Etoricoxib in-situ gel and preparation method thereof

A technology of etoricoxib and in situ gel, which is applied in the field of medicine, can solve the problems of difficult drug administration, complicated process, and easy to cause adverse reactions, etc., and achieve the effect of good drug slow and controlled release performance, simple process, and accurate dosage

Pending Publication Date: 2021-06-01
深圳前海九华国际投资控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of this application is to provide an etoricoxib powder in situ gel and its preparation method, aiming to solve the problems of the existing etoricoxib preparations to a certain extent, which are complex in process, difficult in administration and prone to adverse reactions

Method used

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  • Etoricoxib in-situ gel and preparation method thereof
  • Etoricoxib in-situ gel and preparation method thereof
  • Etoricoxib in-situ gel and preparation method thereof

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preparation example Construction

[0035] The second aspect of the embodiment of the present application provides a preparation method of etoricoxisan in situ gel, comprising the following steps:

[0036] S10. Dissolving the polyethylene glycol block copolymer, poloxamer 188 and poloxamer 407 in the formula amount in a solvent, and swelling to obtain a clear and transparent blank in-situ gel;

[0037] S20. The etoricoxib in situ gel is obtained by mixing the prescribed amount of etoricoxib, the moisturizing agent and the blank in situ gel.

[0038] The preparation method of etoricoxisan in-situ gel provided by the second aspect of the present application comprises dissolving the polyethylene glycol block copolymer, poloxamer 188 and poloxamer 407 in a formula amount in a solvent such as water, and swelling A clear and transparent blank in situ gel was obtained, in which the temperature conditions were favorable for dissolving the polyethylene glycol block copolymer, poloxamer 188 and poloxamer 407 in water, and...

Embodiment 1

[0044] A kind of etoricoxi powder in situ gel, its preparation comprises steps:

[0045] 1. Take purified water, refrigerate overnight, measure purified water with 10% of the content of the gel matrix, put it in an ice-water bath, place it on a magnetic stirrer, and slowly add accurately weighed P407 while stirring (the content is shown in Table 1 shown), after uniform dispersion, store in the refrigerator at 4°C until fully swollen to obtain a clear and transparent blank in-situ gel.

[0046] 2. Take the prescribed amount of etoricoxib (14.1%), sieve it, and mix it with the blank plain gel to obtain the etoricoxib in situ gel.

[0047] The in situ gelation temperature of etoricoxib powder with different P407 content was measured, and the change of P407 content and the test results are shown in Table 1 below:

[0048] Table 1

[0049]

[0050] It can be seen from the test results in Table 1 that with the increase of the content of P407 in the prescription, the gelation te...

Embodiment 2

[0052] An etoricoxisan in situ gel, which differs from Example 1 in that 32% P407 and P188 in the following Table 2 are added in Step 1.

[0053] The in situ gelation temperature of etoricoxib powder with different P188 content was measured, and the change of P188 content and the test results are shown in Table 2 below:

[0054] Table 2

[0055]

[0056]

[0057] It can be seen from the test results in Table 2 that usually P407 is used in combination with P188 to overcome the shortcoming of too low gelling temperature. Fixed P407 prescription content, with the increase of P188 prescription content, the gelation temperature increases, and the gelation temperature can meet the requirements of the preparation, and the human body temperature can achieve phase transition. However, the mechanical strength of etoricoxib powder in situ gel is not obvious and needs to be improved, and the bioviscosity is too high.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to etoricoxib in-situ gel and a preparation method thereof. The etoricoxib in-situ gel is prepared from the following raw material components in parts by weight: 6 to 10 parts of etoricoxib, 20 to 30 parts of polyethylene glycol block copolymer, 1 to 2 parts of poloxamer 188, 15 to 20 parts of poloxamer 407 and 1 to 2 parts of humectant. The etoricoxib in-situ gel provided by the invention belongs to a temperature sensitive type, and can generate phase state reversible transformation between sol and gel when sensing temperature change. Therefore, the gel can exist in a solution form before administration, the administration is convenient, and the dosage is accurate; after administration, the gel can be converted into semi-solid gel along with the rise of temperature in vivo, is long in retention time at an administration part, has good drug sustained and controlled release performance, and is very suitable for being used as a local administration carrier. Meanwhile, the gel has the advantages of convenience in medicine storage, no toxicity, high biological tissue compatibility, good medicine stability and the like.

Description

technical field [0001] The application belongs to the technical field of medicine, and in particular relates to an etoricoxib powder in-situ gel and a preparation method thereof. Background technique [0002] Etoricoxib (etoricoxib), a selective cyclooxygenase-2 inhibitor, has anti-inflammatory, analgesic and antipyretic effects, used for the treatment of acute and chronic osteoarthritis, and can also be used for the treatment of acute gouty arthritis. Etoricoxib, as a COX-2 (cyclooxygenase-2) inhibitor, compared with traditional non-steroidal anti-inflammatory drugs (NSAIDS), the former can make the occurrence of gastrointestinal peptic ulcer, perforation, bleeding The risk is reduced, and there is no sulfonamide group, which has higher safety for patients with sulfa allergy. Etoricoxib significantly reduced common adverse reactions of non-steroidal anti-inflammatory drugs (NSAIDs), including gastrointestinal mucosal damage, liver and kidney toxicity, allergic reactions, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/10A61K31/444A61P29/00A61P19/02A61P19/06
CPCA61K9/06A61K9/0014A61K47/10A61K31/444A61P29/00A61P19/02A61P19/06
Inventor 管悦琴罗雪峰
Owner 深圳前海九华国际投资控股有限公司
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