Composition containing water-insoluble high-activity drug and preparation method thereof

A composition and high-activity technology, applied in the field of medicine, can solve problems such as uneven mixing, and achieve the effects of good drug dissolution, simple process, oral absorption and high bioavailability

Active Publication Date: 2009-09-23
HANGZHOU ZHONGMEI HUADONG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the ratio of drug to excipients is quite different, the traditional fluidized bed preparation method can easily lead to uneven mixing

Method used

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  • Composition containing water-insoluble high-activity drug and preparation method thereof
  • Composition containing water-insoluble high-activity drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: Capsules and tablets with FK506 as active ingredient

[0030] FK506 1g

[0031] HPMC 1g

[0032] Lactose 63g

[0033] Dissolve FK506 in 10mL ethanol, add HPMC to fully disperse, add 15mL dichloromethane to dissolve it. Spray the above solution evenly on the surface of the lactose granules in the fluidized bed, the blast pressure is 0.1MPa, the spraying speed is 1mL / min, the spraying pressure is 0.05MPa, and the material is dried for 5min after the drug application is completed.

[0034] The prepared composition can be added with 66.5g of starch, 7g of croscarmellose sodium and 1.5g of magnesium stearate, mixed evenly and filled into No. 4 capsules to make capsules with a marked amount of 1mg, namely the sample 1.

[0035] The prepared composition can be added with 160g of compressible starch, 60g of microcrystalline cellulose, 14g of croscarmellose sodium and 1g of magnesium stearate, mixed evenly and pressed into tablets, the tablet weight is 300mg, a...

Embodiment 2

[0036] Embodiment 2: Capsules, tablets, dry suspensions with FK506 as active ingredient

[0037] FK506 1g

[0038] PVP 0.5g

[0039] HPMC 1.5g

[0040]Cane sugar core 62g

[0041] Dissolve FK506 in 12mL methanol, add PVP to fully dissolve, then add HPMC to fully disperse, add 18mL chloroform to dissolve. Spray the above solution evenly on the surface of the sucrose pellets in the fluidized bed, the blast pressure is 0.15MPa, the spraying speed is 1mL / min, the spraying pressure is 0.05MPa, and the material is dried for 5min after the drug application is completed.

[0042] The prepared composition can be added with 75g blank ball core, mixed evenly and filled into No. 4 capsules to make capsules with a marked amount of 1 mg, i.e. sample 2.

[0043] The prepared composition can be added with 235g of blank ball cores, mixed evenly, and pressed into tablets with a tablet weight of 300mg and a marked amount of 1mg.

[0044] The prepared composition can be added with 75g of bla...

Embodiment 3

[0045] Embodiment 3: Capsules, tablets, dry suspensions with FK506 as active ingredient

[0046] FK506 1g

[0047] HPC 5g

[0048] Eudragit 2g

[0049] Microcrystalline Cellulose Ball Core 57g

[0050] Dissolve FK506 in 25mL ethanol, add HPC and Eudragit to fully dissolve. Spray the above solution evenly on the surface of the microcrystalline cellulose pellet core in the fluidized bed, the blast pressure is 0.15MPa, the liquid spray speed is 1mL / min, the liquid spray pressure is 0.05MPa, and the material is dried for 5min after the drug application is completed.

[0051] The prepared composition can be added with 75g blank ball core, mixed evenly and filled into No. 4 capsules to make capsules with a marked amount of 1 mg, i.e. sample 3.

[0052] The prepared composition can be added with 235g of blank ball cores, mixed evenly, and pressed into tablets with a tablet weight of 300mg and a marked amount of 1mg.

[0053] The prepared composition can be added with 75g of blan...

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Abstract

The invention discloses a composition containing a water-insoluble high-activity drug and a preparation method thereof. The water-insoluble high-activity drug is dissolved in an organic solvent containing a solid dispersion carrier, evenly sprayed on the surface of filler or blank pellets by adopting a fluidized bed and dried. The invention realizes the one-step completion of preparing the solid dispersion of the water-insoluble high-activity drug, pelleting and drying, has simple and convenient process, and no dust pollution, and effectively avoids the adverse influence of the high-activity drug on the health of production staff. The granules prepared by the method has even granularity, and good liquidity and compression formability, and can be further prepared into oral solid preparation. The composition prepared by the method has good drug dissolvability, and high oral absorption and bioavailability.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically describes a composition containing water-insoluble high-activity medicine and a preparation method thereof. technical background [0002] Poorly water-soluble and highly active drugs refer to drugs with low solubility in water but high biological activity. Solubility is a physical property of a drug. If 1g of a drug cannot be completely dissolved in 10,000ml of water, it is considered a poorly water-soluble drug. Highly active drugs have high biological activity and can produce strong pharmacological effects in small doses. [0003] For example, tacrolimus (English name: Tacrolimus), also known as FK506, has a solubility in water of about 1-2 μg / ml, and an oral dose of 0.1-0.3 mg / kg / day. Tacrolimus is a macrolide antibiotic with strong immunosuppressive activity. It is clinically used in rejection and autoimmune diseases after organ transplantation, and its efficacy is 10 to 1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/34A61K47/32A61K9/14A61K9/20A61K9/48A61K31/436A61K31/4196A61K31/454A61P35/00A61K47/10A61K47/14
Inventor 韩敏龚翼飞姚忠立
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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