Huperzine-A particle long-acting injection and preparation method thereof

A technology of huperzine A and injection, applied in the field of huperzine A microparticle long-acting injection, can solve problems such as low dose and burst release effect, and achieve the effects of dose control, avoidance of side effects and small gaps

Active Publication Date: 2015-07-08
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If an o / w emulsion is used, since huperzine A has a certain water solubility and low dosage, when the solvent volatilizes, the drug in the oil phase will easily migrate to the outer water phase, often causing a serious burst release effect

Method used

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  • Huperzine-A particle long-acting injection and preparation method thereof
  • Huperzine-A particle long-acting injection and preparation method thereof
  • Huperzine-A particle long-acting injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Dissolve 420mg of poly-L-lactic acid in 5ml of acetonitrile, add 180mg of huperzine A, and stir to dissolve.

[0035] Heat to 60°C to gradually evaporate the organic solvent to dryness while stirring to form granules.

[0036] Divide the above granules into 6 parts, add 0.5 g of pure water to each grinding tube, and grind the granules into fine particles with a multifunctional sample homogenizer;

[0037] The rotation speed of the multifunctional sample homogenizer is 5500rpm, the grinding time is 40s, and the grinding time is 4 times with an interval of 30s between each time;

[0038] Centrifuge the formed particles, wash with pure water, collect the particles on the filter membrane under reduced pressure, dry the particles in a vacuum oven at 40°C, and pass through a 120-mesh sieve to obtain long-acting huperzine A for injection with a particle size of less than 120 μm. particle.

Embodiment 2

[0040] Dissolve 546mg of poly-L-lactic acid (poly-L-lactide, PLLA) in 2ml of chloroform, transfer it to a glass mortar, add 54mg of huperzine A to dissolve, keep grinding until the solvent evaporates, and obtain particles with uniform particle size .

[0041] Divide the above granules into 6 parts, add 0.5ml of pure water to each grinding tube, and use a multifunctional sample homogenizer to grind the granules into fine particles;

[0042] The rotation speed of the multifunctional sample homogenizer is 6500rpm, the grinding time is 30s, and the grinding time is 3 times, with an interval of 25s between each time, and repeated 3 times;

[0043] Other operations are the same as Example 1. Long-acting microparticles for huperzine A injection with a particle size of less than 120 μm are obtained.

Embodiment 3

[0045] The drug loading and particle size of Huperzine A microparticles are as follows:

[0046]

[0047] Drug loading detection method:

[0048] The drug loading refers to the weight percentage of the drug contained in the microparticles.

[0049] Weigh huperzine A microparticles, add 50 times the weight of huperzine A microparticles for ultrasonic dissolution in chloroform, dilute with methanol to the final measured concentration, shake well, centrifuge, take the supernatant to determine huperzine A by HPLC method concentration to calculate the drug loading.

[0050] Particle size detection method: Take the huperzine A microparticle suspension, and measure its particle size and distribution with a LS-230 laser scattering particle size analyzer.

[0051] The mixing ratio of the suspension is as follows: 1% of long-acting microparticles for huperzine A injection, 99% of normal saline containing Tween 80, and 0.1% by weight of Tween 80 in the normal saline.

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Abstract

The invention discloses a huperzine-A particle long-acting injection and a preparation method thereof. The huperzine-A particle long-acting injection is composed of huperzine-A and a biodegradable polymer, wherein the percentage by weight of huperzine-A is 9-30%. An emulsification step is not required in the preparation method disclosed by the invention, and the preparation method is simple in preparation process and low in requirements on equipment. The prepared huperzine-A microspheres have not obvious burst release effect and can release medicine for 30 days, thus avoiding the side effects caused by a blood concentration peak-valley phenomenon occurring in case of multiple dosing; a curative effect can be kept for half a month to a month by one-time dosing, thus being beneficial to treatment for patients with dementia; moreover, the huperzine-A microspheres has the characteristic of convenience in dosing.

Description

technical field [0001] The invention relates to a long-acting injection of huperzine A microparticles. technical background [0002] Huperzine A (huperzine A, Hup A) was first isolated from Huperzia serrata (Thunb.) Trev by Liu Jiasen of the Shanghai Institute of Materia Medica in the 1980s, a lycopodium with anti-acetylcholinesterase activity The effective monomer of alkaloid (0.0216% mass fraction) was found to have a strong activity of inhibiting cholinesterase, which has aroused great interest of domestic and foreign pharmaceutical scientists. [0003] Senile dementia, also known as Alzheimer's disease (AD), is essentially a degenerative brain disease characterized by memory loss, cognitive impairment, and personality changes. It is one of the most common senile central nervous system diseases in modern society, and it is second only to cardiovascular disease, cancer, and stroke, which seriously threatens the life and health of the elderly. The reasons for the increase...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/4748A61P25/28A61J3/00
Inventor 贺芬金玉琼马庆明侯惠民
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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