Nasal cavity administrated prepn for treating cerebral tumor

A technology for nasal drug delivery preparations and brain tumors, which can be used in antineoplastic drugs, medical preparations containing active ingredients, drug combinations, etc., and can solve the problems of limited treatment and achieve the effect of no special smell

Inactive Publication Date: 2003-01-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because methotrexate is not easy to pass through the blood-brain barrier, it l

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 prepares solution

[0030] Methotrexate Sodium 1.0g

[0031] β-cyclodextrin 3.0g

[0032] EDTA-2Na 0.1g

[0033] Sodium metabisulfite 0.15g

[0034] Benzalkonium Chloride 0.01g

[0035] Distilled water to 100ml

[0036] Get above-mentioned components and be mixed with the nasal cavity spray containing methotrexate sodium according to conventional method.

[0037]

Embodiment 2

[0038] Embodiment 2 prepares solution

[0039] Methotrexate Sodium 1.0g

[0040] Sorbitol 1.0g

[0041]EDTA-2Na 0.1g

[0042] Sodium metabisulfite 0.15g

[0043] Benzalkonium Chloride 0.01g

[0044] Distilled water to 100ml

[0045] Get above-mentioned components and be mixed with the nasal cavity spray containing methotrexate sodium according to conventional method.

[0046] Continuous collection of cerebrospinal fluid by push-pull perfusion combined with cisterna magna puncture to obtain drug-time data of cerebrospinal fluid after administration of methotrexate nasal spray and intravenous injection; Post-dose plasma drug-time data.

[0047] The two nostrils of the rats were given the above-mentioned nasal cavity spray containing methotrexate sodium at a dose of 3.2 mg / kg. After the administration, artificial cerebrospinal fluid perfusion was started. Blood was collected from the tail vein at 90, 120, 150, 180, 210, and 240 minutes; CSF was collected from the lateral v...

Embodiment 3

[0052] Embodiment 3 prepares gel

[0053] Methotrexate Sodium 1.0g

[0054] Carbopol 934PNF 0.5g

[0055] Sorbitol 4.0g

[0056] EDTA-2Na 0.1g

[0057] Sodium metabisulfite 0.15g

[0058] Benzalkonium Chloride 0.01g

[0059] 1mol / L NaOH to adjust the pH to 6~7

[0060] Distilled water to 100ml

[0061] Add the above-mentioned methotrexate sodium, carbopol 934PNF, sorbitol, EDTA-2Na, sodium metabisulfite, and benzalkonium chloride into 50ml of distilled water, stir magnetically for 24 hours, and adjust the pH to 6-7 with 1mol / L NaOH to form a gel , Add distilled water to 100ml to obtain a yellow gel.

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PUM

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Abstract

The present invention relates to one kind of nasal cavity administrated preparation of methotrexate to target to brain. The present invention is suitable for preventing and treating primary and metastatic cerebral tumor, meningeal leukaemia, cerebral infiltration of leukaemia, etc. The preparation contains methotrexate or its medicinal acceptable salt as well as pharmacological acceptable supplementary material. After being administrated, the medicine reaches brain fast and is enriched in brain to produce high disease preventing and treating effect while the medicine density in blood and other tissues is reduced to decrease general side effect, the preparation has also the advantages of fast release and less nasal cilium toxicity.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a preparation for targeting the antitumor drug methotrexate to the brain through the nasal cavity administration route. Background technique [0002] Malignant tumor is one of the serious diseases that endanger human health and cause death. According to reports, 5.9 million people worldwide develop tumors every year, and 4.3 million people die from them. The incidence of cancer in my country is about 105 / 100,000, and there are about 1.25 million new patients every year, and about 900,000 people die from the disease. [0003] Brain tumors are divided into benign and malignant, primary and metastatic. Among the primary brain tumors, glioma is the most common, accounting for more than 40%, while the brain infiltration of leukemia accounts for more than 50% of children's brain tumors; brain tumors can occur at any age, around 10 years old and 30-40 years old There are ...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P35/00
Inventor 蒋新国王峰陆伟
Owner FUDAN UNIV
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