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CN-122005446-A - Preparation method and application of new penehyclidine hydrochloride dosage form

CN122005446ACN 122005446 ACN122005446 ACN 122005446ACN-122005446-A

Abstract

The invention discloses a preparation method and clinical application of a penehyclidine hydrochloride oral liquid preparation. The weight-volume ratio of the penehyclidine hydrochloride to the auxiliary components is 1:5000-1:100000. The invention develops a novel pharmaceutical formulation of the compound penehyclidine hydrochloride and expands the administration route and clinical application according to the developed novel formulation. The penehyclidine hydrochloride has been successfully developed into a pharmaceutical dosage form on the market as an injection, is used for inhibiting gland secretion and treating organophosphorus poisoning by pre-anesthesia administration, and has limited clinical application indications. The novel medicine adopts oral systemic administration, is convenient to use, can greatly widen the clinical application, and furthest develops new clinical indications of penehyclidine hydrochloride to realize the medical value.

Inventors

  • ZHANG LING

Assignees

  • 张玲

Dates

Publication Date
20260512
Application Date
20241111

Claims (14)

  1. 1. A preparation method and application of a new preparation of penehyclidine hydrochloride.
  2. 2. The new penehyclidine hydrochloride dosage form of claim 1 is an oral liquid preparation, which is characterized in that the oral liquid preparation is an oral solution prepared by taking a penehyclidine hydrochloride compound as a main component and adding pharmaceutically acceptable auxiliary components through a preparation process.
  3. 3. The preparation method and the application of the new penehyclidine hydrochloride dosage form of claim 1, wherein the oral liquid preparation prepared by taking penehyclidine hydrochloride as a main component is orally taken.
  4. 4. The preparation method and the application of the new penehyclidine hydrochloride dosage form according to claim 1, wherein the weight-volume ratio of penehyclidine hydrochloride compound to auxiliary components in the medicine is 1:5000-1:100000.
  5. 5. The preparation method and the application of the new penehyclidine hydrochloride dosage form according to claim 1 or 2, wherein the packaging material directly contacting with the medicine can be a common packaging material of oral liquid preparations such as glass bottles and kits thereof, plastic bottles, composite aluminum foil bags and the like.
  6. 6. The preparation method and application of the new preparation form of penehyclidine hydrochloride according to claim 1 or 2, wherein the new clinical application of the new preparation form prepared by using penehyclidine hydrochloride as a main component is that biliary colic, gastric colic, renal colic, intestinal colic and dysmenorrhea caused by smooth muscle spasm are caused by various reasons.
  7. 7. The preparation method and the application of the new preparation form of penehyclidine hydrochloride according to claim 1 or 2, characterized in that the new preparation form prepared by using penehyclidine hydrochloride as a main component is applicable to clinical new applications, such as gastroscopy, enteroscopy, laparoscopy and operations thereof, cholecystectomy, hysteromyectomy, uterine curettage, etc.
  8. 8. The preparation method and the application of the new penehyclidine hydrochloride dosage form of claim 2 or 4, wherein the pharmaceutically acceptable auxiliary components comprise a solvent, a pH regulator, a flavoring agent and a preservative.
  9. 9. The preparation method and the application of the new penehyclidine hydrochloride dosage form according to claim 2 or 4, wherein the solvent is water.
  10. 10. The preparation method and the application of the new penehyclidine hydrochloride dosage form of claim 2 or 4, wherein the pH regulator is hydrochloric acid, sodium hydroxide, sodium bicarbonate, phosphate, citric acid, boric acid, etc.
  11. 11. The preparation method and the application of the new penehyclidine hydrochloride dosage form according to claim 2 or 4, wherein the flavoring agent is white granulated sugar, stevioside, sucralose, aspartame and other sweeteners.
  12. 12. The preparation method and application of the new penehyclidine hydrochloride dosage form according to claim 2 or 4, wherein the preservative is sodium benzoate, parabens, potassium sorbate and the like.
  13. 13. The method for preparing a new dosage form of penehyclidine hydrochloride according to claim 2 or 4, wherein the content of active ingredient in the pharmaceutical preparation is 0.01mg/ml or 0.02mg/ml or 0.05mg/ml or 0.1mg/ml or 0.2mg/ml, respectively, calculated as penehyclidine hydrochloride.
  14. 14. The preparation method and the application of the new penehyclidine hydrochloride dosage form according to claim 2 or 4, wherein the content of the active ingredient in the pharmaceutical preparation is 0.1 mg/branch or 0.2 mg/branch or 0.5 mg/branch or 1.0 mg/branch or 2.0 mg/branch respectively calculated by penehyclidine hydrochloride.

