Topiramate dry suspension as well as preparation method and application thereof

A technology of dry suspension and topiramate, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Problems such as low drug loading capacity of the resin

Active Publication Date: 2020-11-10
SHANGHAI AUCTA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor has tried and found that the drug-loading capacity of the ion-exchange resin is not high. After mixing with topiramate, the free topiramate drug is absorbed, and the ion-loaded resin can hardly be loaded with drug. Therefore, the applicability of the slow-release resin dry suspension is not strong.
[0010] In addition, when topiramate is prepared for dry suspension, during use, in the process of dissolving with water, i

Method used

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  • Topiramate dry suspension as well as preparation method and application thereof
  • Topiramate dry suspension as well as preparation method and application thereof
  • Topiramate dry suspension as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Table 8 Preparation of taste-masked pellets

[0093] components mg / bag Topiramate (Aurobindo, content = 99%) 100 Microcrystalline Cellulose Core (Asahi Kasei, CP102) 500 Talc powder (Merck, 108070) 50 Cellulose acetate (Colorcon, Opadry CA) 270 Povidone (Basf, PVP K30) 90

[0094] The specific steps are:

[0095] Take the topiramate bulk drug and all auxiliary materials of prescription quantity. Add absolute ethanol to a suitable container. Add the prescribed amount of topiramate and mix the resulting mixture until the topiramate is completely dissolved. The prescribed amount of talc was added and the resulting mixture was mixed for at least 15 minutes to obtain a topiramate suspension.

[0096] The prescribed amount of microcrystalline cellulose spheres was added to the fluidized bed equipped with a Wurster column. Fluidize the microcrystalline cellulose balls, and spray the full amount of topiramate suspension through t...

Embodiment 2

[0112] The topiramate dry suspension obtained in Example 1 is packed in a composite film bag. Place it under accelerated conditions of 40°C and 60% RH for 3 months to investigate the stability. All tests met the limit requirements, and the results are shown in the table below:

[0113] Table 13 Topiramate dry suspension stability investigation

[0114]

Embodiment 3

[0116]Take topiramate taste-masking pellets, suspending components, and silicon dioxide in Example 1, mix them in the hopper according to the following table, and mix for 10 minutes to prepare topiramate dry suspension.

[0117] The preparation of table 14 topiramate dry suspension

[0118] components mg / bag Topiramate taste masked pellets 1010 Suspending component 215 Silica (Evonik, Aerosil 200) 10

[0119] The topiramate dry suspension is packed in a composite film bag. Place it under accelerated conditions of 40°C and 60% RH for 3 months to investigate the stability. All tests met the limit requirements, and the results are shown in the table below:

[0120] Table 15 Stability investigation of microcrystalline cellulose-free topiramate dry suspension

[0121]

[0122] Without microcrystalline cellulose, the content of the suspension is obviously low, but the stability of this product is good after the addition of microcrystalline cell...

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Abstract

The invention relates to a topiramate dry suspension. The topiramate dry suspension is prepared by multi-stage mixing granulation, and comprises topiramate, an inert carrier, a disintegrating agent, ataste masking coating, a pore-foaming agent, a filling agent and a suspending aid, wherein the topiramate, the inert carrier, the disintegrating agent and the taste masking coating form taste maskingparticles, so that the bitter taste of topiramate can be effectively solved. The topiramate dry suspension at least comprises two filling agents which have the functions of forming a suspending aid component and reducing the wall adhesion condition of the dry suspension, and the topiramate dry suspension is found to be convenient to prepare for the first time, improves the compliance and administration accuracy of patients and is suitable for industrial production.

Description

technical field [0001] The invention relates to a topiramate dry suspension, a preparation method and an application thereof, belonging to the field of biological and pharmaceutical preparations. [0002] technical background [0003] The trade name of quick-release topiramate in the U.S. is Topamax, which is the product of U.S. Johnson & Johnson (Janssen pharms). It mainly treats epilepsy in children and adults. [0004] Currently, the U.S. Food and Drug Administration has approved two different dosage forms of Topamax, which are ordinary tablets and capsules. There is no topiramate liquid preparation on the market, so hospitals often need to crush topiramate tablets to prepare liquid reagents when using it, which is convenient for children and patients with dysphagia. [0005] Current characteristics and clinical needs of topiramate: [0006] Topiramate is poorly soluble in water, and the solubility in water at room temperature is only about 9.8 mg / ml. When the pulveriz...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/38A61K31/7048A61P25/08
CPCA61K9/5042A61K9/5078A61K31/7048A61K47/38A61P25/08
Inventor 李守峰李朋朋王勇
Owner SHANGHAI AUCTA PHARMA CO LTD
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