CN-122005554-A - Penehyclidine hydrochloride nasal preparation and application thereof in treating rhinitis

Abstract

The invention discloses a nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis. The upper respiratory tract is infected by bacteria and viruses or is stimulated by foreign matters (such as pollen, hair, dust, cold air, etc.) to cause clinical symptoms of sneeze, nasal obstruction, nasal discharge, etc. in nasal cavity, namely acute rhinitis or chronic rhinitis. The medicine for treating rhinitis is a pharmaceutical preparation such as nasal drops and spray prepared by taking the penehyclidine hydrochloride compound as a main component and adding pharmaceutically acceptable auxiliary components, wherein the administration route is nasal cavity local administration, and the weight-volume ratio of the penehyclidine hydrochloride to the auxiliary components is 1:250-1:10000. The invention widens the application field of the compound penehyclidine hydrochloride, provides a novel medicine for specific crowds with rhinitis symptoms, adopts local administration, and has the advantages of quick effect, high local bioavailability, long duration, smaller dosage and greatly reduced occurrence rate of adverse reaction, and the active ingredients directly reach focus positions.

Inventors

• ZHANG LING

Assignees

• 张玲

Dates

Publication Date

20260512

Application Date

20241111

Claims (11)

1. 1. A nasal preparation prepared from penehyclidine hydrochloride and its application in treating rhinitis are provided.
2. 2. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 1, wherein the medicament for treating nasal inflammation diseases is nasal drops and spray prepared from penehyclidine hydrochloride compound as a main component and pharmaceutically acceptable auxiliary components through a conventional preparation process.
3. 3. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 1 or 2, wherein the administration route of the medicament for treating nasal inflammation disease is nasal cavity local administration, and the administration mode is dripping type or spraying type.
4. 4. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 1 or 2, wherein the weight-to-volume ratio of penehyclidine hydrochloride compound to auxiliary components in the medicament for treating rhinitis is 1:250-1:5000.
5. 5. The nasal preparation prepared from penehyclidine hydrochloride and its use in treating rhinitis according to claim 2, wherein the packaging materials directly contacting the medicine are respectively a nasal drop pharmaceutical packaging kit and a spray pharmaceutical packaging kit.
6. 6. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 2, wherein the pharmaceutically acceptable auxiliary components comprise solvent, osmotic pressure regulator, pH regulator and preservative.
7. 7. The nasal preparation prepared from penehyclidine hydrochloride and its application in treating rhinitis according to claim 2, wherein the solvent is water, glycerol, polyethylene glycol.
8. 8. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 2, wherein the osmotic pressure regulator is sorbitol, propylene glycol or sodium chloride.
9. 9. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 2, wherein the pH regulator is hydrochloric acid, sodium hydroxide, sodium bicarbonate, phosphate, citric acid, boric acid, etc.
10. 10. The nasal preparation prepared from penehyclidine hydrochloride and application thereof in treating rhinitis according to claim 2, wherein the preservative is selected from the group consisting of niplatinum esters, benzoic acid and salts thereof, sorbic acid and salts thereof, benzalkonium bromide, and the like.
11. 11. The nasal preparation prepared from penehyclidine hydrochloride and its use in treating rhinitis according to claim 2, wherein the content of active ingredient in the pharmaceutical preparation is 0.2mg/ml or 0.5mg/ml or 1.0mg/ml or 2.0mg/ml or 4.0mg/ml, respectively, calculated as penehyclidine hydrochloride.

