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Nasal in-situ gel containing mometasone furoate and H1 receptor antagonist

A receptor antagonist, mometasone furoate technology, applied in the field of in situ gel, can solve the problems of undisclosed, decreased drug bioavailability, poor stability of nasal spray, etc., achieve good therapeutic effect and achieve sustained and stable release , Improve the effect of bioavailability

Inactive Publication Date: 2011-06-01
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chinese patent application 97195225.6 discloses a nasal spray containing intranasal corticosteroids and antihistamines. In the application specification, it is believed that the combination of intranasal corticosteroids and antihistamines can take effect quickly and last, and reduce The dosage required by antihistamines, thereby reducing potential side effects such as drowsiness, however, the application does not disclose any specific pharmacological experimental data to prove the above effects, and we found that the nasal drug disclosed in the application The stability of the composition is poor and cannot meet the requirements for stability in the current Pharmacopoeia
[0008] Chinese patent application 03819170 discloses a compound preparation of azelastine hydrochloride and glucocorticoid, and discloses that the compound of azelastine hydrochloride and glucocorticoid is made into dosage forms such as nasal spray, aerosol, powder spray, etc. For among them, we found through experiments that the nasal spray disclosed in the application has poor stability and cannot meet the stability requirements in the current Pharmacopoeia
[0009] Common nasal medicines such as nasal drops and nasal sprays, because the nasal mucous membrane secretes mucus, the movement of nasal mucous membrane cilia can purify the foreign matter and dust on the nasal mucous layer. decreased bioavailability of the drug

Method used

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  • Nasal in-situ gel containing mometasone furoate and H1 receptor antagonist
  • Nasal in-situ gel containing mometasone furoate and H1 receptor antagonist
  • Nasal in-situ gel containing mometasone furoate and H1 receptor antagonist

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0041] 1. Preparation of Levocetirizine Hydrochloride Cyclodextrin Inclusion Compound

[0042] Add 2.5g of β-cyclodextrin, add appropriate amount of distilled water and stir at 60°C until it is completely dissolved, add 0.5g of levocetirizine hydrochloride, continue stirring for 30 minutes, then pour it into an evaporating dish, evaporate to dryness in a water bath at 90°C, and dry in a desiccator , Grind finely to obtain levocetirizine hydrochloride / β-cyclodextrin inclusion compound, set aside.

[0043] 2. Preparation of desloratadine cyclodextrin inclusion aqueous solution

[0044] Dissolve 4 g of 2-hydroxypropyl-β-cyclodextrin in 25 ml of 80% ethanol at room temperature, add 0.2 g of declotadine, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220 nm), add 10 mL of water for injection was stirred for 5 minutes, concentrated under reduced pressure, and the acetone was distilled off to obtain an aqueous solution of deslotetadine / 2-hydrox...

Embodiment 1

[0048] Embodiment 1 prepares ion-sensitive corticosteroid nasal in-situ gel, and the prescription is as follows (see Table 1):

[0049] Table 1 Prescription of ion-sensitive corticosteroid nasal in situ gel

[0050] content%

[0051] Preparation process: Place the above ion-sensitive polymer in an appropriate amount of deionized water, stir in a water bath at 80-100°C to disperse and dissolve, cool down to 4°C and place it in a refrigerator for 12 hours to obtain a clear solution (1). Example 1-1 to Example 1-4 Mix corticosteroid micropowder and H1 receptor antagonist or clathrate / clathate aqueous solution with other water-soluble excipients in water for injection to make suspension (2), Mix (1) and (2), adjust the pH to 6.2, and add water to the full amount. The rheological properties of the above five formulations were measured at room temperature (20° C.) using a Brookfield DV-m rotational viscometer. The viscosity of the above-mentioned prescriptions shows a do...

Embodiment 2

[0052] Embodiment 2 prepares temperature-sensitive corticosteroid nasal in-situ gel, and the prescription is as follows (see Table 2):

[0053] Table 1 Prescription of temperature-sensitive corticosteroid nasal in situ gel

[0054] content%

Example 2-1

Example 2-2

Example 2-3

Example 2-4

Active ingredient content%

mometasone furoate

Hydrate 0.05

mometasone furoate

0.05

mometasone furoate

0.1

mometasone furoate

Hydrate 0.1

H1 receptor antagonist content

%

Levocabaz Hydrochloride

Ting 0.05

Azelastine Hydrochloride

0.1

Levocetirizine Hydrochloride

0.1

Levocabaz Hydrochloride

Ting 0.05

Poloxamer 407

20

35

12

Poloxamer 188

5

28

15

PEG (6000-11000)

2

Polyethylene oxide (PEO)

2.5

Hypromellose

(HPMC)

2

1.5

s...

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PUM

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Abstract

The invention discloses nasal in-situ gel containing mometasone furoate and an H1 receptor antagonist. The nasal in-situ gel is prepared from mometasone furoate serving as an active ingredient and / or a hydrate of mometasone furoate, one or more H1 receptor antagonists, an environmentally-sensitive hydrophilic gel material, other pharmaceutically acceptable auxiliary materials and the balance of water.

Description

Technical field: [0001] The present invention relates to an in situ gel containing corticosteroid and H1 receptor antagonist. Background technique: [0002] Allergic rhinitis, also known as allergic rhinitis, is an allergic disease of the nasal mucosa and can cause various complications. Allergic rhinitis can occur at any age, both men and women, and is easy to see in young people. Allergic rhinitis and its impact on asthma (allergic rhinitis and its impact on asthma.ARIA) guidelines formulated by experts from all over the world in 2001, and became part of the initiative of the World Health Organization (WHO). In the ARIA guidelines, it was pointed out that corticosteroids It is the most effective drug for the treatment of allergic rhinitis and is suitable for the treatment of all degrees of allergic rhinitis from moderate to severe intermittent to moderate to severe persistent. Different from systemic corticosteroids, ideal nasal corticosteroids should have the following ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/00A61K47/34A61K47/38A61K47/36A61K47/40A61P11/02A61P37/08A61K31/58A61K47/10
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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