Nasal pharmaceutical composition of cyclodextrin inclusion cortin and H1 receptor antagonist

A technology of receptor antagonists and corticosteroids, applied in the direction of drug combinations, active ingredients of heterocyclic compounds, non-active ingredients of polymer compounds, etc., can solve the problem of unsatisfactory stability, poor stability of nasal sprays, reduced delivery, etc. problems, to achieve the effect of reducing the possibility of side effects, improving curative effect, and reducing dosage

Inactive Publication Date: 2010-06-30
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0016] 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 dose required for 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 Pharmacopoe

Method used

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  • Nasal pharmaceutical composition of cyclodextrin inclusion cortin and H1 receptor antagonist
  • Nasal pharmaceutical composition of cyclodextrin inclusion cortin and H1 receptor antagonist

Examples

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Embodiment 1

[0059] The preparation of embodiment 1 hydrocortisone cyclodextrin inclusion aqueous solution

[0060] Dissolve 2 g of 3-hydroxypropyl β-cyclodextrin in 15 ml of 95% ethanol at room temperature, add 0.2 g of hydrocortisone, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220 nm), add 8 ml of injection Water, stirred for 5 minutes, concentrated under reduced pressure, and evaporated to remove ethanol to obtain an aqueous solution of hydrocortisone / 3-hydroxypropyl β-cyclodextrin inclusion complex, which is set aside.

Embodiment 2

[0061] The preparation of embodiment 2 dexamethasone acetate cyclodextrin inclusion aqueous solution

[0062] Dissolve 2g of 2-hydroxypropyl-β-cyclodextrin in 20ml of acetone at 40±2°C, add 0.5g of dexamethasone acetate, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm), add 3mL of water for injection was stirred for 5 minutes, concentrated under reduced pressure, and 4ml of water for injection was added twice during the concentration process to remove the acetone to obtain dexamethasone acetate / 2-hydroxypropyl-β-cyclodextrin inclusion complex aqueous solution ,spare.

Embodiment 3

[0063] The preparation of embodiment 3 mometasone furoate cyclodextrin inclusion aqueous solution

[0064] Dissolve 7g of 2-hydroxyethyl-β-cyclodextrin in 20ml of absolute ethanol at room temperature, add 0.5g of mometasone furoate, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm), stir for 5 minutes, concentrate under reduced pressure, add 3.5ml water for injection three times during the concentration process, and evaporate ethanol to obtain mometasone furoate / -hydroxyethyl-β-cyclodextrin inclusion aqueous solution, which is set aside.

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Abstract

The invention relates to a nasal pharmaceutical composition of cyclodextrin inclusion cortin and an H1 receptor antagonist, comprising the cortin and the H1 receptor antagonist which are used as active components. The invention is characterized in that the cortin and/or the H1 receptor antagonist which are used as the active components in the pharmaceutical composition are treated by inclusion of cyclodextrin and/or derivatives thereof. The pharmaceutical composition is used for curing allergic rhinitis of people or mammals.

Description

Technical field: [0001] The invention relates to a cyclodextrin inclusion pharmaceutical composition 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 it is easy to see in young people. The main reasons are: [0003] (1) Inhalational allergens: such as indoor and outdoor dust, dust mites, fungi, animal fur, feathers, cotton wadding, etc., often cause perennial attacks; plant pollen causes mostly seasonal attacks. [0004] (2) Food allergens: such as fish and shrimp, eggs, milk, flour, peanuts, soybeans, etc. Especially certain drugs, such as sulfonamides, quinine, antibiotics, etc. can cause disease. [0005] (3) Contact objects such as cosmetics, gasoline, paint, alcohol, etc. [0006] Others may be certain bacteria and their toxins, physical ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K47/40A61P11/02A61P37/08A61K31/58A61K31/573A61K31/496A61K31/4545A61K31/445
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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