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Oral ciclosporin A sustained-release agent and preparation method thereof

A technology for sustained-release preparations and cyclosporine, which is applied in the directions of cyclic peptide components, pharmaceutical formulations, medical preparations with inactive ingredients, etc. Slow drug release, high bioavailability and improved solubility

Active Publication Date: 2013-05-01
JIANGSU UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the disadvantage is that although the solubilizer polyoxyethylene castor oil contained in it is a good carrier for lipophilic drugs, it can produce a series of biological and physiological side effects, such as nephrotoxicity, allergic reactions, hyperlipidemia, and erythrocyte aggregation , peripheral neuritis, etc.
However, the preparation process of soft capsules is complicated, and liquid alcohol solvents are prone to volatilize through the capsule shell during storage, which accelerates the cross-linking and curing reaction of capsule shell gelatin and makes the disintegration time limit unqualified.
[0009] Chinese Patent No. 99102848 (disclosure date September 13, 2000) discloses "a pharmaceutical composition containing cyclosporine A" consisting of active ingredients, solvents or surfactant auxiliaries, solubilizers, and medium- and long-chain Saturated or unsaturated fatty acids, substituted carboxylic acids and other medicinal organic acids or a mixture of one or more acids or fish oil, although some improvements have been made in the process of this patented formula, but there are many defects in the formula components, which One defect will cause the complexity of the preparation process and the increase in the cost of the corresponding product
[0010] Relatively speaking, solid preparations are convenient to manufacture and store, but because the problem of too low solubility of cyclosporin A has not been solved, the most common solid dosage form in pharmaceuticals has not yet appeared on the market

Method used

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  • Oral ciclosporin A sustained-release agent and preparation method thereof
  • Oral ciclosporin A sustained-release agent and preparation method thereof
  • Oral ciclosporin A sustained-release agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Accurately weigh 1 g of cyclosporine A, 2.5 g of povidone-K30, 0.1 g of phospholipids, and 1.0 g of poloxamer 188, add 20 ml of absolute ethanol to dissolve, put in a water bath at 60 ° C, and 90 rpm rotary evaporation until nearly dry, The solvent was completely evaporated in a water bath at 70°C, placed in a -20°C refrigerator for 2 hours, then placed in a vacuum oven at 60°C for 12 hours, pulverized, and passed through an 80-mesh sieve to obtain a solid dispersion for future use.

[0039] 2. Weigh 2.6g of solid dispersion, mix with hypromellose 4000cPa.s2.41g, microcrystalline cellulose 1g, add 70% syrup to prepare soft material, pass through a 16-mesh sieve to obtain wet granules, and store at 60°C After baking in an oven for 30 minutes, take it out, pass through a 16-mesh sieve for granulation, and press into tablets with a pressure of 4 to 5 kg to obtain about 20 sustained-release tablets.

[0040] 3. The experimental results are as follows: Water, artifici...

Embodiment 2

[0043] 1. Accurately weigh 1g of cyclosporine A, 3.5g of povidone-K30, 0.35g of phospholipid, and 0.45g of poloxamer 188, add 20ml of absolute ethanol to dissolve, put in a 60°C water bath, 90rmp rotary evaporation to nearly dryness, The solvent was completely evaporated in a water bath at 70°C, placed in a -20°C refrigerator for 2 hours, then placed in a vacuum oven at 60°C for 12 hours, pulverized, and passed through an 80-mesh sieve to obtain a solid dispersion for future use.

[0044] 2. Weigh 2.65g of solid dispersion, mix with hypromellose 4000cPa.s1g, hypromellose 15000cPa.s1.285g, microcrystalline cellulose 1.97g and mix evenly, add 70% syrup to prepare soft material, pass Wet granules were obtained through a 16-mesh sieve, dried in an oven at 60°C for 30 minutes, taken out, passed through a 16-mesh sieve for sizing, and compressed into tablets with a pressure controlled at 4 to 5 kg to obtain about 19 sustained-release tablets. The obtained sustained-release table...

Embodiment 3

[0046] 1. Accurately weigh 1g of cyclosporin A, 4.5g of povidone-K30, 0.55g of phospholipids, and 0.55g of poloxamer 188, add 20ml of absolute ethanol to dissolve, put in a water bath at 60°C, 90rmp rotary evaporation until nearly dry, The solvent was completely evaporated in a water bath at 70°C, placed in a -20°C refrigerator for 2 hours, then placed in a vacuum oven at 60°C for 12 hours, pulverized, and passed through an 80-mesh sieve to obtain a solid dispersion for future use.

[0047] 2. Weigh 3.3g of solid dispersion, mix with hypromellose 4000cPa.s1.5g, hypromellose 15000cPa.s0.75g, microcrystalline cellulose 1.5g, add 70% syrup to prepare soft material , passed through a 16-mesh sieve to obtain wet granules, baked in an oven at 60°C for 30 minutes, took them out, passed through a 16-mesh sieve for sizing, and pressed into tablets with a pressure controlled at 4-5kg to obtain about 19 sustained-release tablets.

[0048] 3. The solubility and in vitro drug release ...

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Abstract

The invention provides an oral ciclosporin A sustained-release agent. The sustained-release agent comprises the following components in part by mass: 1 part of ciclosporin A, 2.5 to 7.5 parts of polyvidone-K30, 0.15 to 4.82 parts of hydroxypropyl methyl cellulose 4000cPa.s, 0.1 to 3.94 parts of microcrystalline cellulose, 0 to 2.57 parts of hydroxypropyl methyl cellulose 15000cPa.s and 0.1 to 1.0part of phospholipid. By combining a solid dispersing technology and a sustained-release hydrophilic gel matrix technology and based on the 'double release' principle of fast release first and slow release second, the method prepares the insoluble medicament of ciclosporin A sustained-release agent; and the method has the obvious advantages that the solubility of ciclosporin A is improved, and the oral agent can quickly play the effect first and then smoothly and slowly release drug. The ciclosporin A sustained-release tablets reduce the lowered blood concentration peak-valley phenomenon and lower the drug-taking frequency. The invention also discloses a method for preparing the oral ciclosporin A sustained-release agent.

Description

technical field [0001] The invention relates to an oral slow-release preparation of an insoluble drug and a preparation method thereof, in particular to an oral cyclosporine A sustained-release preparation and a preparation method thereof. Background technique [0002] Sustained / controlled release preparations (sustained / controlled release preparations) have the advantages of reducing the peak and valley phenomenon of blood concentration, reducing the number of medications and side effects, and improving patient compliance, etc., and are increasingly widely used in clinical practice. The preparation of slow / controlled release preparations usually requires dissolving the drug first, then adding slow / controlled release excipients, and using appropriate technology to make slow / controlled release preparations. Water-soluble drugs are easy to dissolve in water and can be easily made into slow / controlled release preparations. Currently, there are many varieties on the market. For...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K38/13A61K47/38A61P37/06
Inventor 徐希明闻晓光梁雷张正艮刘宏飞余江南
Owner JIANGSU UNIV
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