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Rizatriptan benzoate oral spray

A technology of rizatriptan benzoate and oral spray, which is applied in the field of rizatriptan benzoate preparations, can solve the problems of high production cost and low bioavailability of freeze-drying process, and achieves easy labor protection, biological The effect of high utilization and low production cost

Active Publication Date: 2012-06-06
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the dissolution rate of freeze-dried instant tablets is fast, the production cost of the freeze-drying process is high
At the same time, the first-pass effect of oral administration of rizatriptan benzoate is obvious, and the bioavailability is low, so it is necessary to use formulation technology to improve its bioavailability

Method used

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  • Rizatriptan benzoate oral spray
  • Rizatriptan benzoate oral spray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Formula: Rizatriptan Benzoate 7.3g

[0042] Sodium caprate 0.3g

[0043] Aspartame 0.5g

[0044] Ethanol 25g

[0045] Propylene glycol 10g

[0046] Menthol 0.4g

[0047] EDTA-2Na 0.05g

[0048] Sorbic acid 0.1g

[0049] Distilled water to 100ml

[0050] Preparation method: take rizatriptan benzoate 7.3g, add 25g ethanol, 10g propylene glycol and 50ml distilled water, stir to dissolve. Add 0.3 g of sodium caprate, 0.5 g of aspartame, 0.05 g of EDTA-2Na, 0.1 g of sorbic acid, and 0.4 g of menthol. After dissolving, add distilled water and dilute to 100 ml. The solution was passed through a 0.22 μm microporous membrane, and filled in a spray bottle with a quantitative valve.

Embodiment 2

[0052] Formula: Rizatriptan Benzoate 3.6g

[0053] Water-soluble Azone 0.8g

[0054] Ethanol 10g

[0055] Propylene glycol 10g

[0056] Hypromellose 0.1g

[0057] Neotame 0.3g

[0058] Lemon essence 0.2g

[0059] EDTA-2Na 0.1g

[0060] Potassium sorbate 0.15g

[0061] Distilled water to 100ml

[0062] Preparation method: Dissolve 0.1g of hydroxypropylmethylcellulose in 70ml of pure water, add 10g of ethanol, 10g of propylene glycol, and 3.6g of rizatriptan benzoate, and stir to dissolve. Add 0.8g of water-soluble azone, 0.6g of neotame, 0.2g of lemon essence, 0.1g of EDTA-2Na, and 0.15g of potassium sorbate. After dissolving, add distilled water to make the volume to 100ml. The solution was passed through a 0.22 μm microporous membrane, and filled in a spray bottle with a quantitative valve.

Embodiment 3

[0064] Formula: Rizatriptan Benzoate 14.5g

[0065] Citric acid 2g

[0066] Propylene glycol 15g

[0067] Ethanol 25g

[0068] Caprylic Capric Macrogol Glycerides 0.5g

[0069] Sucralose 0.3g

[0070] Menthol 0.4g

[0071] EDTA-2Na 0.1g

[0072] Methylparaben 0.15g

[0073] Distilled water to 100ml

[0074] Preparation method: Dissolve 2 g of citric acid in 15 g of ethanol, 15 g of propylene glycol and 50 g of water, add 14.5 g of rizatriptan benzoate, and stir to dissolve. Add 0.3g of sucralose, 0.15g of methylparaben, and 0.1g of EDTA-2Na. After dissolving, add 10g of ethanol solution in which 0.4g of menthol and 0.5g of caprylic capric acid macrogolglyceride are dissolved, mix well, and add Distilled water to make up to 100ml. The solution was passed through a 0.22 μm microporous membrane, and filled in a spray bottle with a quantitative valve.

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Abstract

The invention discloses a rizatriptan benzoate oral spray taking water as a solvent and containing the following components by content: 3.6-14.5 g / 100 ml of rizatriptan benzoate, 0.1-50 g / 100 ml of solubilizers, 0.05-5 g / 100 ml of sorbefacients and 0.01-3 g / 100 ml of flavoring agents. The rizatriptan benzoate oral spray sprays for drug administration through an oral cavity or a hypoglossis, and then drugs can be absorbed by mucosae of the oral cavity or the hypoglossis so as to avoid liver first-pass effect and food influence and realize fast absorption, quick effect and high bioavailability;in addition, the rizatriptan benzoate oral spray is convenient to use without being taken with water during drug administration and is especially suitable for patients who are not obedient to oral administration and injection drug administration; and besides, the rizatriptan benzoate oral spray is a liquid formulation, has no dust in the production process, and has easy labor protection and lowercost of mass production.

Description

technical field [0001] The invention relates to a rizatriptan benzoate preparation. technical background [0002] Rizatriptan benzoate is a second-generation 5-hydroxytryptamine (5-HT) receptor agonist, launched in the United States in 1998, for the treatment of acute migraine, with rapid onset, good curative effect, low dose, and wide application range advantages such as wide range and few side effects. Oral administration of rizatriptan benzoate 5mg has a higher migraine relief rate than the first-generation putan drug sumatriptan 100mg, and has milder side effects than sumatriptan, and can be used for acute treatment of migraine attacks with or without aura , effective for recurrent migraine. The salient feature of rizatriptan benzoate is that it has high affinity for 5-HT1B and 5-HT1D, but low affinity for other 5-HT1 receptors and 5-HT7 receptors, and low affinity for 5-HT2, 5-HT3, Adrenaline, DA, histamine, choline, or BZ receptors have no apparent activity, so they...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/38A61K47/16A61K47/10A61K9/12A61K31/4196A61P25/06
Inventor 侯惠民王健陈芳夏怡然
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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