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Cyclosporine A fast release solid dosage forms and preparation thereof

A solid dosage form, cyclosporine technology, applied in the field of medicine, can solve the problems of accelerating the cross-linking and curing reaction of capsular gelatin, biological and physiological side effects, injection injection pain, etc., and achieves increased apparent solubility, simple process, and improved precision. degree of effect

Inactive Publication Date: 2008-08-13
SHANGHAI JIAO TONG UNIV
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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.
In addition, the preparation process of soft capsules is complicated, and liquid alcohol solvents are prone to volatilize through the capsule shell during storage, which accelerates

Method used

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  • Cyclosporine A fast release solid dosage forms and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0020] Example 1: 0.5% CyA, 75% lipid material, 24.5% porous material

[0021] (1) Dissolve 1 g of cyclosporin A in 150 g of lipid material soy phospholipid which is melted by heating;

[0022] (2) Add 49g of the porous material calcium sulfate to adsorb the drug-lipid melt, and cool and solidify to obtain a solid composition powder;

[0023] (3) Fill the obtained solid composition powder into capsules.

[0024] Implementation effect: The cyclosporin A quick-release solid dosage form prepared by the present invention has no residual organic solvent, accurate dosage, and rapid release in vitro. It can dissolve about 80% of CyA within 30 minutes in 37°C water, 0.1M HCl and phosphate buffer. , More than 85% within 60min, the particle size distribution of the drug emulsion is 1~500nm. The drug exists in a molecular state and has good stability.

Example Embodiment

[0025] Example 2: 25% CyA, 5% lipid material, 70% porous material

[0026] (1) Dissolve 25g of cyclosporin A in 5g of the lipid material combination corn oil and soybean phospholipids that are heated and melted;

[0027] (2) Add 70g of the porous material methylcellulose to adsorb the drug-lipid melt, and cool and solidify to obtain a solid composition powder;

[0028] (3) Fill the obtained solid composition powder into capsules.

[0029] Implementation effect: The cyclosporin A quick-release solid dosage form prepared by the present invention has no residual organic solvent, accurate dosage, and rapid release in vitro. It can dissolve about 80% of CyA within 30 minutes in 37°C water, 0.1M HCl and phosphate buffer. , More than 85% within 60min, the particle size distribution of the drug emulsion is 10-600nm. The drug exists in a molecular state and has good stability.

Example Embodiment

[0030] Example 3: 25% CyA, 40% lipid material, 35% porous material

[0031] (1) Dissolve 40 g of cyclosporin A in 64 g of lipid material vitamin E polyethylene glycol 1000 succinate that is heated and melted;

[0032] (2) Add 56 g of porous material combined methyl cellulose and starch to adsorb the drug-lipid melt, and cool and solidify to obtain a solid composition powder;

[0033] (3) Fill the obtained solid composition powder into capsules.

[0034] Implementation effect: The cyclosporin A quick-release solid dosage form prepared by the present invention has no residual organic solvent, accurate dosage, and rapid release in vitro. It can dissolve about 80% of CyA within 30 minutes in 37°C water, 0.1M HCl and phosphate buffer. , More than 85% within 60min, the particle size distribution of the drug emulsion is 100-800nm. The drug exists in a molecular state and has good stability.

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Abstract

The invention relates to a Cyclosporin A rapidly releasing solid dosage forms in the medicine technical field and the preparation method. The components weight contents of the solid dosage forms of the invention are that: 0.5 to 5 percent CyA, 5 to 75 percent lipide, and 5 to 70 percent porosint. The invention adopts CyA as the medicine activity component which is dissolved in the heating meltdown lipid material and added with the porosint in order to be richly adsorbed, then solid combined powder is prepared to be further suppressed to tablet or filled into capsule. The moisture content of the invention permeates into the porosint as meeting with water so as to make the wrapped medicine-lipide dispersoid inflate by absorbing water, pile out the gape structure and the medicine can be released. The invention can amplify the solubility and stripping speed of CyA, is useful for the absorption of medicine, has good stability, prevents the uses of organic solvent and polyoxyethylene castor oil, has safe operation, reduces the poison as well as side effects of medicine and has immunological rejection resisting function.

Description

technical field [0001] The invention relates to a solid composition in the technical field of medicine and a preparation method thereof, in particular to a cyclosporin A immediate-release solid dosage form and a preparation method thereof. Background technique [0002] The solubility of the immunosuppressant cyclosporine A (Cyclosporine A, CyA) in water is extremely low, lower than 10ug / ml at 37°C, and reported in the literature as 3.7-7.3ug / ml, making it actually a water-insoluble substance. Clinically, CyA is mainly used to prevent and treat immune rejection in liver, kidney, heart, lung, pancreas and other organ transplants and certain autoimmune diseases. [0003] The dosage forms of CyA currently on the market are soft capsules, oral liquids and injections, which self-emulsify in the body when it encounters water to form microemulsions, which improve the apparent solubility of the drug and facilitate the absorption of the drug. But the disadvantage is that although the...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K38/13A61K47/24A61K47/38A61K47/02A61P37/06
Inventor 金拓胡清松
Owner SHANGHAI JIAO TONG UNIV
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