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Self-microemulsifying soft capsule content combination of ciclosporin A and preparation method thereof

A technology for cyclosporine and contents, which is applied in the field of self-microemulsifying soft capsule contents combination of cyclosporine A and the field of preparation thereof, can solve the problems such as cyclosporine nephrotoxicity that cannot effectively increase the clinical efficacy of cyclosporine, and the like, Achieve the effect of improving bioavailability, simple preparation process and improving dissolution

Active Publication Date: 2014-09-24
无锡曙辉药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some improvements have been made in the formulation process of these two patents and some other patents, there are defects in the treatment, which cannot effectively increase the clinical efficacy of cyclosporine and reduce the nephrotoxicity in the clinical application of cyclosporine. Serious side effects such as liver toxicity

Method used

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  • Self-microemulsifying soft capsule content combination of ciclosporin A and preparation method thereof
  • Self-microemulsifying soft capsule content combination of ciclosporin A and preparation method thereof
  • Self-microemulsifying soft capsule content combination of ciclosporin A and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0020] Weigh 10 parts of cyclosporine A, 10 parts of phosphatidylcholine (80% pure soybean lecithin), 15 parts of absolute ethanol, 6 parts of propylene glycol, 45 parts of polyoxyethylene hydrogenated castor oil CremophorRH4045 parts, 8019 parts of Span and medium chain fatty acid 25 parts of triglycerides were placed in a homogeneous emulsification pot and heated to 50°C, heated for 0.5h, and stirred to dissolve the drug to make a content solution; the content solution was pressed into soft capsules with a rotary molding machine, and processed with 95% ethanol Surface treatment, wash off the surface oil layer, ventilate and dry to get the finished product; the drying temperature is 25°C.

Embodiment 2

[0022] Weigh 12 parts of cyclosporine A, 12 parts of phosphatidylcholine (80% pure egg yolk lecithin), 10 parts of absolute ethanol, 10 parts of propylene glycol, 4060 parts of polyoxyethylene hydrogenated castor oil CremophorRH, 8010 parts of Span and medium chain fatty acid Put 20 parts of triglycerides in a homogeneous emulsification pot and heat to 60°C, heat for 0.8h, and stir to dissolve the drug to make a content solution; press the above-prepared content solution into a soft capsule with a rotary molding machine, And use 95% ethanol to carry out surface treatment, wash off the surface oil layer, ventilate and dry to obtain the finished product, and the drying temperature is 27°C.

Embodiment 3

[0024] Weigh 8 parts of cyclosporine A, 8 parts of phosphatidylcholine (45% pure soybean lecithin), 6 parts of absolute ethanol, 16 parts of propylene glycol, 65 parts of polyoxyethylene hydrogenated castor oil CremophorRH4065 parts, 808 parts of Span and medium chain fatty acid 15 parts of triglycerides were placed in a homogeneous emulsification pot and heated to 40°C, heated for 1.0 h, and stirred to dissolve the drug to make a content solution; the content solution prepared above was pressed into a soft capsule with a rotary molding machine, And use 95% ethanol for surface treatment, wash off the surface oil layer, and ventilate and dry to obtain the finished product; the drying temperature is 28°C.

[0025] Cyclosporine A self-microemulsifying soft capsules prepared by using the above three components are suitable for preventing rejection of allogeneic kidney, liver, heart, bone marrow and other organ or tissue transplants, and are also suitable for preventing and treating...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a self-microemulsifying soft capsule content combination of ciclosporin A. The self-microemulsifying soft capsule content combination of ciclosporin A comprises 1-12 parts of ciclosporin A, 1-12 parts of phosphatidylcholine, 5-20 parts of anhydrous ethanol, 5-20 parts of propylene glycol, 30-80 parts of polyoxyethylene hydrogenated castor oil, 5-30 parts of span 80 and 10-30 parts of medium-chain triglycerides. The invention further provides a preparation method of the self-microemulsifying soft capsule content combination of ciclosporin A. The raw materials selected by the invention are easily available and low in cost, and the preparation process is simple, so that the self-microemulsifying soft capsule content combination of ciclosporin A is suitable for large-scaled industrialized production. The bad character that ciclosporin A is low in bioavailability can be overcome and the disparity of bioavailability of individuals can be reduced as far as possible. Dissolubility of water insoluble medicines is greatly improved, and the bioavailability of the medicines is improved. Particularly, combination with phosphatidylcholine increases the clinical curative effect of ciclosporin and reduces severe side effects of renal toxicity and hepatotoxicity in clinical application of ciclosporin.

Description

technical field [0001] The invention relates to a cyclosporin A self-microemulsifying soft capsule content composition and a preparation method thereof, in particular to a self-microemulsifying soft capsule containing cyclosporine A and phosphatidylcholine and a preparation method thereof. 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 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] Cyclosporin A is a new type of high-efficiency immunosuppressant, which was first developed by the Swiss Sandoz Pharmaceutical Company. In 1983, the...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K38/13A61K47/40A61P37/06
Inventor 贾祥波陆继好
Owner 无锡曙辉药业有限公司
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