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A kind of freeze-dried oral preparation containing ebiprazole and preparation method thereof

An oral preparation, ebiprazole technology, applied in the field of freeze-dried oral preparations containing ebiprazole and its preparation, can solve problems such as blanks, and achieve the goals of avoiding irritation and damage, realizing pregastric absorption, and improving bioavailability Effect

Active Publication Date: 2018-05-22
CHENGDU XINJIE HIGH TECH DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] And the technology of using lyophilization to prepare ebiprazole into oral lyophilized preparations is still in the blank

Method used

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  • A kind of freeze-dried oral preparation containing ebiprazole and preparation method thereof
  • A kind of freeze-dried oral preparation containing ebiprazole and preparation method thereof
  • A kind of freeze-dried oral preparation containing ebiprazole and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] This embodiment provides three kinds of freeze-dried oral preparations containing ebiprazole, and their prescriptions and contents are shown in Table 1 below:

[0042] Table 1

[0043] prescription

1

2

3

Ebiprazole

0.25mg

2.1mg

4mg

Hydroxypropyl-β-cyclodextrin

5mg

15mg

25mg

gelatin

1mg

5.5mg

10mg

Mannitol

2mg

13mg

25mg

aspartame

0.001mg

0.005mg

0.01mg

Anhydrous citric acid

0.1mg

0.395 mg

0.8mg

[0044] In the above prescription, aspartame and anhydrous citric acid can also be used as flavoring agents alone, and the dosage is 0.001~0.81mg. Preferably, aspartame and anhydrous citric acid are selected as flavoring agents at the same time to adjust the sweetness and sourness of the medicine. The above-mentioned D-mannitol is used as a propping agent for the skeleton support of the lyophilized oral preparation, hydroxypropyl-β-cyclodextrin ...

Embodiment 2

[0047] This embodiment provides a method for preparing the lyophilized oral preparation containing ebiprazole described in Example 1, comprising the following steps:

[0048] A. Measure 400ml of purified water into the container, add the prescribed amount of hydroxypropyl beta cyclopaste and stir until clarified; then add ebiprazole in batches, and continue stirring; after the solution is clarified, add in sequence Gelatin, mannitol, aspartame, and anhydrous citric acid were stirred separately until clarified and diluted to 500ml with purified water to obtain a clarified medicinal solution.

[0049] B. Pour the clarified medicinal solution obtained in step A into a cold aluminum foil mold in a 0.5ml single-dose package, use liquid nitrogen (-80°C) spray technology to freeze quickly, and transfer it to a freeze dryer for freeze-drying. The moisture content is <2%, and the lyophilized oral preparation is obtained.

[0050] The above-mentioned freeze-drying includes four stages:...

Embodiment 3

[0054] In order to make the weight of the lyophilized oral preparation lighter, this embodiment optimizes the prescription in Example 1, because hydroxypropyl-β-cyclodextrin can not only be used as a solubilizing excipient, but also as a proppant, Therefore, the use of D-mannitol was canceled. The prescription of this lyophilized oral preparation is shown in Table 2 below:

[0055] Table 2

[0056] prescription

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Abstract

The invention provides a freeze-dried oral preparation containing ebiprazole and a preparation method thereof, belonging to the field of pharmaceutical preparations. The freeze-dried oral preparation includes medicinal dose of ebiprazole and other pharmaceutical auxiliary materials. The preparation method prepares raw materials and auxiliary materials into a freeze-dried oral preparation by adopting a freeze-drying method. The present invention fills the blank of ebiprazole in the technical field of freeze-dried preparations by preparing ebiprazole bulk drug into freeze-dried oral preparations, not only provides clinical patients with a variety of drug dosage forms, but also contains ebiprazole The lyophilized oral formulation of azole can disintegrate quickly, so that the ebiprazole can be quickly dissolved and absorbed by the patient, and the bioavailability is improved; at the same time, the lyophilized oral formulation can be disintegrated in the patient's mouth without water, so that Part of the drug can be absorbed through mucosal transport, thus realizing pregastric absorption, avoiding the stimulation and damage of the drug to the stomach, and improving the compliance of clinical patients.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried oral preparation containing ebiprazole and a preparation method thereof. Background technique [0002] Brexpiprazole (Brexpiprazole) is used as an adjuvant treatment for schizophrenia and major depressive disorder (MDD). Its chemical name is 7-[4-4(4-benzo[b]thiophen-4-yl-piperazine- 1-yl) oxo]-1H-quinolin-2-one, the chemical structure is as follows: [0003] [0004] The compound has been approved for marketing by the U.S. Food and Drug Administration. Its dosage form is an ordinary oral solid tablet, produced by direct compression method, and its specifications are 0.25mg, 0.5mg, 1mg, 2mg, 3mg, 4mg. Inactive prescription excipients used in conventional tablets, such as lactose monohydrate, corn starch, microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate, and gastric-soluble film-coating po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/496A61K47/40A61K47/42A61P25/18A61P25/24
Inventor 蒲洪高红刘晓琳
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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