Budesonide flexible liposome temperature-sensitive gel and preparation method thereof

Abstract

The invention discloses budesonide flexible liposome temperature-sensitive gel and a preparation method thereof. The budesonide flexible liposome temperature-sensitive gel consists of the following components in percentages by weight: 0.01 to 0.5 percent of budesonide, 0.05 to 5 percent of a lipid material, 0.02 to 1.0 percent of a surfactant, 10 to 80 percent of a temperature-sensitive material and 0.1 to 5 percent of biological adhesive. The preparation is a rectal directional administration system which can be in a liquid state at normal temperature and quickly gelatinize at physiological temperature, and is a budesonide rectal directional administration preparation which is convenient to administrate and has high bioavailability, the release time of drugs in vivo can be prolonged, and adverse reactions are reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a budesonide flexible liposome body temperature-sensitive gel for rectal directional administration and a preparation method thereof. Background technique [0002] Ulcerative colitis (Ulcerative colitis, UC) is a chronic disease that is limited to the colon, relapses and remissions alternately, and is characterized by diffuse mucosal inflammation. UC is mostly related to rectal inflammation, and often extends from the rectum to other areas of the colon. The etiology is not yet clear, and there is no cure for it. [0003] The clinical symptoms of UC are persistent or recurrent bloody diarrhea, usually accompanied by prominent symptoms of tenesmus and rectal urgency. If the treatment is not timely and sufficient, the development of inflammation may lead to persistent intestinal injury, mucosal injury, and infection, hospitalization, Thromboembolism, even the need for colectomy or...

AI Technical Summary

Problems solved by technology

Mild and moderate UC with poor response to 5-aminosalicylic acid often requires systemic glucocorticoid therapy, but there are many adverse reactions to systemic medication, such as infection, Cushing's syndrome, osteoporosis, etc.

However, there is no corresponding preparation approved for marketing in China. Budesonide suspension for inhalation is often used as an enema for off-label medication in clinical practice, and it has almost no bioadhesion. Under the rectal peristalsis, it has a short retention time in the intestinal tract. , poor local absorption; on the other hand, budesonide is almost insoluble in water, which limits the local absorption of the drug and affects the efficacy of the drug

Although budesonide sustained-release tablets have entered the clinical trial stage, they are administered throughout the colon, and the drug concentration in the distal rectum, sigmoid colon and other lesions is low, and it is difficult to achieve the desired curative effect

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