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A double-coated cyclosporin A sustained-release pellet preparation and preparation method thereof

A technology of sustained-release pellets and cyclosporine, which is applied in the direction of pill delivery, sugar-coated pills, and medical preparations of non-active ingredients. It can solve problems that are not suitable for industrial production and improve drug compliance and reproducibility. Good, easy to get the effect of excipients

Active Publication Date: 2016-12-14
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, almost none of them are suitable for industrial production

Method used

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  • A double-coated cyclosporin A sustained-release pellet preparation and preparation method thereof
  • A double-coated cyclosporin A sustained-release pellet preparation and preparation method thereof
  • A double-coated cyclosporin A sustained-release pellet preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 80 g of blank sugar pills, place them in a Mini250 extrusion spheroid fluidized coating machine, and preheat for 30 minutes.

[0034] Weigh 4g of cyclosporin A, 4g of polyvinylpyrrolidone k30, 0.8g of polyethylene glycol 400, 1880.8g of poloxamer, 1g of micropowder silica gel, and magnetically stir with 100ml of 40% (v / v, the same below) ethanol aqueous solution Dissolve, coat, take out after coating, and dry at 50°C for 2 hours to obtain cyclosporine A immediate-release pellets. The cyclosporine A quick-release pellets were carried out in vitro drug release test, the results are shown in figure 2 .

[0035] Weigh 3 g of ethyl cellulose, 0.6 g of diethyl phthalate, 0.9 g of polyethylene glycol 4000, and 3 g of micropowder silica gel, and dissolve them with 150 ml of 60% ethanol aqueous solution with magnetic stirring, and take the cyclosporin A prepared above. Release the pellets for coating, take them out after coating, and dry at 50°C for 2 hours to obtain cy...

Embodiment 2

[0037] Weigh 90 g of blank sugar pills, place them in a Mini250 extrusion spheronizing fluidized coating machine, and preheat for 30 minutes.

[0038] Weigh 6 g of cyclosporine A, 4 g of polyvinylpyrrolidone k30, 1.2 g of polyethylene glycol 400, 1880.9 g of poloxamer, and 1.5 g of micropowder silica gel, and dissolve them with 100 ml of 60% ethanol aqueous solution with magnetic stirring, and coat them. After the coating is completed, take it out and dry at 50°C for 2 hours to obtain cyclosporine A immediate-release pellets. The cyclosporine A quick-release pellets were carried out in vitro drug release test, the results are as follows: figure 2 .

[0039] Weigh 8 g of ethyl cellulose, 0.8 g of diethyl phthalate, 0.8 g of polyethylene glycol 4000, and 3 g of micropowder silica gel, and dissolve them with 200 ml of 40% ethanol aqueous solution with magnetic stirring, and take the cyclosporin A prepared above. Release the pellets for coating, take them out after coating, and...

Embodiment 3

[0041] Weigh 100 g of blank microcrystalline cellulose pellets, place them in a Mini250 extrusion spheronizing fluidized coating machine, and preheat for 30 minutes.

[0042] Weigh 10g of cyclosporine A, 10g of polyvinylpyrrolidone k30, 1g of polyethylene glycol 400, 1.8g of Tween 80, and 3g of talcum powder, and dissolve them with 200ml of 60% ethanol aqueous solution with magnetic stirring, and then coat them. Take it out and dry at 50°C for 2 hours to obtain cyclosporin A immediate-release pellets. The cyclosporine A quick-release pellets were carried out in vitro drug release test, the results are as follows: figure 2 .

[0043] Weigh 5 g of cellulose acetate, 1 g of polyethylene glycol 4000, and 2 g of micropowdered silica gel, and dissolve them with 250 ml of absolute ethanol magnetic stirring, take the cyclosporine A quick-release pellets prepared above for coating, and take out after coating is completed, Dry at 50°C for 2 hours to obtain cyclosporine A sustained-re...

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Abstract

A cyclosporine A sustained-release pellet preparation is obtained by bland pellets coated by two layers of coatings. A quick-release coating solution is obtained by dissolving 1 part of cyclosporine A, 0.67 to 3 parts of polyvinylpyrrolidone (PVP) K30, 0.067 to 1 part of poloxamer 188, 0.1 to 1 part of polyethylene glycol (PEG) 400 and 0.18 to 1 part of superfine silica powder in an ethanol solution; and a sustained-release coating solution is formed by dissolving 1 part of ethyecellulose, 0 to 0.2 part of phthalic acid diethyl ester, 0.1 to 0.3 part of polyethylene glycol 4000 and 0.12 to 1 part of superfine silica powder in ethanol. For the sustained-release pellet preparation, the blank pellet serves as a pellet core, quick-release coating and sustained-release coating technologies are combined, indissolvable drug cyclosporine A sustained-release pellets are prepared according to the double drug release principle of first quick release and then sustained release, and the purpose that a sustained-release preparation first rapidly effects and then steadily releases the drug when being taken orally is achieved. A preparation method for the sustained-release pellet preparation is also provided.

Description

technical field [0001] The invention relates to an oral sustained-release pellet preparation of an insoluble drug and a preparation method thereof, in particular to an oral cyclosporine A sustained-release pellet preparation and a preparation method thereof. Background technique [0002] The third generation highly effective immunosuppressant cyclosporine A (Cyclosporine A, CsA) is a cyclic peptide isolated from the culture fluid of filamentous fungi. It is a potent immunosuppressant that has been widely used in the transplantation of kidneys, liver, heart, lungs, pancreas and other organs as well as in the treatment of autoimmune diseases. [0003] At present, the main dosage forms of cyclosporine A on the market include injections, oral liquids and soft capsules. Due to the poor water solubility of the drug, a large amount of solubilizer, polyoxyethylene castor oil (Cremophor EL), is added to cyclosporine A injections currently used clinically. This excipient can easily c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K38/13A61K47/32A61K47/34A61K47/38A61K47/14A61K47/04A61P37/06
CPCA61K9/16A61K9/28
Inventor 徐希明姜冬梅余江南朱源
Owner JIANGSU UNIV
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