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Ulipristal acetate medicine composition

A technology of unilast acetate and a composition, applied in the field of pharmaceutical preparations, can solve problems such as poor dissolution, and achieve the effects of improving solubility or dissolution, good stability, and excellent pharmaceutical technical characteristics

Inactive Publication Date: 2013-05-08
四川尚锐生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the inventors found that, for the specific compound of uliplast acetate, only micronization is not enough to completely solve the problem of its poor dissolution.

Method used

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  • Ulipristal acetate medicine composition
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  • Ulipristal acetate medicine composition

Examples

Experimental program
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Effect test

Embodiment 1

[0042] The following formulation was used for the preparation of tablets each containing 30 mg of micronized uliplast acetate.

[0043]

[0044] Manufacturing process: Tablets were prepared using standard wet granulation procedures. Sieve and mix micronized uliplast acetate (d90≤5), lactose monohydrate, and hypromellose evenly; use a high-efficiency wet mixing granulator or any other suitable wet granulator, and use purified water The mixed material is granulated; the wet granules are dried in a fluidized bed or an oven; after drying, the granules are sized; the sodium carboxymethyl starch and magnesium stearate are sieved and mixed with the dried granules; The final granules are compressed into tablets.

Embodiment 2

[0046] The following formulation was used for the preparation of tablets containing 10 mg of micronized uliplast acetate each.

[0047]

[0048]

[0049] Manufacturing process: Tablets were prepared using standard direct compression procedures. Sieve and mix micronized uliplast acetate (d90≤5), microcrystalline cellulose, hydroxypropylmethyl cellulose, and sodium carboxymethyl starch; Mix well; use a tablet machine to compress the mixture into tablets.

Embodiment 3-4

[0051] The following formulation is used for the preparation of hard capsules containing 20 mg of micronized uliplast acetate per tablet.

[0052]

[0053]

[0054]Preparation process: Standard wet granulation steps are used to prepare capsule granules. Sieve and mix micronized uliplast acetate (d90≤5 or d90≤10), microcrystalline cellulose, mannitol, hypromellose, and sodium carboxymethyl starch; use a high-efficiency wet mixing granulator or Any other suitable wet granulator, use purified water to granulate the mixed material; wet granules are dried in a fluidized bed or an oven; granulated after drying; sieved and mixed with the dried granules evenly; The capsule filling machine makes the mixed granules into hard capsules.

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Abstract

The invention relates to an ulipristal acetate medicine composition comprising, by weight, 3-10% of ulipristal acetate micro-particles, 70-90% of a diluting agent, 3-6% of a bionding agent, 4-12% of a disintegrant, and 0-2% of a lubricating agent. The particle size D90 of the micro-particles is no higher than 10mum. The diluting agent is selected from lactose, microcrystalline cellulose, mannitol, and mixtures thereof. The bonding agent is hydroxypropyl methylcellulose. The disintegrant is sodium carboxymethyl starch. The lubricating agent is selected from magnesium stearate, silicon dioxide, talc powder, and mixtures thereof. The composition has excellent dissolution profile, good friability, and good homogeneity.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing uliplast acetate. Background technique [0002] Ulipristal acetate, formerly known as CDB-2914, has a chemical structure shown in Formula I below. Uliplast acetate and its preparation methods have been disclosed in US Patent Nos. 4954490, 5073548 and 5929262 and International Patent Applications WO2004 / 065405 and WO2004 / 078709. [0003] [0004] Uliplast acetate is a steroid with known antipregnancy and antiglucocorticoid activity indicated for the prevention of pregnancy after unprotected intercourse or after known or suspected contraceptive failure, uterine fibroids, endometriosis, and Treatment of Cushing's syndrome and glaucoma. [0005] Since uliplast acetate is a poorly soluble drug with poor water solubility, in order to improve solubility, micronized powder is often an option. CN101594875A discloses the method of mic...

Claims

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Application Information

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IPC IPC(8): A61K31/57A61K9/20A61P15/18A61P15/00A61P35/00A61P27/06
Inventor 宋凡叶子峥戴萍彭显峰
Owner 四川尚锐生物医药有限公司
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