Instant gelling agent for treating allergic rhinitis

An anti-allergic, gel technology, applied in allergic diseases, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of high viscosity, affecting the accuracy of dosage, and clinical efficacy question

Inactive Publication Date: 2007-08-15
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently commercially available mometasone furoate and budesonide are both suspension nasal sprays. Since the surface of the human nasal mucosa contains a large number of nasal cilia and nasal mucus, their movement results in a very short retention time of the drug in the nasal mucosa. Only 15-30 minutes (Adv.Drug.Del.Rev.1993.11:329-347), therefore, the drug is often cleared before fully exerting its therapeutic effect, resulting in a certain impact on the clinical efficacy
Although some bioadhesive preparations such as nasal gels can prolong the residence time of drugs in the nasal mucosa, their viscosity is high, difficult to prepare, and greatly affects the accuracy of dosage

Method used

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  • Instant gelling agent for treating allergic rhinitis
  • Instant gelling agent for treating allergic rhinitis
  • Instant gelling agent for treating allergic rhinitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1. Prescription screening of ion-sensitive instant gel for nasal use

[0032] Taking the viscosity and suspension-sedimentation ratio of the formulation as indicators, and using the method of single-factor investigation, the formulations of ion-sensitive instant gel for nasal use were screened and determined, as shown in Table 1.

[0033] Table 1 The prescription (w / w%) of ion-sensitive nasal instant gel

[0034] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

Prescription 6

mometasone furoate

Monohydrate

0.5％

0.05％

1.0％

0.01％

0.2％

0.5％

deacetylated gellan gum

0.5％

0.4％

1％

0.2％

sodium alginate

1％

6％

suspending agent

xanthan gum

0.15%

Methylcellulose

3%

gum arabic

5%

HPMC

0.1%

HPMC

0.45%

Methylcellulose

2.5%

...

Embodiment 2

[0054] 1. Prescription screening of temperature-sensitive nasal ready-to-use gel

[0055] Taking the viscosity of the preparation and the suspension-sedimentation ratio as indicators, the single-factor investigation method was used to screen and determine the prescription of the temperature-sensitive nasal instant gel as shown in Table 2.

[0056] Table 2 Prescription (w / w%) of temperature-sensitive nasal instant gel

[0057] Prescription 14

Prescription 15

Prescription 16

Prescription 17

mometasone furoate

Monohydrate

0.1％

1.0％

0.15％

0.5％

Pluronic F127

20％

20％

10％

Pluronic F68

10％

15％

30％

suspending agent

HPMC0.5%

Methylcellulose 3%

Xanthan Gum 0.5%

Western tragacanth 2%

lubricant

Glycerin 15%

Propylene Glycol 10%

Tween-65 0.2%

Tween-85 0.4%

preservatives

Chlorhexidine acetate 0.0...

Embodiment 3

[0074] 1. Prescription screening of pH-sensitive instant gel for nasal use

[0075] Taking the viscosity of the preparation and the suspension-sedimentation ratio as indicators, the single-factor investigation method was used to screen and determine the prescription of the pH-sensitive instant gel for nasal use as shown in Table 4.

[0076] Table 4 pH-sensitive nasal instant gel preparation prescription (w / w%)

[0077] Prescription 24

Prescription 25

Prescription 26

Prescription 27

Prescription 28

Prescription 29

mometasone furoate

Monohydrate

0.02％

0.55％

1.0％

0.5％

0.1％

Budesonide

0.1％

CAP

40％

10％

AEA

9％

1％

Carbopol 940P

0.65％

0.59％

suspending agent

HPMC

HPMC

CMC-Na

CMC-Na

HPMC

HPMC

[0078] 0.5％

...

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Abstract

The invention belongs to the field of western medicinal preparation, and relates to a preparation with suitable phase variation, detention time prolonging effects and topically administered in nasal cavity, and its preparation method. The method comprises dispersing momestasone furoate or budesonide in hydrophilic gel substrate prepared from acetyl-removed gellan gum and sodium alginate in micro powder form. the gel preparation is prepared and stored in solution from, and administered in solution spraying form; generates phase variation due to the change of environmental ionic strength, pH, or temperature after contacting with tunica mucosa of nasal cavity, and forms gel. The invention has the advantages of simple preparation and accurate administered dose; can prolong the contact time of medicine and schneiderian membrane; and improves therapeutic effect of the medicine to anaphylactic rhinitis.

Description

technical field [0001] The invention belongs to the field of western medicine preparations, and relates to a novel nasal instant gel preparation containing glucocorticoids and a preparation method thereof. Background technique [0002] Allergic rhinitis is an allergic inflammatory disease caused by a variety of allergens. It is prone to attack in spring and autumn and in cold climates. It is an allergic reaction that often occurs in the nasal mucosa. The incidence has increased in recent years. This disease can occur in men and women of any age, more common with 15-40 years old. Typical symptoms are nasal itching, nasal congestion, sneezing, a large amount of watery nasal discharge, and decreased sense of smell. When allergic rhinitis attacks, the patient is very painful and needs active treatment to relieve symptoms. For allergic rhinitis, we must first pay attention to remove the cause and incentives, such as keeping warm and cold, avoiding contact with pollen, preventin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K9/00A61K47/36A61K47/38A61P11/02A61P37/08
Inventor 蒋新国曹师磊任晓维陈念祖陈恩徐丰
Owner FUDAN UNIV
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