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Cyclosporine soft capsule for immunosuppression and preparation method of cyclosporine soft capsule

A soft capsule, cyclosporine technology, applied in the field of pharmaceutical preparations and immunosuppressive drugs, can solve the problems of high toxicity, easy migration of ethanol, hypersensitivity reactions of patients, etc., and achieve the effects of reducing toxicity and enhancing drug stability.

Active Publication Date: 2015-10-28
CARBIOGENE THERAPEUTICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this patent and the previous existing patent technology, ethanol is added as a solvent to dissolve cyclosporine, but because ethanol is easy to migrate, during storage, ethanol will migrate out through the capsule shell, resulting in the decrease of cyclosporine solubility and precipitation
At the same time, polyoxyethylene castor oil is used as a surfactant in most patents, but its toxicity is relatively high, and it is easy to cause hypersensitivity reactions in patients

Method used

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  • Cyclosporine soft capsule for immunosuppression and preparation method of cyclosporine soft capsule
  • Cyclosporine soft capsule for immunosuppression and preparation method of cyclosporine soft capsule
  • Cyclosporine soft capsule for immunosuppression and preparation method of cyclosporine soft capsule

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Experimental program
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Effect test

Embodiment 1

[0023]

[0024] Preparation:

[0025] Add water into the dispensing tank, heat it to 76°C and keep it at a constant temperature, then add gelatin, glycerin, and sorbitol, wherein the mass ratio of gelatin: glycerin: sorbitol: water is 1:0.5:0.1:1, stir with a mixer, and make each Dissolve the components, keep the negative pressure greater than 0.08 MPa, and stir for 6 hours, so that all the gelatin is dissolved and the air bubbles in the liquid are completely discharged, and the capsule shell glue is obtained. The prescription quantity takes cyclosporine and dissolves it in the prescription quantity of poloxamer 124, adds polyethylene glycol 400 and glycerol monolinoleate, stirs to dissolve, and then rolls it into soft capsules on a soft capsule machine. The obtained soft capsules were washed with absolute ethanol, and ventilated and dried at 25°C.

Embodiment 2

[0027]

[0028] Preparation:

[0029] Add water into the dispensing tank, heat it to 85°C and keep it at a constant temperature, then add gelatin, glycerin, and sorbitol, wherein the mass ratio of gelatin: glycerin: sorbitol: water is 1:0.5:0.1:1, stir with a mixer, and make each Dissolve the components, keep the negative pressure greater than 0.08MPa, and stir for 8 hours to completely dissolve the gelatin and completely discharge the bubbles in the liquid to obtain the capsule shell glue. The prescription quantity takes cyclosporine and dissolves it in the prescription quantity of poloxamer 124, adds polyethylene glycol 400 and glycerol monolinoleate, stirs to dissolve, and then rolls it into soft capsules on a soft capsule machine. The obtained soft capsules were washed with absolute ethanol, and ventilated and dried at 25°C.

Embodiment 3

[0031]

[0032]

[0033] Preparation:

[0034] Add water into the dispensing tank, heat it to 80°C and keep it at a constant temperature, then add gelatin, glycerin, and sorbitol, wherein the mass ratio of gelatin: glycerin: sorbitol: water is 1:0.5:0.1:1, stir with a mixer, and make each Dissolve the components, keep the negative pressure greater than 0.08MPa, and stir for 7 hours to completely dissolve the gelatin and completely discharge the bubbles in the liquid to obtain the capsule shell glue. The prescription quantity takes cyclosporine and dissolves it in the prescription quantity of poloxamer 124, adds polyethylene glycol 400 and glycerol monolinoleate, stirs to dissolve, and then rolls it into soft capsules on a soft capsule machine. The obtained soft capsules were washed with absolute ethanol, and ventilated and dried at 25°C.

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Abstract

The invention belongs to the technical field of pharmaceutical preparation and discloses a cyclosporine soft capsule for immunosuppression and a preparation method of the cyclosporine soft capsule. The preparation comprises a capsule shell and capsule content. The capsule content comprises cyclosporine, poloxamer, polyethylene glycol and single linoleic acid glyceride. Compared with the prior art, organic solvents such as ethanol and propylene glycol do not need to be added, and drug stability is enhanced. Polyoxyethylene castor oil does not need to be added as surfactants, and toxicity of an existing preparation is reduced. The preparation method is simple, and industrial mass production can be achieved easily.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to the technical field of immunosuppressant drugs, in particular to a soft capsule containing cyclosporine and a preparation method thereof. Background technique [0002] Cyclosporin, also known as cyclosporine A (Crclosporine A, CyA), belongs to the metabolites of fungi, is a high-level peptide compound composed of 11 amino acids, and is a white needle-like crystal. Because it is markedly hydrophobic and practically insoluble in water, it is rarely absorbed by the body after oral administration, has very low bioavailability (30% or less), and has been reported to vary greatly in absorption between humans, When administered for a long time, serious side effects such as nephrotoxicity and hepatotoxicity may appear. [0003] Since the listing of cyclosporine, researchers have done a lot of research to overcome its adverse properties, and developed many improved ph...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K38/13A61K47/34A61K47/14A61P37/06
Inventor 孙号
Owner CARBIOGENE THERAPEUTICS CO LTD