777results about "Anaesthetics" patented technology

The invention belongs to the technical field of medical and mechanical combinations, and discloses a high-permeability and low-sensitivity ripdicaine wound patch and a preparation method thereof.The high-permeability and low-sensitivity ripdicaine wound patch comprises a wound patch body, and the wound patch body is prepared from, by mass, 0.1%-0.4% of sodium hyaluronate, 1.5%-3.5% of lidocaine, 1.5%-3.5% of prilocaine, 3%-10% of solvent, 0.5%-8% of emulsifier, 2%-10% of humectant, 0.1%-5% of soothing agent, 0.1%-1.5% of stabilizer, 0.1%-1% of thickener and the balance water. According to the present invention, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, the total amount of the raw materials is 100%, and the total amount of the raw materials is 100%. And the anesthetic has the advantages of quick effect taking, low sensitivity, capability of resisting moist heat sterilization and good stability.

The present invention relates to the technical field of pharmaceutical chemistry, and provides a heterocyclic compound and a pharmaceutical use thereof. The structure of the heterocyclic compound is as shown in formula II. The compound of the present invention has high-efficiency sedative, hypnotic and / or anesthetic effects, can control status epilepticus, and also has an analgesic effect, providing a new choice for clinical preparation of a drug having the analgesic effect, a drug having the anesthetic, sedative, and hypnotic effects and / or capable of controlling status epilepticus, and a drug having both the anesthetic, sedative, and hypnotic effects and / or capable of controlling status epilepticus and also having the analgesic effect.

The invention provides a surface anesthesia application and a preparation method thereof, and belongs to the technical field of application. The surface anesthesia application is composed of a base material and anesthetic liquid, and the anesthetic liquid is prepared from, by mass, 0.5-10% of anesthetic, 0-1% of sodium hyaluronate, 0.1-10% of penetration enhancer, 0.1-1% of thickening agent, 0.01-0.5% of pH value regulator, 0.1-1% of preservative, 0-5% of emulsifier and the balance water. The surface anesthesia application prepared by the invention takes effect quickly, has a good anesthesia effect, reduces the dosage of anesthetics, and is convenient to use and low in cost.

Compositions and methods for administration of local anesthetics that are delivered by a single injection and enable repeated on-demand or high influx analgesia over extended periods have been developed. Pharmaceutical compositions including an effective amount of one or more sodium channel blockers including site 1 sodium channel blockers, optionally one or more alpha-2-adrenergic agonists, which are optionally encapsulated in liposomes, particles or microbubbles, and one or more triggerable elements are provided. The triggerable elements allow delivery of the encapsulated anesthetic drugs when an appropriate triggering stimuli are applied. Exemplary triggering agents or stimuli include near-infrared irradiation, UV- and visible light, ultrasound and magnetic field. In one embodiment, ultrasound is used to trigger a burst of microbubbles to enhance penetration of local anesthetic.

The invention relates to a cucurbituril compound and medical application thereof. Specifically, the invention relates to a compound as shown in a formula (I) and a pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition containing the compound and application thereof as a therapeutic agent, especially application in treatment or prevention of proliferative diseases, cardiovascular related diseases or hematologic cancers, use in reversing drug-induced neuromuscular block and / or anesthesia. I) # imgabs0 #

The present application relates to the field of pharmaceutical preparation technology, and specifically discloses a preparation process of lidocaine hydrochloride gel. The preparation process of lidocaine hydrochloride gel provided by the present application, comprising the following steps: batching, sterilization, step-by-step cooling; the specific process of the step-by-step cooling is: the first stage: first, keep warm at 90-60°C for 1-2h, and the stirring speed is 10-60rpm; the second stage: then keep warm at 60-40°C for 1-2h, and the stirring speed is 10-60rpm; the third stage: finally stand and keep warm at 40-10°C for 5-15h. The preparation process of lidocaine hydrochloride gel provided by the present application can obtain colorless and transparent lidocaine hydrochloride gel with high uniformity and good stability, greatly improving the practical reliability and safety of lidocaine hydrochloride gel.

