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Capsule type Eletriptan nose inhalation powder aerosols and preparation method and application thereof

A technology of eletriptan and inhalation powder spray, applied in the field of pharmaceutical preparations, can solve the problems of dryness, itching, burning sensation, reduced medication compliance, low bioavailability, etc. Eliminate irritation and discomfort, reduce drug dosage

Inactive Publication Date: 2019-12-20
ZHUHAI RESPROLY PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the existing drugs for the treatment of migraine are oral preparations of triptan, but due to the first-pass effect of the liver, the bioavailability is low, the drug takes effect slowly, the dosage is large, and the side effects are large
Because triptan nasal spray contains citric acid, disodium hydrogen phosphate, purified water and other excipients, it is easy to cause nasal mucosal irritation when used, such as dryness, itching, burning sensation, etc., or discomfort flowing from the nasal cavity to the throat. reduce medication adherence

Method used

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  • Capsule type Eletriptan nose inhalation powder aerosols and preparation method and application thereof
  • Capsule type Eletriptan nose inhalation powder aerosols and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Recipe: eletriptan 2g, lactose 15g, made into 1000 capsules in total.

[0028] Take 2 g of eletriptan, dry at 50°C for 1.5 hours, and let cool to room temperature; the raw material is micronized with a jet mill; 15 g of lactose is ultrafinely pulverized, passed through a 60-mesh sieve, and the sieved lactose is placed in In a fluidized bed granulator, ethanol is used for granulation, the inlet air temperature is 60°C, the material temperature is 45°C, the liquid spray speed is 2g / min, and the fan frequency is 20Hz. After spraying, continue to dry for 15 minutes.

[0029] Take the micronized eletriptan and lactose granules, and mix them in equal amounts. The mixing speed is 5 rpm, and the mixing time is 20 minutes, and the mixed powder is filled into capsules with a microcapsule filling machine.

Embodiment 2

[0031] Recipe: 4g of eletriptan, 25g of lactose, made into 1000 capsules in total.

[0032] Take 4g of eletriptan, dry at 60°C for 1 hour, and let cool to room temperature; the raw material is micronized by a jet mill; 30g of lactose is ultrafinely pulverized, passed through a 80-mesh sieve, and the sieved lactose is placed in In a fluidized bed granulator, ethanol is used for granulation, the air inlet temperature is 70°C, the material temperature is 60°C, the liquid spray speed is 3g / min, and the fan frequency is 30Hz. After spraying, continue to dry for 25 minutes.

[0033] Take the micronized eletriptan and lactose granules, and mix them in equal amounts. The mixing speed is 10 rpm, the mixing time is 30 minutes, and the mixed powder is filled into capsules with a microcapsule filling machine.

Embodiment 3

[0035] Formula: Eletriptan 5g, lactose 40g, made into 1000 capsules in total.

[0036] Take 8g of eletriptan, dry at 60°C for 2 hours, and let cool to room temperature; the raw material is micronized with a jet mill; 60g of lactose is ultrafinely pulverized, passed through a 100-mesh sieve, and the sieved lactose is placed in In the fluidized bed granulator, ethanol is used for granulation, the air inlet temperature is 70°C, the material temperature is 60°C, the liquid spray speed is 4g / min, and the fan frequency is 40Hz. After the spraying is completed, continue to dry for 20 minutes.

[0037] Take the micronized eletriptan and lactose granules, and mix them in equal amounts. The mixing speed is 12 rpm, the mixing time is 40 minutes, and the mixed powder is filled into capsules with a microcapsule filling machine.

[0038] The present invention has carried out " membrane penetration test " according to following method:

[0039] Method: Take fresh toad mucous membrane, cut ...

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Abstract

The invention discloses capsule type Eletriptan nose inhalation powder aerosols. The capsule type Eletriptan nose inhalation powder aerosols consist of Eletriptan micro powder and carrier micro powder. The capsule type Eletriptan nose inhalation powder aerosols are characterized in that the particle sizes of raw material micro powder of the Eletriptan are d10=5-30[mu]m, d50=10-100[mu]m and d90=30-150[mu]m, and the particle size of the carrier micro powder is d90=20-320[mu]m. The invention also provides a preparation method of the capsule type Eletriptan nose inhalation powder aerosols. The preparation method comprises the working procedures of performing Eletriptan micronizing, performing lactose particle preparation, performing mixing and performing subpackaging, wherein during mixing, the micronized Eletriptan and lactose particles are taken, mixing is performed in an equal progressively-increased manner, the mixing speed is 2-15 revolutions per minute, and the mixing time is 5-45 minutes. The capsule type Eletriptan nose inhalation powder aerosols disclosed by the invention comprise 2 kinds of inhalation manners of nose inhalation and oral inhalation, and the Eletriptan can alsoexist in the form of normal saline. The capsule type Eletriptan nose inhalation powder aerosols can reach pain locations in a nose and brain targeting administration manner and can take effect quickly, first-pass effects of the liver are avoided, the biological availability can be improved, the first-pass effects of the liver can be avoided through direct inhalation of the capsule type Eletriptannose inhalation powder aerosols, and consumption and side effects of the medicine are reduced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, and relates to an inhalation powder, in particular to a capsule type eletriptan nasal inhalation powder and its preparation method and application. Background technique [0002] Migraine (Migraine) is a common chronic neurovascular disease, manifested by recurrent headaches, autonomic dysfunction, and various combinations of other neurological symptoms. Attacks are often accompanied by numerous autonomic nervous system symptoms, such as nausea, vomiting, pale complexion, rapid heart rate, rapid breathing, and gastrointestinal dysfunction. Premonitory manifestations such as numbness, speech difficulties, numbness of one limb or hemiparesis, which lasted for several minutes or half an hour. Most of the onsets are in children and adolescence, and the peak incidence is reached in young and middle-aged adults. It is more common in women, and the ratio of male to female patients is...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/48A61K47/26A61K31/404A61P25/06
CPCA61K9/0043A61K9/0053A61K9/4858A61K31/404A61P25/06
Inventor 陈永奇李宝茹胡芳
Owner ZHUHAI RESPROLY PHARM TECH CO LTD
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