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Rizatriptan benzoate capsule and preparation method thereof

A technology of rizatriptan benzoate and triptan capsules, which is applied in the field of rizatriptan benzoate capsules and its preparation, can solve the problems of no obvious activity and low affinity, and achieve good dissolution rate and long storage life. Long, portable and easy to use effect

Active Publication Date: 2011-03-16
四川梓橦宫药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For other 5-HT 1 receptors and 5-HT 7 Receptor affinity is low, for 5-HT 2 , 5-HT 3 , adrenaline, DA, histamine, choline, or BZ receptors have no apparent activity

Method used

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  • Rizatriptan benzoate capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A kind of rizatriptan benzoate capsule (specification: 5mg / grain, calculated by rizatriptan), the formula that every 10000 capsules needs to be prepared is as follows:

[0035] Rizatriptan Benzoate

72.65g

microcrystalline cellulose

200g

starch

670g

15% polyvinylpyrrolidone ethanol solution

250ml

Magnesium stearate

8g

[0036] The preparation method of rizatriptan benzoate capsule, comprises the steps:

[0037] Step 1: respectively pulverize rizatriptan benzoate, microcrystalline cellulose, starch and magnesium stearate through a 100-mesh sieve, and set aside;

[0038] Step 2: Weigh the raw material rizatriptan benzoate and auxiliary materials microcrystalline cellulose, starch and magnesium stearate according to the above composition formula;

[0039] Step 3: Preparation of adhesive: Add polyvinylpyrrolidone to 80 to 98% ethanol, stir to dissolve completely, and prepare a 15% polyvinylpyrrolidone eth...

Embodiment 2

[0046] A kind of rizatriptan benzoate capsule (specification: 5mg / grain, calculated according to rizatriptan.), the formula that every 10000 capsules required for preparing is as follows:

[0047] Rizatriptan Benzoate

72.65g

microcrystalline cellulose

300g

starch

700g

15% polyvinylpyrrolidone ethanol solution

300ml

Magnesium stearate

10g

[0048] The preparation method of rizatriptan benzoate capsule, comprises the steps:

[0049] Step 1: respectively pulverize rizatriptan benzoate, microcrystalline cellulose, starch and magnesium stearate through a 100-mesh sieve, and set aside;

[0050] Step 2: Weigh the raw material rizatriptan benzoate and auxiliary materials microcrystalline cellulose, starch and magnesium stearate according to the above composition formula;

[0051] Step 3: Prepare adhesive: add 45g of polyvinylpyrrolidone to 95% ethanol to make 300ml, stir to dissolve completely, and prepare a 15% po...

Embodiment 3

[0058] A kind of rizatriptan benzoate capsule (specification: 10mg / grain, calculated according to rizatriptan.), the formula that every preparation 10000 capsules needs is as follows:

[0059] Rizatriptan Benzoate

145.3g

microcrystalline cellulose

400g

starch

800g

[0060] 15% polyvinylpyrrolidone ethanol solution

500ml

Magnesium stearate

8g

[0061] The preparation method of rizatriptan benzoate capsule, comprises the steps:

[0062] Step 1: respectively pulverize rizatriptan benzoate, microcrystalline cellulose, starch and magnesium stearate through a 100-mesh sieve, and set aside;

[0063] Step 2: Weigh the raw material rizatriptan benzoate and auxiliary materials microcrystalline cellulose, starch and magnesium stearate according to the above composition formula;

[0064] Step 3: Prepare adhesive: add 75g of polyvinylpyrrolidone to 95% ethanol to make 500ml, stir to dissolve completely, and pr...

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Abstract

The invention discloses a medicinal preparation rizatriptan benzoate capsule for treating migraine and a preparation method thereof. Every 10000 capsules are prepared from the following formulation constituents: 29-250g of rizatriptan benzoate, 20-400g of microcrystalline cellulose, 220-1100g of starch, 100-400ml of 10-20% polyvinyl pyrrolidone ethanol solution and 4-30g of magnesium stearate. The invention also provides a preparation method of the rizatriptan benzoate capsule. The capsule of the invention covers the foreign taste of the main medicine; release and absorption of the medicine are accelerated; medical particles in the capsule are not punched or molten, thereby overcoming some defects of tablets; after the capsule is taken orally, the medicine is directly dispersed in the gastrointestinal fluid and is moistened by the gastrointestinal fluid, thus the effective surface area is large; and the medicine has higher dissolving rate in the gastrointestinal fluid, can be better absorbed and has high bioavailability.

Description

technical field [0001] The invention relates to a medicine and a preparation method thereof, in particular to rizatriptan benzoate capsules and a preparation method thereof. Background technique [0002] Rizatriptan benzoate, its chemical name is: N, N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indole-3- Base] ethanolate, the molecular formula is C 15 h 19 N 5 ·C 7 h 6 o 2 , the molecular weight is 391.47. Rizatriptan on 5-HT in humans 1B and 5-HT 1D Receptors have high affinity. For other 5-HT 1 receptors and 5-HT 7 Receptor affinity is low, for 5-HT 2 , 5-HT 3 , adrenaline, DA, histamine, choline, or BZ receptors had no apparent activity. Rizatriptan stimulates 5-HT on dilated extracerebral and intracranial blood vessels and trigeminal nerve endings during migraine attacks 1B / 1D , lead to intracranial vasoconstriction, inhibit the release and transmission of neuropeptides in the trigeminal nerve pain pathway, and play its role in the treatment of migraine. ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/4196A61K47/38A61K47/36A61P25/06
Inventor 陈健李威唐铣黄学兵
Owner 四川梓橦宫药业股份有限公司
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