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Rivastigmine slow-release microspheres and preparation method thereof

A technology of slow-release microspheres and rivastigmine bitartrate, which is applied in pharmaceutical formulations, medical preparations of non-active ingredients, nervous system diseases, etc., and can solve problems such as tartrate/rivastigmine bitartrate preparations that have not yet been found. Achieve the effects of sustained slow release, high drug loading, and high encapsulation efficiency

Inactive Publication Date: 2010-05-19
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, no research on rivastigmine tartrate / hydrotartrate preparations has been found, so developing a long-acting sustained-release preparation for the treatment of senile diseases such as Alzheimer's disease and Parkinson's disease has great clinical significance and applicable value

Method used

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  • Rivastigmine slow-release microspheres and preparation method thereof
  • Rivastigmine slow-release microspheres and preparation method thereof
  • Rivastigmine slow-release microspheres and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Example 1: W 1 / O / W 2 Preparation of sustained-release microspheres of rivastigmine tartrate by double emulsification-solvent evaporation

[0043] Dissolve 25mg rivastigmine tartrate and 50mg poloxamer 188 in 0.2mL water as the inner aqueous phase; dissolve 100mg PLGA (RG502H, PLA:PGA=50:50, Mw=20000) in 2.0mL ethyl acetate , forming the oil phase. Add the inner water phase to the oil phase, ultrasonically emulsify the probe, work at a frequency of 200 watts, work for 1 second, rest for 1 second, and get W 1 / O colostrum. Quickly pour the colostrum into 40mL of rapidly stirred 0.1% PVA aqueous solution (adjust the pH to 9.0 with glycine-sodium hydroxide, which contains 1% sodium chloride), stir at 7,000 rpm, and emulsify for 2 minutes at room temperature Continue stirring at a speed of 500 rpm for 6 hours to evaporate the organic solvent, collect the solidified microspheres by centrifugation, wash with distilled water three times, and freeze-dry to obtain the micros...

Embodiment 2

[0044] Embodiment 2: O / W emulsification-solvent volatilization method prepares rivastigmine tartrate sustained-release microspheres

[0045] Dissolve 25 mg of rivastigmine tartrate and 100 mg of PLGA (RG502H, PLA:PGA=50:50, Mw=20000) in a mixed solvent consisting of 2 mL of ethyl acetate and 0.2 mL of propylene glycol to form an oil phase. Pour the oil phase into rapidly stirred 40mL 0.1% PVA aqueous solution (adjust pH 9.0 with glycine-sodium hydroxide, which contains 1% sodium chloride), stir at 7,000 rpm, emulsify for 2 minutes, at room temperature Continue stirring at a speed of 500 rpm for 6 hours to evaporate the organic solvent, collect the solidified microspheres by centrifugation, wash with distilled water three times, and freeze-dry to obtain the microspheres.

Embodiment 3

[0046] Example 3: O 1 / O 2 Preparation of sustained-release microspheres of rivastigmine tartrate by emulsification-in-liquid drying method

[0047] Dissolve 20mg of rivastigmine tartrate and 200mg of PLGA (RG502H, PLA:PGA=50:50, Mw=20000) in 2mL of a mixed solvent composed of dichloromethane and acetonitrile (volume ratio 3:2), and ultrasonically vibrate to make it Dissolve to form the internal oil phase; inject the internal oil phase into 40mL liquid paraffin containing 0.2% Span 80, stir at 800 rpm for 15 minutes to emulsify, continue stirring at 500 rpm for 6 hours at room temperature to evaporate the organic solvent, filter , followed by washing the microspheres with n-hexane and water, redissolving in a small amount of water, and freeze-drying to obtain the microspheres.

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Abstract

The invention discloses slow-release microspheres coated with rivastigmine tartrate / rivastigmine for PLGA / PLA injection and a preparation method thereof. The slow-release microspheres mainly comprise rivastigmine tartrate / rivastigmine and PLGA and PLA serving as biodegradable polymer medicinal materials, and can be prepared by adopting a W1 / O / W2 composite emulsified solvent volatilization method, an O / W emulsified solvent volatilization method, an O1 / O2 emulsion drying method and a spray drying method. The grain diameter of the microspheres is less than 100 microns. The slow-release microspheres have high medicament loading amount, have no obvious burst release effect, can be continuously released for one week, one mouth or three mouths, are used for treating senile diseases such as Alzheimer's disease, Parkinson disease and the like, and can prolong the acting time of the medicament, reduce the application times and greatly improve the administration compliance of patients.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a sustained-release microsphere for tartrate / rivastigmine bitartrate PLGA / PLA injection and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a type of senile central nervous system degenerative disease, and its exact etiology is not yet fully understood. At present, the hypothesis of cholinergic nerve damage is widely accepted. It is generally believed that the cognitive deficits in patients with Alzheimer's disease are caused by the dysfunction of cholinergic nerve conduction in the cerebral cortex and forebrain base. Through cholinergic nerve conduction to improve symptoms. Acetylcholinesterase inhibitors restore the normal level of acetylcholine and increase the excitability of cholinergic neurons by inhibiting the activity of acetylcholinesterase, which has been proved to be effective both th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/27A61K47/34A61P25/28
Inventor 崔京浩缪文俊崔载胜
Owner SUZHOU UNIV
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