50 results about "Lornoxicam" patented technology

The invention relates to lomoxicam freeze-dried powder injection and a preparation method thereof. The freeze-dried powder injection comprises omoxicam, mannite, tromethamine, EDTA and pH regulator. The dosage of the mannite is 3.5 to 8.5 g of mannite per gram of lomoxicam, and the dosage of the EDTA is 0.015 to 0.025g of EDTA per gram of lomoxicam. The invention adopts EDTA to replace EDTA-disodium salt and selects the dosages of the mannite and EDTA so that the clarity of the reconstituted obtained freeze-dried powder is greatly improved, and the formability is good; in addition, the invention adopts two pH regulators, in the process, one pH regulator is used to regulate the solution to a pH range, then the other pH regulator is used to regulate the solution to another pH range, and the freeze drying technology is controlled strictly. The prepared freeze-dried powder injection has great improvement of stability and favorable resolubity.

The present invention relates to orally quick disintegrating lornoxicam composition and its preparation process. The orally quick disintegrating lornoxicam composition includes lornoxicam in 100 weight portions, pharmaceutically acceptable lipoid taste mask 25-100 weight portions, and pharmaceutically acceptable disintegrating agent 50-500 weight portions. The present invention also provides the preparation process of the oral disintegrating lornoxicam composition. The composition of the present invention can disintegrate inside oral cavity in good taste and act in stomach. The composition of the present invention is easy taken, especially for those people with dysphagia.

The invention relates to the technical field of medicine synthesis, and particularly relates to a synthesis method of lornoxicam. The method comprises the steps of taking 6-chlorine-4-hydroxyl-2-methyl-2-H-thieno[2,3-e]-1,2-thiazine carboxylic acid methyl ester-1,1-dioxide and 2-aminopyridine as raw materials and dimethylbenzene as a solvent, adding a stabilizer, performing heating reflux to perform ammonolysis reaction, reducing the temperature, performing reduced pressure concentration to remove the solvent, adding an organic solvent, pulping, and filtering to obtain a lornoxicam crude product; and refining to obtain the lornoxicam. According to the method, p-toluenesulfonic acid is used as a stabilizer, the reaction temperature is reduced, meanwhile, the reaction is promoted to be carried out forwards, and the product quality and yield are improved; and meanwhile, the dosage of an industrial solvent is reduced, the post-treatment process is optimized, and the three-waste treatment cost is reduced.

The invention aims at providing a method for preparing an optimal preparation of lornoxicam flexible liposome in a screening mode with the Box-Behnken response surface method. The response surface method has the advantages that experiment design is comprehensive, scientific and accurate, and the interaction of multiple factors can be studied. According to the method, four factors including the phospholipid concentration, the phospholipid-cholesterol mass ratio, the total lipid-Tween 80 mass ratio and the total lipid-medicine mass ratio which influence the flexible liposome preparing process greatly are investigated separately, Box-Behnken response surface experiment design is conducted with the encapsulation rate and the particle size as the optimization indexes, and the optimal preparation of the lornoxicam flexible liposome is obtained through optimization. The lornoxicam flexible liposome obtained through optimization is high in encapsulation rate and uniform in size distribution and has the characteristic of slow release, which provides a good experimental basis for the process of preparing the lornoxicam flexible liposome into hydrophilic gel at the later stage.

