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Nasal gel agent containing risperidone and preparation method of nasal gel agent

A risperidone nasal and gel technology, applied in the field of pharmaceutical preparations, can solve problems such as unsatisfactory curative effect, unfavorable industrial production, low bioavailability, etc. effect of time

Inactive Publication Date: 2015-03-11
内蒙古医科大学附属医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the above invention patent application, although the risperidone sustained-release gel injection and the transdermal absorption patch can prolong the drug effect time, the drug in the preparation still needs to pass through the blood-brain barrier by the blood circulation, and the amount of drug entering the brain tissue is small, so Slow onset and poor curative effect, and their preparation process is complicated, the production cycle is long, and the cost is high, which is not conducive to the realization of industrialized production
However, both the osmotic pump controlled-release preparation and the orally disintegrating tablet of the drug are administered orally, both of which have a significant first-pass effect in the liver, resulting in low bioavailability of the drug in the body, and a small amount of drug entering the brain from the blood circulation, so the curative effect Also not ideal

Method used

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  • Nasal gel agent containing risperidone and preparation method of nasal gel agent
  • Nasal gel agent containing risperidone and preparation method of nasal gel agent
  • Nasal gel agent containing risperidone and preparation method of nasal gel agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Prescription 1: The following are all calculated by mass fraction

[0035]

[0036]

[0037] Preparation process: Weigh the prescribed amount of carbomer and sodium alginate, sprinkle them in an appropriate amount of purified water, and let them sit for 24 hours to fully swell, then adjust the pH to 6.0 with hydrochloric acid to obtain a blank gel matrix; separately take risperidone, azone, After ethylparaben is mixed with propylene glycol and kneaded evenly, add an appropriate amount of purified water, heat it in a water bath at 60°C to dissolve completely, add it to the blank gel matrix under constant stirring, knead it well, and finally add water to the full amount, That is, the drug nasal gel is obtained.

Embodiment 2

[0039] Prescription 2: The following are all calculated by mass fraction

[0040]

[0041] Preparation process: Weigh the prescribed amount of sodium carboxymethyl cellulose, sprinkle it in an appropriate amount of purified water, let it swell fully, heat it to dissolve, adjust the pH to 6.5 with sodium hydroxide, and obtain a blank gel matrix; take another dimethyl cellulose - After adding purified water to β-cyclodextrin to dissolve, then add glycerin, risperidone, benzalkonium bromide, and sodium chloride in sequence, heat in a water bath at 60°C to dissolve completely, and add it to the Grind thoroughly in the blank gel matrix, and finally add water to the full amount to obtain the nasal gel of the drug.

Embodiment 3

[0043] Prescription 3: The following are all calculated by mass fraction

[0044]

[0045] Preparation process: Weigh the prescribed amount of carbomer, sprinkle it in an appropriate amount of purified water, let it stand for 24 hours to fully swell, adjust the pH to 6.0 with triethanolamine, and obtain a blank gel matrix; separately take risperidone and Tween-80 to fully grind After uniformity, add purified water, heat in a water bath at 60°C to dissolve, then add chlorobutanol, sorbitol, and glucose to dissolve in sequence, and add them to the blank gel matrix under constant stirring, fully Grind well, and finally add water to the full amount to obtain the nasal gel of the drug.

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Abstract

The invention discloses a nasal gel agent containing risperidone and a preparation method of the nasal gel agent, and belongs to the field of pharmaceutical preparations. The nasal gel agent comprises risperidone, a matrix material, pharmaceutically acceptable water and other pharmaceutically effective auxiliary materials such as an osmotic pressure regulator, an absorption enhancer, a preservative, a humectant and a pH regulator. The preparation method comprises the following steps: dissolving risperidone and the other pharmaceutically effective auxiliary materials in the water in sequence, adding into a blank gel matrix in sequence, and fully and uniformly grinding. The nasal gel agent is simple in preparation process and has the characteristics of remarkable brain-targeting characteristic, high absorption and action speed, high bioavailability, good clinical curative effect and high convenience and safety in use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a risperidone nasal gel and a preparation method thereof. Background technique [0002] Risperidone is a white powder, which is a new generation of atypical antipsychotic drugs, and has significant curative effect on both positive and negative symptoms of schizophrenia. The chemical name is 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetra Hydrogen-2-methyl-4H-piperido[1,2-α]pyrimidin-4-one, its structural formula is as follows: [0003] [0004] Molecular formula: C 23 h 27 FN 4 o 2 ;Molecular weight: 410.49. Because of its advantages of small dose, definite curative effect, and small extrapyramidal side effects, it has been widely used in clinic as a first-line drug for the treatment of schizophrenia. [0005] Currently, risperidone has been marketed in the form of oral tablets and solutions. Patent application (CN101584652B) discl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/519A61P25/18
Inventor 谷福根王毅马瑞莲马维娜吴春芝孟根达来解红霞
Owner 内蒙古医科大学附属医院
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