The invention discloses a long-acting analgesic compound as well as a preparation method and application thereof. The preparation method comprises the following steps: preparing a mixed solution containing a polymer, a local anesthetic, a non-steroidal anti-inflammatory drug and a solvent into drug-loaded microspheres through an electrostatic spraying technology; the preparation method comprises the following steps: dissolving poloxamer and a natural polymer material in water to obtain a hydrogel solution; and uniformly mixing the drug-loaded microspheres and a hydrogel solution to prepare the long-acting analgesic compound. The long-acting analgesic compound comprises drug-loaded microspheres and hydrogel, the long-acting analgesic compound and the hydrogel are both of a three-dimensional porous network structure, the drug-loaded microspheres are evenly dispersed in the hydrogel, and the drug-loaded microspheres are of a solid spherical structure. The advantages of electrostatic spraying microspheres and hydrogel are combined, the preparation method is mild in condition and simple in process, and the preparation process is non-toxic and harmless; the long-acting analgesic compound has the advantages of thermosensitivity, injectability, high drug loading rate and the like, and can be effectively applied to preparation of analgesic products.

The present invention discloses a drug conjugate based on ε-poly-L-lysine, its intermediate and its use. The present invention provides an ε-poly-L-lysine derivative-drug conjugate compound having a controllable number of group bonds and a controllable number of group bond sites as shown in formula (I). The drug conjugate of the present invention has one or more advantages of low renal clearance, low hepatic clearance and low splenic clearance, long plasma half-life, rapid accumulation of effective drug concentration in the lesion, and better therapeutic effect. [Case 1] TIFF2024542139000558.tif28169

The invention relates to the technical field of biological pharmacy, and discloses a QS-21 saponin adjuvant as well as a preparation method and application thereof, the adjuvant is a composite liposome and comprises a liposome skeleton composed of distearoyl phosphatidylcholine and cholesterol, and QS-21 saponin, monophosphoryl lipid A and a local anesthetic are jointly entrapped in the liposome skeleton. The problem that high reactogenicity and immunogenicity of potent adjuvants are difficult to consider at the same time is solved, the immunostimulation component and the pain inhibition component are jointly entrapped in the same nano-carrier, collaborative delivery in injection local is achieved, and therefore pain and swelling caused by the adjuvants are accurately inhibited. The co-entrapment structure avoids the potential inhibition effect of the free anesthetic on the immune system, the potent body fluid and cellular immune enhancement activity of the adjuvant is completely reserved, and a new technical scheme is provided for developing vaccines with high safety and strong immune efficacy.

The present technology relates to polymer implants. In some embodiments, the polymer implant may have a volume having minimum cross-sectional dimension of 400 μm. The polymer implant may be configured to be implanted within a mammalian body for at least 3 days without undergoing core acidification.

Disclosed in the present invention are a benzodiazepine compound, a pharmaceutical composition and the use thereof. Specifically provided is a compound represented by formula I, or a stereoisomer thereof, a deuterated compound thereof, or a pharmaceutically acceptable salt thereof. The compound provided in the present invention has one or more of the following advantageous effects: (1) the compound of the present invention exhibits good intravenous sedative and anesthetic effects; (2) the compound of the present invention exhibits low drug accumulation and a good tolerance; and (3) the compound of the present invention achieves an anesthetic effect with faster recovery.

The present invention relates to the technical field of pharmaceutical chemistry, and provides a heterocyclic compound and a use thereof. The structure of the heterocyclic compound is as shown in formula II. The compound of the present invention has efficient sedative, hypnotic and / or anesthetic effects, can control the status epilepticus, further has an analgesic effect, and provides a new option for clinically preparing a drug having an analgesic effect, a drug having anesthetic, sedative and hypnotic effects and / or capable of controlling the status epilepticus, and a drug having anesthetic, sedative and hypnotic effects and / or capable of controlling the status epilepticus and also having the analgesic effect.

The invention provides a deuterated etomidate derivative as well as a preparation method, an intermediate and application thereof. Particularly, the invention relates to a deuterated etomidate derivative shown in a general formula I ', a preparation method and an intermediate of the deuterated etomidate derivative, a pharmaceutical composition containing the deuterated etomidate derivative, and application of the deuterated etomidate derivative or the pharmaceutical composition of the deuterated etomidate derivative as a GABBA receptor agonist in preparation of drugs in the field of central nervous systems.

