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Dexamethasone injecta coated with 2-hydroxypropyl-beta-cyclodextrin

A technology for dexamethasone and injection, which is applied in the field of cyclodextrin inclusion dexamethasone injection, can solve the problem that the degree of substitution affects the effect of inclusion injection, the undisclosed degree of substitution of hydroxypropyl-β-cyclodextrin, and the undisclosed Applicability and other issues, to achieve consistent physical and chemical properties, stable dissociation speed, and increased blood drug concentration

Inactive Publication Date: 2010-12-29
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application CN200410071922.8 discloses a hydroxypropyl-β-cyclodextrin inclusion compound of borneol and its preparation and preparation method. Methasone and other corticosteroids have very different physical, chemical properties, and chemical molecular structures. The process and formula used for inclusion of borneol are not suitable for dexamethasone and other corticosteroids.
[0006] Chinese patent application CN200610130124.7 discloses a corticosteroid inclusion aqueous solution and its application, and discloses a corticosteroid inclusion aqueous solution with dexamethasone and fluorometholone as active ingredients. Among the technical solutions of this application, 2- Hydroxypropyl-β-cyclodextrin is used as an auxiliary material for inclusion. However, according to the content disclosed in the European Pharmacopoeia, the substitution degree of hydroxypropyl-β-cyclodextrin is in the range of 2.8-10.5. However, the hydroxypropyl-β-cyclodextrin used is not disclosed in the above applications The degree of substitution of propyl-β-cyclodextrin, and the inclusion ability of hydroxypropyl-β-cyclodextrin are closely related to nephrotoxicity and hemolysis
If the substitution is too low or too high, it will affect the effect of inclusion injection. Therefore, a suitable substitution degree of hydroxypropyl-β-cyclodextrin is preferably used to prepare inclusion drug injections. Problems in the prior art

Method used

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  • Dexamethasone injecta coated with 2-hydroxypropyl-beta-cyclodextrin
  • Dexamethasone injecta coated with 2-hydroxypropyl-beta-cyclodextrin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dissolve 20g of 2-hydroxypropyl-β-cyclodextrin in 150ml of acetone (with a degree of substitution ranging from 4.1 to 5.9) at room temperature, add 5g of dexamethasone, stir to dissolve, stir for another 30 minutes, and filter through a microporous membrane ( 220 nm), add 200ml of water for injection, stir for 5 minutes, concentrate under reduced pressure, and evaporate the solvent to obtain an aqueous solution of dexamethasone / 2-hydroxypropyl β-cyclodextrin inclusion complex.

[0022]Add another 1g of EDTA-2Na to water for injection, adjust the pH of the phosphate buffer solution to 7.5, then adjust it to isotonicity with sodium chloride, filter it through a microporous membrane (220nm), and add it to the aforementioned dexamethasone / 3-hydroxypropyl β The cyclodextrin clathrate aqueous solution is added to 1000ml, filtered, sterilized and packaged, and the concentration of the obtained injection solution is 5mg / ml.

Embodiment 2

[0024] Dissolve 4g of 2-hydroxypropyl-β-cyclodextrin (the degree of substitution ranges from 4.1 to 5.9) in 80ml of acetone at 40±2°C, add 1g of dexamethasone, stir to dissolve, and then stir for 30 minutes to obtain a microporous membrane Filter (220nm), add 6mL of water for injection, stir for 5 minutes, concentrate under reduced pressure, add water for injection twice during the concentration process, each time 6ml, remove the solvent to obtain dexamethasone / 2-hydroxypropyl β-cyclodextrin Inclusion aqueous solution, spare.

[0025] Add another 1g of EDTA-2Na to water for injection, adjust the pH of the phosphate buffer solution to 6.5, then adjust to isotonicity with sodium chloride, filter through a microporous membrane (220nm), add to the aforementioned dexamethasone / 2-hydroxypropyl β The cyclodextrin clathrate aqueous solution is added to 1000ml, filtered, sterilized, packaged, and the preparation process is carried out under nitrogen protection, and the concentration of...

Embodiment 3

[0027] Dissolve 28g of hydroxypropyl-β-cyclodextrin (the degree of substitution ranges from 4.1 to 5.9) in 80ml of absolute ethanol at room temperature, add 2g of dexamethasone, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm ), stirred for 5 minutes, and concentrated under reduced pressure. During the concentration process, water for injection was added three times, each 15ml, and the ethanol was evaporated to obtain the dexamethasone / hydroxypropyl-β-cyclodextrin inclusion aqueous solution, which was set aside.

[0028] Add another 1g of EDTA-2Na to water for injection, adjust the pH of the phosphate buffer solution to 7, then adjust to isotonicity with sodium chloride, filter through a microporous membrane (220nm), add to the aforementioned dexamethasone / 3-hydroxypropyl β The cyclodextrin clathrate aqueous solution is added to 1000ml, filtered, sterilized, packaged, and the preparation process is carried out under the protection of ...

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Abstract

The invention relates to a dexamethasone injecta coated with 2-hydroxypropyl-beta-cyclodextrin. The molar ratio of a dexamethasone to the 2-hydroxypropyl-beta-cyclodextrin is 1:1-20, the substitution degree of the utilized 2-hydroxypropyl-beta-cyclodextrin is preferably 4-7, and the molar ratio of the dexamethasone to the 2-hydroxypropyl-beta-cyclodextrin is preferably 1:2-5.

Description

[0001] The invention relates to a corticosteroid injection, in particular to a cyclodextrin inclusion dexamethasone injection. Background technique [0002] Dexamethasone is a potent glucocorticoid with strong pharmacological effects such as anti-inflammatory, anti-endotoxin, immune suppression, anti-shock and enhancement of stress response. Dexamethasone and its different esters or salts are widely used in Various departments treat a variety of diseases, such as autoimmune diseases, allergies, inflammation, asthma, dermatology, and eye diseases. When dexamethasone is used for intravenous injection treatment, dexamethasone sodium phosphate is often used as the active ingredient injection Liquid dosage form. Due to the powerful anti-inflammatory and anti-shock effects of dexamethasone, dexamethasone sodium phosphate injection has become an essential first-aid drug for rescuing dying patients. Since dexamethasone sodium phosphate is a prodrug, after injection, it needs to be di...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/48A61K31/573A61P37/02A61P37/08A61P29/00A61P11/06A61P17/00A61P27/02A61K47/61
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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