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Constant-speed medicament release system and preparation method thereof

A drug release and fixed-rate technology, which is applied in the fields of medical technology and polymer chemistry, can solve the problems of increasing patient pain, short biological half-life, and inability to sustain long-term release, so as to avoid surgical implantation and removal, and operate under mild conditions , good biocompatibility and biodegradability

Inactive Publication Date: 2011-07-06
SHANGHAI UNIV OF ENG SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, diclofenac sodium (diclofenac sodium), which has already been on the market, is made into a sustained-release preparation to overcome its shortcomings such as rapid oral absorption and short biological half-life (1-2h).
However, the existing technology has defects such as the effective time of the drug after oral administration for up to 24 hours, which cannot be sustained for a long time; the gel sustained-release preparation needs surgical implantation and removal, which increases the pain of the patient and cannot meet the needs of clinical application.

Method used

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  • Constant-speed medicament release system and preparation method thereof
  • Constant-speed medicament release system and preparation method thereof
  • Constant-speed medicament release system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] (1) Dissolve 0.02 g of model drug Huperzine A and 0.1 g of polylactic acid in 5 ml of ethyl acetate, and use a dispersion homogenizer to disperse for 30 seconds at a speed of 10000 r / min to obtain an oil phase for use;

[0061] Add 100 g of a polyvinyl alcohol solution with a weight concentration of 0.1% to the oil phase at a stirring speed of 600 r / min, react for 2 hours, filter, wash, freeze-dry, and collect microspheres for use;

[0062] (2) Dissolve 0.4 g of ethyl cellulose in 10 g of hot water at 80°C and cool; add 10 g of distilled water and 1 g of NaCl under magnetic stirring to dissolve, add 0.4 g of polyvinylpyrrolidone, and after dissolving, add 1% by weight 10g of polyvinyl alcohol was finally added to 10g of distilled water to dissolve for 2h, stirred, and stored at 4°C after sterilization to obtain reverse temperature sensitive gel for use

[0063] (3) Disperse 0.1g of the microspheres of step (1) ultrasonically in 5g of the reverse thermosensitive gel of step (2)...

Embodiment 2

[0065] (1) Dissolve 0.02 g of model drug Huperzine B and 0.6 g of chitosan, with a molecular weight of 100,000, in 10 ml of ethyl acetate, and use a dispersion homogenizer to disperse at 10000 r / min for 30 seconds to obtain an oil phase;

[0066] Add 100 g of a polyvinyl alcohol solution with a weight content of 2% to the oil phase at a stirring speed of 800 r / min to react for 2 hours, filter, wash, freeze-dry, and collect microspheres for later use.

[0067] (2) Dissolve 1g of methyl cellulose in 10g of hot water at 80°C and cool; add 10g of distilled water and 2g of NaCl under magnetic stirring to dissolve, add 0.5g of polyvinylpyrrolidone after dissolution, and add 5% by weight polyvinylpyrrolidone after dissolution. 10g of vinyl alcohol; finally add 10g of distilled water to dissolve for 2h, stir evenly, and store at 4℃ after sterilization to obtain reverse temperature sensitive gel for use;

[0068] (3) Disperse 0.1 g of the microspheres of step (1) ultrasonically in 2 g of the ...

Embodiment 3

[0070] (1) Dissolve 0.02g of model drug galantamine and 0.2g of polylactic acid-polyvinyl alcohol copolymer with a molecular weight of 30,000 in 10ml ethyl acetate, and disperse for 30s with a dispersing homogenizer at a speed of 13000r / min , Obtain the oil phase for standby;

[0071] Add 100 g of a polyvinyl alcohol solution with a weight content of 0.1% to the oil phase at a stirring speed of 1000 r / min, react for 2 hours, filter, wash, freeze-dry, and collect microspheres for later use.

[0072] (2) Dissolve 2g of methyl cellulose in 10g of hot water at 80℃ and cool; add 10g of distilled water and 3g of sodium citrate to dissolve under magnetic stirring; add 1g of polyvinylpyrrolidone after dissolution; add 5% by weight after dissolution 10g of polyvinyl alcohol; finally add 10g of distilled water, dissolve for 2h, stir evenly, store at 4℃ after sterilization, and obtain reverse temperature sensitive gel for later use;

[0073] (3) Disperse 0.15g of the microspheres of step (1) u...

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Abstract

The invention discloses a constant-speed medicament release system and a preparation method thereof. The constant-speed medicament release system comprises medicament-containing microspheres and reverse thermo-sensitive gel, and the proportioning of the medicament-containing microspheres to the reverse thermo-sensitive gel by weight is 1: 5-1: 50. The microspheres and the reverse thermo-sensitive gel are combined, thereby avoiding the shortcomings of the microspheres; and simultaneously, the reverse thermo-sensitive gel can be injected into a patient in the injection way for quickly forming in-situ gel, so that the constant-speed medicament delivery can be achieved through the degradation of the gel and the diffused medicament release of the microspheres. In the system, materials selected by the system have good biocompatibility and biodegradability, the operation conditions are mild, the process is safe, the medicament release process is safe and controllable, and injection is adopted, thereby avoiding surgical implantation and extraction.

Description

Technical field [0001] The invention relates to a fixed and rapid drug release system and its preparation, and belongs to the fields of medical technology and polymer chemistry. Background technique [0002] Biodegradable sustained and controlled release formulations are a hot spot in current research. This kind of drugs brings good news to many diseases, especially those who need long-term medication. Frequent administration has great side effects on patients. It is possible to make the drug into a sustained-release dosage form to reduce the frequency of administration while maintaining the same effect. It makes a lot of sense. [0003] The fixed-rate release technology is a type of slow-controlled release technology, which specifically refers to that the formulation releases the drug in the body at a certain rate, which basically conforms to the kinetic law of zero-order release. The fixed-rate release can reduce the fluctuation of blood concentration and increase the complianc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/34A61K47/36A61K47/38
Inventor 孙蕊陈思浩邢晨晨
Owner SHANGHAI UNIV OF ENG SCI