Self-micro emulsifying soft capsule of cyclosporine A and method of producing the same

A technology of soft capsules and cyclosporine, which is applied in the direction of capsule delivery, cyclic peptide components, oil/fat/wax non-effective ingredients, etc. It can solve the problems of increased product cost, many formula components, complicated preparation process, etc., and achieve granular Uniform diameter, improved dissolution, and improved bioavailability

Inactive Publication Date: 2008-02-27
无锡曙辉药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although some improvements have been made in the formulation process of these two patents and some other patents, they all have similar defects...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The ratio of its components (prescription amount) of the self-microemulsifying soft capsule of cyclosporine A of the present invention is counted in parts: the preparation method of the self-microemulsifying soft capsule of its cyclosporin A adopts the following process steps:

[0017] The present invention takes cyclosporin A: 10 parts, absolute ethanol: 15 parts, propylene glycol: 6 parts, polyoxyethylene hydrogenated castor oil Cremophor RH40: 45 parts, Span-80: 19 parts and medium chain Fatty acid triglycerides: 25 parts. Weigh anhydrous ethanol, propylene glycol, Span-80, medium-chain fatty acid triglycerides, polyoxyethylene hydrogenated castor oil RH40 and cyclosporin A in the above-mentioned prescription amount and heat to 50°C in a homogeneous emulsification pot. : 0.5h, and stir to dissolve the medicine, and make a content solution; the content solution (the content solution includes: absolute ethanol, propylene glycol, Span-80, medium-chain fatty acid triglyc...

Embodiment 2

[0019] The ratio of its components (prescription amount) of the self-microemulsifying soft capsule of cyclosporine A of the present invention is counted in parts: the preparation method of the self-microemulsifying soft capsule of its cyclosporin A adopts the following process steps:

[0020] The present invention takes cyclosporin A: 12 parts, absolute ethanol: 10 parts, propylene glycol: 10 parts, polyoxyethylene hydrogenated castor oil Cremophor RH40: 60 parts, Span-80: 10 parts and medium chain Fatty acid triglycerides: 20 parts. Weigh anhydrous ethanol, propylene glycol, Span-80, medium-chain fatty acid triglycerides, polyoxyethylene hydrogenated castor oil RH40 and cyclosporin A in the above-mentioned prescription amount and heat to 60°C in a homogeneous emulsification pot. : 0.8h, and stirred to dissolve the medicine to make a content solution; the above-prepared content solution (the content solution includes: absolute ethanol, propylene glycol, Span-80, medium-chain f...

Embodiment 3

[0022] The ratio of its components (prescription amount) of the self-microemulsifying soft capsule of cyclosporine A of the present invention is counted in parts: the preparation method of the self-microemulsifying soft capsule of its cyclosporin A adopts the following process steps:

[0023] The present invention takes cyclosporin A: 8 parts, absolute ethanol: 6 parts, propylene glycol: 16 parts, polyoxyethylene hydrogenated castor oil Cremophor RH40: 65 parts, Span-80: 8 parts and medium chain Fatty acid triglycerides: 15 parts. Weigh anhydrous ethanol, propylene glycol, Span-80, medium-chain fatty acid triglycerides, polyoxyethylene hydrogenated castor oil RH40 and cyclosporin A in the above-mentioned prescription amount and heat to 40°C in a homogeneous emulsification pot. : 1.0h, and stir to dissolve the medicine, and make a content solution; the above-prepared content solution (the content solution includes: absolute ethanol, propylene glycol, Span-80, medium-chain fatty...

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PUM

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Abstract

The invention relates to a self micro emulsifying soft capsule with cyclosporin A and the preparing method. The preparing method comprises the following steps: heating and dissolving cyclosporin A, absolute ethyl alcohol, methyl ethylene glycol, polyoxyethylene hydrogenated castor oil, span 80 and medium chain fatty acid triglyceride in the homogenized emulsified pan; making soft capsule; and getting the product by treating the surface with alcohol and drying. The disintegrated self micro emulsifying soft capsule is dispersed into the transparent microemulsion, and the determined result indicates that the grain diameter of microemulsion is uniform. The invention has the easy getting solvent, the low price and the simple technology, which is fit for the large scale industry production, overcomes the low bioavailability of cyclosporin A , reduces the enormous difference of bioavailability among the individual, improves the digestion of the water-insoluble medicine, and improves bioavailability of the medicine.

Description

technical field [0001] The invention relates to a self-microemulsifying soft capsule of cyclosporine A and a preparation method thereof, in particular to a self-microemulsifying soft capsule containing cyclosporine A. Background technique [0002] Cyclosporine A (CrclosporineA, CyA) is a metabolite of fungi, a high-level peptide compound composed of 11 amino acids, and is a white needle-like crystal. Because it is significantly hydrophobic and almost insoluble in water, it is rarely absorbed by the body after oral administration, and its bioavailability is very low (30% or less). And it has been reported that the absorption varies greatly between human bodies by 4-60%, and severe side effects such as nephrotoxicity and hepatotoxicity will appear when administered for a long time. [0003] Cyclosporin A is a new type of high-efficiency immunosuppressant, which was first developed by the Swiss Sandoz Pharmaceutical Company. In 1983, the US Food and Drug Administration (FDA) a...

Claims

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Application Information

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IPC IPC(8): A61K38/13A61K9/48A61K47/34A61P37/06A61K47/44
Inventor 贾祥波陆继好
Owner 无锡曙辉药业有限公司
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