Ophthalmic preparation of sirolimus or derivative thereof

The technology of an ophthalmic preparation, sirolimus, is applied in the field of drug ophthalmic drug delivery preparations to achieve the effects of easy filling, simple preparation method and accurate dosage

Active Publication Date: 2017-11-10
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are few researches on everolimus dosage forms, sirolimus has been attracting attention. There are tablets, capsules and oral solutions on the market at home and abroad, but they are limited to oral preparations, and ophthalmic suspensions are in clinical practice. research stage

Method used

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  • Ophthalmic preparation of sirolimus or derivative thereof
  • Ophthalmic preparation of sirolimus or derivative thereof
  • Ophthalmic preparation of sirolimus or derivative thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Everolimus micelles

[0057] Composed of the following raw materials in weight percent:

[0058]

[0059] Preparation method: Prepared by an improved film hydration method, the specific method is as follows: First, dissolve everolimus and polyethylene glycol 40 stearate in ethanol according to the above ratio, and the polymer is in the flask after rotary evaporation to remove the solvent ethanol Form a thin film on the surface, add hydration medium containing osmotic pressure regulator mannitol, antibacterial agent benzalkonium chloride and polysorbate 80, oscillate ultrasonically, driven by hydration force, water molecules penetrate into the polymer through the gap film, forming micelles.

[0060] After testing, the pH value of the obtained everolimus micelles was 7.1; the osmotic pressure was 293 mOsmol / kg. The drug loading is 2%, and the encapsulation efficiency is 93.0%.

[0061] Get the obtained everolimus micelles, add deionized water to disperse, and measur...

Embodiment 2

[0065] everolimus suspension

[0066] Composed of the following raw materials in weight percent:

[0067]

[0068] Preparation method: first prepare a polyvinyl alcohol (PVA) solution, weigh 1.4g of low-viscosity PVA, add purified water to about 100mL, stir and dissolve in a water bath at 80-85°C, and let it sit for a certain period of time to swell to form a PVA solution. Then weigh 100 mg of everolimus, add 2 g of propylene glycol to dissolve everolimus. Add the above-mentioned everolimus solution into the PVA solution dropwise, and keep stirring. Add 0.02g of benzalkonium chloride, and finally quantify the suspension to 100mL, and sonicate for 10min.

[0069] After testing, the pH value of the obtained everolimus suspension was 5.7; the osmotic pressure was 286 mOsmol / kg.

[0070] Take an appropriate amount of the resulting everolimus suspension, add deionized water to disperse, and measure the particle size with a Malvern particle size potentiometer. The results are ...

Embodiment 3

[0086] Everolimus micellar in situ gel

[0087] Composed of the following raw materials in weight percent:

[0088]

[0089] Preparation method: preparation by improved film hydration method. The specific method is as follows: First, dissolve everolimus and polyethylene glycol 40 stearate in a certain amount of ethanol according to the above ratio, and the polymer forms a film on the inner surface of the flask after the solvent is removed by rotary evaporation. Separately take hypromellose and gellan gum, add water and stir to dissolve in a water bath at 80-85°C, add osmotic pressure regulator mannitol, bacteriostatic agent benzalkonium bromide and polysorbate 80 to 100mL to form a hydration medium . Add the hydration medium into the above flask and shake it. Driven by the hydration force, water molecules penetrate into the polymer film through the gap to form a micelle-in-situ gel composite carrier.

[0090] After testing, the pH value of the obtained everolimus micella...

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Abstract

The invention discloses an ophthalmic preparation of sirolimus or a derivative thereof, the ophthalmic preparation includes the following raw materials by weight: 0.02 to 0.2% of everolimus and the sirolimus; 0-3% of a solvent; 0-7% of an emulsifier and a surfactant; 0-8% of an osmotic pressure regulator; 0-0.5% of a pH regulator; 0-5% of an antibacterial agent; 0-2% of a thickening agent; and balance of purified water, wherein the solvent and the emulsifier and the surfactant are not simultaneously zero. The ophthalmic preparation of the sirolimus or the derivative thereof is simple in preparation, suitable for industrial production, convenient in application and good in application prospects.

Description

technical field [0001] The invention relates to the field of drug ophthalmic drug delivery preparations in pharmacy, in particular to an ophthalmic preparation of sirolimus or derivatives thereof. Background technique [0002] 90% of the marketed ophthalmic drugs are made into eye drops, but the drugs with strong fat solubility are not easy to dissolve in the water matrix. How to increase the solubility of drugs to overcome the physiological barrier of the eyeball and explore efficient drug delivery systems to improve the bioavailability of drugs is a hot and difficult point in the research of insoluble drugs. In recent years, with the rapid development of nanotechnology and polymer material science, eye drug delivery systems based on nanotechnology and bioadhesive materials have developed rapidly, such as liposomes, dendritic copolymers, chitosan nanoparticles, micelles, emulsions and Nanosuspension, etc. In these new ophthalmic drug delivery systems, micelles have the ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/06A61K9/10A61K47/14A61K47/26A61K31/436A61P27/02A61P37/06
CPCA61K9/06A61K9/10A61K9/1075A61K31/436A61K47/14A61K47/26
Inventor 申屠建中王俏汤湛
Owner ZHEJIANG UNIV
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