Description

Penehyclidine hydrochloride nasal preparation and application thereof in treating rhinitis Technical Field The invention belongs to the field of medicines, and particularly relates to a novel preparation of a compound penehyclidine hydrochloride and application thereof, in particular to application of penehyclidine hydrochloride in preparation of medicines for treating rhinitis. Background Nasal inflammation is a clinical symptom that the upper respiratory tract is infected by virus or is stimulated by foreign matters (such as pollen, hair, dust, cold air and the like) to cause sneeze, nasal obstruction, nasal discharge and the like in the nasal cavity, namely acute rhinitis or chronic rhinitis. There are a number of different kinds of drugs for treating rhinitis clinically, including antihistamines, glucocorticoids, decongestants, anticholinergic agents, antibiotics, chinese patent drugs, mucolytic and excretion promoters. The novel medicine is innovative in that the capillary vessel dilation of nasal mucosa can be obviously inhibited, so that nasal secretions are obviously reduced. Studies of the prior art (Hanxia. Drug selection for allergic rhinitis, open-roll benefit-doctor asking 2017 (04) show that ipratropium bromide aerosol in anticholinergic agents can significantly alleviate runny nose, sneeze symptoms. Studies of the prior art (Xiezhong. Influence of anticholinergic agent on Th1/Th2 and Treg cells of mice with variability rhinitis, the scientific research of ear-nose-throat department of three hospitals in Hunan eley) show that anticholinergic agent can effectively relieve runny nose of mice with variability rhinitis, and has a certain curative effect on sneeze, nasal itching and nasal obstruction. Anticholinergic agent can reverse the immune response advantage of Th2 cell factor relative to Th1 cell factor in nasal mucosa of variability rhinitis mouse, and make them to be normal. Anticholinergic agents enhance local Treg cell expression in nasal mucosa of variability rhinitis mice, possibly responsible for reversing the immune response dominance of Th2 cytokines over Th1 cytokines. From the specification of ipratropium bromide aerosol, common adverse reactions are dry mouth, tremors, excitement and palpitation, and some patients may suffer from headache, dry nasal mucosa or dry eyes, bronchospasm and the like. The penehyclidine hydrochloride is a selective anticholinergic agent, has the advantages of long drug effect maintenance time, no frequent administration, difficult occurrence of adverse reactions such as palpitation, excitation, tremor and the like. Penehyclidine hydrochloride, english name PENEHYCLIDINE HYDROCHLORIDE, chemical name 3- (2-cyclopentyl-2-hydroxy-2-phenylethoxy) quinine hydrochloride, molecular formula C 20H29NO2.hcl, molecular weight 351.92. Modern research results (Xie Jianping, mo Zhengji. Therapeutic effect of penehyclidine hydrochloride nasal drops on guinea pig rhinitis model, chinese journal of New medicine 2014 (04)) observe the influence of drugs on mucous membrane secretion, edema and capillary permeability by establishing a model of guinea pig nasal mucosa edema, runny nose and sneeze. As a result, nasal drops of penehyclidine hydrochloride of 1mg/mL can reduce the number of sneezes, 3 dosage groups of 1.0,0.5 and 0.25mg/mL can inhibit nasal mucosa secretion and reduce nasal discharge, and 1mg/mL can also obviously reduce capillary permeability of nasal mucosa. The conclusion is that the penehyclidine hydrochloride obviously relieves nasal obstruction, nasal mucosa edema and sneeze symptoms caused by histamine. The penehyclidine hydrochloride is a novel anticholinergic agent, has selective antagonism of M 1、M3 and N 1、N2 receptors, has strong anticholinergic action on the center and the periphery, has no obvious action on M 2 receptors, and is mainly concentrated in the fields of pre-anesthesia medication and organophosphorus pesticide poisoning rescuing medication in clinical application at present, and has not been applied to the field of preparing anti-rhinitis pharmaceutical preparations. Disclosure of Invention The invention aims at providing a new preparation of the compound penehyclidine hydrochloride and application thereof, and widening the application field of the compound penehyclidine hydrochloride. It is another object of the present invention to provide a new anticholinergic agent for relieving rhinitis symptoms, which is different from the existing anticholinergic agent, and provides a new alternative agent for specific people with rhinitis symptoms. The pharmacodynamics test of the penehyclidine hydrochloride in the preparation of the medicament for treating rhinitis is verified by adopting a model test of rhinitis syndrome created by administration of histamine phosphate to guinea pigs. The implementation of the invention is tested by adopting a common pharmaceutical preparation method in pharmacy to prepare the penehyclidine hydrochloride compou