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Biodegradable in-situ solidification sustained-release injector

A slow-release injection, in-situ curing technology, applied in the direction of drug delivery, active ingredients of heterocyclic compounds, and medical preparations of non-active ingredients, etc., can solve the problem of low tolerance, uneven drug distribution, and release batch differences. major problems, to achieve the effect of easy acceptance and good clinical application potential

Inactive Publication Date: 2011-07-20
无锡德赛诺医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The advantage of this type of preparation is that there is no obvious burst release, but the implant has the following disadvantages: (1) high temperature operation is required in the preparation, especially not suitable for drugs with low tolerance, such as macromolecular drugs; The distribution in the drug is not uniform, and the difference between release batches is large; (3) The patient has an obvious foreign body sensation after drug administration, and is prone to discomfort at the implantation site
KukYoung Cho et al. found that PLLA-mPEG, in situ solidification, has a certain slow-release effect, but the burst release is still severe [In Situ Micro-Sized Gel-Forming Injectable Implant Using Biodegradable Amphiphilic Graft Copolymer, Macromolecular Bioscience, 7(6): 784- 788 (2007)】

Method used

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  • Biodegradable in-situ solidification sustained-release injector
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  • Biodegradable in-situ solidification sustained-release injector

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Study on the Technical Route and Quality of PDLLA-mPEG2000 Synthesis

[0043] 1.1 Synthesis, structural analysis and quality research of PDLLA-mPEG2000: The PDLLA-mPEG2000 (injection) studied by our research group has submitted an application for registration of new pharmaceutical excipients to the State Food and Drug Administration. Therefore, the synthesis, structural analysis of the polymer and quality studies will be conducted with reference to it.

[0044] Synthesis: PDLLA-mPEG 2000 98 / 2, 95 / 5, 90 / 10, 80 / 20 and 70 / 30 were synthesized by ring-opening polymerization method. That is: weigh methyl polyethylene glycol and lactide in proportion, place them in a closed reactor, raise the temperature to 120-140°C under nitrogen flow to melt the solid, add 0.5% stannous octoate, and raise the temperature to React at 150-180°C for 3-6 hours. After cooling, a white solid crude product was obtained. After the crude product is dissolved in an appropriate amount of dichlorome...

Embodiment 2

[0049] Preparation and in vitro release study of tinidazole in-situ solidified sustained-release injection

[0050] Accurately weigh a certain proportion of polymer and drug tinidazole powder according to the prescription and place it in a 10mL centrifuge tube, add a certain volume of NMP, and vortex for 30 minutes to form a transparent and uniform solution. That is, the in-situ solidified slow-release injection of tinidazole is obtained.

[0051] In vitro release test: Tinidazole in-situ solidified sustained-release injection was prepared, placed in a 10 mL centrifuge tube, and 5 mL of 0.1 mol / L, pH 7.4 PBS buffer solution at 37°C was added to solidify the preparation in situ. Put it into a constant temperature shaker to vibrate at a speed of 100 rpm, and keep the temperature at 37°C. Take 1.5mL release solution 2, 4, 6, 8, and 12 hours after in-situ solidification, and quickly add 1.5mL blank PBS buffer solution, and then take samples every 24 hours until the 8th day. Take...

Embodiment 3

[0054] Preparation and in vitro release study of leuprolide acetate in situ solidified sustained-release injection

[0055] To prepare leuprolide acetate in-situ solidified sustained-release injection that can be sustained-released for 1 month, the polymer PDLLA-mPEG was dissolved in the organic solvent NMP, vortexed and mixed until the state of a clear and transparent solution was put into syringe A, and Put 7.5mg of leuprolide acetate into syringe B, and sterilize it with gamma-ray radiation. Connect the two syringes before use, and push the piston back and forth until the drug and polymer solution are fully mixed, showing a viscous suspension state. When using, push the preparation completely into one of the syringes, remove the other syringe and connect the injection needle, and inject the preparation under the patient's skin. Take 500 μL of the injection and inject it into the back of the SD rat, and kill it 12 hours later, cut the injection site in the back, and observe ...

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Abstract

The invention relates to a biodegradable in-situ solidification slow-release injection, which consists of an amphiphilic block polymer, a medicament and an organic solvent, wherein the weight proportion of the amphiphilic block polymer to the medicament to the organic solvent is that amphiphilic block polymer: medicament: organic solvent is equal to 100: 1-90: 1-10,000.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation, which belongs to the field of polymer chemistry and pharmacy. To be precise, it is an injectable in-situ solidification preparation with both degradability and controlled release characteristics. It is a new type of biodegradable implantable drug delivery system (Biodegradable Implantable Drug Delivery Systems, hereinafter referred to as BIDDS), which is a kind of long-term drug delivery system that is surgically implanted or injected into the body. Background technique: [0002] In recent years, BIDDS has become an important research area of ​​drug delivery systems. BIDDS has many advantages, including: (1) patients do not need frequent administration, and the compliance is better; (2) compared with oral preparations, it is less affected by the environment of the gastrointestinal tract and the "first-pass effect" of the liver, and the bioavailability of the drug is less High, individual differe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K9/10A61K47/34A61K38/08A61K31/337A61K31/4164A61K31/4422A61K31/445A61K31/65
Inventor 涂家生张东晓吴建梅苏丹刘婧
Owner 无锡德赛诺医药科技有限公司
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