Pramipexole sustained-release preparation for injection and preparation method thereof

A technology of pramipexole and sustained-release preparations, applied in the field of medicine, can solve problems such as difficult to control exercise-related symptoms, easily lead to exercise complications, and reduce patient compliance, so as to improve compliance, improve biocompatibility, and sustain The effect of steady drug release

Active Publication Date: 2018-10-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The traditional treatment of Parkinson's disease usually uses levodopamine, but long-term use can easily lead to motor complications
At present, the new concept of treatment of Parkinson's disease is continuous dopaminergic stimulation (continuous dopaminergic stimulation, CDS), continuous dopaminergic stimulation is mainly achieved by continuous administration of levodopa or dopamine receptor agonists, however, due to the " "Peak-valley" phenomenon, treating Parkinson's disease through continuous dopaminergic stimulation is likely to cause pulse-like stimulation, resulting in difficulty in controlling motor-related symptoms and reducing patient compliance

Method used

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  • Pramipexole sustained-release preparation for injection and preparation method thereof
  • Pramipexole sustained-release preparation for injection and preparation method thereof
  • Pramipexole sustained-release preparation for injection and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0060] This example provides a pramipexole sustained-release preparation for injection, which is composed of the following raw materials: pramipexole hydrochloride 150mg, internal aqueous phase additive 25mg, PLGA 0.75g, organic phase additive 0.25g, poloxa 200mg / ml Mu 188 and 20mg / ml chitosan gel solution 10ml, mannitol 100mg.

[0061] The pramipexole hydrochloride is a dopamine receptor agonist, which is highly selective and specific in binding to the D2 subfamily of dopamine receptors, has preferential affinity for the D2 receptors, and has complete intrinsic activity. Dopamine receptors in the striatum alleviate motor impairment in Parkinson's disease. The half-life of the pramipexole hydrochloride is short, being 8-12 hours.

[0062] Described poloxamer (Poloxamer) is polyoxyethylene-polyoxypropylene block copolymer, trade name is Pluronic (Pluronic), according to the proportioning of ethylene oxide and propylene oxide in polymerization, poloxamer There are a series of ...

Embodiment 2

[0125] This embodiment provides a pramipexole sustained-release preparation for injection, which consists of the following raw materials: 150 mg of pramipexole hydrochloride, 25 mg of internal aqueous phase additives, 1.0 g of PLGA, 0.25 g of organic phase additives, 10 ml of gel solution, manna Alcohol 100mg.

[0126] The internal water phase additive is a mixture of poloxamer and chitosan, wherein the mass ratio of poloxamer shell to polysaccharide is 20mg / 5mg.

[0127] The molar ratio of lactide and glycolide in the PLGA is 75 / 25, and the molecular weight of the PLGA is 50kDa.

[0128] The organic phase additive is a mixture of poloxamer 407 and chitosan, wherein the mass ratio of poloxamer 407 to chitosan is 0.2g / 0.05g.

[0129] The gel solution was formed from 150 mg / ml poloxamer 188 and 75 mg / ml chitosan.

[0130] This embodiment also provides a preparation method of the pramipexole sustained-release preparation for injection, comprising the following steps:

[0131] ...

Embodiment 3

[0144] This embodiment provides a pramipexole sustained-release preparation for injection, which consists of the following raw materials: 150 mg of pramipexole hydrochloride, 25 mg of internal aqueous phase additives, 1.0 g of PLGA, 0.25 g of organic phase additives, 10 ml of gel solution, manna Alcohol 100mg.

[0145] The internal water phase additive is a mixture of poloxamer and chitosan, wherein the mass ratio of poloxamer to chitosan is 20mg / 5mg.

[0146] The molar ratio of lactide and glycolide in the PLGA is 50 / 50, and the molecular weight of the PLGA is 60kDa.

[0147] The organic phase additive is a mixture of poloxamer 407 and chitosan, wherein the mass ratio of poloxamer 407 to chitosan is 0.2g / 0.05g.

[0148] The gel solution was formed from 50 mg / ml chitosan and 200 mg / ml poloxamer 188.

[0149] This embodiment also provides a preparation method of the pramipexole sustained-release preparation for therapeutic injection, comprising the following steps:

[0150] ...

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Abstract

The invention relates to a pramipexole sustained-release preparation for injection and a preparation method thereof, belonging to the technical field of medicines. The preparation method comprises thefollowing steps: dissolving a main drug and an internal water phase additive into water for injection so as to form a main drug-containing internal water phase solution; dissolving PLGA and an organic phase additive into an organic solvent so as to form an organic phase solution; mixing the main drug-containing internal water phase solution with the organic phase solution and carrying out ultrasonic treatment so as to form a primary water-in-oil emulsion; adding the primary water-in-oil emulsion into an external water phase solution, and carrying out stirring so as to form a water-in-oil-in-water multiple emulsion; solidifying the water-in-oil-in-water multiple emulsion so as to form microspheres, carrying out centrifugal washing, and collecting the microspheres so as to obtain wet microspheres; adding a gel solution and a freeze-drying protective agent into the wet microspheres so as to obtain a microsphere gel solution; and subjecting the microsphere gel solution to freeze-drying. The pramipexole sustained-release preparation for injection provided by the invention has high drug loading capacity and good temperature sensitivity and biological compatibility, sustainably and stably releases drugs, can effectively reduce the occurrence of motor complications, and improves the compliance of a patient.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pramipexole sustained-release preparation for injection and a preparation method thereof. Background technique [0002] Parkinson's disease (PD), also known as Parkinson's paralysis, is an extrapyramidal disorder and one of the most common neurodegenerative diseases. The main pathological change of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the midbrain, which leads to a significant decrease in the content of dopamine in the striatum and causes the disease. [0003] The traditional treatment of Parkinson's disease usually uses levodopamine, but long-term use can easily lead to motor complications. At present, the new concept of treatment of Parkinson's disease is continuous dopaminergic stimulation (continuous dopaminergic stimulation, CDS), continuous dopaminergic stimulation is mainly achieved by continuous administ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/16A61K9/06A61K47/10A61K47/36A61K31/428A61P25/16
CPCA61K9/0002A61K9/0019A61K9/06A61K9/1641A61K9/1647A61K9/1652A61K9/19A61K31/428A61K47/10A61K47/34A61K47/36
Inventor 王淑君童超叶田田
Owner SHENYANG PHARMA UNIVERSITY
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