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Disulfiram implant and preparation method thereof

A technology of disulfiram and implants, which is applied in the field of medicine, can solve the problems of poor patient compliance and low bioavailability, and achieve the effects of improving compliance, avoiding the first-pass effect, and improving bioavailability

Active Publication Date: 2015-08-12
SHENZHEN SCIENCARE MEDICAL INDUSTRIES CO. LTD.
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, when used as a drug for the treatment of tumors and alcohol dependence, patients need to take long-term medication, and the oral administration route, due to the existence of the first-pass effect, leads to low bioavailability, and long-term injection administration, the patient's compliance is very poor, and needs to be developed A new drug delivery formulation suitable for long-term administration, thus meeting the clinical needs of patients

Method used

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  • Disulfiram implant and preparation method thereof
  • Disulfiram implant and preparation method thereof
  • Disulfiram implant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A disulfiram implant, 80g of disulfiram, 20g of racemic polylactic acid, the selective viscosity coefficient of racemic polylactic acid is 0.9dl / g (chloroform, 25°C), and the average molecular weight is about 80,000;

[0037] The preparation method is,

[0038] 1) Prepare 0.5%~3% PVA aqueous solution as the continuous item, polylactic acid and disulfiram are dissolved in dichloromethane as the dispersed phase,

[0039] 2) Stir the dispersed phase at a stirring speed of 800 rpm;

[0040] 3) Slowly add the dispersed phase to the continuous phase while stirring;

[0041] 4) Continue stirring to volatilize the organic solvent to prepare microspheres, and the size of the obtained microspheres is 30-50 microns;

[0042] 5) Compress plain tablets with 5kN pressure, and coat with 6% polylactic acid dichloromethane solution. The diameter of the tablet is 8mm, the hardness test size is 6kg, and the thickness of the coating is 0.1mm.

[0043] Using the in vitro release test met...

Embodiment 2

[0045] A disulfiram implant, 60g of disulfiram, 40g of racemic polylactic acid, the selective viscosity coefficient of racemic polylactic acid is 0.7dl / g (chloroform, 25°C), and the average molecular weight is about 70,000;

[0046] The preparation method is,

[0047] 1) Prepare 0.5%~3% PVA aqueous solution as the continuous item, and dissolve polylactic acid and disulfiram in dichloromethane as the dispersed phase;

[0048] 2) Stir the dispersed phase at a stirring speed of 800 rpm;

[0049] 3) Slowly add the dispersed phase to the continuous phase while stirring;

[0050] 4) Continue stirring to volatilize the organic solvent to prepare microspheres, and the size of the obtained microspheres is 30-50 microns;

[0051] 5) Press 10kN pressure into plain tablets, and coat with 3% polylactic acid dichloromethane solution. The tablet diameter is 8mm, the hardness test size is 7kg, and the coating thickness is 0.2mm.

[0052] Using the in vitro release test method, continuous mea...

Embodiment 3

[0054] A disulfiram implant, 60g of disulfiram, 40g of racemic polylactic acid, the selective viscosity coefficient of racemic polylactic acid is 0.7dl / g (chloroform, 25°C), and the average molecular weight is about 70,000;

[0055] The preparation method is,

[0056] 1) Prepare 0.5%~3% PVA aqueous solution as the continuous item, and dissolve polylactic acid and disulfiram in dichloromethane as the dispersed phase;

[0057] 2) Stir the dispersed phase at a stirring speed of 800 rpm;

[0058] 3) Slowly add the dispersed phase to the continuous phase while stirring;

[0059] 4) Continue stirring to volatilize the organic solvent to prepare microspheres, and the size of the obtained microspheres is 30-50 microns;

[0060] 5) Press 10kN pressure into plain tablets, and coat with 5% polylactic acid dichloromethane solution. The tablet diameter is 8mm, the hardness test size is 7kg, and the coating thickness is 0.2mm.

[0061] Using the in vitro release test method, continuous m...

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Abstract

The invention relates to a disulfiram implant and a preparation method thereof. The disulfiram medicinal composition can be slowly and stably released in a human body, and the disulfiram implant comprises 60-80 parts of disulfiram and 20-40 parts of a biodegradable high polymer material. The disulfiram implant can be injected and implanted into the human body, and patients suffering from alcohol dependence can be treated so as to avoid repeated drinking. The therapeutic concentration can be maintained for a long time after administration, a first-pass effect is avoided, the bioavailability is improved, the compliance of the patients is improved, and the clinical requirements of the patients can be met.

Description

technical field [0001] The disulfiram implant and its preparation method related to the present invention can slowly and stably release the disulfiram pharmaceutical composition in the human body, and belong to the technical field of medicine. Background technique [0002] Disulfiram (disulfiram, DS), also known as tetraethylthiuram disulfide, disulfiram, was first synthesized in 1881, and was originally used as a catalyst for rubber vulcanization in the rubber industry. In the 1930s, DS was first used as a drug to treat scabies; later, it was found that disulfiram has a strong chelation effect on copper ions, which can reduce the activity of copper-containing respiratory enzymes, while intestinal worms have a strong chelation effect on copper ions. Sulfiram is extremely sensitive, so disulfiram is used as an insect repellent; in 1948, two doctors in Copenhagen, Hald and Jacobsen, accidentally discovered that drinking a small amount of alcohol after taking the insect repelle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/32A61K31/145A61K47/34A61P25/32A61K47/14
Inventor 尹述贵李金禄王实强刘庆哲张涛
Owner SHENZHEN SCIENCARE MEDICAL INDUSTRIES CO. LTD.
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