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A kind of budesonide rectal thermosensitive gel and its preparation method and application

A temperature-sensitive gel, in-situ technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Contamination of clothing and other problems, to achieve the effect of improving the convenience of medication, reducing the difficulty of medication, and preventing medication leakage

Active Publication Date: 2021-04-23
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the commonly used dosage forms such as enemas and suppositories for the rectum are still not suitable for the actual needs of the treatment of ulcerative colitis.
A large number of clinical applications have found that enema drugs have a large diffusion area and good clinical efficacy, but there are still three common problems: first, the course of treatment for this type of disease is long, and it is extremely inconvenient for medical staff to use professional equipment for drug administration; First, it cannot stay in the intestine. In order to ensure the duration of drug action, patients are required to lie flat for a long time after administration, and the action time is still limited; third, it is easy to leak and pollute clothes, affecting normal work and life.

Method used

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  • A kind of budesonide rectal thermosensitive gel and its preparation method and application
  • A kind of budesonide rectal thermosensitive gel and its preparation method and application
  • A kind of budesonide rectal thermosensitive gel and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] prescription

[0030] Budesonide 0.002%

[0031] Hypromellose (bioadhesive) 1.002%

[0032] Poloxamer 407 (temperature-sensitive material) 18.19%

[0033] Poloxamer 188 (temperature regulator) 1.823%

[0034] Benzalkonium bromide (preservative) 0.02%

[0035] The rest is pH 4.5 aqueous solution (adjusted with 0.27% citric acid, 0.55% sodium citrate)

[0036] Preparation Process

[0037] a. Weigh the raw materials according to the prescription ratio;

[0038] b, boil pH 4.5 aqueous solution, cool;

[0039] c. Add benzalkonium bromide to the solution in step b, stir and dissolve completely, and then add hypromellose and poloxamer 188 in the same way;

[0040] d, adding budesonide to the solution in step c, stirring and mixing;

[0041] e. Add the poloxamer 407 temperature-sensitive material to the solution in step d, stir and wet it fully, add water to make up for the weight loss, and place it at 4°C until it swells completely.

Embodiment 2

[0043] prescription

[0044] Budesonide 0.002%

[0045] Hypromellose 0.923%

[0046] Poloxamer 407 18.308%

[0047] Poloxamer 188 2.001%

[0048] Benzalkonium Bromide 0.02%

[0049] The rest is pH 5.5 aqueous solution (adjusted with 0.029% citric acid, 0.20% sodium citrate)

[0050] Preparation Process:

[0051] a. Weigh the raw materials according to the prescription ratio;

[0052] b, boil pH 5.5 aqueous solution, cool;

[0053] c. Add benzalkonium bromide to the solution of step b, stir and dissolve completely, then add hypromellose and poloxamer 188 temperature regulator successively in the same way;

[0054] d, adding budesonide to the solution in step c, stirring and mixing;

[0055] e. Add the poloxamer 407 temperature-sensitive material to the solution in step d, stir and wet it fully, add water to make up for the weight loss, and place it at 4°C until it swells completely.

Embodiment 3

[0057] prescription

[0058] Budesonide 0.002%

[0059] Hypromellose 1.148%

[0060] Poloxamer 407 18.322%

[0061] Poloxamer 188 2.210%

[0062] Benzalkonium Bromide 0.02%

[0063] The rest is pH 6.8 aqueous solution (adjusted with 0.68% potassium dihydrogen phosphate concentration and 0.09% sodium hydroxide)

[0064] Preparation Process

[0065] a. Weigh the raw materials according to the prescription ratio;

[0066]b, boil pH 6.8 aqueous solution, cool;

[0067] c. Add benzalkonium bromide to the solution of step b, stir and dissolve completely, then add hypromellose and poloxamer 188 temperature regulator successively in the same way;

[0068] d, adding budesonide to the solution in step c, stirring and mixing;

[0069] e. Add the poloxamer 407 temperature-sensitive material to the solution in step d, stir and wet it fully, add water to make up for the weight loss, and place it at 4°C until it swells completely.

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Abstract

The invention discloses a budesonide rectal in-situ temperature-sensitive gel and a preparation method thereof. The preparation is composed of a main drug, a temperature-sensitive material, a temperature regulator, a bioadhesive agent, a stabilizer and acidified water. The budesonide rectal in situ thermosensitive gel provided by the present invention has solution-gel transition characteristics and bioadhesive properties, and compared with conventional budesonide enemas, the preparation can quickly gel at the administration site to achieve localized administration , and can be tightly adhered to the medication site, and has the advantages of acting on the lesion for a long time and effectively preventing drug leakage.

Description

technical field [0001] The invention relates to a budesonide rectal thermosensitive gel, which belongs to the field of pharmaceutical preparations. Background technique [0002] Ulcerative colitis / proctitis is a chronic non-specific intestinal inflammatory disease whose etiology is not yet clear, which is related to immune, environmental, genetic and infection factors, and immune abnormalities play a central role in the pathogenic mechanism. The lesions of ulcerative colitis / proctitis are mainly located in the mucosal layer of the colon / rectum, and can extend proximally, so as to spread throughout the entire colon / rectum. In recent years, with the improvement of living standards in our country, changes in people's diet structure and living habits, and the advancement of diagnostic techniques, the incidence rate has also shown an upward trend year by year. Because the etiology is not yet very clear, the severity of the disease varies, and it is mostly a chronic course of rec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/10A61K47/32A61K47/38A61K47/36A61K31/58A61P1/04A61P1/00
CPCA61K9/0031A61K9/06A61K31/58A61K47/10A61K47/32A61K47/36A61K47/38A61P1/00A61P1/04
Inventor 谢兴亮陈林殷雅卓盛艳梅许小红张全苏青
Owner CHENGDU MEDICAL COLLEGE