36 results about "Dezocine" patented technology

A composition comprising the tannate of an opioid. Suitable opioids include alfentanil, buprenorphine, butorphanol, carfentanil, cocaine, codeine, dezocine, diacetylmorphine, dihydrocodeine, dihydromorphine, diphenoxylate, diprenorphine, etorphine, fentanyl, heroin, hydrocodone, hydromorphone, beta-hydroxy-3-methylfentanyl, levo-alpha-acetylmethadol, levorphanol, lofentanil, meperidine, methadone, morphine, nalbuphine, nalmefene, o-methylnaltrexone, naloxone, naltrexone, oxycodone, oxymorphone, pentazocine, pethidine, propoxyphene, remifentanil, sufentanil, tilidine and tramadol. The opioid tannate may be readily prepared by reacting an opioid free base with tannic acid, either neat or in the presence of up to about 30 wt. % water, at a temperature of about 60 to about 150° C. and thereafter recovering the resultant opioid tannate. The opioid tannate may also be prepared by an alternative process that involves reacting the opioid free base with water at a temperature such that not more than about 10 wt. % of the opioid tannate will be decomposed and thereafter removing the water by freeze-drying.

The present invention discloses a method for preparing a high-sensitivity nano-zirconia-doped dezocine molecular imprinting electrochemical sensor, the high-sensitivity nano-zirconia-doped dezocine molecular imprinting electrochemical sensor is prepared by use of dezocine as a template molecule, (5s, 8s)-3-(4'-chloro-3'-fluoro-4-propenyl-biphenyl-3-yl)-4-hydroxy-8-methoxy-1-aza-spiro [4.5] dec-3-ene-2-one as a single function monomer, azobisisobutyronitrile as an initiator, nano-zirconia as a dopant and maleic rosin ethylene glycol acrylate as a crosslinking agent, wherein the maleic rosin ethylene glycol acrylate is prepared from rosin as a raw material, and the method is simple and practical, and overcomes the shortcomings that a conventional analysis method is complicated, expensive in equipment, and low in sensitivity.

The invention discloses an injection of dezocine. Every milliliter of the injection consists of the following ingredients: 10.1mg to 25mg of dezocine, 1mg to 15mg of sodium chloride, 5mg to 20mg of lactic acid, 300mg to 450mg of propanediol, sodium hydroxide and the balance of nitrogen saturated injection water, wherein the consumption of the sodium hydroxide is determined as follows: the dezocine, sodium chloride, lactic acid and propanediol are dissolved by utilizing 30 to 70 percent by volume of the nitrogen saturated injection water to obtain a solution 1, and the pH value of the solution 1 is adjusted by utilizing a sodium hydroxide aqueous solution to 3.5 to 5.0. The injection is good in stability, stable in quality and suitable for being stored for a long time.

The invention provides a detection method for dezocine related substances. Octadecyl silane bonded silica gel is adopted as a chromatographic column of a filling agent, and an acetonitrile-triethylamine solution is adopted as a mobile phase, wherein the acetonitrile-triethylamine solution is obtained by taking 1000 ml of water, adding 5 ml of triethylamine and 2 ml of a tetrabutyl ammonium hydroxide water solution, and adjusting pH to 3.2 through diluted phosphoric acid (1-5), and the ratio of acetonitrile to triethylamine is 200:800; the flow rate is 0.6 ml per min, and the detection wavelength is 281 nanometers. According to the detection method for dezocine related substances, the concentration of buffer salts is increased, elution is enhanced, an ion-pairing agent is added, the peak shape is improved, and the problems that due to the fact that the number of theoretical plates of an original method is small and a main peak cannot be rapidly eluted, the peak width is large and trailing is serious are solved.

The invention provides a dezocine A crystal form. Cu-Kalpha ray radiation, X-ray powder diffraction represented by an angle 2theta has characteristic peaks at 9.261+/-0.1, 11.142+/-0.1, 12.334+/-0.1, 13.007+/-0.1, 14.068+/-0.1, 14.709+/-0.1, 15.142+/-0.1, 18.538+/-0.1, 19.420+/-0.1, 19.675+/-0.1, 23.218+/-0.1, 24.720+/-0.1, 25.710+/-0.1, 27.183+/-0.1, 28.081+/-0.1, 28.348+/-0.1 and 31.040+/-0.1. The invention further provides a preparation method of the dezocine A crystal form. The dezocine A crystal form disclosed by the invention has extremely high bioavailability. The preparation method of the high-purity dezocine A crystal form disclosed by the invention has the technical effects that the impurity content is reduced, the individual impurity content is reduced from 0.15% to 0.05% or less, the total impurity content is reduced from 1.0% to 0.3% or less, the enantiomer content is not more than 0.2%, and the technical effect of simple and convenient operation is achieved.

