Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition

A slow-release drug, topiramate technology, applied in the field of medicine and chemical industry, can solve the problems of affecting the dissolution state of the main drug, increasing the compatibility reaction of topiramate, and high production costs

Active Publication Date: 2012-07-18
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] CN1988889A discloses a slow-release topiramate preparation prepared by secondary particles. First, the solid dispersion particles of topiramate are prepared by melting method, and then the slow-release material and the above-mentioned solid dispersion particles are selected to prepare topiramate by one-step granulation or wet granulation technology. Slow-release granules, high production cost and complex process
[0013] Yet above prepared sustained-release or controlled-release topiramate small beads (or micropills), in its preparation topiramate drug-loaded pellet core (or being referred to as topiramate drug-loaded matrix core) technology, all used binding agent, as HPMC or MC et al. have increased the possibility of a compatibility reaction with the main drug topiramate. At the same time, the existence of the binder will affect the dissolution state of the main drug, causing fluctuations in the release rate and thus affecting the controlled release effect of the preparation. During the drug loading process, if the solution contains a binder, it will increase the adhesion of the pellets and reduce the yield

Method used

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  • Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition
  • Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition
  • Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Example 1: Comparison of drug-coating of drug-containing solutions with and without binder

[0072] prescription:

[0073]

[0074] Preparation:

[0075] Weigh 4 parts of 230g topiramate raw materials, add an appropriate amount of 50% ethanol respectively, stir and dissolve under heating at 40°C-50°C; then weigh 6.9g each of HPMC (E 5), PVP K30, and HPC, and add the first In the solution of 1, 2, and 3 parts, the fourth part does not add adhesive, stir and dissolve under heating at 40°C-50°C, add 50% ethanol to 1150ml, that is, the solution containing different adhesives is obtained. Drug-containing coating solution.

[0076] Weigh 500g sucrose ball cores (710-850μm), place them in a fluidized bed bottom spray coating pan, set the air inlet temperature to 55°C (keep the temperature in the pot at 40±2°C); the air inlet pressure is 0.35bar ; The atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjusted at any time according to the fluidization state). ...

Embodiment 2

[0080] Example 2: Drug-coating results of drug-containing coating solutions with different solvents

[0081] Weigh 4 parts of 230g topiramate raw materials, add an appropriate amount of 50% ethanol, 70% ethanol, 95% ethanol, and anhydrous ethanol, stir and dissolve under heating at 40°C-50°C, and add the corresponding solvent to 1150ml, That is, a drug-containing coating solution with different solvents as a solvent.

[0082] Weigh 500g sucrose ball cores (710-850μm), place them in a fluidized bed bottom spray coating pan, set the air inlet temperature to 55°C (keep the temperature in the pot at 40±2°C); the air inlet pressure is 0.35bar ; The atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjusted at any time according to the fluidization state). When the sucrose pellet core is in a fluidized state, the drug-containing coating solution using different solvents as a solvent is sprayed on the surface of the blank pellet core by bottom spraying. The drug-loaded...

Embodiment 3

[0085] Example 3: Comparison of release degrees of topiramate sustained-release pellets with blank pellet cores of different particle sizes

[0086] prescription

[0087] 1) Prescription of drug-loaded pellets:

[0088]

[0089] 2) Sustained release coating layer formulation:

[0090]

[0091] Preparation:

[0092] (1) Weigh 230g of topiramate raw materials, add an appropriate amount of 50% ethanol, stir under heating at 40°C-50°C, dissolve, and add 50% ethanol to 1150ml to obtain a drug-containing coating solution.

[0093] Weigh 500g each of 300μm-400μm, 500μm-610μm, 710μm-850μm sucrose pellet cores, place them in a fluidized bed bottom spray coating pot, set the air inlet temperature to 55°C (keep the temperature in the pot at 40±2°C) ); the air inlet pressure is 0.35bar; the atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjusted at any time according to the fluidization state). When the sucrose pellet core is in a fluidized state, the drug-contai...

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Abstract

The invention belongs to the field of pharmaceutical chemicals, and relates to a Topiramate sustained-release drug composition, a method for preparing the same and an application of the Topiramate sustained-release drug composition. Specifically, the drug layer of the Topiramate sustained-release drug composition does not contain a bonding agent. Concretely, the Topiramate sustained-release drug composition is a sustained-release pellet. The Topiramate sustained-release drug composition has the advantages of good sustained-release effect, strong controllability, high stability, good repeatability, simple prescription, easiness in operation and preparation and the like.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a sustained-release pharmaceutical composition of topiramate, a preparation method and application thereof. Specifically, the topiramate sustained-release pharmaceutical composition is sustained-release pellets. Background technique [0002] Topiramate (2,3,4,5-bis-0-(1-methylethylene)-β-D-fructopyranosulfamate) (as shown in Formula 1 below), is A broad-spectrum neurotherapeutic, approved by the FDA in 1995, has been used clinically for many years for the treatment of certain seizure disorders and the prevention of migraine (E. Faught et al. (1996) Neurology 46: 1684-1690), and A large number of documents disclose that topiramate has good curative effect in the treatment of diabetes (US7109174B2 and US6362220B1), neurological dysfunction (US6908902B2), depression (US6627653B2), psychosis (US6620819B2), headache (US6319903B1) and hypertension (US6201010B1). [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/7048A61K47/38A61K47/32A61P25/06A61P25/08A61P3/10A61P25/00A61P25/24A61P25/18A61P9/12
CPCA61K31/7048A61K9/5078A61K9/5026A61K9/5047A61K9/1676A61P13/00A61P13/02A61P25/00A61P25/06A61P25/08A61P25/18A61P25/24A61P29/00A61P9/12A61P3/10A61K9/5042A61K9/5089A61K31/357
Inventor 李松高春生钟武王玉丽杨美燕单利周辛波郑志兵王晓奎
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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