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L-dopa methyl ester sustained-release microsphere composite and preparation method thereof

A technology of levodopa methyl ester and slow-release microspheres, which can be used in drug combinations, nervous system diseases, bulk delivery, etc. It can solve the problems of insufficient microspheres for initial sudden release and incomplete release, and achieve a smooth and rounded surface , regular particles, and good redispersibility

Inactive Publication Date: 2013-05-01
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the above-mentioned deficiencies in the prior art, the present invention provides a levodopa methyl ester slow-release microsphere composition and its preparation method, which solves the problems of insufficient initial burst release and incomplete release of the existing technology for long-term preparation of microspheres , using oil-in-water-solid-in-oil (S / O / W) method to prepare microspheres to further microencapsulate levodopa methyl ester particles in polymer materials with sustained release

Method used

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  • L-dopa methyl ester sustained-release microsphere composite and preparation method thereof
  • L-dopa methyl ester sustained-release microsphere composite and preparation method thereof
  • L-dopa methyl ester sustained-release microsphere composite and preparation method thereof

Examples

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Effect test

Embodiment 1

[0026] ①Preparation of levodopa methyl ester microparticles

[0027] Take 100mg of levodopa methyl ester purchased in the market, first use a microscope to observe whether it is 0.4-10 μm, if not, you can use a pulverizer to crush it into 0.4-5 μm;

[0028] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0029] (a) The polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide48-54% Mole; molecular weight is 5000-6000) that weighs 495mg is formulated into a concentration of 30% by weight The organic solution of dichloromethane and 5 mg of levodopa methyl ester microparticles obtained in ① were mixed and stirred, vortexed or ultrasonicated for 1-5 minutes to form a uniform suspension, i.e. solid-in-oil (S / O) emulsion; the prepared The theoretical percentage of levodopa methyl ester is 1% sustained-release microspheres.

[0030] (b) Add the emulsion obtained in step (a) to 10 mL of aqueous solution of 1% sodium chloride a...

Embodiment 2

[0035]①Preparation of levodopa methyl ester microparticles

[0036] Take 100mg of levodopa methyl ester purchased in the market, first use a microscope to observe whether it is 0.4-10 μm, if not, you can use a pulverizer to crush it into 0.4-5 μm;

[0037] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0038] (a) 37.5 mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide48-54% Mole; molecular weight is 5000-6000) is formulated to be 15% by weight The organic solution of dichloromethane and 12.5 mg of levodopa methyl ester microparticles obtained in ① were mixed and stirred, vortexed or ultrasonicated for 1-5 minutes to form a uniform suspension, that is, solid-in-oil (S / O) emulsion; The theoretical percentage content of the prepared levodopa methyl ester is 25% slow-release microspheres.

[0039] (b) Add the emulsion obtained in step (a) to 10 mL of aqueous solution of 5% sodium chloride and 1% polyvinyl alc...

Embodiment 3

[0044] ①Preparation of levodopa methyl ester microparticles

[0045] Take 100mg of levodopa methyl ester purchased in the market, first use a microscope to observe whether it is 0.4-10 μm, if not, you can use a pulverizer to crush it into 0.4-5 μm;

[0046] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0047] (a) 25 mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide48-54% Mole; molecular weight is 6000) is formulated into a dichloride with a weight percentage concentration of 10%. The organic solution of methane and 25 mg of the levodopa methyl ester particles weighed in ① are mixed and stirred, vortexed or ultrasonicated for 1-5 minutes to form a uniform suspension, that is, solid-in-oil (S / O) emulsion; Theoretical percentage content of dopa methyl ester is 50% sustained-release microspheres.

[0048] (b) adding the emulsion obtained in step (a) to the polyvinyl alcohol (PVA) (molecular weight is 110,00...

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Abstract

The invention discloses an L-dopa methyl ester sustained-release microsphere composite and a preparation method thereof, which belong to the technical field of medicament preparation. The L-dopa methyl ester sustained-release microsphere composite comprises the following components in percentage by weight: 50 to 99 percent of one or mixtures of polylactic acid-glycollic acid, polylactic acid and polycaprolactone and 1 to 50 percent of L-dopa methyl ester. In the invention, L-dopa methyl ester particles are prepared first and then the L-dopa methyl ester release microsphere composite is prepared by oil-in-water-oil lease solids. In the invention, the L-dopa methyl ester particles are further encapsulated in a sustained-release macromolecular material in a micro-capsule form. The surfaces of prepared microspheres are smooth and round, the homogeneous degree is high, the particles are regular and not adhered; and the encapsulation rate is high, the burst release rate is low and the drug-loading rate is high.

Description

technical field [0001] The invention relates to a composition in the technical field of pharmaceutical preparations and a preparation method thereof, in particular to a levodopa methyl ester slow-release microsphere composition and a preparation method thereof. Background technique [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. A considerable part of the drugs need long-term frequent administration to be cured; some of them need local administration due to the high toxicity of systemic administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release or controlled-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor bl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/223A61K47/34A61P25/16
Inventor 袁伟恩刘振国陈伟任甜甜杨新新
Owner SHANGHAI JIAO TONG UNIV
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