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Brexpiprazole-containing freeze-dried oral preparation and preparation method thereof

A technology for oral preparation and epipiprazole, which is applied in the field of freeze-dried oral preparation containing epipiprazole and its preparation, can solve problems such as blank, and achieve the effects of low water content, improved bioavailability and light weight

Active Publication Date: 2015-12-02
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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  • Brexpiprazole-containing freeze-dried oral preparation and preparation method thereof
  • Brexpiprazole-containing freeze-dried oral preparation and preparation method thereof
  • Brexpiprazole-containing freeze-dried oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] This example provides three kinds of freeze-dried oral preparations containing ebiprazole, and their prescriptions and contents are shown in Table 1 below.

[0043]

[0044] Table 1

[0045] It is easy to understand that the above-mentioned excipients of the freeze-dried preparation can also be replaced by other similar excipients, and the dosage of each excipient should be adjusted accordingly according to the actual usage, so as to meet the medicinal dosage requirements of the excipients.

[0046]In the above prescription, aspartame or anhydrous citric acid can also be used alone as a flavoring agent, and the dosage is 0.001-0.81 mg. Preferably, aspartame and anhydrous citric acid are used as flavoring agents at the same time to adjust sweetness and sourness.

Embodiment 2

[0048] This embodiment provides a method for preparing the lyophilized oral preparation containing ebiprazole described in Example 1, comprising the following steps:

[0049] A. Measure 1400ml of purified water into a container, add the prescribed amount of D-mannitol, aspartame and anhydrous citric acid, stir to dissolve and then add medicinal gelatin; after the medicinal gelatin is stirred and dissolved, add The pulverized ebiprazole raw material is stirred to form a suspension solution, and water is added to the prescribed amount according to the weight of the dosing solution, and then fully sheared and stirred, and stirred for more than 30 minutes to obtain a stable suspension solution.

[0050] B. Pour the stable suspension solution in step A into a cold aluminum foil model in a 0.3ml single-dose package, use liquid nitrogen (-80°C) spray technology to freeze quickly, and transfer it to a freeze dryer for sublimation drying. Drying and constant temperature drying, so that...

Embodiment 3

[0057] This embodiment evaluates the quality of three lyophilized oral preparations containing ebiprazole in Example 1, including:

[0058] (1) Evaluation of disintegration: put the product on a glass plane, add 1 drop of water (about 0.02ml) to the surface of the product at a distance of 0.5cm from the tablet and time it accurately; it is required to measure 10 tablets, and the standard limit of disintegration time for each tablet For no more than 10 seconds.

[0059] (2) Taste evaluation: 10 volunteers evaluated the taste, put the product on the tip of their tongues, observed the disintegration situation and recorded the time, whether there is a sandy feeling after complete disintegration, whether the sweet and sour taste is good, etc.

[0060] (3) Character evaluation: The surface of the product is required to be smooth; the packaging is completely stripped of the film.

[0061] (4) Moisture evaluation: The Fischer method is used to measure the moisture, and the moisture c...

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Abstract

The invention provides a brexpiprazole-containing freeze-dried oral preparation and a preparation method thereof and belongs to the field of medicinal preparations. The freeze-dried oral preparation comprises brexpiprazole and pharmaceutic adjuvants in medical dosage. The preparation method for the freeze-dried oral preparation comprises the step that raw materials and auxiliary materials are used to prepare the freeze-dried oral preparation through a freeze-drying method. According to the invention, since brexpiprazole crude drug is used to prepare the freeze-dried oral preparation, the blank of brexpiprazole in the technical filed of freeze-dried preparations is filled, diverse selection of dosage forms is provided for clinical patients, and in addition, the brexpiprazole-containing freeze-dried oral preparation can be rapidly disintegrated, therefore, brexpiprazole is dissolved out quickly and quickly absorbed by patients, and bioavailability is improved; meanwhile, the freeze-dried oral preparation can be disintegrated in the mouth of the patient without water, so that partial medicines can be transferred through the mucous membrane and then absorbed, therefore, the partial medicines are absorbed before reaching the stomach, the medicine is prevented from stimulating and damaging the intestines and stomach and clinical patient compliance is improved.

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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IPC IPC(8): A61K9/19A61K31/496A61K47/40A61K47/42A61P25/18A61P25/24
Inventor 蒲洪高红刘晓琳许娟
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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