Description

Preparation method and application of new penehyclidine hydrochloride dosage form Technical Field The invention belongs to the field of medicines, and particularly relates to a preparation method and application of a new preparation of penehyclidine hydrochloride, the preparation method of the new preparation is particularly a formula and a preparation process of an oral solution preparation, and the new application relates to biliary colic, gastric colic, renal colic, intestinal colic and dysmenorrheal caused by smooth muscle spasm due to various reasons, and can also be used for gastroscopy, enteroscopy, laparoscopy and operations thereof, cholecystectomy, hysteromyectomy, uterine curettage and the like. Background The penehyclidine hydrochloride is a novel selective anticholinergic agent which is independently developed in China, has selective antagonism of M 1、M3 and N 1、N2 receptors, has strong anticholinergic effect on the central and peripheral, has no obvious effect on M 2 receptors, is an injection which is clinically approved at present, and has approved application in inhibiting gland secretion by pre-anesthesia medication and rescuing organophosphorus pesticide poisoning. The penehyclidine hydrochloride has wide pharmacological actions as anticholinergic agent, so that new application of penehyclidine hydrochloride needs to be developed as much as possible to exert clinical value of penehyclidine hydrochloride to the greatest extent. The penehyclidine hydrochloride is rapidly absorbed and widely distributed in blood, smooth muscle, gland, bronchus and other parts after injection or oral administration, and provides a development foundation for developing new dosage forms and indications. The clinical discussion of gastrointestinal spasmolysis medicine (Lin Xuan Liang Ying. The university of the medical institute of Guangdong in 2016) shows that the purpose of the study on the anticholinergic agent for relieving gastrointestinal smooth muscle spasm, namely the effect of the gastrointestinal spasmolysis medicine, is discussed. The method analyzes the relevant information of the gastrointestinal spasmolytic medicines by the clinical medicines of 100 hospitalized gastrointestinal disease patients. As a result, the gastrointestinal antispasmodics are suitable for treating gastric hyperacidity, gastralgia, gastric and duodenal ulcer, renal colic, bladder irritation, gastritis, etc. The atropine sulfate has the best effect on the gastrointestinal smooth muscle spasm, but has larger side effect and less dosage, the belladonna fluid extract (compound belladonna) mainly aims at gastric and duodenal ulcers and mild gastrointestinal spasm, plays roles in relieving pain and inhibiting secretion, and the bromopropion has lasting and stronger inhibition effect on the gastrointestinal smooth muscle because of having selectivity on the gastrointestinal smooth muscle. In addition, scopolamine butylbromide (spasmolytic), isocorydine hydrochloride, pinaverium bromide (Desulte), belladonna tincture and other medicines are also used. In the prior art (the stomach diseases should be selected by the health 2012 (01) of the human body), the commonly used spasmolytic and analgesic drugs are atropine sulfate, belladonna, anisodamine hydrobromide (654-2), procaine, and gastric ulcer and the like in clinic, and are clinically used for treating a plurality of acute diseases of the digestive tract due to the effects of inhibiting gastric acid secretion, relaxing smooth muscle of the gastrointestinal tract, but the old people need to pay caution when taking the drugs, because the drugs have the effects of relieving spasm and pain, but also have the effects of relaxing pupils and raising intraocular pressure, and the symptoms of glaucoma are extremely likely to be induced or aggravated after taking the drugs, and in addition, the symptoms of palpitation, shortness of breath, chest distress and the like can also occur when taking the drugs, and cardiovascular patients should also pay caution when taking the drugs. The clinical observation of 96 cases of acute biliary colic treatment by using penehyclidine hydrochloride in the prior art (Yang Wenjun, dansheng, ministry of national emergency medical science and Association of Chinese medical science for twenty years celebration paper assembly treatise) shows that the curative effect of penehyclidine hydrochloride on biliary colic is observed. The method comprises randomly dividing patients with biliary colic into treatment group (penehyclidine hydrochloride group), control group (atropine sulfate group), and observing and comparing spasmolytic and analgesic effects between the two groups, and heart rate and blood pressure changes. As a result, the total effective rate (99%) in the treatment group was significantly different from that in the control group (63%) in 2 hours (P0.01). Conclusion that penehyclidine hydrochloride has strong spasmolytic and analgesic effects and long acti