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CN-121987567-A - Serocaine mucilage and preparation method thereof

CN121987567ACN 121987567 ACN121987567 ACN 121987567ACN-121987567-A

Abstract

The application discloses a salcaine mucilage which comprises 1-3% of salcaine, 0.3-0.6% of carboxymethylcellulose sodium, 0.1-0.3% of chitosan, 1-3% of glycerol, 0.03-0.08% of L-menthol, 0.1-0.6% of glacial acetic acid and purified water, wherein the salcaine comprises salcaine a, b and c, the particle sizes D90 of the salcaine a, b and c are respectively 200-400nm, 700-1100nm and 1500-2000nm, and the dosage ratio of the salcaine a, b and c is (1-1.5): 1 (0.5-1) in terms of weight ratio. The celecoxib mucilage prepared by the application prolongs the action time, is uniformly released, has more stable drug effect, meets the treatment requirement of operation and has excellent stability.

Inventors

  • WANG HONGYAN
  • YANG XINTAO
  • CHEN ZONGYONG
  • LIU YUJING

Assignees

  • 北京阳光诺和药物研究股份有限公司

Dates

Publication Date
20260508
Application Date
20241108

Claims (10)

  1. 1. A salcaine mucilage is characterized by comprising 1-3% of salcaine, 0.3-0.6% of carboxymethylcellulose sodium, 0.1-0.3% of chitosan, 1-3% of glycerol, 0.03-0.08% of L-menthol, 0.1-0.6% of glacial acetic acid and purified water, wherein the salcaine comprises salcaine a, b and c, particle sizes D90 of the salcaine a, b and c are respectively 200-400nm, 700-1100nm and 1500-2000nm, and the dosage ratio of the salcaine a, b and c is (1-1.5): 1 (0.5-1) in terms of weight ratio.
  2. 2. The salcaine cement according to claim 1, wherein the particle sizes D90 of salcaine a, b and c are 300nm, 900nm and 1800nm, respectively.
  3. 3. The salcaine cement according to claim 1, wherein the particle sizes D90 of salcaine a, b and c are 300nm, 1000nm and 2000nm, respectively.
  4. 4. The salcaine cement according to claim 1, wherein the salcaine a, b, c is used in a weight ratio of 1.2:1:0.8.
  5. 5. The salcaine cement according to claim 1, wherein the salcaine a, b, c is used in a weight ratio of 1:1:1.
  6. 6. The celecoxib cement according to claim 1, wherein the celecoxib cement comprises 2% of celecoxib, 0.4% of carboxymethylcellulose sodium, 0.2% of chitosan, 2% of glycerol, 0.05% of L-menthol, 0.4% of glacial acetic acid and purified water.
  7. 7. The salcaine cement according to claim 4, wherein the particle sizes D90 of the salcaine a, b and c are respectively 300nm, 900nm and 1800nm, and the dosage ratio of the salcaine a, b and c is 1.5:1:0.5 in terms of weight ratio.
  8. 8. The salcaine cement according to claim 4, wherein the particle sizes D90 of the salcaine a, b and c are 400nm, 1100nm and 1500nm respectively, and the dosage ratio of the salcaine a, b and c is 1.2:1:0.8 in terms of weight ratio.
  9. 9. The salcaine cement according to claim 4, wherein the particle sizes D90 of the salcaine a, b and c are respectively 200nm, 700nm and 1500nm, and the dosage ratio of the salcaine a, b and c is 1.2:1:0.8 in terms of weight ratio.
  10. 10. A process for the preparation of a salcaine cement according to any one of claims 1 to 9, comprising the steps of: (1) Uniformly mixing the celecoxib a, b and c, placing the mixture into purified water, stirring the mixture to completely dissolve the mixture, then adding glycerol, and uniformly stirring the mixture; (2) Adding new purified water into glacial acetic acid to prepare an acetic acid solution, adding chitosan and L-menthol to dissolve in the acetic acid solution, then adding sodium carboxymethylcellulose, and stirring to completely swell, wherein the viscosity of the chitosan is 100-200mPa.s; (3) Mixing (1) and (2) uniformly, regulating pH to be 6.2-6.8 by adopting sodium hydroxide solution, adding purified water to 1000mL, mixing uniformly, filling the obtained mucilage, capping, sterilizing by 105-125 ℃ steam for 20-40min, and packaging after the finished product is inspected to be qualified.

