Composition and tablet of mifepristone and anorethidrane dipropionate

A technology of anordrin and mifepristone, applied in pill delivery, drug combination, pharmaceutical formulation, etc., can solve the problem of solubilized products of mifepristone and anordrin compound

Active Publication Date: 2005-07-06
武汉九珑人福药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no reports of solubilized products of mifepristone and anordrin compound

Method used

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  • Composition and tablet of mifepristone and anorethidrane dipropionate
  • Composition and tablet of mifepristone and anorethidrane dipropionate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The tablet prescription of this method is (1000 tablets)

[0034] Recipe 1:

[0035] Mifepristone 30g

[0036] Anordrin 5g

[0037] Macrogol 4000 50g

[0038] Lactose 20g

[0039] Starch 400g

[0040] Microcrystalline Cellulose 65g

[0041] Sodium Carboxymethyl Starch 20g

[0042] Talc powder 7g

[0043] Hypromellose (HPMC) 0.2g

[0044] After melting polyethylene glycol 4000, add mifepristone and anordrin, pour it evenly into an appropriate amount of dry ice, solidify, and then grind it into a fine powder with a mill, and evaporate the CO 2 Then add lactose and starch, use HPMC slurry as the binder to granulate, add other ingredients after drying, mix and then compress into tablets to obtain. The dissolution rate is shown in Table 1.

Embodiment 2

[0050] Prescription 2: (1000 tablets)

[0051] Mifepristone 30g

[0052] Anordrin 5g

[0053] β-cyclodextrin 350g

[0054] Starch 10g

[0055] Microcrystalline Cellulose 5g

[0056] Talc powder 4g

[0057] Hypromellose (HPMC) 0.2g

[0058]Process: Dissolve anordrin in 300ml of ethanol, add different amounts of β-cyclodextrin, put it in a grinder and grind it to a paste (note: the ventilation device is placed above), add mifepristone, and take it out after drying , put in a vacuum desiccator to remove the residual solvent, add starch, granulate with HPMC pulp, add microcrystalline cellulose, talcum powder, and tablet. The dissolution rate of this tablet is shown in Table 2.

Embodiment 3

[0064] Prescription 3: (1000 tablets)

[0065] Mifepristone 30g

[0066] Anordrin 5g

[0067] Polyvinylpyrrolidone 50g

[0068] Starch 40g

[0069] Microcrystalline Cellulose 65g

[0070] Sodium carboxymethyl starch 20g

[0071] Talc powder 7g

[0072] Preparation process: dissolve polyvinylpyrrolidone in 100ml ethanol, add anordrin and stir to dissolve, then continue stirring in the fume hood while adding mifepristone, then add microcrystalline cellulose, stir evenly, take out, and dry After being pulverized, it is made into granules, and sodium carboxymethyl starch is added, and the bone stone powder is compressed into tablets and wrapped in double-layer aluminum foil. The in vitro dissolution profile of the tablet is shown in figure 2 .

[0073] from figure 2 Visible 30min dissolution rate anordrin is more than 80%, and mifepristone is about 90%.

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PUM

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Abstract

The invention relates to a composition and tablet of mifepristone and anorethidrane dipropionate, wherein the compound comprises (by weight ratio) Mifepristone 6 parts, anorethidrane dipropionate 1 part. The tablet provided by the invention comprises the compound of Mifepristone and anorethidrane dipropionate and auxiliary solvent, wherein the Mifepristone and anorethidrane dipropionate have rather high dissolving degree.

Description

technical field [0001] The invention relates to a compound and tablet of mifepristone and anordrin. Background technique [0002] Mifepristone, (its chemical name is 11β-[4-(N,N-dimethylamino)phenyl-17β-hydroxy-17α-(1-propynyl)-estro-4,9-di En-3-one] and 2α-17α-diethynyl, A ring anordrostane, 2β, 17β-dihydroxydipropionate (ie anordrin) are two kinds of widely used anti-early pregnancy, Anti-implantation drugs. [0003] The total dose of mifepristone currently used clinically is 150mg, and the effective rate of anti-early pregnancy is 92-94%. If the dosage is reduced, the curative effect will be reduced, but excessive dosage will inevitably cause side effects. [0004] Mifepristone is insoluble in water, but soluble in 0.1m / L hydrochloric acid solution, and anordrin is insoluble in water and acid. Therefore, the dissolution rate of the two substances in water is very low. Obviously, after taking, the curative effect will be affected or the curative effect will be unstable....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/565A61P15/04
Inventor 侯惠民贺芬
Owner 武汉九珑人福药业有限责任公司
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