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Nasal administration preparation for anti-AIDS-virus brain infection and use thereof

A nasal administration preparation and anti-AIDS technology, applied in antiviral agents, drug delivery, pharmaceutical formulations, etc., can solve the problems of high HIV survival rate, achieve increased drug concentration, low toxicity of nasal mucosa and cilia, and rapid release and absorption Effect

Inactive Publication Date: 2005-02-16
武凤兰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Scientists have found that due to the existence of the blood-brain barrier (BBB), drugs that are currently administered intravenously or orally cannot or rarely enter the CNS
Although good therapeutic effects can be achieved in the systemic system through combination drugs, the survival rate of HIV in the CNS is still high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The present embodiment is solution type nasal drops and nasal spray.

[0031] Components of the following quality are dissolved in the phosphate buffered saline solution of pH7.7 to make the nasal cavity administration preparation of 100ml present embodiment:

[0032] Didanosine 2.0g, hydroxypropylmethylcellulose 0.3g, benzalkonium bromide 0.02g, hydroxypropyl-β-cyclodextrin 5g, sodium chloride 0.45g.

Embodiment 2

[0034] The present embodiment is solution type nasal drops and nasal spray.

[0035] The drug didanosine was dissolved in an aqueous solution containing the following components, and the pH was adjusted to 6.80 with sodium bicarbonate to make the solution-type nasal administration preparation of 100ml of the present embodiment:

[0036] Didanosine 1.5g, Carbopol 0.5g, methylparaben and butylparaben (2:1 by mass ratio) 0.05g, β-cyclodextrin 1.8g, sodium chloride 0.9g.

Embodiment 3

[0038] The present embodiment is suspension type nasal drops and nasal spray.

[0039] Prepare liposomes with lecithin and cholesterol as membrane materials, encapsulate or adsorb didanosine in liposome vesicles or on the surface, add it and the following components to a phosphate buffer system at pH 7.0 to prepare Become the solution type nasal administration preparation of 100ml present embodiment:

[0040] Didanosine 0.5g, lecithin 3.0g, cholesterol 0.5g, gum arabic 1.0g, chlorhexidine acetate 0.04g, sodium chloride 0.6g.

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Abstract

The invention discloses a nasal cavity administration preparation which can resist the brain infection of aids, it belongs to medicine preparation technology field for anti-aids virus, it uses hydroxyl inosine as pharmacologic active ingredient, adds in pH value regulator, penetration advancing agent, thickener, equal-penetration regulator, antiseptic and produces them into preparation suitable for nose cavity, solves the problem that the current medicine with oral, muscle injection or other modes the medicine can penetrate the vein blood brain barrier to the brain, the release and absorption of the preparation in the invention are quick, the medicine can gathers in the brain, the medicine density in brain is upgraded prominently, at the same time, the invention has character that the nose cavity mucous coat and cilium toxin are small.

Description

technical field [0001] The present invention relates to an anti-AIDS virus pharmaceutical preparation and application, in particular, the present invention relates to a nasal administration preparation and application of didanosine as an active ingredient for anti-AIDS virus brain infection. Background technique [0002] At present, the prevention and treatment of AIDS worldwide has become a major issue facing all mankind. So far, nearly 40 million people have been infected with HIV worldwide, and the number of AIDS patients in my country is also increasing rapidly. According to the latest statistics from the Ministry of Health, the number of people infected with HIV in my country is It has reached 1 million, and some of them have entered the onset period. Central nervous system (CNS) disorder is a very common phenomenon in AIDS patients. In the early stage of AIDS, 7-20% of the patients' nervous system is damaged, and in the later stage, it reaches 30-70%. Autopsy shows that...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/70A61P31/18
Inventor 武凤兰赵莹王智瑛
Owner 武凤兰
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