Nimodipine gel for nasal cavity

A technology of nimodipine gel and nasal cavity, which is applied in the field of chemical pharmacy and can solve the problems of large dosage

Inactive Publication Date: 2005-10-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Have research to adopt O / W type microemulsion to solubilize nimodipine, its maximum solubility can reach 6.4mg / ml, and there is no nose cilia toxicity, but the consumption of surfactant and co-surfactant in the microemulsion preparation is bigger (up to 30%), its potential central toxicity needs further study (Int J Pharm 2004, 275, 85-96)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Nimodipine nasal gels were prepared with different hydrophilic gel materials. Table 1 is the prescription (w / w%) of nimodipine nasal gel preparation.

[0020] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

Prescription 6

Nimodipine

0.1-15％

0.1-15％

0.1-15％

0.1-15％

0.1-15％

0.1-15％

Carbopol 934P

1％

-

-

-

-

-

Noveon

CA-1

-

1％

-

-

-

-

MC

-

-

3％

-

-

-

CMCNa

-

-

-

4％

-

-

HPMC

-

-

-

-

2％

-

Chitosan

-

-

-

-

-

3％

Other accessories

Glycerin 10%

Glycerin 10%

Glycerin 15%

Glycerin 20%

Glycerin 20%

Propylene Glycol 20%

Thimerosal

0.01%

Chlorobutanol

0.5%

Ethylparaben

0.02%

Methylparaben

0.1%

Ethylparaben

0.03%

Chlorhexid...

Embodiment 2

[0027]Carbopol 934P is used as the hydrophilic gel material, ethanol, propylene glycol, Transcutol P, polyethylene glycols, polysorbates, and cyclodextrins are used as solubilizers, and the optional amount of ethanol is 5-30% , Propylene Glycol 5-60%, Transcutol P 5-20%, Polyethylene Glycols 5-30%, Polysorbates 0.2-5%, βCD 2-10%, HPβCD 2-20% , MeβCD is 2-10%.

[0028] Table 2 is the prescription (w / w%) of nimodipine nasal gel preparation.

[0029] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

Prescription 6

Nimodipine

1％

15％

5％

10％

0.1％

2％

Carbopol 934P

0.2％

1％

0.5％

0.5％

0.3％

1.5％

ethanol

5％

20％

-

-

-

-

PEG400

-

10％

20％

-

-

-

TranscutolP

-

-

-

20％

-

-

Propylene Glycol

-

-

-

- ...

Embodiment 3

[0038] Cellulose derivatives are used as the hydrophilic gel material, and ethanol, PEG 400, propylene glycol, Tween-80, and MeβCD are added to the prescription as solubilizers. The optional dosage of ethanol is 5-30%, and PEG 400 is 5- 30%, Propylene Glycol 5-50%, Tween-80 0.2-5%, MeβCD 2-5%. Table 3 is the prescription (w / w%) of nimodipine nasal gel preparation.

[0039] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

Prescription 6

Nimodipine

6％

3％

0.5％

1％

8％

2％

MC

2％

6％

-

-

-

-

CMCNa

-

-

2％

10％

-

-

HPMC

-

-

-

-

2％

5％

ethanol

20％

-

-

-

-

-

PEG400

-

20％

-

-

-

-

Propylene Glycol

-

-

30％

-

-

-

...

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PUM

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Abstract

A gel of nimodipine for nasal cavity is prepared from nimodipine, hydrophilic gel and pharmacologically acceptable additive (pH regulator, humectant, anticeptic, etc). Its advantages are high biological utilization and no toxin to vibrissae.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a nasal gel of nimodipine. Background technique [0002] Nimodipine is a second-generation dihydropyridine calcium channel antagonist with the chemical name isopropyl-2-methoxyethyl-1,4-dihydro-2,6-dimethyl-4-(3- Nitrophenyl)-3,5-pyridine dibasic acid ester. It has the functions of selectively expanding cerebral blood vessels, increasing cerebral blood flow, protecting brain cells, and promoting the recovery of neuron functions. Clinically, it is mainly used to treat ischemic cerebrovascular diseases, improve the memory loss of the elderly and prevent Alzheimer's disease. There are two routes of administration of nimodipine, oral and parenteral. Injection is used for intravenous infusion and cisternal infusion. Although the onset of effect is fast and the effect is definite, it needs to be operated by professional medical personnel, and the latter still has certain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4422A61P9/10A61P25/28
Inventor 张奇志蒋新国
Owner FUDAN UNIV
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