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Micelle loaded with Tacrolimus or pharmaceutical salts thereof, lyophilized preparation as well as preparation methods and applications

A technology of tacrolimus and freeze-dried preparations, which is applied in the field of pharmaceutical dosage forms and nano-medicine preparations, can solve the problems of neurotoxicity, insensitivity, inability to move, mutism, seizures, etc., and achieve good stability

Inactive Publication Date: 2011-09-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because it contains a large amount of organic solvent and HCO-60, intravenous injection of FK506 has the risk of hemolysis, and neurotoxicity often occurs. In mild cases, headache, tremor, insomnia, nightmares, photophobia, and insensitivity may occur. In severe cases, akinesia, Mutism, epileptic seizures, encephalopathy, etc., aggravate the suffering of patients
[0003] Those skilled in the art have been working on reducing toxic and side effects, or increasing its drug concentration in target organs, in order to better exert its curative effect, but there is no effective solution to tacrolimus or its medicinal salts in clinical anti-tumor. the puzzle

Method used

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  • Micelle loaded with Tacrolimus or pharmaceutical salts thereof, lyophilized preparation as well as preparation methods and applications
  • Micelle loaded with Tacrolimus or pharmaceutical salts thereof, lyophilized preparation as well as preparation methods and applications
  • Micelle loaded with Tacrolimus or pharmaceutical salts thereof, lyophilized preparation as well as preparation methods and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] (1) 85 mg of methoxypolyethylene glycol poly(ε-caprolactone) polymer (MPEG 2000 -PCL 2000 ) and 15 mg of tacrolimus were dissolved in 2 ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0085] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0086] (3) Add 5ml of preheated water for injection into gel B, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10nm-100nm;

[0087](4) Freeze-dry the micelles C to obtain the final stable nano-medicine freeze-dried powder D; before the clinical use of the freeze-dried powder, adding water for injection will automatically form a sustained-release nano-sized glue under the condition of heating. bundle.

[0088] The obtained micelles C, lyophilized powder D and final reconstituted m...

Embodiment 2

[0090] (1) 92 mg of methoxypolyethylene glycol poly(ε-caprolactone) polymer (MPEG 2000 -PCL 2000 ) and 8 mg of tacrolimus were dissolved in 2 ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0091] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0092] (3) Add 5ml of preheated water for injection into gel B, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10nm-100nm;

[0093] (4) Freeze-dry the micelles C to obtain the final stable nano drug freeze-dried powder D.

[0094] Before the clinical use of the lyophilized powder, adding water for injection will automatically form sustained-release nano-sized micelles under the condition of heating.

[0095] The obtained micelles C, lyophilized powder D and the final reconstituted...

Embodiment 3

[0097] (1) 92mg poly(ε-caprolactone)-polyethylene glycol-poly(ε-caprolactone) triblock polymer (PCL 850 -PEG 2000 -PCL 850 ) and 8 mg of tacrolimus were dissolved in 2 ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0098] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0099] (3) Add 5ml of preheated water for injection into gel B, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10nm-100nm;

[0100] (4) Freeze-dry the micelles C to obtain the final stable nano-medicine freeze-dried powder D; before the clinical use of the freeze-dried powder, adding water for injection will automatically form a sustained-release nano-sized glue under the condition of heating. bundle.

[0101] The drug loading of the obtained micelles wa...

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Abstract

The invention belongs to the technical field of pharmaceutical dosage forms and nano medicine preparation, and more particularly relates to a micelle loaded with Tacrolimus or pharmaceutical salts thereof, a lyophilized preparation as well as preparation methods and applications thereof. In order to achieve the clinical application of the micelle provided by the invention, the drug loading, the encapsulation rate and the stability of the preparation need to be ensured. The micelle is prepared from biodegradable polymer materials and Tacrolimus or pharmaceutical salts thereof in parts by weight: 1 part of Tacrolimus or pharmaceutical salts thereof and 1.5-99 parts of degradable polymer materials, wherein the degradable polymer materials are diblock polymer methoxy polyethylene glycol-polycaprolactone (the molecular weight ratio of MPEG to PCL is 0.5-2), and triblock polymer polycaprolactone-polyethylene glycol-polycaprolactone (the molecular weight ratio of PCL to PEG is 0.5-3). The micelle using Tacrolimus or pharmaceutical salts thereof or the lyophilized preparation of the micelle can be used in medicines for anti-rejection in liver transplantation, kidney transplantation, lung transplantation, corneal transplantation and other organ transplantations.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical dosage forms and nano-medicines, and in particular relates to micelles loaded with tacrolimus or a pharmaceutically acceptable salt thereof, a freeze-dried preparation and a preparation method and application thereof. Background technique [0002] Tacrolimus (Tacrolimus, FK506) is a macrolide antibiotic extracted from the fermentation broth of steptomyces tsukubaensis, and is a representative drug of the second generation of immunosuppressive drugs. The action and mechanism are similar to cyclosporine, but its inhibitory effect on various immune reactions is 100 times stronger than that of cyclosporine; the inhibitory effect on rejection reactions that have occurred is also better than that of cyclosporine; patients who use this drug, bacteria And the virus infection rate is also lower than cyclosporine treatment, especially the drug has a strong pro-hepatotropic effect on li...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/436A61K47/34A61P37/06A61P43/00
Inventor 钱志勇魏于全王成赵霞
Owner SICHUAN UNIV
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