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A kind of paliperidone oral fast-dissolving film preparation and its preparation process

A technology of paliperidone and fast-dissolving film, which is applied in the field of paliperidone oral fast-dissolving film preparation and its preparation, and can solve the problem of no paliperidone oral fast-dissolving film, no drug product and research and development, and uneven drug dispersion To achieve the effect of improving drug compliance, reducing serious side effects, and facilitating drug administration

Active Publication Date: 2021-04-09
广州迈凯安生物医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most of the commonly used film-forming materials are water-swellable polymer materials. The dissolution properties of these materials are slightly poor, and other film-forming polymer materials are needed to achieve satisfactory results, which makes the composition of the formula more complicated.
[0005] At present, no literature reports on paliperidone oral instant film have been found, and domestic pharmaceutical companies have no related drug products and research and development
However, the formula and method of instant film preparations of other drugs are not suitable for the production of paliperidone.
For example, the Chinese patent "Methylphenidate Hydrochloride Instant Film and Its Preparation Method" with the application number CN 201510119169.3, because the original drug methylphenidate hydrochloride is soluble, the requirements for film-forming materials are not high, if its formula is applied mechanically On paliperidone, the drug film may not be extensible, brittle, and the drug may be dispersed unevenly.

Method used

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  • A kind of paliperidone oral fast-dissolving film preparation and its preparation process
  • A kind of paliperidone oral fast-dissolving film preparation and its preparation process
  • A kind of paliperidone oral fast-dissolving film preparation and its preparation process

Examples

Experimental program
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Effect test

Embodiment 1

[0027] An oral fast-dissolving film preparation of paliperidone, the formula of which is shown in Table 1.

[0028] The formula of table 1 embodiment 1 paliperidone oral fast-dissolving film preparation

[0029] Paliperidone 3g Polyvinyl alcohol 5-88 7g Polyvinyl alcohol 17-88 4g glycerin 4g Polysorbate 80 0.2g Sucralose 0.2g purified water 81.6g

[0030] Preparation Process:

[0031] a. Dissolve polyvinyl alcohol 5-88 and polyvinyl alcohol 17-88 in purified water at 50-60°C, add sucralose, polysorbate 80, and glycerin and stir to dissolve, add paliperidone while stirring, and use a homogenizer Homogenize at 6000 rpm for 5 minutes, let stand to remove air bubbles, and obtain coating solution;

[0032] b. The coating solution is coated on the board, and dried at 50°C to obtain a drug film;

[0033] c. The drug film is cut to obtain a paliperidone instant film with an area of ​​1×1 cm, and each film contains 3 mg of paliperido...

Embodiment 2

[0036] An oral fast-dissolving film preparation of paliperidone, the formula of which is shown in Table 2.

[0037] The formula of table 2 embodiment 2 paliperidone oral fast-dissolving film preparation

[0038] Paliperidone 2g Polyvinyl alcohol 5-88 7g Polyvinyl alcohol 17-88 4g glycerin 4g Polysorbate 80 0.2g Sucralose 0.1g purified water 82.7g

[0039] Preparation Process:

[0040] a. Dissolve polyvinyl alcohol 5-88 and polyvinyl alcohol 17-88 in purified water at 50-60°C, add sucralose, polysorbate 80, and glycerin and stir to dissolve, add paliperidone while stirring, and use a homogenizer Homogenize at 6000 rpm for 5 minutes, let stand to remove air bubbles, and obtain coating solution;

[0041] b. The coating solution is coated on the board, and dried at 50°C to obtain a drug film;

[0042] c. The drug film is cut to obtain a paliperidone instant film with an area of ​​1×1 cm, and each film contains 2 mg of paliperido...

Embodiment 3

[0045] An oral fast-dissolving film preparation of paliperidone, the formula of which is shown in Table 3.

[0046] The formula of table 3 embodiment 3 paliperidone oral fast-dissolving film preparation

[0047]

[0048]

[0049] Preparation Process:

[0050] a. Dissolve polyvinyl alcohol 5-88 and polyvinyl alcohol 17-88 in purified water at 50-60°C, add sucralose, polysorbate 80, and glycerin and stir to dissolve, add paliperidone while stirring, and use a homogenizer Homogenize at 6000 rpm for 5 minutes, let stand to remove air bubbles, and obtain coating solution;

[0051] b. The coating solution is coated on the board, and dried at 50°C to obtain a drug film;

[0052] c. The drug film is cut to obtain a paliperidone instant film with an area of ​​1×1 cm, and each film contains 1 mg of paliperidone.

[0053] The paliperidone instant film prepared by the formula has uniform color, dissolves rapidly in the mouth, and has good taste.

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Abstract

The invention discloses an oral fast-dissolving film preparation of paliperidone and a preparation process thereof, belonging to the field of pharmacy. The intermediate coating liquid of the paliperidone oral instant film comprises the following components: paliperidone, polyvinyl alcohol, purified water, polysorbate 80, glycerin, and sweetener. The present invention adopts polyvinyl alcohol 5-88 and polyvinyl alcohol 17-88 as a film-forming agent, which can well promote the dissolution of water-insoluble paliperidone in water. The film forming agent is compounded with the plasticizer glycerin to obtain a film agent with good flexibility, good dispersibility and gloss. Further adding polysorbate 80 can disperse paliperidone well, and obtain a film product with uniform drug dispersion; moreover, the film will not stick to the plate after drying. The invention discloses the paliperidone product obtained in the form of an oral instant-dissolving film for the first time, which is the first in the market. It can improve the medication compliance of patients with schizophrenia and reduce the serious side effects caused by patients biting off the tablets.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to an oral instant film preparation of paliperidone and a preparation process thereof. Background technique [0002] Paliperidone, whose chemical name is 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy- 2-Methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one is clinically used to treat schizophrenia and schizoaffective disorder. Launched in the United States in 2006, Paliperidone Sustained-release Tablets currently on the market in China are suitable for the treatment of acute schizophrenia. Ruida is a sustained-release tablet based on the principle of osmotic pump drug release. The production process is complicated and the price is relatively high. Patients with schizophrenia in the acute stage have relatively poor insight. Under the influence of delusions and hallucinations, many patients think that they are not sick, and they have more resistance to tak...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/519A61K47/32A61K47/10A61K47/26A61P25/18
CPCA61K9/006A61K9/7007A61K31/519A61K47/10A61K47/26A61K47/32
Inventor 张欣黄和意江文敏柳莹陶艳陈敏
Owner 广州迈凯安生物医药研究院有限公司