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Ciclosporin A microemulsion formulation for injection and preparation method thereof

A technology for injection and cyclosporine, which is applied in the field of medicine, can solve the problems of decreased renal blood flow and glomerular filtration rate, poisoning cells, and cholestasis, and achieves good absorption and bioavailability and low emulsifier dosage. Minimal effects with few side effects

Inactive Publication Date: 2012-10-17
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since it contains more than 65% of the solubilizer polyoxyethylene castor oil, it is easy to cause allergic reactions and release of histamine, reduction of renal blood flow and glomerular filtration rate, cholestasis, and poisoning of cells, neurotoxicity and liver toxicity and other side effects, thus limiting the use of the drug to some extent

Method used

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  • Ciclosporin A microemulsion formulation for injection and preparation method thereof
  • Ciclosporin A microemulsion formulation for injection and preparation method thereof
  • Ciclosporin A microemulsion formulation for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] The preparation of embodiment 1 microemulsion preparation

[0033] Heat 9g of miglitol, 12g of HS 15 and 6g of lecithin in a water bath at 40°C to make them evenly mixed. After cooling to room temperature, add 6g of PEG-400 and 12g of ethanol, and then dissolve 2.5g of cyclosporine A In the above mixture of oil and surfactant, add water for injection to 100g, adjust the pH value to 5.0-7.0, stir well to obtain the microemulsion concentrate, and filter the obtained product with a 0.45μm microporous membrane, potting , Sterilize.

[0034] Particle size investigation: The particle size of the microemulsion was measured by a Malvern laser scattering particle size analyzer (Zetasizer 3000, Malvern, UK), the light scattering degree was set at 90°, and the measurement temperature was 25±1°C. The particle diameter of prescription 1 drug-containing microemulsion is measured within 100nm (55.7nm), which is suitable for injection.

Embodiment 2

[0036] Heat 10g medium carbon chain triglycerides (GTCC), 15g HS15 and 5g lecithin in a water bath at 40°C to mix them evenly, add 5g PEG-400 and 10g ethanol after cooling to room temperature, and then add 2.5g Dissolve cyclosporin A in the mixture of the above-mentioned oil and surfactant, add water for injection to 100g, and adjust the pH value to 5.0-7.0, stir well to obtain the microemulsion concentrate, and the obtained product is filtered through a 0.45 μm microporous filter Membrane filtration, potting and sterilization.

Embodiment 3

[0037] Embodiment 3: hemolytic test of cyclosporin A injection microemulsion preparation of the present invention

[0038] (1) Test materials and conditions:

[0039] Test material: prepare cyclosporin A microemulsion preparation for injection according to the method of above-mentioned embodiment 1, the concentration of this microemulsion prescription is 2.5% (w / w), dilutes 25 times with 0.9% sodium chloride injection, serves as Test solution; the control group is normal saline;

[0040] Experimental animal: 1 clean grade New Zealand white rabbit, weighing 2-3 kg (purchased from the Animal Experiment Center of Shenyang Pharmaceutical University);

[0041] Animal feeding environment: Room temperature: 20°C

[0042] Humidity: 30%-70%

[0043] Lighting: artificial light, 12 hours daylight, 12 hours dark

[0044] Laboratory animal facility certificate number: SYXK (Liao) 2006-0012

[0045] (2) Test method

[0046]Take 1 female New Ze...

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Abstract

The invention belongs to the technical field of medicine, and discloses an injection microemulsion preparation containing ciclosporin A and a preparation method thereof. The preparation consists of the following components: 1 to 5 percent of basic medicine, 1 to 30 percent of oil phase, 2 to 40 percent of a surfactant, 2 to 40 percent of a cosurfactant, and the balance being water for injection. The preparation method comprises the following steps: dissolving the oil phase and the surfactant of the recipe dosage into liquid through a water bath at 40 DEG C, adding the cosurfactant at a room temperature into the liquid and mixing the mixture evenly, adding the medicine into the mixture, stirring the mixture slightly to dissolve the medicine, dropping water so as to regulate the pH value from 5.0 to 7.0, and obtaining the microemulsion preparation. The invention takes the safe and nonirritant non-ion surfactant to replace polyoxyethylene castor oil capable of easily causing an allergic reaction in the prior injection, thereby improving the safety of the medicine, and reducing toxicity and adverse reactions.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a microemulsion preparation for injection containing cyclosporine A and a preparation method of the microemulsion preparation for injection. Background technique [0002] Cyclosporine A (cyclosporine A, CysA) is a cyclic polypeptide substance composed of 11 amino acids, and is a new type of potent immunosuppressant. The drug was discovered by Borel from 1969 to 1970, and it is obtained by extracting metabolites produced by mold culture. In 1972, it was found that it has a strong immunosuppressive effect, and has a specific inhibitory effect on the activation and proliferation of T lymphocytes. It was first used clinically in 1978 and was successfully used to greatly reduce the mortality rate of transplant patients. It has been widely used in anti-rejection after solid organ and bone marrow transplantation, and is a popular new immunosuppressant. [0003] Cyclosporine A is insolu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K38/13A61P37/06
Inventor 袁悦
Owner SHENYANG PHARMA UNIVERSITY
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