Ulipristal acetate dispersible tablet and preparation method thereof

A technology of uliplast acetate and dispersible tablets, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., which can solve the problem of low dissolution rate and bioavailability, which affects the effect of emergency contraception and other issues to achieve the effect of promoting dissolution

Inactive Publication Date: 2013-01-16
CHINA RESOURCES ZIZHU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problems in the prior art that the dissolution rate and bioavailability of uliplast acetate tablets are low and affect the effect of emergency contraception, the present invention provides a method that can make uliplast acetate take effect quickly in the body, making emergency contraception more effective, Uliplast Acetate Dispersible Tablets with Wider Applicability

Method used

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  • Ulipristal acetate dispersible tablet and preparation method thereof
  • Ulipristal acetate dispersible tablet and preparation method thereof
  • Ulipristal acetate dispersible tablet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029]

[0030] 1) Low-substituted hydroxypropyl cellulose is passed through a 200-mesh sieve, and its fine powder is mixed with 70%-90% of Uliplast acetate whose particles are less than or equal to 50 microns for 10 minutes to obtain Ulipast acetate and low-substituted Premix of hydroxypropyl cellulose;

[0031] 2) The premix is ​​mixed evenly with lactose and microcrystalline cellulose in a granulator;

[0032] 3) adding an appropriate amount of 5% hydroxypropylmethylcellulose to make granules, drying at 40°C, sizing the granules, adding magnesium stearate, mixing evenly, and tableting to obtain 1000 tablets.

[0033] According to the Chinese Pharmacopoeia 2010 edition appendix IA method check dispersion uniformity, the result meets the requirements.

Embodiment 2

[0035]

[0036] 1) Mix 70%-90% of uliplast acetate with particles less than or equal to 50 microns and Polyplasdone XL-10 (<74 μm) in a granulator for 5 minutes to obtain uliplast acetate and Premix of crospovidone;

[0037] 2) Mix evenly with the mannitol and microcrystalline cellulose of prescription quantity again;

[0038] 3) adding an appropriate amount of 10% ethanol solution of povidone K30 to make granules, drying at 40-50° C., sizing the granules, adding the prescribed amount of magnesium stearate, mixing evenly, and tableting to obtain 1000 tablets.

[0039] According to the Chinese Pharmacopoeia 2010 edition appendix IA method check dispersion uniformity, the result meets the requirements.

Embodiment 3

[0041]

[0042] 1) First, put 70%-90% of uliplast acetate whose particles are less than or equal to 20 microns and the prescribed amount of crospovidone Kollidon Cl-M (<15 μm accounts for more than 90%) in a granulator and stir and mix for 5 Minutes to obtain the premixed material of uliplast acetate and crospovidone;

[0043] 2) Add the prescribed amount of lactose and microcrystalline cellulose to the premix and mix for 5 minutes;

[0044] 3) Then add an appropriate amount of 5% hydroxypropylmethylcellulose aqueous solution to make granules, dry at 50-60° C., after sizing, add magnesium stearate to mix, and compress into tablets to obtain 10,000 tablets.

[0045] According to the Chinese Pharmacopoeia 2010 edition appendix IA method check dispersion uniformity, the result meets the requirements.

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Abstract

The invention relates to a ulipristal acetate preparation and a preparation method thereof, and particularly relates to a ulipristal acetate dispersible tablet with improved dissolution rate and a preparation method thereof. In order to solve the problem that the ulipristal acetate tablet in the prior art is low in dissolution rate and bioavailability and affects emergency contraception effects, the invention provides the ulipristal acetate dispersible tablet. The ulipristal acetate dispersible tablet is prepared from a premix compound of ulipristal acetate and a disintegrating agent and a excipient, wherein the content of ulipristal acetate is 1-30%(w/w) and accounts for 50-80% of the total weight of the premix compound, the particle sizes of 70-100% ulipristal acetate and the disintegrating agent are less than or equal to 75 micrometers. The ulipristal acetate dispersible tablet disclosed by the invention can take effect quickly in vivo, can realize more effective emergency contraception effect, and is wider in application range.

Description

technical field [0001] The invention relates to a preparation of uliplast acetate and a preparation method thereof, in particular to a dispersible tablet of uliplast acetate with improved dissolution rate and a preparation method thereof. Background technique [0002] Ulipristal acetate, also known as: ulipristal acetate, the chemical name is 17α-acetoxy-11β-[4-(N,N-dimethylamino)-phenyl]-19- Norpregna-4,9-diene-3,20-dione is a steroidal antiprogestin. It can be used for emergency contraception within 120 hours of unprotected sexual intercourse or contraceptive failure, low doses are taken daily for routine contraception, and can also be used for the treatment of uterine fibroids. The currently marketed product ella (30 mg uliplast acetate tablet) is used for emergency contraception, and CN200980149309 discloses uliplast acetate tablet, which is micronized. However, due to the relatively poor water solubility of uliplast acetate, the dissolution rate of ordinary tablets ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/56A61K47/38A61K47/36A61P15/18A61P15/00A61P35/00
Inventor 章俊麟邵正飞赵红欣贺颖
Owner CHINA RESOURCES ZIZHU PHARMA
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