Injectable long-acting microsphere suspension contg.

A technology of huperzine A and suspension, which is applied in emulsion delivery, neurological diseases, liquid delivery, etc., and can solve problems such as waste, inconvenient use, and inability to guarantee needle penetration rate

Inactive Publication Date: 2006-01-25
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The release curve of the microspheres described in the above-mentioned published patents is obviously in two phases, wherein the release amount on the first day is about 30% (sustained release for more than two weeks), and there is almost no drug release in the following week, so it is difficult to reach a certain level. The therapeutic effect of
Although literature research shows that the side effects of huperzine A are very small, the recommended daily oral dose should be less than 450 μg. If the dose is too large, it will cause dizziness, nausea, gastrointestinal discomfort, chest tightness, fatigue, bradycardia and other reactions
For a sustained-release formulation that has been released for more than two weeks, it is obviously not ideal to release 30% of the one-time burst; another big problem of this patent is to use physiological saline to suspend the microspheres (diameter 1-250 micron) ) is difficult to achieve a good suspension state so that a good needle pass rate cannot be guaranteed, resulting in inconvenience and waste

Method used

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  • Injectable long-acting microsphere suspension contg.
  • Injectable long-acting microsphere suspension contg.
  • Injectable long-acting microsphere suspension contg.

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]Weigh 40 mg of huperzine A, 400 mg of PLGA-COOH (75 / 25) in a small beaker, add 1 mL of dichloromethane (DCM) to dissolve them, and inject the drug-PLGA-DCM mixed solution with a syringe under mechanical stirring In 100mL aqueous solution containing 2% polyvinyl alcohol, fully emulsify for 30 minutes, reduce the stirring speed, collect microspheres after the organic solvent evaporates, wash with water, and dry. The whole operation process adopts aseptic operation. The drug loading of the obtained microspheres was 5.04%.

Embodiment 2

[0036] Weigh 30 mg of huperzine A, 100 mg of PLGA-COOH (75 / 25) in a small beaker, add 1 mL of dichloromethane (DCM) to dissolve them, and inject the drug-PLGA-DCM mixed solution into 10 mL with a syringe under magnetic stirring In an aqueous solution containing 1% polyvinyl alcohol, after fully emulsifying for 30 minutes, reduce the stirring speed, collect the microspheres after the organic solvent is evaporated, wash with water, and dry, and sterilize the obtained microspheres with ethylene oxide at 30°C for 48 hours to ensure The residual amount of ethylene oxide is below 5ppm. The drug loading of the obtained microspheres was 5.96%.

Embodiment 3

[0038] Weigh 20 mg of huperzine A, 100 mg of PLGA-COOH (75 / 25) in a small beaker, add 1 mL of dichloromethane (DCM) to dissolve them, and inject the drug-PLGA-DCM mixed solution into 10 mL with a syringe under magnetic stirring In an aqueous solution containing 1% polyvinyl alcohol, after fully emulsifying for 30 minutes, reduce the stirring speed, collect the microspheres after the organic solvent is evaporated, wash with water, and dry, and sterilize the obtained microspheres with ethylene oxide at 30°C for 48 hours to ensure The residual amount of ethylene oxide is below 5ppm. The drug loading of the obtained microspheres was 4.39%.

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Abstract

A durable micro-spherical suspension of huperzine A without sudden release for treating senile hypomnesia and AD is disclosed. Its preparing process features that the PLGA-COOH or PLA-COOH is used and its process is simplified. Its action period is 20-40 days.

Description

Technical field: [0001] The invention relates to the technical field of pharmaceutical preparations. To be precise, it is a huperzine A long-acting microsphere suspension for injection without burst release effect. Background technique: [0002] Huperzine A (Huperzine A), chemical name (5R,9R,11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5,9- Methylenecyclooctano(b)pyridin-2(1H)one is a new structural alkaloid extracted from Huperzia serrata (Thμnb) Trev by Chinese medical researchers. Pharmacological research results It shows that huperzine A is a potent and reversible cholinesterase inhibitor, which has a strong inhibitory effect on true cholinesterase (AChE). It easily enters the brain tissue, inhibits AChE at cholinergic synapses, and corrects central cholinergic insufficiency. The efficacy of huperzine A in the treatment of middle-aged and elderly memory loss and Alzheimer's syndrome (AD) has been clinically verified (Wang Hongxin, Wang Jian. Research progr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4353A61K9/10A61P25/00A61P25/28
Inventor 丁平田高萍
Owner SHENYANG PHARMA UNIVERSITY
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