The invention relates to the technical field of aquatic animal living body transportation, and discloses a sea urchin long-distance transportation synergistic method based on dry transportation and anhydrous volatile anesthesia, which comprises the following steps: placing sea urchin in a closed container, using a natural volatile substance as an anesthetic, loading and volatilizing through an adsorption material, and performing anhydrous anesthesia on the sea urchin; the anesthetized sea urchin is inversely placed on a fixing support with a mesh structure in a transportation container in the posture that the mouth face faces upwards and the thorns face downwards, and the sea urchin is prevented from rolling over in the transportation process through the self-locking effect of the thorns and meshes; a functional interlayer is arranged in the fixing support, and a temperature control material and a moisturizing material are placed in the functional interlayer at the same time to maintain the temperature and humidity of the transportation environment; after transportation, the sea urchins are placed in seawater containing the cactus extract for initial recovery and then transferred to flowing natural seawater to complete unified recovery, a whole-process collaborative protection chain of anhydrous anesthesia loss prevention, dry transportation steady state maintenance and rapid water phase restoration can be constructed, and the dry transportation survival rate and quality are remarkably improved.

The invention provides a lidocaine stable cream, which relates to the field of pharmacy, and comprises lidocaine, prilocaine, sodium hyaluronate, cholesterol-PEG-biotin, butylated hydroxyanisole, an emulsifier, a humectant, a thickener, a preservative, an oil phase solvent, purified water and a pH regulator. The cream can solve the problems of poor drug permeation effect, large skin irritation, poor long-term storage stability and the like of the existing riptacaine cream; meanwhile, the prepared emulsifiable paste is high in stability and safety, stable in quality and high in permeability, can be uniformly and slowly released, and can prolong the anesthesia time and reduce the use amount of the emulsifiable paste on the premise of quickly exerting the drug effect, so that the anesthesia effect of the emulsifiable paste and the use comfort and stability of a patient are effectively improved.

The invention provides a heterocyclic compound and a pharmaceutical composition and application thereof, and belongs to the technical field of pharmaceutical chemistry. The series of heterocyclic compounds prepared by the invention have efficient sedative, hypnotic and / or anesthetic effects, can control the state of epilepsy, also have an analgesic effect, and have great significance for clinically preparing drugs with the analgesic effect and drugs with anesthetic, sedative, hypnotic and / or capable of controlling the state of epilepsy. The invention provides a new choice for the medicine which has the effects of anesthesia, sedation and hypnosis and / or can control epilepsy persistence and also has an analgesic effect.

The invention discloses a novel compound rapid surface anesthetic and a preparation method thereof, and belongs to the field of pharmaceutical preparations. According to the anesthetic, core anesthetic components of lidocaine and tetracaine are compounded with propylene glycol-laurocapram synergistic penetration enhancer, menthol auxiliary penetration enhancer, carbomer 980 gel matrix, triethanolamine pH regulator, glycerol humectant, panthenol soothing agent, purified water and the like, a surface smearing agent is prepared through a specific process, and the anesthetic can be administered in combination with an iontophoresis technology. Compared with the existing surface anesthetic for the cosmetic surgery, the surface anesthetic disclosed by the invention solves the problems of slow effect taking and poor effect, can realize rapid penetration of local skin, has short anesthesia effect taking time, long duration and good effect, has no obvious irritation to the skin, has good product stability, can effectively reduce the drug toxicity, and has a good application prospect. The device is suitable for surface anesthesia of non-surgical medical beauty items such as skin beauty, laser treatment and water-light micro-needles.

