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Stage releasing CsA solid tiny milk agent and tiny milk curing method thereof

A technology of cyclosporine and microemulsion, applied in cyclic peptide components, emulsion delivery, oil/fat/wax inactive ingredients, etc., can solve the problems of rejection, complicated production, prone to kidney damage and nerve damage, etc. Achieve stable blood drug concentration and good curing effect

Inactive Publication Date: 2011-03-30
安徽省药物研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The problem in the clinical application of cyclosporine is that the blood drug concentration needs to be continuously monitored. Adverse reactions such as kidney damage and nerve damage are prone to occur when the blood drug concentration exceeds the therapeutic concentration, and rejection reactions will occur when the blood drug concentration is lower than the therapeutic concentration
Patent 01807863 mentions the technology of microemulsion solidification, but this technology adopts spray drying method, the production is complicated and the loss is large, and at the same time, the solidified microemulsion is not made into a delayed release preparation

Method used

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  • Stage releasing CsA solid tiny milk agent and tiny milk curing method thereof
  • Stage releasing CsA solid tiny milk agent and tiny milk curing method thereof
  • Stage releasing CsA solid tiny milk agent and tiny milk curing method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0057] Enteric-coated granules

[0058] Cyclosporine A 1kg

[0059] Caprylic acid glyceride 2kg

[0060] Polyoxyethylene hydrogenated castor oil 5kg

[0061] Propylene glycol 3kg

[0062] Polyvinylpyrrolidone K30 4kg

[0063] Micro powder silica gel 5kg

[0064] Domestic II resin 6kg

[0065] Stomach dissolving granules

[0066] Cyclosporine A 1kg

[0067] Caprylic acid glyceride 2kg

[0068] Polyoxyethylene hydrogenated castor oil 5kg

[0069] Propylene glycol 3kg

[0070] Polyvinylpyrrolidone K30 4kg

[0071] Micro powder silica gel 5kg

[0072] Domestic IV resin 4kg

[0073] Add cyclosporine A to glyceryl caprylate and propylene glycol, stir to dissolve, add polyoxyethylene hydrogenated castor oil, stir and mix, add polyvinylpyrrolidone K30 and stir quickly to make it fully dispersed and dissolved in the solution. Then add micropowder silica gel and stir to make the adsorption solid. Dissolve the No. II resin with an appropriate amount of ethanol and add it to the microemulsion absorption sol...

example 2

[0075] Enteric-coated granules

[0076] Cyclosporine A 1kg

[0077] Caprylic acid glyceride 2kg

[0078] Polyoxyethylene hydrogenated castor oil 5kg

[0079] Propylene glycol 3kg

[0080] Polyvinylpyrrolidone K30 4kg

[0081] Micro powder silica gel 5kg

[0082] Starch 5kg

[0083] Domestic II resin 6kg

[0084] PEG 400 0.5kg

[0085] Talc 1kg

[0086] Ethanol 80kg

[0087] Stomach dissolving granules

[0088] Cyclosporine A 1kg

[0089] Caprylic acid glyceride 2kg

[0090] Polyoxyethylene hydrogenated castor oil 5kg

[0091] Propylene glycol 3kg

[0092] Polyvinylpyrrolidone K30 4kg

[0093] Micro powder silica gel 5kg

[0094] Domestic IV resin 4kg

[0095] Add cyclosporine A to glyceryl caprylate and propylene glycol, stir to dissolve, add polyoxyethylene hydrogenated castor oil, stir and mix, add polyvinylpyrrolidone K30 and stir quickly to make it fully dispersed and dissolved in the solution. Then add micropowder silica gel and stir to make the adsorption solid. The solidified microemulsion is...

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Abstract

The invention discloses a stage-releasing-type cyclosporine A solid micro-emulsion preparation and the solidification method of the micro-emulsion. With the containing cyclosporine A serving as the active component, the micro-emulsification technique and the micro-emulsion solidification technique are adopted to solidify the cyclosporine A micro-emulsion; then corresponding auxiliary material fordelayed release is adopted to prepare into particles which can release at the specific intestine; the gastric juice soluble particles and the enteric soluble particles are mixed in a certain proportion to get the cyclosporine stage-releasing preparation which can be slowly released by stage. The new preparation overcomes the deficiency of the big fluctuation of the blood concentration of the ordinary preparation, prolongs the effective concentration time of the medicine and reduces the incidence of adverse reaction. The preparation method is applied to the industrialized production.

Description

1. Technical Field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a stage-release cyclosporin A solid microemulsion preparation and a microemulsion solidification method. 2. Background technology [0002] Cyclosporin A (Ciclosporin A) is a fat-soluble cyclic undecapeptide compound produced by the mold Tolypocladium inflatum. It was discovered in 1969 and first used in clinical practice in 1978. At present, cyclosporine A is mainly used for clinical immunosuppression, which has been produced by many pharmaceutical companies. The chemical name of cyclosporine is: cyclo[[(E)-(2S,3R,4R)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl]-L-2 amino Butyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl -N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl] [0003] Its structural formula is: [0004] [0005] Cyclosporine can selectively act on the initial stage of T lymphocyte activation. Help...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/13A61K9/107A61K9/16A61K47/34A61K47/38A61P37/06A61P37/02A61K47/44
Inventor 孙备吕凌柏俊姚磊陆忠祥戴萍萍崔颖李姜晖
Owner 安徽省药物研究所
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