Intranasal pharmaceutical preparation for treating vomit caused by cancer chemo-treatment, radiation-treatment or operation

A nasal administration preparation and nasal administration technology are applied in a new dosage form of vomiting caused by radiotherapy or surgery. The treatment is in the field of cancer chemotherapy. It can solve the problem of low irritation of nasal cilia, and achieve huge business opportunities and social benefits. The preparation process easy effect

Inactive Publication Date: 2007-09-26
吴祥根
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nasally administered formulations mu

Method used

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  • Intranasal pharmaceutical preparation for treating vomit caused by cancer chemo-treatment, radiation-treatment or operation
  • Intranasal pharmaceutical preparation for treating vomit caused by cancer chemo-treatment, radiation-treatment or operation
  • Intranasal pharmaceutical preparation for treating vomit caused by cancer chemo-treatment, radiation-treatment or operation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1: Palonosetron spray

[0060] Ingredient Amount

[0061] Palonosetron hydrochloride (calculated as palonosetron 250mg) 278mg

[0062] Ethylparaben 30mg

[0063] Sodium chloride 1.8g

[0064] Water for injection to 100ml

[0065] Prescription basis: First, according to the dose of Palonosetron’s existing marketed injection, the dose of its nasal spray was determined to be 0.25mg / spray; combined with the physical and chemical properties of the drug, the prescription was screened with water as the solvent to Ethyl hydroxybenzoate is a preservative, and its dosage is 0.03%; the pH control range is 4.5 to 6.5; a nasal cavity spray pump with good airtightness and accurate spray volume has also been selected through tests.

[0066] Preparation method: Pass the Palonosetron Hydrochloride crude drug through an 80-mesh sieve, dissolve it in 90ml of water for injection, then add ethyl p-hydroxybenzoate and sodium chloride, shake to dissolve, add water for injection...

Embodiment 2

[0072] Embodiment 2: Palonosetron nasal drops

[0073] According to the prescription and preparation method of Example 1, but the prepared palonosetron liquid is divided into quantitative nasal drop bottles to obtain palonosetron nasal drops.

Embodiment 3

[0074] Embodiment 3: Palonosetron spray

[0075] Palonosetron hydrochloride (calculated as palonosetron 250mg) 278mg

[0076] Chlorobutanol 500mg

[0077] Hydroxypropyl-β-cyclodextrin 2.5g

[0078] Mannitol 1.8g

[0079] Macrogol 400 1.0ml

[0080] Water for injection to 100ml

[0081] Preparation method: Pass the raw drug of palonosetron hydrochloride through an 80-mesh sieve, dissolve it in 90ml of water for injection, add chlorobutanol, hydroxypropyl-β-cyclodextrin, mannitol, and polyethylene glycol 400 , shake to dissolve, add water for injection to the full amount of 100ml, and filter under reduced pressure with a 0.45 μm microporous membrane to obtain the medicinal solution of palonosetron spray. The above liquid medicine can be divided into spray pumps or quantitative drop pumps.

[0082] The results of the sheep nasal mucosa in vitro penetration test showed that the permeation amount of the above preparation reached 197 mg after each administration. Different pe...

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Abstract

The invention provides an agent fed via nasal to treat the emesis caused by cancer chemotherapy, radiotheraphy or surgery. The inventive agent comprises palosnon drug, or medical accept salt, and medical effective findings. The inventive agent fed via nasal can effectively be absorbed by schneiderian membrane to restrain emesis, without simulation on schneiderian membrane and little cilium toxicity.

Description

field of invention [0001] The invention specifically relates to a new dosage form for treating vomiting caused by cancer chemotherapy, radiotherapy or operation through the nasal cavity administration route. The preparation of the invention contains palonosetron prototype drug or pharmaceutically acceptable salt as the main component, and pharmaceutically effective auxiliary materials. technical background [0002] The chemical structure of Palonosetron Hydrochloride is: [0003] [0004] The Chinese chemical name is: 2-[(S)-1-azabicyclo[2,2,2]octane-3-yl]-2,3,3a(S),4,5,6-hexahydro- 1H-Benzisoquinolin-1-one hydrochloride. The English chemical name is: (3aS)-2,3,3a,4,5,6-Hexahydro-2[(S)-1-Azabicyclo[2.2.2]oct-3-yl]2,3,3a,4 , 5, 6-hexahydro-1-oxo-1 Hbenz[de]isoquinoline. [0005] Palonosetron hydrochloride is white or off-white crystalline powder, odorless and tasteless. Dissolved in water, insoluble in ethanol. [0006] Cancer seriously threatens human life and has b...

Claims

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Application Information

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IPC IPC(8): A61K31/473A61K9/12A61K9/08A61P1/08
Inventor 吴祥根
Owner 吴祥根
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