Provided herein are compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein n, R 19 , R 5 , R 3a , R 6a , R 6b , R 1 , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 17b , R 15a , R 15b , R 16a and R 16b is defined herein. Also provided herein are pharmaceutical compositions comprising compounds of formula (I) and methods of using such compounds, for example, in the treatment of CNS-related disorders. JPEG2022504607000068.jpg4662(I)

The invention belongs to the technical field of pharmaceutical preparations, and relates to a riptacaine cream as well as a preparation method and application thereof, and the preparation method of the riptacaine cream comprises the following steps: preparing carbomer gel, preparing an oil phase, preparing a water phase, primarily emulsifying, homogenizing and gelating, finely homogenizing and filling. According to the invention, polyoxyethylene (54) hydrogenated castor oil is innovatively used as an auxiliary material, triple functions of a co-melting solvent, an emulsifying agent and a stabilizing agent are realized at the same time, and any liquid grease, solvent or other surfactants do not need to be additionally added in the prescription. Through a unique'water-gel-oil 'composite structure design, oil drops are physically wrapped by a carbomer gel network and are positioned in network pores, so that the mechanical stability superior to that of a conventional emulsion is provided, and no layering is generated through high-speed centrifugal test verification. In conclusion, the invention develops the riptacaine preparation which has the advantages of few types of auxiliary materials, higher stability, quicker effect taking and capability of expanding a new dosage form and a new process.

The present invention relates to a soluble microneedle for local anesthesia and a local anesthesia patch comprising same, the soluble microneedle comprising an amide-based local anesthetic, hyaluronic acid, and polyvinylpyrrolidone in a specific content ratio. The present invention uses the soluble microneedle to implement direct drug delivery by physically permeating through the stratum corneum and mucosa, and thus a precise and rapid anesthetic effect may be exhibited. Especially, the microneedle comprising a specific amount of polyvinylpyrrolidone is dissolved, and the anesthetic contained in the microneedle is rapidly delivered to nerve cells, and thus the disadvantage of a long waiting time of conventional anesthetic creams may be overcome, and thus the present invention has the advantage of being usable in various ways in dental, dermatology, and other surgical procedures requiring local anesthesia.

The invention belongs to the technical field of pharmaceutical preparations, and relates to an external gel emplastrum containing local anesthetics as well as a preparation method and application of the external gel emplastrum. The gel emplastrum comprises a backing layer, an emplastrum body layer and an anti-sticking film from bottom to top, wherein the pasty fluid layer adopts organic water-retaining resin as a framework structure, and contains local anesthetics accounting for 1-20% of the weight of the pasty fluid layer. The external gel emplastrum containing the local anesthetic can have a higher transdermal release rate, and can improve the stability of a supply chain of the added part of neutralized polyacrylic acid.

The invention provides an analgesic microneedle patch based on 3D printing and a preparation method and application thereof, and belongs to the technical field of biomedical materials.The preparation method of the hydrogel microneedle patch based on 3D printing comprises the following steps that 1, cold water fish skin gelatin is dissolved in DPBS, and a gelatin solution is obtained; (2) mixing methacrylic anhydride and gelatin liquid to generate polymerization reaction, so as to obtain a hydrogel material; and 3) loading an anesthetic and analgesic drug on the hydrogel material, and printing by a photocuring 3D printing method to obtain the hydrogel microneedle patch. The 3D printing technology is combined with a microneedle which is a dysmenorrhea-free skin drug delivery system, local anesthetics are loaded into the microneedle patch, on the basis of painless drug delivery, the drug delivery efficiency is improved, the drug onset time is shortened, and then the effect of effectively, rapidly and safely playing a local anesthesia role is achieved.

The invention relates to particular prodrugs and analogs of (3α,5α)-3-hydroxy-21-(1H-imidazol-1-yl)-3-methoxymethyl)-pregnan-20-one, in free or pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use as sedatives, hypnotics, anxiolytics, and / or anesthetics, and methods for treatment of depression, anxiety, insomnia, epilepsy, and other central nervous system disorders, as well as to combinations with other agents.

The invention belongs to the technical field of medical polymer materials, relates to an amphiphilic block copolymer, a hydrogel material containing the amphiphilic block copolymer and a preparation method and application of the amphiphilic block copolymer, and particularly discloses a poly (2-ethyl-2-oxazoline)-polyamino acid block copolymer and a preparation method and application of a hydrogel material of the poly (2-ethyl-2-oxazoline)-polyamino acid block copolymer. The hydrogel material provided by the invention has excellent injectability, and the modulus and gelation temperature of a gel preparation can be adjusted by changing the molecular weight and concentration of the amphiphilic block copolymer, so that the hydrogel material adapts to different physiological environments, is applied to different indications, and can be applied to various diseases. Compared with other hydrogel in which the chemical structure of the polymer needs to be changed, the hydrogel is more convenient.

