97 results about "Propofolum" patented technology

The invention relates to a phosphoryl carboxylic acid propofol ester derivative which has the general formula (I). The method comprises the following steps: propofol reacts with 2-halogenated carboxylic acid and a derivative thereof by alkali to obtain corresponding ester and then the product reacts with phosphoric acid or thiophosphoric acid and the derivative thereof by dissolvent to obtain a water-soluble product or the propofol reacts with a 2-halogenated carboxylic acid phosphate ester derivative by the alkali to obtain the corresponding ester and then the ester is catalyzed, hydrogenated and salified to obtain the water-soluble product (I). The preparation method has mild reaction condition, high yield, simple operation and industrialized prospect, and a prepared oral preparation has the characteristics of high bioavailability, rapid absorption, high stability, and the like; and auxiliary materials with safety defects, such as a surface active agent, and the like can not be added into the prepared injection, thereby improving the stability of the preparation, reducing or removing injection pain, increasing the compliance of patients, overcoming the defects of propofol emulsion and having the advantage of obvious effect. The invention has the structural general formula (I).

The invention discloses a method for monitoring traced propofol narcotic rapidly and sensitively. In the method, an ion mobility spectrometry technology is taken as a basic detection technology, and an anion mode is adopted to establish a method for monitoring traced propofol narcotic. The method comprises the following steps: feeding a gas sample containing propofol into an ion mobility spectrometry tester for analysis to obtain a detecting signal, and then carrying out qualitation and quantitation. According to the invention, the measurement of a narcotic sample can be detected in real time, and the limit of detection of the propofol narcotic can reach 0.5ppb. The detecting method is simple, convenient, rapid and efficient and is good in reliability.

The invention discloses a formula and preparation method of a novel propofol fat emulsion preparation which causes no pain or can be used for obviously lowering injection stimulation and pain. The novel preparation comprises the main constituents of propofol, an emulsifier, refined soybean oil or other refined oil as an oil-soluble diluent, oleic acid or oleate with the effect of assisting emulsification, vitamin E or derivatives thereof with an antioxidation effect, an ionic complexing agent, and glycerol or micro molecular sugar as an isoosmotic adjusting agent.

The invention discloses a freeze-drying preparation of a water-solubility propofol precursor compound and a preparation method thereof. The freeze-drying preparation of the propofol precursor compound, prepared in the method of the invention, has the advantages of favorable water solubility, stability and safety.

The invention provides a preparation method of propofol, which includes following steps: (1) performing Friedel-crafts reaction to p-nitrophenol and isopropanol or 2-halogenated propane under catalysis of an acid to prepare a compound I; (2) performing acylation protection to the compound I to prepare a compound II; (3) performing a reduction reaction to the compound II to prepare a compound III; (4) performing a diazo-reaction to the compound III to prepare a compound IV; and (5) under a weak reducing agent condition, performing a decomposition reaction to the compound IV and meanwhile carrying out hydrolysis under an alkaline condition to obtain the propofol V. The raw materials of the preparation method are easy to obtain. The preparation method is simple in process and is high in yield.

The invention relates to a medicinal composition containing propofol and process for preparation, wherein each 1kg of the freeze-dried product comprises propofol 1g, oil for injection 0-20g, emulsifying agent 0.1-10g, auxiliary emulsifying agent 0.001-5g, other stabilizing agent 0-2g, freeze-drying protective agent 1-40g, and right amount of pH modifier. The invention can achieve better constancy.

The invention belongs to the technical field of medicine and particularly relates to a double-effect anesthetic and a preparation method and application thereof.The invention discloses a compound shown in the general formula (I).The compound can generate analgesic flurbiprofen and anesthetic propofol after hydrolysis, the analgesic and the tranquilizer are combined, dosage frequency of anesthetists is reduced, the anesthetic process is quicker, the occurrence rate and the severity of propofol injection pain can be remarkably reduced, adverse reactions of single drug are reduced, and the anesthetic has the advantages that the anesthetic takes effects quick, lasting time is short, anesthetic efficiency is high, controllability in operation is high, and patients recover quickly.Please see the structural formula in the description, wherein R refers to O or a radical group in the description, and n is 2-4.

The invention relates to a water-soluble amino acid ester derivative of propofol and application thereof. Amino acid ester of the propofol has a structure with a formula (I), wherein R is shown in the description. The invention also relates a preparation method for a compound with the formula (I), a medicinal salt thereof, a compound-containing medicinal composition and application of the compound serving as narcotic medicines.

Belonging to the field of organic chemistry and pharmaceutical chemicals, the invention discloses preparation and application of a monodisperse polyethylene glycol monomethyl ether modified propofol prodrug with a novel structure. Monodisperse polyethylene glycol monomethyl ether and propofol can be connected by an in-vivo degradable chemical bond to prepare a series of carbonic ester type and acetic ester type prodrugs respectively. By adjusting the length of the monodisperse polyethylene glycol monomethyl ether chain, the method can synthesize corresponding water-soluble propofol prodrugs, the longer the monodisperse polyethylene glycol monomethyl ether chain is, the better the water solubility is, along with the improvement of the water solubility, the prodrug can be made into aqueous solution preparations so as to avoid the defects of fat emulsion in propofol fat emulsions. The method provided by the invention has the advantages of simple reaction, mild conditions and low cost, andis convenient for industrial production.

