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Composition of ciclosporin A and amphipathic chitosan derivatives and preparation thereof

The technology of a composition and cyclosporine is applied in the directions of drug combination, non-active medical preparations, cyclic peptide components, etc., which can solve the problems of low drug loading, achieve simple production process, improve clinical compliance, The effect of high encapsulation

Inactive Publication Date: 2011-07-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN 1698899 discloses a chitosan directly modified with a hydrophobic carbon chain, which can form a micelle in an aqueous medium at a suitable molecular weight and a suitable degree of substitution, but the drug loading capacity is relatively low

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Cyclosporin A N, O-carboxymethyl N-cholic acid chitosan (carboxymethyl substitution degree 110%, cholic acid substitution degree 5%, chitosan molecular weight 100,000) micelles

[0022] Take 90 mg of N, O-carboxymethyl N-cholic acid chitosan, dissolve it in 15 mL of double-distilled water, stir at room temperature for 0.5 h to fully swell; dissolve 50 mg of cyclosporine A in 1.25 mL of methanol, and add it dropwise Stir in the solution; ultrasonic probe (200w, 30min); dialysis bag (MWCO=12,000~14,000) single-distilled water dialysis for 8h, the obtained nano-solution passes through a 0.45μm microporous membrane; add 1% (w / v) manna to the filtrate Alcohol, mixed evenly, subpackaged, and freeze-dried.

[0023] The test results show that the drug-loaded micelles have a drug-loading capacity of 27.14%, an encapsulation efficiency of 67.05%, an average particle diameter of 199.1 nm, and a zeta potential of -31.2 mV.

Embodiment 2

[0025] Cyclosporine AN, O-carboxymethyl N-cholic acid chitosan (carboxymethyl substitution degree 103%, cholic acid substitution degree 7%, chitosan molecular weight 20,000)

[0026] Take 90 mg of N, O-carboxymethyl N-cholic acid chitosan, dissolve it in 15 mL of double-distilled water, stir at room temperature for 0.5 h to fully swell; dissolve 50 mg of cyclosporine A in 1.25 mL of methanol, and add it dropwise solution, 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 micro pore filter membrane; add 1% (w / v) mannitol to the filtrate, mix well, subpackage, freeze-dry to obtain.

[0027] The test results show that the drug-loaded micelles have a drug-loading capacity of 25.88%, an encapsulation efficiency of 62.85%, an average particle diameter of 193.1 nm, and a zeta p...

Embodiment 3

[0029] Cyclosporine A N, O-carboxymethyl N-cholic acid chitosan (87% carboxymethyl substitution, 3.6% cholic acid substitution, chitosan molecular weight 250,000)

[0030] Take 90 mg of N, O-carboxymethyl N-cholic acid chitosan, dissolve it in 15 mL of double-distilled water, stir at room temperature for 0.5 h to fully swell; dissolve 50 mg of cyclosporine A in 1.25 mL of methanol, and add it dropwise solution, 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 micro pore filter membrane; add 1% (w / v) mannitol to the filtrate, mix well, subpackage, freeze-dry to obtain.

[0031] The test results showed that the drug-loaded micelles had a drug-loading capacity of 22.57%, an encapsulation efficiency of 52.47%, an average particle diameter of 215.3nm, and a zeta potential of...

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Abstract

The invention relates to the field of pharmaceutic preparations, and discloses a composition of ciclosporin A and amphipathic chitosan derivatives (N,O-carboxymethyl N-cholic acid chitosan) and a preparation method thereof. The composition has the characteristics of high medicament loading rate, high stability and high possibility of being absorbed, and can be used for overcoming the defects such as serious toxic or side effect of the existing ciclosporin A. The preparation method of the composition is simple, and the process is mature, thus the preparation method id applicable to large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a composition of cyclosporine A and amphiphilic chitosan derivatives and a preparation method thereof. Background technique [0002] Cyclosporine A (Cyclosporine A, CsA) is a cyclic polypeptide composed of 11 amino acids. It is a third-generation selective immunosuppressant and is mainly used for the prevention and treatment of rejection and autoimmunity after organ or tissue transplantation. disease treatment. 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 produ...

Claims

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Application Information

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IPC IPC(8): A61K38/13A61K9/00A61K47/36A61K47/48A61P37/06A61K47/61
Inventor 周建平霍美蓉坎扎彭小玲王竞
Owner CHINA PHARM UNIV
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