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Memantine insoluble salt sustained-release injection and preparation method thereof

A technology of sustained-release injections and memantine, applied in the field of medicine, to achieve excellent sustained-release effects, reduce social burdens, and facilitate industrial production

Inactive Publication Date: 2018-12-11
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no memantine sustained-release preparation that can be released for several days or even weeks to improve the medication compliance of patients with Alzheimer's disease and reduce social burdens

Method used

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  • Memantine insoluble salt sustained-release injection and preparation method thereof
  • Memantine insoluble salt sustained-release injection and preparation method thereof
  • Memantine insoluble salt sustained-release injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation of memantine-stearate sustained-release injection:

[0035] A. Synthesis of memantine-stearate

[0036] Weigh an appropriate amount of sodium stearate, disperse it into 100mL of 75°C distilled water, stir to dissolve, and prepare a sodium stearate aqueous solution with a concentration of 0.1mol / L; weigh an appropriate amount of memantine hydrochloride, dissolve it in 100mL of 75°C distilled water, A memantine hydrochloride aqueous solution with a concentration of 0.1 mol / L was obtained. At 75°C, under stirring, add the above memantine hydrochloride aqueous solution into the sodium stearate aqueous solution dropwise, centrifuge at 10,000r / min for 10min, filter with suction, collect the precipitate, wash with hot water three times, and vacuum-dry the obtained filter cake at 40°C for 24h , that is, memantine-stearate.

[0037] B. Preparation of Memantine-Stearate Sustained Release Injection

[0038] 25g of memantine-stearate (calculated as memantine) is disp...

Embodiment 2

[0040] Preparation of memantine-palmitate extended-release injection:

[0041] A. Synthesis of memantine-palmitate

[0042] Weigh an appropriate amount of sodium palmitate, disperse it into 100mL of 75°C distilled water, stir to dissolve, and prepare a sodium palmitate aqueous solution with a concentration of 0.1mol / L; weigh an appropriate amount of memantine hydrochloride, dissolve it in 100mL of 75°C distilled water, and obtain the concentration 0.1mol / L memantine hydrochloride aqueous solution. At 75°C, under stirring, add the above-mentioned memantine hydrochloride aqueous solution into the sodium palmitate aqueous solution dropwise, centrifuge at 10,000r / min for 10min, filter with suction, collect the precipitate, wash with hot water three times, and vacuum-dry the obtained filter cake at 40°C for 24h. That is, memantine-palmitate.

[0043] B. Preparation of memantine-palmitate sustained-release injection

[0044] Disperse 25g of memantine-palmitate (calculated as mema...

Embodiment 3

[0046] Preparation of Memantine-Oleate Sustained Release Injection:

[0047] A. Synthesis of memantine-oleate

[0048] Weigh an appropriate amount of sodium oleate, disperse it into 100mL of 75°C distilled water, stir to dissolve, and prepare a sodium oleate aqueous solution with a concentration of 0.1mol / L; weigh an appropriate amount of memantine hydrochloride, dissolve it in 100mL of 75°C distilled water, and obtain the concentration 0.1mol / L memantine hydrochloride aqueous solution. At 75°C, under stirring, add the above-mentioned memantine hydrochloride aqueous solution into the sodium oleate aqueous solution dropwise, centrifuge at 10000r / min for 10min, collect the oily viscous liquid in the upper layer, wash it with hot water three times, and vacuum the obtained oily viscous liquid at 40°C Dry for 24 hours to obtain memantine-oleate.

[0049] B. Preparation of Memantine-Oleate Sustained Release Injection

[0050] Disperse 25 g of memantine-oleate (calculated as meman...

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Abstract

The invention discloses a memantine insoluble salt sustained-release injection and a preparation method thereof. The memantine insoluble salt sustained-release injection is characterized by being prepared from the following materials by mass percentage: 1% to 30% of memantine insoluble salt as an active ingredient, 0.1% to 10% of stabilizer , 0% to 1% of pH adjuster, 0.1% to 5% of isotonic regulator and 60% to 98% of injection water; the memantine insoluble salt includes one of memantine-oleate, memantine-linoleate, memantine-linolenate, memantine-arachidonate, memantine-stearate, memantine-laurate, memantine-tannate, memantine palmitate, memantine-pamoate, and memantine-furanate. An insoluble salt technology is adopted to prepare the memantine insoluble salt, and the drug release time isprolonged by reducing the solubility of the drug. Compared with memantine hydrochloride, the solubility of the memantine insoluble salt is reduced by 40 to 600 times, and the memantine insoluble saltcan be slowly released for several days to several weeks.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a slow-release injection of memantine insoluble salt and a preparation method thereof. Background technique [0002] Alzheimer's disease is a neurodegenerative disease with progressive development. Its main clinical features are memory loss, cognitive dysfunction, social impairment and personality behavior changes, which seriously reduce the quality of life of patients and aggravate family burden and social burden. At present, the cause of Alzheimer's disease is not yet clear, so there is no drug that can effectively prevent or even reverse the progress of Alzheimer's disease. Most of the existing treatments are to improve certain symptoms of patients or delay the development of Alzheimer's disease. . [0003] So far, only tacrine, donepezil, rivastigmine, galantamine, huperzine A, and memantine hydrochloride have been marketed for the treatment of Alzheimer's dise...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K9/19A61K47/26A61K47/38A61K31/13A61P25/28
CPCA61K9/0019A61K9/10A61K9/145A61K9/146A61K9/19A61K31/13A61K47/26A61K47/38A61P25/28
Inventor 林霞杨子毅刘蕾
Owner JIANGNAN UNIV
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