Budesonide flexible liposome temperature-sensitive gel and preparation method thereof

A temperature-sensitive gel and flexible lipid technology, applied in the field of medicine, can solve the problems of limited local absorption of drugs, difficult to achieve ideal curative effect, short intestinal retention time, etc., to improve adhesion and local concentration, and prolong local effect. time, the effect of reducing adverse reactions

Active Publication Date: 2021-11-30
THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Budesonide flexible liposome temperature-sensitive gel and preparation method thereof
  • Budesonide flexible liposome temperature-sensitive gel and preparation method thereof
  • Budesonide flexible liposome temperature-sensitive gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Prescription: Budesonide 50mg, soybean lecithin 195mg, cholesterol 30mg, sodium cholate 50mg, poloxamer 55g, carboxymethylcellulose sodium 5g, guar gum 240mg, polyacrylic acid 80mg.

[0028] Preparation Process:

[0029] (1) Preparation of flexible liposomes: Put an appropriate amount of budesonide, cholesterol and soybean phospholipids in a round-bottomed flask, add 450mL chloroform and ultrasonically dissolve them, then add sodium cholate aqueous solution, place in an ultrasonic cleaner and ultrasonically Form a stable W / O emulsion in 10 minutes; transfer to a rotary evaporator (120 rpm) in a vacuum constant temperature water bath at 40°C to remove the organic solvent; Ultrasound with the lower probe for 20s, that is (the concentration of the main drug is 0.25mg / ml).

[0030] (2) Preparation of flexible lipid body temperature-sensitive gel: Slowly add the prescribed amount of poloxamer, sodium carboxymethylcellulose, guar gum and polyacrylic acid into (1), and stir (...

Embodiment 2

[0032] Prescription: budesonide 50mg, soybean lecithin 180mg, cholesterol 40mg, sodium cholate 40g, poloxamer 48g, carboxymethylcellulose sodium 10g, guar gum 220mg, polyacrylic acid 100mg.

[0033] Preparation Process:

[0034] (1) Preparation of flexible liposomes: Put an appropriate amount of budesonide, cholesterol and soybean phospholipids in a round-bottomed flask, add 400mL chloroform and ultrasonically dissolve them, then add sodium cholate aqueous solution, place in an ultrasonic cleaner and ultrasonically Form a stable W / O emulsion in 10 minutes; move to a rotary evaporator (100 rpm) in a vacuum constant temperature water bath at 30°C to remove the organic solvent; then add an appropriate amount of water, continue hydration for 1.5 hours, and then place Ultrasound probe for 20s under conditions, that is (concentration of the main drug is 0.25mg / ml).

[0035] (2) Preparation of flexible lipid body temperature-sensitive gel: Slowly add the prescribed amount of poloxam...

Embodiment 3

[0037] Prescription: Budesonide 50mg, soybean lecithin 190mg, cholesterol 35mg, sodium cholate 40mg, poloxamer 50g, carboxymethylcellulose sodium 10g, guar gum 200mg, polyacrylic acid 80mg.

[0038] Preparation Process:

[0039] (1) Preparation of flexible liposomes: Put an appropriate amount of budesonide, cholesterol and soybean phospholipids in a round-bottomed flask, add 400mL chloroform and ultrasonically dissolve them, then add sodium cholate aqueous solution, place in an ultrasonic cleaner and ultrasonically Form a stable W / O emulsion in 10 minutes; transfer to a rotary evaporator (150 rpm) in a vacuum constant temperature water bath at 35°C to remove the organic solvent; Ultrasound with the lower probe for 20s, that is (the concentration of the main drug is 0.25mg / ml).

[0040] (2) Preparation of flexible lipid body temperature-sensitive gel: Slowly add the prescribed amount of poloxamer, sodium carboxymethylcellulose, guar gum and polyacrylic acid into (1), and stir ...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/58A61K47/26A61K47/32A61K47/36A61K47/38A61K9/127A61P1/00A61P1/04A61P29/00
CPCA61K31/58A61K9/06A61K9/127A61K47/26A61K47/38A61K47/32A61K47/36A61K9/0031A61P1/00A61P1/04A61P29/00Y02A50/30
Inventor 杨东亮马桂芝马瑞丽赵宇郁滕亮
Owner THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY
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