The invention discloses a preparation method of a dezocine impurity A and homologues thereof. The method includes the steps of: taking dezocine and homologues thereof as the raw material, adopting a transition metal as the catalyst and using a peroxide as the oxidizing agent, and carrying out reaction to obtain the dezocine impurity A and homologues thereof. The invention has the advantages that:a new chemical method is provided to convert phenolic substances into epoxides, at the same time the used reagents are simple and easily available, the operation is simple, and parts of the unreactedraw materials can be recovered.

Disclosed are a sustained release suspension containing dezocine analogue ester and a preparation method therefor. According to the present invention, an injectable oily auxiliary material which may pharmaceutically serve as a sustained-release depot and an excipient are selected, and micronization technology is used jointly with high pressure homogenization technology and an anti-solvent technique to prepare an injectable long-acting suspension. The main components of the suspension are a compound represented by formula (I), the injectable oil, and the like.

The invention discloses a dezocine separation and purification method, and relates to the technical field of medicine production, separation and purification are carried out according to organic compounds, and the dezocine separation and purification method comprises the following steps: step 1, preparing materials and reagents; 2, carrying out sample treatment; and step 3, separation and purification of dezocine. According to the invention, dezolamide salt, melizocine salt and dezocine are purified and prepared, dezocine is stored, and synthesis steps and reaction conditions are optimized, so that the synthesis period is shortened, the purification preparation route is simple, the steps are few, the yield is high, the operation is simple, the synthesis period is greatly shortened, the reaction conditions are mild, the process safety is improved, the raw material cost is low, and industrialization is facilitated; key process parameters and product quality standards are determined, so that key control points in the dezocine purification process can be quickly mastered, dezocine purification preparation can be efficiently and stably carried out, and convenience is brought to operation.

The present invention relates to the technical field of medicine, in particular to a conjugate of dezocine and polyethylene glycol and a pharmaceutical composition thereof. The conjugate of dezocine and water-soluble oligomer provided by the present invention has better pharmacokinetic properties and a high drug absorption degree, may reduce the side effects of the drug, and achieve a smaller administration dosage and a more diverse mode of administration, such as oral administration, in clinic. Compared with dezocine, the conjugate of the present invention has a stronger analgesic effect and a longer analgesic duration, may reduce the frequency of drug administration, improve patient compliance, and has advantages in effectiveness and safety of the drug, as well as drug tolerance, etc.

The invention discloses a preparation method of a dezocine impurity. (5R,11S,13S)-3-methoxy-5-methyl-5-methyl-5,6,7,8,9,10,11,12-octahydro-5,11-methylbenzocyclononene-13-amine is used as an initial raw material to efficiently synthesize and prepare (5R,11S)-3-hydroxy-5-methyl-5-methyl-5,6,7,8,9,10,11,12-octahydro-5,11-methylbenzocyclononene-13-imine. The preparation method has the advantages of simple operation, easily available raw materials, mild reaction conditions, high product purity and high yield, and is suitable for large-scale preparation. The synthesized impurity can be used for qualitative and quantitative analysis of impurities, so the medication safety of dezocine can be improved.

The invention discloses an asymmetric synthesis method of a dezocine key intermediate. The method comprises the following steps of carrying out nucleophilic reaction on a compound 1 and a compound 2 in an ether solvent C under the condition of alkali A to obtain a compound 3, carrying out coupling reaction on the compound 3 in an aprotic organic solvent D under the action of alkali B, a palladium catalyst and a chiral ligand (R)-BINAP at 80-110 DEG C to obtain a compound 4, wherein the palladium catalyst is selected from any one or more than two of Pd(OAc)2, Pd(dba)2 and Pd2(dba)3, and reacting the compound 4 in an ether solvent F under the action of alkali E and a methylation reagent to obtain a compound 5. The method is simple and easy to operate, the dezocine key intermediate with high optical purity can be obtained, and the method is suitable for industrial production.