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Oral matrix type cyclosporin A slow-release pellet preparation and preparation method thereof

A technology for slow-release pellets and cyclosporine, which is applied in the directions of cyclic peptide components, pharmaceutical formulations, and inactive medical preparations, etc. Good reproducibility and Cmax reduction effect

Active Publication Date: 2014-12-24
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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  • Oral matrix type cyclosporin A slow-release pellet preparation and preparation method thereof
  • Oral matrix type cyclosporin A slow-release pellet preparation and preparation method thereof
  • Oral matrix type cyclosporin A slow-release pellet preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1. Preparation of Oral Skeletal Cyclosporine A Sustained-release Pellets

[0032]1. Weigh 10g of cyclosporine A, 25g of povidone-K30, 10g of poloxamer 188, and 5g of soybean lecithin, dissolve in absolute ethanol, evaporate to nearly dryness at 60°C and 90rmp, and place in a vacuum oven at 60°C After removing the residual solvent, freeze in a -20°C refrigerator for 4 hours, place it again in a 60°C vacuum oven to dry for 12 hours, pulverize, pass through an 80-mesh sieve to obtain a solid dispersion, and set aside.

[0033] 2. Weigh 30g of the solid dispersion, mix it with 3g of hypromellose HPMC k4M, 27g of microcrystalline cellulose, 15g of lactose, and 2g of croscarmellose sodium, and then add double-distilled water to make a soft material. Put it into a Mini250 extrusion spheronization fluidized coating machine, extrude spheronization, and dry at 50° C. to obtain oral skeleton type cyclosporine A sustained-release pellet preparation.

Embodiment 2

[0034] Example 2. Preparation of Oral Skeletal Cyclosporine A Sustained-release Pellets

[0035] 1. Weigh 10g of cyclosporine A, 50g of povidone-K30, and 5g of soybean lecithin, dissolve in absolute ethanol, evaporate to near dryness at 60°C and 90rmp, place in a vacuum drying oven at 60°C to remove residual solvent, and place in Freeze in a refrigerator at -20°C for 4 hours, place again in a vacuum oven at 60°C for 12 hours, pulverize, pass through an 80-mesh sieve to obtain a solid dispersion, and set aside.

[0036] 2. Weigh 30g of the solid dispersion, mix it with 30g of hypromellose HPMC k100LV, 75g of microcrystalline cellulose, 9g of lactose, and 3g of croscarmellose sodium, and then add double-distilled water to make a soft material. Put it into a Mini250 extrusion spheronization fluidized coating machine, extrude spheronization, and dry at 50° C. to obtain oral skeleton type cyclosporine A sustained-release pellet preparation.

Embodiment 3

[0037] Example 3. Preparation of Oral Skeletal Cyclosporine A Sustained-release Pellets

[0038] 1. Weigh 10g of cyclosporin A, 35g of povidone-K30, 25g of poloxamer 188, and 6g of soybean lecithin, dissolve in acetone, evaporate to near dryness at 60°C and 90rmp, and place in a vacuum oven at 60°C to remove After residual solvent, freeze in -20°C refrigerator for 4h, place again in 60°C vacuum drying oven for 12h, pulverize, pass through 80-mesh sieve to obtain solid dispersion, and set aside.

[0039] 2. Weigh 30g of solid dispersion, mix with 3g of hypromellose HPMC k4M, 45g of microcrystalline cellulose, 45g of lactose, and 7g of croscarmellose sodium, and then add double-distilled water to make a soft material. Put it into a Mini250 extrusion spheronization fluidized coating machine, extrude spheronization, and dry at 50°C to obtain sustained-release pellets.

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Abstract

The invention discloses an oral matrix type cyclosporin A slow-release pellet preparation which is prepared by extrusion and spheronization of a cyclosporin A solid dispersoid and a hydrophilic matrix material, wherein the cyclosporin A solid dispersoid comprises cyclosporin A, povidone-K30, poloxamer 188 and soyabean lecithin. The slow-release pellet preparation comprises the solid dispersoid, microcrystalline cellulose, lactose, hydroxypropyl methylcellulose and croscarmellose sodium. The difficultly dissolved drug-cyclosporin A slow-release pellet preparation is prepared according to a 'double drug release' principle of quick release at first and then slow release by combining a solid dispersion technology with a hydrophilic matrix technology. A result shows that the solubility of cyclosporin A is remarkably improved by the solid dispersoid; the accumulated drug release rates of 2 hours, 6 hours, 12 hours and 24 hours for slow-release pellets in a dissolution medium are 27%, 51%, 76% and 94% respectively, and the slow-release pellets have remarkable slow-release characteristics; the pharmacokinetic result of a Beagle dog shows that compared with a control preparation, the cyclosporin A slow-release pellets have the characteristics that Cmax is remarkably reduced, Tmax, t1 / 2 and MRT (mean residence time) are remarkably prolonged, and the slow-release effect is remarkable.

Description

technical field [0001] The invention relates to an oral slow-release pellet preparation of an insoluble drug and a preparation method thereof, in particular to an oral skeleton type cyclosporine A sustained-release pellet preparation and a preparation method thereof. Background technique [0002] According to the statistics of relevant institutions, about 65 billion US dollars of drugs are wasted in patients' drug treatment due to poor bioavailability every year in the world. At present, about 40% of the active substances screened by high-throughput drugs are insoluble in water. Insoluble drugs are difficult to be absorbed by the body due to their low solubility in water, and the elimination speed in the body is fast, and the blood drug concentration is prone to peaks. Valley phenomenon, the bioavailability of oral preparations is low, and it is difficult to realize the diversification of dosage forms. [0003] There are many studies on solid dispersions, and the commonly u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/12A61K47/38A61P31/04
Inventor 徐希明姜冬梅余江南朱源王强
Owner JIANGSU UNIV
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