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Sirolimus preparation and preparation process thereof

A technology of sirolimus and preparations, which is applied in the field of medicine, can solve the problems of poor solubility of sirolimus, narrow therapeutic window, and large difference in dissolution of solid preparations, and achieve low oral bioavailability, simple prescription, and good operability effect

Active Publication Date: 2012-01-04
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] The object of the invention is to overcome the defects of sirolimus poor solubility, narrow therapeutic window, and large dissolution differences between solid preparations

Method used

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  • Sirolimus preparation and preparation process thereof
  • Sirolimus preparation and preparation process thereof
  • Sirolimus preparation and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Prescription: Sirolimus 2g

[0058] Povidone K30 6g

[0059] Microcrystalline Cellulose 200g

[0060] 95% ethanol 170ml

[0061] Appropriate amount of water

[0062] Makes 1000 pieces

[0063] Preparation Process:

[0064] Take sirolimus and povidone K30, mix well, add 95% ethanol, stir in a water bath at 60°C to dissolve, add this solution into microcrystalline cellulose, stir and granulate, dry in a fluidized bed, measure the moisture 5% or less, then add a concentration of 3% povidone K30 aqueous solution to the dry granules by weight 0.8:1 to make a soft material, extrude with a pore size of 0.6 mm, spheroidize for 1 minute, and dry in a fluidized bed at a speed of 600 rpm. Measure moisture below 3%, get the granule that is thicker than 80 meshes, add 0.5% magnesium stearate. Fill to capsule. That is, sample 1 was obtained.

[0065] The dissolution profile of sample 1 (6 grains) is as follows figure 1 shown. Depend on figure 1 It can be seen that the unif...

Embodiment 2

[0067] Prescription: Sirolimus 2g

[0068] Povidone K30 6g

[0069] Microcrystalline Cellulose 200g

[0070] Cross-linked PVP 10g

[0071] 95% ethanol 170ml

[0072] Appropriate amount of water

[0073] Makes 1000 pieces

[0074] Preparation Process:

[0075] Take sirolimus and povidone K30, mix well, add 95% ethanol, stir in a water bath at 60°C to dissolve, add this solution to microcrystalline cellulose and cross-linked PVP, stir to granulate, and use a fluidized bed Dry, measure the water content below 5%, then add water-based soft material to the dry granules according to the weight of 1:1, extrude with 1mm aperture, spheroidize for 3 minutes, rotate at 800rpm, dry in a fluidized bed, measure the water content below 3%, take For particles coarser than 80 meshes, 0.5% magnesium stearate is added. Fill to capsule. Sample 2 is obtained.

[0076] The dissolution of sample 2 (6 capsules) is as follows figure 2 shown. Depend on figure 2 It can be seen that the uni...

Embodiment 3

[0077] Embodiment 3: in vitro cumulative dissolution comparative test:

[0078] According to CN200810071842.0 embodiment 2, the capsule is sample 3.

[0079] Commercially available product (produced by U.S. Wyeth, batch number: c70282) was purchased as sample 4

[0080] Solid dispersion without sustained release, that is, the preparation intermediate of Example 2 without the extrusion and spheronization process is directly encapsulated, which is sample 5.

[0081] The test method is: according to the dissolution method (Chinese Pharmacopoeia version two appendix XC first method in 2005), with 0.4% sodium lauryl sulfate solution 500ml as the dissolution medium, the rotating speed is 120 revolutions per minute, operated according to the law, after 10 , 20, 30, 45, 60, and 120 minutes of sampling, take 10ml of the solution and filter it, and take the subsequent filtrate as the test solution; take an appropriate amount of sirolimus reference substance, weigh it accurately, dissol...

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Abstract

The invention provides a Sirolimus preparation and a preparation process thereof. The process comprises the following steps: preparing an intermedium by a solid dispersion technology; preparing pellets by an extrusion spheronization process; and finally filling capsules. The preparation and the process of the preparation ensure the high leaching ability of Sirolimus, achieve the aim of slow release, have smaller leaching difference among the capsules and better solve the application limit caused by low bioavailability and narrow therapeutic window of the oral administration of the Sirolimus.

Description

technical field [0001] The invention relates to an oral preparation with sirolimus as an active ingredient, belonging to the technical field of medicine. Background technique [0002] Sirolimus is a kind of lipophilic triene nitrogen-containing macrolide immunosuppressive drug produced by Streptomyceshygroscopicus isolated from the soil samples of Easler Island in the Pacific Ocean by Ayerst et al. in Canada in 1975. It is soluble in methanol, Organic solvents such as ethanol, propanol and chloroform, very slightly soluble in water, almost insoluble in ether. The structural formula of sirolimus is shown in the figure below: [0003] [0004] Figure Structural formula of sirolimus [0005] Sirolimus is an immunosuppressant with antilymphocyte proliferative, antineoplastic and antifungal properties. The drug inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (IL-2, IL-4). Its mechanism of action is completely different from o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K9/48A61P37/06A61P31/10A61K31/436A61K9/52
Inventor 卢良华
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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