Combination of cyclosporine A and alkylation serum albumin and preparation method thereof

A serum albumin and composition technology, which is applied in the direction of non-active ingredients of polymer compounds, drug combinations, medical preparations of non-active ingredients, etc., can solve problems such as hypersensitivity, liver and kidney toxicity, and achieve low irritation, The effect of high drug loading and simple production process

Inactive Publication Date: 2011-05-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most commonly used cyclosporine A preparation in clinical practice-Sandimmune uses more than 65% polyoxyethylene castor oil (Cremophor EL) as a solubilizer, and this excipient can easily cause hypersensitivity reactions, liver and kidney toxicity, etc.

Method used

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  • Combination of cyclosporine A and alkylation serum albumin and preparation method thereof
  • Combination of cyclosporine A and alkylation serum albumin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Cyclosporin A Octyl Human Serum Albumin Nanoparticles

[0026] Take 90mg of octyl-modified human serum albumin derivative, dissolve it in 15mL double-distilled water, stir at room temperature for 0.5h to fully swell; ; Probe ultrasound (200w, 30min); dialysis bag (MWCO=12,000~14,000) single-distilled water dialysis for 8h, the resulting nano-solution passed through a 0.45μm microporous membrane; add 1% (w / v) mannitol to the filtrate, mix well , aliquoted and freeze-dried.

[0027] The test results showed that the cyclosporin A octyl human serum albumin nanoparticles had a drug loading capacity of 31.14%, an encapsulation efficiency of 81.41%, an average particle diameter of 199.1nm, and a zeta potential of -31.2mV.

[0028] See attached figure 1 , figure 1It is the X-ray diffraction (XRD) pattern of various substances: wherein, curve a is an alkylated serum albumin derivative; curve b is cyclosporine A; curve c is cyclosporine A and alkylated serum albumin A physica...

Embodiment 2

[0031] Cyclosporine A Octyl Recombinant Human Serum Albumin Nanoparticles

[0032] Take 90mg of octyl-modified recombinant human serum albumin derivative, dissolve it in 15mL of double-distilled water, stir at room temperature for 0.5h to fully swell; dissolve 50mg of cyclosporine A in 1.25mL of absolute ethanol, and add it dropwise Medium, stirring; high-pressure homogenization (200bar, 2 times of circulation; 500bar, 2 times of circulation; 800bar, 3 times of circulation); dialysis bag (MWCO=12,000~14,000) single distilled water dialysis for 8h, the obtained nano solution passed through 0.45μm micropore filter membrane; add 1% (w / v) mannitol to the filtrate, mix evenly, subpackage, freeze-dry to obtain.

[0033] The test results show that the cyclosporin A octyl recombinant human serum albumin nanoparticles have a drug loading capacity of 30.48%, an encapsulation efficiency of 79.36%, an average particle diameter of 193.1nm, and a zeta potential of -33.0mV.

Embodiment 3

[0035] Cyclosporine A Octyl Porcine Serum Albumin Nanoparticles

[0036] Take 90mg of octyl-modified porcine serum albumin derivative, dissolve it in 15mL double-distilled water, stir at room temperature for 0.5h to fully swell; dissolve 40mg cyclosporin A in 1.0mL chloroform, add dropwise to the above carrier solution, stir Probe ultrasound (200w, 30min); Vacuum rotary evaporation for 2h to remove the organic solvent, the resulting nano-solution through a 0.45μm microporous membrane; add 1% (w / v) mannitol to the filtrate, mix well, sub-package, freeze-dry have to.

[0037] The test results show that the cyclosporin A octyl porcine serum albumin nanoparticles have a drug loading capacity of 24.61%, an encapsulation efficiency of 72.20%, an average particle diameter of 236.5nm, and a zeta potential of -33.6mV.

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Abstract

The invention relates to the field of pharmaceutical preparation, and discloses a combination of cyclosporine A and alkylation serum albumin and a preparation method thereof. The combination has the characteristics of high drug-loading rate and stability, and can overcome the defects of serious side effects in traditional cyclosporine A preparation and the like. The preparation method has mature process, is simple and suitable for industrialized mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a composition of cyclosporin A and alkylated serum albumin and a preparation method thereof. Background technique [0002] Cyclosporine A (Cyclosporine A, CsA) is a cyclic polypeptide composed of 11 amino acids. The drug was discovered by Borel in 1969 and isolated from the culture fluid of the filamentous fungus (Tolypocladium inflatum). In 1972, it was discovered that it has a strong immunosuppressive ability and has a specific inhibitory effect on the activation and proliferation of T lymphocytes, and it was first used clinically in 1978. In 1983, the US FDA approved it for clinical kidney transplantation. Swiss Novartis successfully launched the cyclosporine A product Sandimin in 1984, and modified the dosage form of Sandimin in 1995, forming the new Sandimin microemulsion preparation that is now clinically used. In 1991, Fujian Microbiology Research and Hangzhou Z...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K47/48A61P37/06A61K47/42A61K47/62
Inventor 周建平霍美蓉彭小玲李静崔蓓
Owner CHINA PHARM UNIV
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