Description

Serocaine mucilage and preparation method thereof Technical Field The application belongs to the technical field of western medicine preparations, in particular relates to a local anesthetic pharmaceutical preparation, and particularly relates to a celecaine mucilage for surface local anesthesia. Background Seroka is a local anesthetic and antiarrhythmic. Clinically, it is mainly used for infiltration anesthesia, epidural anesthesia, surface anesthesia (including mucosal anesthesia in thoracoscopy or abdominal surgery) and nerve conduction block. Can also be used for ventricular premature beat and ventricular tachycardia after acute myocardial infarction, digitalis poisoning, cardiac surgery, and ventricular arrhythmia caused by cardiac catheter. Serocaine is an amide local anesthetic. After blood absorption or intravenous administration, the medicine has obvious excitation and inhibition dual-phase effect on the central nervous system, can not excite the central nervous system, can produce analgesia and sleepiness when the blood concentration is low, can improve the pain threshold, has anticonvulsant effect when the blood concentration of the sub-poisoning is increased along with the increase of dosage, and can produce convulsion when the blood concentration exceeds 5 mug.ml < -1 >. The corocaine can promote the outflow of K+ in myocardial cells at low dosage, reduce the automatic property of cardiac muscle, and has the effect of resisting ventricular arrhythmia, and has no obvious influence on the electrical activity of myocardial cells, atrioventricular conduction and myocardial contraction at therapeutic dosage, and the further increase of blood concentration can cause the reduction of heart conduction speed, atrioventricular conduction block, inhibit myocardial contractility and reduce heart blood volume. 1935 SwedishAnd Lundquist found that the synthetic isomer of phytoalkali gramine was narcotic, and through investigation of such various derivatives, lidocaine was successfully synthesized in 1943. Then toGoldberg, gordh a number of basic and clinical trials have been conducted by researchers, and the product was introduced by Astra corporation (AstraZeneca) in Sweden in 1948. In 7 months 2017, aspen japan (SAND PHARMA corporation) inherited the production and sales approval (trade name Xylocaine Viscous%) specification of 2% (100 ml:2 g), and was clearly a raw product in the japan IF file. The oral surface anesthetic is applied to surface anesthesia, and the application method is that the oral surface anesthetic is used for the anesthesia of other throat and esophagus parts in endoscopy, and the oral surface anesthetic is not required to be swallowed at one time, but is required to be swallowed slowly. In intraoral anesthesia, in order to avoid anesthesia of unnecessary parts, the patient is not allowed to swallow and is allowed to diffuse only into the oral cavity. When the stomach is anesthetized (damping syndrome, pylorospasm, etc.), it is allowed to swallow rapidly and washed out with half a cup of water. In CN111388416B, the content of a viscous agent sodium carboxymethylcellulose is reduced, gastrointestinal tract foam is remarkably eliminated, and a certain amount of chitosan is added at the same time, so that the problem that the local anesthesia time is too short and the longer operation time cannot be met due to the fact that the medicine release is too fast due to the fact that the medicine liquid viscosity is reduced is solved. However, the inventor experiment finds that the action time of the celecaine mucilage prepared by the method is still shorter, and the treatment requirement of the operation time in medical treatment is difficult to meet. Disclosure of Invention The application provides the celecoxib mucilage, which prolongs the action time, releases uniformly, has more stable drug effect, meets the treatment requirement of operation and has excellent stability. The application provides a salcaine mucilage which comprises 1-3% of salcaine, 0.3-0.6% of carboxymethylcellulose sodium, 0.1-0.3% of chitosan, 1-3% of glycerol, 0.03-0.08% of L-menthol, 0.1-0.6% of glacial acetic acid and purified water, wherein the salcaine comprises salcaine a, b and c, the particle sizes D90 of the salcaine a, b and c are respectively 200-400nm, 700-1100nm and 1500-2000nm, and the dosage ratio of the salcaine a, b and c is (1-1.5): 1 (0.5-1). Preferably, the particle sizes D90 of the celecoxib a, b, c are 300nm, 900nm, 1800nm respectively. Preferably, the particle sizes D90 of the celecoxib a, b, c are 300nm, 1000nm, 2000nm respectively. Preferably, the dosage ratio of the celecoxib a, b and c is 1.2:1:0.8 in terms of weight ratio. Preferably, the dosage ratio of the celecoxib a, b and c is 1:1:1 in terms of weight ratio. Preferably, the celecoxib mucilage comprises 2% of celecoxib, 0.4% of carboxymethylcellulose sodium, 0.2% of chitosan, 2% of glycerol, 0.05% of L-menthol, 0.4% of glacial acetic acid a