Fluticasone propionate foaming agent composition

Abstract

The invention discloses a fluticasone propionate foaming agent composition, which contains fluticasone propionate serving as an active ingredient and one or more pharmaceutically acceptable auxiliary materials for a foaming agent, wherein the content of the fluticasone propionate serving as the active ingredient is 0.05 to 0.2 percent (weight / weight), and the volume expansion ratio of the foaming agent composition is 25 to 50.

Description

field of invention [0001] The invention relates to a foam composition, in particular to a foam composition containing mometasone furoate. Background technique [0002] Chronic nonspecific ulcerative colitis (ulcerative colitis, UC, referred to as ulcerative colitis) is a chronic disease whose etiology is not very clear. , can gradually progress to the proximal colon and even the entire colon in a continuous manner. The clinical symptoms vary in severity, and there may be remissions and attacks alternately. Patients may only have colonic symptoms or may be accompanied by systemic symptoms. Drugs for the treatment of UC mainly include aminosalicylic acids such as mesalamine, antibiotics, glucocorticoids and corticotropins, and immunomodulatory drugs. Among them, the short-term curative effect of glucocorticoids is better, and the effective rate can reach 90%, which can inhibit inflammation and immune response and relieve poisoning symptoms. It is generally applicable to cas...

AI Technical Summary

Problems solved by technology

However, this preparation can only reach the proximal sigmoid colon due to its low expansion

Poor expansion of the distal colon

And in this foam agent, budesonide as active ingredient is soluble in propylene glycol, although the U.S. Food and Drug Administration (FDA) and the U.S. Cosmetic Ingredient Review Committee generally believe that propylene glycol is safer, and the 2005 edition of the Chinese Pharmacopoeia No. 896 The page contains propylene glycol, but in the material safety data sheet (Material Safety Date Sheets) of propylene glycol, it is mentioned that propylene glycol has a primary stimulating effect on the skin, which may cause subjective burning sensation, tingling and itching In addition, because propylene glycol has the characteristics of a fat-soluble solvent, long-term use of high-concentration propylene glycol will have an impact on the epidermal sebum structure; in addition, due to the irritation of propylene glycol to the skin and mucous membranes, it may cause irritant dermatitis, especially at high concentrations Higher, in the case of sealed use, it is more likely to cause skin redness, rash, peeling itching and roughness; about 1 to 5% of people will have local skin allergic eczema reactions when exposed to propylene glycol, that is, allergies Dermatitis, and for people with allergic systems, taking or using foods or medicines containing propylene glycol can cause systemic skin allergic reactions

Thus, propylene glycol is potentially irritating to the colonic mucosa and may aggravate ulcers

In addition, in the stability test, we found that although the active ingredient of the foam can meet the requirements within the validity period, the decomposition of the active ingredient is still relatively serious, which has a negative impact on the production of the drug preparation and storage and sales

[0004] Chinese patent application CN200780002784.x discloses a high expansion ratio glucocorticoid foam without emulsifying wax and / or mineral oil, although it is also disclosed in the application description that its active ingredients can be budesonide, trimethyl Tecortisone acetate, mesalazine and their pharmaceutically acceptable salts, but the instructions only disclose a water-soluble sodium salt of prednisolone-prednisolone sodium sulfobenzoate as the active The technical scheme of preparing the foam agent from the ingredients does not disclose any method of preparing the foam agent with the above-mentioned non-water-soluble active ingredients.

[0008] However, there is no report in the prior art for the use of mometasone furoate to treat ulcerative colon

We take 0.25mg each time, once a day for 7 days in a clinical trial of oral administration of mometasone furoate to rats with ulcerative colitis model, however, this experiment shows that mometasone furoate can No significant benefit compared to placebo

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