1139results about "Anaesthetics" patented technology

New Treatments for Pain The Application describes new SOS1 inhibitors for use in the treatment of pain and cancer.

The invention provides a compound phospholipid gel sustained release preparation and a preparation method thereof. The preparation mainly comprises a local anesthetic, a non-steroidal anti-inflammatory drug, phospholipid and water for injection. The preparation can be injected around a surgical incision or directly instilled or coated at the surgical incision to achieve the purpose of long-acting analgesia, and is used for postoperative analgesia.

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 invention belongs to the technical field of medicine preparation, and relates to PLGA gel used as an injectable long-acting local anesthesia medicine as well as application and a preparation method of the PLGA gel. The PLGA gel comprises the PLGA gel which is loaded with superparamagnetic Fe3O4 particles and a small molecule local anesthetic, namely, levobupivacaine (Levobupi). The PLGA hydrogel containing Fe3O4 and levobupivacaine can be used as an injectable long-acting local anesthesia medicine, and the hydrogel can be changed from liquid to solid after being injected into a living body, so that the release efficiency of the medicine is slowed down, and the local action time of the hydrogel is prolonged. In addition, the hydrogel can undergo a phase change from a solid state to a liquid state under magnetocaloric therapy (MHT), increase pore diameter, promote release of levobupivacaine, and provide enhanced pain relief in vivo. Compared with the prior art, the invention has the beneficial effects of simple synthesis and easy industrialization. The drug release rate is adjusted through the phase change of the hydrogel, super-long-acting analgesia is realized, and the analgesia time is gt; 20 days. The gel can be loaded with various local anesthesia drugs such as L-bupivacaine, and pain management can be carried out on various pain scenes clinically.

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.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a preparation process of lidocaine hydrochloride gel. The preparation process of the lidocaine hydrochloride gel provided by the invention comprises the following steps: preparing materials, sterilizing and carrying out stepped cooling, the step-type cooling process comprises the following specific steps: in the first stage, firstly preserving heat at 90-60 DEG C for 1-2 hours, wherein the stirring rotating speed is 10-60 rpm; in the second stage, heat preservation is conducted for 1-2 h at the temperature of 60-40 DEG C, and the stirring rotating speed is 10-60 rpm; and a third stage: finally standing and preserving heat at 40-10 DEG C for 5-15 hours. According to the preparation process of the lidocaine hydrochloride gel provided by the invention, the colorless and transparent lidocaine hydrochloride gel with high uniformity and good stability can be obtained, and the practical reliability and safety of the lidocaine hydrochloride gel are greatly improved.

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.

Implantable depots for delivering therapeutic agents and associated systems and methods are provided. In some embodiments, an implantable depot for treating pain in a subject after a surgical procedure includes a therapeutic region having a first polymer and an analgesic agent, a first control region including a second polymer, and a second control region including a third polymer. The first and second control regions can cover first and second surfaces of the therapeutic region to inhibit release of the analgesic agent therefrom. The depot can include one or more holes extending through the first and second control regions and the therapeutic region to form one or more exposed portions. When implanted in the subject, the implantable depot can release the analgesic agent from a lateral surface of the therapeutic region between the first and second surfaces, and from the exposed portions of the therapeutic region.

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.

There is provided methods for insect control, including controlling myiasis, in animals by affixing to the animal an elastomeric band having infused or contained within an insecticide, an insect repellant, lidocaine, or any combination thereof. The insect control may be a dual-mode control and may be in respect of existing or impending open wounds, including open wounds caused by castration, tail docking, umbilical cord ligation, or dehorning of an animal. There is also provided methods for castration, docking, umbilical cord ligation, or dehorning of an animal with concurrent insect control. Also provided are elastomeric bands for insect control and methods for preparing such elastomeric bands.

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 discloses a substituted phenol compound as well as a preparation method and application thereof. According to the present invention, the propofol is subjected to structure optimization to obtain the compound having the structure represented by the formula (I), such that the safety is significantly improved, the anesthetic effect is excellent, various preparation forms can be conveniently prepared, the clinical application in various drug delivery forms can be easily achieved, the structure is novel, and the preparation method is simple. # imgabs0 #

The invention discloses a benzodiazepine # imgabs0 # compound with a structure as shown in a formula I or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a polymorphic substance, a solvate, a metabolite or a prodrug of the benzodiazepine # imgabs0 # compound. The benzodiazepine # imgabs 1 # compound disclosed by the invention has the characteristics of low toxicity, high safety, quick action, short action time, stable anesthesia, quick metabolism, quick reviving and the like. The invention further discloses application of the benzodiazepine # imgabs2 # compound or pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, metabolite or prodrug thereof in preparation of sedative or anesthetic drugs, and further discloses application of the benzodiazepine # imgabs2 # compound or pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, metabolite or prodrug thereof in preparation of sedative or anesthetic drugs. # imgabs3 #

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.