Topiramate sustained-release capsule and preparation method thereof
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A technology for sustained-release capsules and topiramate, which is applied in directions such as capsule delivery, microcapsules, and pharmaceutical formulations, can solve problems such as complex preparation processes and achieve the effect of stabilizing blood drug concentrations.
Pending Publication Date: 2020-01-03
ZHEJIANG POLY PHARMA +1
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Embodiment 1
[0027] Embodiment 1: preparation of topiramate sustained-release capsules
[0028] prescription:
[0029]
[0030]
[0031] Preparation Process:
[0032] (1) Preparation of drug-containing sustained-release pellets by extrusion spheronization technology
[0033] Topiramate, microcrystalline cellulose (filler) and hypromellose (binder) of recipe quantity are mixed homogeneously in Mycromix high-shear wet granulator, and process parameter is as follows:
[0034]
[0035] After premixing, add purified water to the premix powder for granulation. The process parameters are as follows:
[0036]
[0037] After the wet granulation is completed, the material is discharged, and the prepared soft material is pelletized through the E550 / S-250 extrusion spheronizer. The process parameters are as follows:
[0038]
[0039] After pellet making, use a fluidized bed to dry the wet pellets until the water content is less than 5%, to obtain drug-loaded sustained-release pellets...
Embodiment 2
[0051] Embodiment 2: Preparation of topiramate sustained-release capsules
[0052] prescription:
[0053]
[0054]
[0055] Preparation Process:
[0056] (1) Preparation of drug-loaded immediate-release pellets
[0057] Dissolve the prescribed amount of hydroxypropyl methylcellulose in purified water, then add the prescribed amount of topiramate, homogenize for 5-10 minutes with a high-shear emulsifier, prepare a suspension coating solution, and coat the coating solution containing topiramate On the outside of the blank microcrystalline pellet core, the immediate-release pellets were obtained, and the parameters of the coating process were as follows:
[0058]
[0059] (2) Sustained release layer coating
[0060] Dissolve the prescribed amount of ethyl cellulose and PEG-6000 in ethanol solution, then add magnesium stearate, homogenize for 5-10 minutes in a high-shear emulsifier, prepare a slow-release layer coating solution, and use a fluidized bed to The coating ...
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Abstract
The invention relates to the field of antiepileptic drug preparations, in particular to a topiramate sustained-release capsule and a preparation method thereof. The topiramate sustained-release capsule comprises a drug-containing sustained-release pill core, an enteric coating layer and an immediate-release layer. The weight ratio of pharmaceutical active ingredient topiramate to the drug-containing sustained-release pill core is 40%-80%, and the weight ratio of the topiramate to the immediate-release layer is 20%-60%. According to the opiramate sustained-release capsule, a part of the pharmaceutical active ingredient topiramate is distributed in the drug immediate-release layer, when the topiramate sustained-release capsule enters the gastrointestinal tract, the drug immediate-release layer begins to disintegrate, the topiramate is dissolved, and the effective blood concentration can be quickly reached, at the moment, the sustained-release part of the drug is not dissolved under the protection of enteric coating, when the drug enters the intestine, the topiramate is released in a sustained mode under the action of the sustained-release coating, and effective and stable blood drugconcentration can be continuously maintained.
Description
technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to antiepileptic drugs, in particular to topiramate sustained-release capsules and a preparation method thereof. Background technique [0002] Topiramate is a white crystalline powder with a bitter taste. It is easily soluble in alkaline solutions with a pH value of 9-10 such as sodium hydroxide or sodium phosphate, and easily soluble in acetone, chloroform, dimethyl sulfoxide and ethanol. The solubility in water is 9.8mg / mL, the pH value of its saturated solution is 6.3, and the melting point is 125-126°. [0003] Its chemical name: 2,3:4,5-bis-O-(1-methylethylene)-β-D fructopyranose sulfamate, molecular formula: C 12 h 21 NO 8 S, molecular weight: 339.36. [0004] Its structural formula: [0005] [0006] Topiramate is a new broad-spectrum antiepileptic drug, which is effective for all types of seizures, especially for primary and secondary generalized tonic-clon...
Claims
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