The invention relates to a lornoxicam freeze-dried powder injection and a preparation method thereof. The powder injection includes lornoxicam, mannitol and trometamol, and also includes EDTA and a pH regulator, the dosage of the mannitol is 3.5-8.5 grams per gram of lornoxicam, and the dosage of the EDTA is 0.015- 0.025 g / g Lornoxicam. In the present invention, EDTA is used to replace EDTA-disodium salt, and the dosage of EDTA and mannitol is screened at the same time, the clarity of the prepared lyophilized product after reconstitution has been significantly improved, and the formability is good; in addition, the present invention Two kinds of pH regulators are selected. In the preparation process, first use one pH regulator to adjust the solution to a pH value range, then use another pH regulator to adjust the solution to another pH value range, and freeze it. The drying process is strictly controlled, and the stability of the prepared freeze-dried powder injection is significantly improved, and the reconstitution property is good.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a synthesis method of high-purity lornoxicam. The method comprises the following steps: by taking 6-chloro-4-hydroxy-2-methyl-2-H-thieno [2, 3-e]-1, 2-thiazine carboxylic acid methyl ester-1, 1-dioxide and 2-aminopyridine as raw materials and xylene as a solvent, carrying out distillation reaction, condensing mixed gas obtained by the distillation reaction to obtain condensate, adsorbing methanol in the condensate by adopting a solid acid catalyst, and recycling the adsorbed condensate. According to the invention, the methanol generated by the reaction is distilled out so as to promote the reaction to proceed forwards, and then the methanol is absorbed under the catalysis of H2SO4 / MxOy superacid solid acid, so that the xylene returned to the reaction system does not contain methanol, and the coking of the reaction is reduced so as to improve the product quality and yield; and the purity of the prepared lornoxicam is high and can reach 99.9% or above, the solvent amount is reduced, and the method is suitable for industrial production.

The invention discloses a lornoxicam and puerarin eutectic crystal, which is formed by combining lornoxicam and puerarin according to a molar ratio of 1: 1, and has a powder X-ray diffraction patternexpressed by a 2theta angle value, and an infrared spectrogram. The method comprises the following steps: dissolving the lornoxicam and the puerarin into an organic solvent according to a certain molar ratio, carrying out reduced pressure rotary evaporation on the solvent, carrying out vacuum drying, and putting into a resistance furnace to remove the solvent, thereby obtaining the lornoxicam andpuerarin eutectic crystal. The eutectic crystal is different from a lornoxicam monomer, a puerarin monomer and a physical mixture of the lornoxicam monomer and the puerarin monomer in powder X-ray diffraction and infrared ray, the crystal form of the eutectic crystal is a new crystal form different from the monomers and the physical mixture, and the compressibility of lornoxicam and the water solubility of the lornoxicam and the puerarin are improved.

The invention discloses Lornoxicam microspheres, in which polylactic acid-glycolic acid copolymer is used as a carrier and Lornoxicam as a sustained-released medicament; the average diameter of the microspheres is 1-15mum, the span thereof is 1-2, and Lornoxicam accounts to 1-15 percent of the whole microsphere mass. The preparation method of the Lornoxicam microspheres is that: polylactic acid-glycolic acid copolymer is dissolved in dichloromethane to form an organic phase; the sustained-released medicament is mixed and suspended in distilled water to form an internal aqueous phase, and then the internal aqueous phase is added into the organic phase in a dropwise way, thus a primary emulsion is obtained. Next, the primary emulsion is injected by an injector into an external aqueous phase, and a W / O / W multiple emulsion is obtained, and then stirred to fully evaporate dichloromethane, the multiple emulsion is centrifugated to remove the supernatant liquid, cleaned by distilled water; and then the microspheres are obtained, and the microspheres are dried in vacuum, thus the dried powder of Lornoxicam microsphere is obtained. The microspheres enhances the curative effect of the medicament, reduces the toxicity and side effects, and avoids the shortcomings of long term administration, which has quite good effect on the treatment of arthritis.

The invention discloses a freeze-drying technology for injection lornoxicam. The freeze-drying technology is characterized by sequentially comprising the following steps: (1) conducting pre-freezing; (2) conducting sublimation drying in a mode of six-sectional stepped temperature raising as follows: a, heating up a coolant to a minus (6-4) DEG C, preserving heat for 0.5-1.5h, conducting automatic pulsation to promote air permeation when a vacuum degree is 12-18Pa and stopping the air permeation when the vacuum degree is 22-28Pa; b, heating up the coolant to a temperature ranging from minus 1 DEG C to 1 DEG C, preserving heat for 1-1.5h and conducting pulsation to promote air permeation to 22-28Pa; c, heating up the coolant to 4-6 DEG C, preserving heat for 2-2.5h and conducting pulsation to promote air permeation to 22-28Pa; d, heating up the coolant to 9-11 DEG C, preserving heat for 2-2.5h and conducting pulsation to promote air permeation to 22-28Pa; e, heating up the coolant to 14-16 DEG C, preserving heat for 2-2.5h and conducting pulsation to promote air permeation to 22-28Pa; and f, heating up the coolant to 24-26 DEG C, preserving heat for 1-1.5h and conducting pulsation to promote air permeation to 30-36Pa; and (3) conducting secondary sublimation drying. With the application of the freeze-drying technology provided by the invention, moisture content and impurity limit of the product (the injection lornoxicam) can conform to requirements prescribed within, and meanwhile, the time of an entire freeze-drying process can be also shortened.