A container for a lyophilized rapidly infusing composition is described. The container comprises a planar lidding layer attached to a well layer comprising pockets for the therapeutic product. The lidding layer may comprise an aluminum layer, a thermoplastic polymer layer, and a labeling layer. The well layer may comprise an aluminum layer, two polyamide layers, and two thermoplastic polymer layers. A drug product assembly is also disclosed, which includes at least one therapeutic product sealed within the at least one pocket of the container.

Provided in the present application are a cyclic quaternary ammonium salt compound, and a preparation method therefor and the use thereof. Further provided are the cyclic quaternary ammonium salt compound as represented by general formula (I), or an isomer or a solvate thereof and a composition thereof and the use thereof in the preparation of anesthetic or analgesic drugs. Each substituent in the general formula (I) is the same as that defined in the description.

The invention discloses a dexmedetomidine and propofol combined reagent and a combination method, and relates to the technical field of combined use of anesthetic drugs. According to the method, firstly, dexmedetomidine is subjected to intravenous pump injection within 5-15 minutes according to the dosage of 0.5-1.0 mu g / kg, propofol is given within 2 minutes after the dexmedetomidine is subjected to general anesthesia, and the dosage of the propofol can be reduced by 10%-50% compared with that of propofol which is independently used. Through pretreatment of dexmedetomidine, the anesthetic effect of propofol can be enhanced, adverse reactions such as blood pressure drop and respiratory depression can be effectively reduced, and anesthetic safety and controllability are improved. The combined reagent comprises independent containers for respectively loading the dexmedetomidine injection and the propofol emulsion, and can be packaged by adopting a double-cavity pre-filled injector, and sequential injection is realized through a controllable opening mechanism, so that unstable emulsification and titer change caused by physical mixing of medicines are avoided.

The invention provides a nitrogen-containing heteroaryl compound as well as a preparation method and application thereof. In particular, the present invention relates to a nitrogen-containing heteroaryl compound represented by general formula I, a preparation method thereof, a pharmaceutical composition containing the nitrogen-containing heteroaryl compound, and an application of the nitrogen-containing heteroaryl compound or the pharmaceutical composition thereof as a GABBA receptor agonist in preparation of drugs in the field of central nervous systems. # imgabs0 #

The invention discloses a ripdicaine emulsifiable paste, and a preparation method and application of the ripdicaine emulsifiable paste. The preparation method of the lidocaine emulsifiable paste comprises the following steps: (1) melting a mixture of lidocaine, prilocaine and an emulsifier to prepare an oil phase; mixing the oil phase with water, and homogenizing for 28 to 50 minutes, so as to obtain primary emulsion; (2) homogenizing the carbomer solution, mixing the homogenized carbomer solution with an alkaline pH regulator, and regulating the pH value of the system to 8.2-9.2 to prepare a carbomer matrix; and (3) mixing the prepared milk, the carbomer matrix and the balance of water to prepare the ripdicaine emulsifiable paste. According to the present invention, the preparation method of the riprodicaine cream is optimized, such that the prepared riprodicaine cream has high stability, the stability of the lidocaine and the prilocaine is ensured during the preparation process, the content of the related substances is reduced, the ideal in vitro release effect is provided, and the local anesthesia effect is rapidly achieved.

This invention provides a novel GABA structure with better efficacy, reduced side effects, and greater safety for clinical use. A This invention relates to receptor agonists, specifically a phenol derivative, its preparation method, and its use in the central nervous system. The phenol derivative provided by this invention offers more and better drug options for inducing or maintaining anesthesia in animals or humans, promoting sedation and hypnosis, and treating and / or preventing anxiety, nausea, vomiting, migraines, seizures, epilepsy, neurodegenerative diseases, and other central nervous system-related disorders.