The invention belongs to the field of pharmacology and pharmaceutics, and relates to a propofol composition used for injection, a preparing method thereof and uses of the propofol composition. A product of the propofol composition is good in fluidity and free of wall hanging, has a single-phase, transparent, clear and bright appearance, can be subjected to clarity detection, and is free of preparation layering phenomena after the product is repeatedly frozen and thawed. In a process of forming a propofol fat emulsion system when the product encounters water, homogenization treatment is not needed, and spontaneous emulsification can occur only by slight oscillation. During clinical using, the product can spontaneously emulsify to form a fat emulsion system meeting injection requirements after the product is diluted with normal saline or a glucose solution, and other aqueous solutions and is slightly oscillated. A preparation process is simple. Only a common physical stirring step is needed, and a homogenizing step or a water removing step is not needed. A prepared propofol fat emulsion concentrate liquid can be sterilized by passing through a microporous filtration membrane having a size of 0.22 [mu]m. After emulsification, the content of free propofol is low, and the phenomenon of pain during administration caused by existence of the free propofol is reduced. The propofol composition, the preparing method and uses have advantages of simple preparation process, low production cost, and easy transportation and storage, and have a good application prospect.

The invention relates to a carbonic acid diester water-soluble derivant of amino acid and propofol, and application of the carbonic acid diester water-soluble derivant of amino acid and propofol. The amino acid carbonic acid diester of propofol has the structure which is shown as a formula (1), wherein R is shown in the specifications; and the invention also discloses a preparation method for the compound with the formula (I), pharmaceutical salt of the compound, a medical composition of the compound and the pharmaceutical salt of the compound, and application of the compound used as a dope.

The invention provides a propofol derivative as well as a preparation method and purpose thereof. The propofol derivative is obtained by chemically modifying the hydroxyl group in the structure of propofol. The related propofol derivative can be used in pharmaceutical composition and can be used for producing medicaments for anaesthesia.

The invention relates to a synthesis method for fospropofol disodium. The synthesis method for the fospropofol disodium comprises the following steps of: 1, reacting bromochloromethane with propofol under the action of sodium hydroxide at the temperature of between 30 and 40 DEG C to obtain 2-chloromethoxy-1,3-diisopropyl benzene, wherein the equivalent ratio of the bromochloromethane to the propofol is (5-7):1; 2, reacting the 2-chloromethoxy-1,3-diisopropyl benzene with 60 percent phosphoric acid, adding triethylamine and tetrabutyl ammonium bromide, reacting at the temperature of between 90 and 100 DEG C, and performing treatment by using sodium hydroxide to obtain the fospropofol disodium. The synthesis method has the advantages of low cost, short reaction route, environment friendliness, high purity of the obtained product and the like.

The invention discloses a propofol composition for injection. The composition is prepared from, by mass, 0.1-0.5% of propofol, 0.1-2% of emulsifier, 5-30% of oil for injection, 2-3% of osmotic pressure regulator, an appropriate amount of pH value regulator and an appropriate volume of water for injection. All links of the production process of propofol injection are strictly controlled so that the core quality of propofol fat emulsion injection can be remarkably improved; in addition, the process is easy to implement, and the industrialization of the high-quality propofol fat emulsion injection is achieved.

The invention discloses a medicine capable of treating refractory insomnia, and a preparation method of the medicine. The medicine comprises the following ingredients: propofol, hyoscine hydrobromide,croscarmellose sodium, mannitol, low-substituted hydroxypropyl cellulose and magnesium stearate. Specifically, the medicine is optimally a sublingual tablet, and the medicine can effectively alleviate the symptoms of patients and improve the sleep and living quality of a patient by aiming at the inducement of the refractory insomnia.

The invention relates to a compound propofol water-based injection for dogs, a preparing method thereof and application, and belongs to the technical field of veterinary medicine preparation. The compound propofol water-based injection is suitable for immobilizing and narcotizing dogs. The injection uses propofol and xylazine hydrochloride as active components, and a carrier acceptable pharmaceutically is added. The compound propofol water-based injection has hypnosis, calming and abirritation functions and can achieve the effect of anesthesia induction or anesthesia maintenance through one-time injection delivery, and the anesthesia process is more convenient; dosage of all single drugs is reduced, and a good anesthesia effect is achieved with the minimum side effect. The injection is stable in quality and suitable for subcutaneous, muscle and intravenous injection, and pain is avoided in the injection process. A fat emulsion carrier applied the most extensively is abandoned from the preparation, a water-based solution is prepared, microorganism growth can be limited, the injection can be sucked for multiple times, and the problem of medicine waste of a propofol fat emulsion preparation is avoided.

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 alkaline amino acid ester salt of propofol, a preparation method and applications thereof. The preparation method comprises the following steps: taking alkaline amino acid as the raw material, subjecting alkaline amino acid to carry out reactions with ditertbutyl dicarbonate ester in an alkaline condition so as to obtain N-Boc alkaline amino acid, then subjecting the N-Boc alkaline amino acid to carry out condensation reactions with propofol in the presence of DCC/DMAP, and finally removing the Boc protection groups in an acidic condition so as to obtain the pharmaceutically-acceptable propofol alkaline amino acid ester salt represented by the structural formula I. The propofol alkaline amino acid ester salt can be used to prepare drugs for tranquilizing, hypnotics, and narcotics, has a good solubility in water, can release propofol in human body to generate pharmaceutical activity, is capable of being made into different dosage forms to apply to the clinic, and overcomes the shortages brought by single using of propofol. The synthesis method has the advantages of simple operation, available raw material, low cost, and strong versatility.