105 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 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 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 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.