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Topiramate sustained release preparation pharmaceutical composition

A technology of sustained-release preparations and topiramate, which is applied in the pharmaceutical composition of topiramate sustained-release preparations and its preparation field, can solve the problems of complex preparation process of cyclodextrin inclusion compound, increase the risk of drug degradation, reduce drug degradation, etc., and achieve stable and stable production. Effect of effective blood concentration, reduction of incidence, and reduction of side effects

Inactive Publication Date: 2016-02-17
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN201210162377 uses dry granulation technology to prevent the drug from going through the hot and humid process to reduce drug degradation, but dry granulation requires high equipment and low yield. Repeated platen granulation will also increase the risk of drug degradation
CN201410358987 prepared drug cyclodextrin inclusion compound to reduce drug degradation, but the preparation process of cyclodextrin inclusion compound is complex and the yield is low

Method used

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  • Topiramate sustained release preparation pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-4

[0026] Embodiment 1-4 sustained-release granule prescription:

[0027] Material name effect Example 1(g) Example 2(g) Example 3(g) Example 4(g) Topiramate Main drug 45 45 45 45 microcrystalline cellulose filler 50 50 50 50 hypromellose Adhesive 3 3 3 3 calcium carbonate stabilizer 3 3 3 3 Ethyl cellulose Coating material - 5.73 6.88 8.60 hypromellose Coating porogen - 2.45 2.94 3.68 Diethyl phthalate Coating plasticizer - 1.82 2.18 2.73

[0028] Embodiment 1-4 Sustained-release granule preparation process:

[0029] a. Add the prescription amount of topiramate, filler and stabilizer into the fluidized bed, preheat to 35°C, and then spray the binder hypromellose aqueous solution on the added material through the top spraying process, and granulate.

[0030] b. Sizing the drug-containing granules, collecting 250-550 μm particles and adding them to the fluidized bed, and performing ...

Embodiment 5-6

[0037] Embodiment 5-6 sustained-release granule prescription:

[0038] Material name effect Example 5(g) Example 6(g) Topiramate Main drug 45 45 microcrystalline cellulose filler 50 50 hypromellose Adhesive 3 3 calcium carbonate stabilizer - 1 Ethyl cellulose Coating material 5.73 5.73 hypromellose Coating porogen 2.45 2.45 Diethyl phthalate Coating plasticizer 1.82 1.82

[0039] Embodiment 5-6 Sustained-release granule preparation process:

[0040] a. Add the prescription amount of topiramate, filler, and stabilizer into the fluidized bed, preheat to 35°C, and then spray the binder hypromellose aqueous solution on the added material through the top spraying process, and granulate.

[0041] b. Sizing the drug-containing granules, collecting 250-550 μm particles and adding them to the fluidized bed, and performing slow-release coating on the drug-containing granules through the bottom spraying pro...

Embodiment 2、5、6

[0043] Embodiment 2, 5, 6 Influencing factors 10 days related substance (%) determination result

[0044]

[0045] From the above experimental results, it can be seen that the stabilizer has a protective effect on the sample and prevents the degradation of the drug, and the more the stabilizer is used, the more beneficial it is for the stability of the sample.

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Abstract

The invention relates to a topiramate sustained release preparation pharmaceutical composition and a preparation method thereof. The topiramate sustained release preparation pharmaceutical composition is prepared from sustained release particles and preparation auxiliary materials; and the sustained release particles consist of 35%-45% of topiramate, 40%-50% of filler, 2.5%-6% of adhesives, 2%-10% of stabilizer, 5.0%-6.5% of sustained release coating materials, 2.0%-3.0% of porogen materials and 1%-2% of plasticizer. By the stabilizer, stability of the preparation can be improved obviously, and degradation of medicines is reduced. After a patient orally takes the topiramate sustained release preparation, stable and effective blood concentration can be maintained, occurrence rate of side reaction is reduced, and epilepsy is controlled well. In addition, the patient orally takes the preparation once every day, and compliance of the patient is greatly improved. Granulation is implemented at one step by a fluidized bed, special technologies are not required, and industrial production is facilitated.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a topiramate sustained-release preparation pharmaceutical composition and a preparation method thereof. Background technique [0002] Topiramate is a white crystalline powder with a bitter taste. Soluble in acetone, chloroform, dimethyl sulfoxide and ethanol, very soluble in alkaline solutions with a pH value of 9-10 such as sodium hydroxide or sodium phosphate, very slightly soluble in water (at room temperature), and its solubility is only about 9.8mg / mL, the pH of its saturated solution is 6.3. Melting point of topiramate: 125-126°C. [0003] Topiramate chemical name: 2,3:4,5-bis-O-(1-methylethylene)-β-D fructopyranose sulfamate, molecular formula: C12H21NO8S, molecular weight: 339.36. Its structural formula: [0004] [0005] Topiramate is a new broad-spectrum antiepileptic drug, which is effective for all kinds of epileptic seizures, es...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/22A61K9/16A61K47/38A61K47/02A61K31/7048A61P25/08
CPCA61K9/2054A61K9/0002A61K9/16A61K31/7048A61K47/02A61K47/38
Inventor 于红霞张庭
Owner BEIJING VENTUREPHARM BIOTECH
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