The invention relates to a double-layer sustained release lornoxicam tablet which comprises (a) a quick release layer and (b) a sustained release layer, wherein, the quick release layer comprises (a1) the lornoxicam, (a2) alkaline matter and (a3) an other optional carrier or pharmaceutically acceptable excipient and the sustained release layer comprises the (b1) lornoxicam, (b2) sustained releasesubstance and (b3) the other optional carrier or the pharmaceutically acceptable excipient. The weight proportion of (a1) and (b1) is 1:50 to 50:1. The invention also provides a preparation method ofthe double-layer sustained release lornoxicam tablet. The double-layer sustained release preparation of the invention has the advantages of the quick effect of the quick release preparation and the sustained effect of sustained release preparation. In addition, the double-layer sustained release preparation can maintain the effect of effective blood concentration continuously and stably after theeffective blood concentration is reached rapidly.

The invention discloses a lornoxicam compound and a purifying method thereof. In the method, a simple silicagel column chromatography method is used, and a proper stationary phase and a proper mobile phase are used, i.e. silicagel is used as the stationary phase and a mixed solvent of isopropanol and acetone with a certain proportion is used as the mobile phase, the temperature of the column is kept to be higher than the room temperature, and the lornoxicam can be efficiently purified. The method can achieve high yield and high purity, thereby being an effective method for obtaining the lornoxicam with high purity.

The invention discloses a co-crystal of lornoxicam and puerarin, the co-crystal is formed by combining lornoxicam and puerarin at a molar ratio of 1:1, and has a powder X-ray diffraction pattern represented by 2θ angle value , and infrared spectra. The preparation method comprises the steps of: dissolving lornoxicam and puerarin in an organic solvent according to a certain molar ratio, rotating the solvent under reduced pressure, drying in vacuum, and placing it in a resistance furnace to remove the solvent, thereby obtaining lornoxicam puerarin eutectic. The eutectic of the present invention is different from the powder X-ray diffraction and infrared of lornoxicam monomer and puerarin monomer and their physical mixtures, and the crystal form of the eutectic is a new one different from monomers and physical mixtures. Crystal form, improve the compressibility of lornoxicam, and the water solubility of lornoxicam and puerarin.

The present disclosure relates to the technical field of drug synthesis, in particular to a method for preparing lornoxicam. The method includes the following steps: using 6-chloro-4-hydroxy-2-methyl-2-H-thieno[2,3-e]-1,2-thiazine methyl carboxylate-1,1-dioxide and 2-aminopyridine as raw materials, and xylene as a solvent; mixing the raw material and solvent, and adding a stabilizer, to obtain a mixture; subjecting the mixture to an ammonolysis; cooling the resulting reactant; conducting a vacuum concentration to remove the solvent; adding an organic solvent and slurrying, and filtering, to obtain a crude lornoxicam; and refining the crude lornoxicam to obtain the lornoxicam. In the present disclosure, p-toluenesulfonic acid is used as a stabilizer to reduce the reaction temperature and promote the reaction to proceed forward, thereby improving the quality and yield of the product.

The invention provides a lornoxicam sustained release tablet and the preparation method thereof. The sustained release tablet includes 2.0-60.00 parts of lornoxicam by weight and 10.00-95.00 parts of sustained release block material by weight; wherein, the sustained release block material includes hydroxypropyl methyl cellulose or compound of hydroxypropyl methyl cellulose and other celluloses. The preparation method is that raw material prescription doses of lornoxicam, sustained release block material and filler are evenly mixed, then added with adhesive to be prepared into soft material; pelletization, drying and finishing granule are carried out according to the conventional technique of the tablet preparation, and the dry grain after finishing granule is added with lubricant, evenly mixed and pressed to make the preparation. Compared with conventional oral lornoxicam preparation, the lornoxicam sustained release tablet can maintain a longer effect after oral administration of thedrug.