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Tacrolimus sustained-release preparation and preparation method thereof

A technology of tacrolimus and controlled-release preparations, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, and medical preparations containing active ingredients. Predict and increase drug solubility and other issues to achieve the effects of reducing the incidence of adverse reactions, improving bioavailability, and improving solubility

Inactive Publication Date: 2010-03-10
宋洪涛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The object of the present invention is to provide a tacrolimus sustained and controlled release preparation and its preparation method, which solves the shortcomings of the tacrolimus prepared by the prior art method, which are difficult to control the dosage, the dissolution rate is often difficult to predict, and the bioavailability is very low. Among them, the tacrolimus intermediate can increase the solubility of the drug. The tacrolimus sustained and controlled release preparation has a good sustained and controlled release effect, thereby maintaining a stable blood drug concentration, reducing the incidence of adverse reactions, and improving the safety of clinical medication. properties, and the raw materials are easy to obtain, the preparation process is simple and feasible, the yield is high, the cost is low, and industrialized large-scale production can be realized, with significant economic benefits

Method used

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  • Tacrolimus sustained-release preparation and preparation method thereof
  • Tacrolimus sustained-release preparation and preparation method thereof
  • Tacrolimus sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Preparation of Tacrolimus Hydrophilic Gel Matrix Tablets

[0076] Tacrolimus

1g

Hydroxypropyl-β-cyclodextrin

20g

Hydroxypropyl Methyl Cellulose K4M

50g

microcrystalline cellulose

92g

lactose

3.3g

Magnesium stearate

0.8g

A total of 1000 pieces

[0077] Preparation Process:

[0078] After dissolving tacrolimus and hydroxypropyl-β-cyclodextrin with an appropriate amount of absolute ethanol, after ultrasonicating in an ultrasonic instrument for 20 minutes, transfer it to a rotary evaporator to evaporate the solvent to dryness at a temperature of 30-40°C, and precipitate Put the product in a vacuum drying oven at 25-40°C for 24 hours, take it out, grind it, pass through an 80-mesh sieve, and mix it with hydroxypropyl methylcellulose K4M, microcrystalline cellulose, lactose, and magnesium stearate in equal amounts Evenly, the powder is directly compressed ...

Embodiment 2

[0080] Example 2 Preparation of Tacrolimus Film Controlled Release Tablets

[0081]

[0082]

[0083] Preparation Process:

[0084] Dissolve tacrolimus in an appropriate amount of ethanol solution, heat polyethylene glycol 6000 in a water bath at 60-70°C until it melts, mix well, stir vigorously, and pour the melt on a stainless steel plate to form a thin layer, making Cool it quickly into a solid, then place the solid in a vacuum oven at 25-40°C for 24 hours, take it out, add a small amount of micropowder silica gel to grind (micropowder silica gel as a lubricant can reduce the loss of solid dispersion during the grinding process), and pass After an 80-mesh sieve, mix it with lactose evenly, add an appropriate amount of 1% polyoxyethylene pyrrolidone aqueous solution, make a soft material, granulate, dry, sieve, granulate, add magnesium stearate, mix evenly, and compress into tablets. The above-mentioned coating material is used for coating, and the release degree is c...

Embodiment 3

[0086] Example 3 Preparation of Tacrolimus Osmotic Pump Tablets

[0087] Chip

Tacrolimus

1g

Hydroxypropyl-β-cyclodextrin

15g

polyoxyethylene

28g

Sodium chloride

72g

Magnesium stearate

0.7g

Coating material

Cellulose acetate

12g

polyethylene glycol 400

1.5g

Acetone:water (100:1, v:v)

Appropriate amount

A total of 1000 pieces

[0088] Preparation Process:

[0089] After dissolving tacrolimus and hydroxypropyl-β-cyclodextrin with an appropriate amount of absolute ethanol, after ultrasonicating in an ultrasonic instrument for 20 minutes, transfer it to a rotary evaporator to evaporate the solvent to dryness at a temperature of 30-40°C, and precipitate Put the product in a vacuum oven at 25-40°C for 24 hours, take it out, grind it, pass through an 80-mesh sieve, mix it with polyoxyethylene, sodium chloride, and magnesium ste...

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Abstract

The invention provides a tacrolimus sustained-release preparation and a preparation method thereof. The invention adopts a solid dispersion technology, or cyclodextrin inclusion technology or a solubilizing method for micronizing drugs and then adding one or more types of surfactants and the like, and obviously improves solubility thereof so as to improve the bioavailability thereof, then adds oneor more types of skeleton materials and other auxiliary materials so as to prepare a skeleton type sustained-release preparation, or adopts a sustained-release material to carry out coating so as toprepare a diaphragm-controlled type or osmotic pump type sustained-release preparation. The tacrolimus sustained-release preparation has better solubility and dissolution rate, high bioavailability and sustained-controlled-release effect, thus maintaining stable blood and drug concentration, reducing the occurrence rate of adverse reaction, and improving clinical drug safety; in addition, the invention has easy obtaining for materials, simple and feasible preparation technique, high yield and low cost, can realize large-scale industrialized production and has obviously economical benefit.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a tacrolimus sustained and controlled release preparation and a preparation method thereof. Background technique [0002] Tacrolimus (Tacrolimus, FK506) is a new type of potent immunosuppressant, its immunosuppressive effect is 10-100 times that of cyclosporine A, and it is mainly used clinically to prevent and treat immune rejection after organ transplantation, especially As the first-line drug for liver and kidney transplantation, it has been marketed in 14 countries including Japan and the United States, with remarkable curative effect. Although tacrolimus has fewer adverse reactions than cyclosporine, the therapeutic index of tacrolimus is narrow and individual differences are large, and there are still some serious adverse reactions in clinical practice, the most important of which are nephrotoxicity, neurotoxicity, high Blood pressure, diabetes, etc., and the incid...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K9/32A61K9/36A61K9/16A61K47/12A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61K47/48A61K31/439A61P37/06
Inventor 宋洪涛王娟何仲贵唐星张晶周欣
Owner 宋洪涛
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