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Dexamethasone slow-release microsphere for injection in glass body

A technology of dexamethasone and sustained-release microspheres, which is applied in microcapsules, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Inappropriate path and other problems, achieve good stability and reconstitution ability, facilitate clinical application, and reduce the effect of drug burden

Inactive Publication Date: 2019-10-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there have been a large number of studies on dexamethasone microspheres, there are still many shortcomings in these research results, such as low drug loading rate, unsuitable particle size, and severe burst release, which cannot be avoided when applied to intravitreal drug delivery.
Professor J. Siepmanna's research group at the University of Lille (Gasmi H, Siepmann F, Hamoudi MC, et al. Towards a better understanding of the different release phases from PLGA microparticles: Dexamethasone-loaded systems[J]. Int J Pharm, 2016, 514 (1): 189-199.) Obtained a series of dexamethasone microspheres with different release curves in the 52-61 μm average particle diameter by adjusting the drug loading rate, but its 8% drug loading rate also Leads to an overall bulky formulation that is not conducive to intravitreal administration
Teng Yan from Zhejiang University (Teng Yan. Preparation of microspheres for intravitreal injection [D]. Zhejiang University, 2005.) tried to prepare dexamethasone microspheres for intravitreal injection, but the release of the drug on the first day was as high as 40 %, the cumulative drug release rate has reached over 80% on the 4th day, which cannot meet the research requirements

Method used

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  • Dexamethasone slow-release microsphere for injection in glass body
  • Dexamethasone slow-release microsphere for injection in glass body
  • Dexamethasone slow-release microsphere for injection in glass body

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Dexamethasone 300mg

[0039] Ester-terminated glycolide-lactide copolymer ( RG 502) 400mg

[0040] Carboxyl-terminated glycolide-lactide copolymer ( RG 502 H) 0mg

[0041] (1) take by weighing the dexamethasone of formula quantity, ester group terminal glycolide lactide copolymer and carboxyl terminal glycolide lactide copolymer, be dissolved in 1.75ml dichloromethane and dimethyl sulfoxide volume ratio is In the mixed solvent of 5:2, make the inner oil phase for standby;

[0042] Weigh polyvinyl alcohol and add water, and prepare an aqueous solution with a mass concentration of 1% at 60-80° C., which is used as the external aqueous phase I for subsequent use;

[0043] Weigh polyvinyl alcohol and add water to prepare an aqueous solution with a mass concentration of 0.2% at 60-80°C, which will be used as the external aqueous phase II for later use;

[0044] (2) Add the above-mentioned inner oil phase into 300ml of outer water phase I, and emulsify at 1700rpm for...

Embodiment 2

[0049] Dexamethasone 300mg

[0050] Ester-terminated glycolide-lactide copolymer ( RG 502) 0mg

[0051] Carboxyl-terminated glycolide-lactide copolymer ( RG 502 H) 400mg

[0052] (1) take by weighing the dexamethasone of formula quantity, ester group terminal glycolide lactide copolymer and carboxyl terminal glycolide lactide copolymer, be dissolved in 1.75ml dichloromethane and dimethyl sulfoxide volume ratio is In the mixed solvent of 5:2, make the inner oil phase for standby;

[0053] Weigh polyvinyl alcohol and add water, and prepare an aqueous solution with a mass concentration of 1% at 60-80° C., which is used as the external aqueous phase I for subsequent use;

[0054] Weigh polyvinyl alcohol and add water to prepare an aqueous solution with a mass concentration of 0.2% at 60-80°C, which will be used as the external aqueous phase II for later use;

[0055] (2) Add the above-mentioned inner oil phase into 300ml of outer water phase I, and emulsify at 1700rpm for...

Embodiment 3

[0060] Dexamethasone 150mg

[0061] Ester-terminated glycolide-lactide copolymer ( RG 502) 250mg

[0062] Carboxyl-terminated glycolide-lactide copolymer ( RG 502 H) 250mg

[0063] (1) take by weighing the dexamethasone of formula quantity, ester group terminal glycolide lactide copolymer and carboxyl terminal glycolide lactide copolymer, be dissolved in 1.75ml dichloromethane and dimethyl sulfoxide volume ratio is In the mixed solvent of 5:2, make the inner oil phase for standby;

[0064] Weigh polyvinyl alcohol and add water, and prepare an aqueous solution with a mass concentration of 1% at 60-80° C., which is used as the external aqueous phase I for subsequent use;

[0065] Weigh polyvinyl alcohol and add water to prepare an aqueous solution with a mass concentration of 0.2% at 60-80°C, which will be used as the external aqueous phase II for later use;

[0066] (2) Add the above-mentioned inner oil phase into 300ml of outer water phase I, and emulsify at 2500rpm f...

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Abstract

The invention relates to a dexamethasone slow-release microsphere for injection in a glass body. The microsphere contains dexamethasone and poly(lactide-co-glycolide). A solvent volatilizing method isadopted to prepare the microsphere, the preparation conditions are mild, the requirements for equipment are low, industrial production is easy, and a conventional injection needle can be used for completing administration in the glass body. The drug loading ratio of the prepared dexamethasone slow-release microsphere reaches 10-20%, the release behavior of the first-day release rate being less than or equal to 10%, the 7th day cumulative release rate being less than or equal to 30%, the 14th day cumulative release rate being 30% to 80% and the 21st day cumulative release rate being greater than or equal to 55% can be achieved, the effective treatment concentration is maintained for six months, through a stability test, it is shown that the quality characteristic is not changed significantly, the redissolving effect is good, and the microsphere is convenient for clinical application.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dexamethasone slow-release microsphere, which can be used for intravitreal injection. [0002] technical background [0003] Dexamethasone is a glucocorticoid drug with various pharmacological effects such as anti-inflammatory, anti-allergic and immune suppression. It is widely used in various diseases, such as autoimmune diseases, asthma, allergies, inflammation, and dermatology and ophthalmology diseases. At present, ophthalmic drugs are mainly used in the treatment of iridocyclitis, iritis, keratitis, allergic conjunctivitis, blepharitis, dacryocystitis and other anterior segment diseases in clinical practice. Its commercially available dosage forms are mainly eye drops, eye ointments, and suspensions. These traditional dosage forms are restricted by factors such as corneal barrier, tear dilution, and nasolacrimal duct elimination. They have weak retention capacity,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/34A61K31/573A61P27/02
CPCA61K9/0048A61K9/5031A61K31/573A61P27/02
Inventor 操锋朱宣羽李佳俐
Owner CHINA PHARM UNIV
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