcotic drug and a preparation method thereof, and belongs to the field of traditional Chinese medicines. Raw materials of effective components of the drug comprise cow pea pod, honey mushroom, cinnamomum bodinieri, adiantum capillus veneris, trigonotis peduncularis, lotus seeds, kweichow sage herb, java marsh pennywort, denseflower bulbophyllum herb, valerian, platycladi seeds, citronella, tubeflower dutchmanspipe roots, ants, acorus calamus and decumbent corydalis tuber. Selected medicinal materials are suitable in compatibility and complement each other, are combined to achieve the functions of easing pain, nourishing heart, calming endogenous wind, calming liver, dispelling wind, dredging collaterals, regulating qi, relieving pain, calming nerves and strengthening tendons and bones and can directly reach narcotic portions. The drug has remarkable narcotic effects in clinical operative treatment and has the advantages that the drug is an ideal narcotic product and rapid in effect, safe, convenient, free from toxic and side effects, low in price and easy to prepare.