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Captopril-carrying nano-grade fiber sustained-release system and preparation method thereof

A nanofiber and sustained-release body technology, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, can solve the problem of few reports on captopril sustained-release fibers, etc. The effect of reducing the toxic and side effects of drugs, low equipment cost, and improving the effective utilization rate

Inactive Publication Date: 2012-10-17
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are also reports that captopril is made into sustained-release tablets, sustained-release pellets and other sustained-release mechanisms, but there are not many reports about captopril sustained-release fibers

Method used

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  • Captopril-carrying nano-grade fiber sustained-release system and preparation method thereof
  • Captopril-carrying nano-grade fiber sustained-release system and preparation method thereof
  • Captopril-carrying nano-grade fiber sustained-release system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] (1) Prepare a poly-L-lactic acid (PLLA) solution with a concentration of 10wt%, and the solvent is a mixed solvent of dichloromethane and acetone; in the formulated drug-carrying polymer, the concentration of captopril is 8%;

[0026] (2) In (1) the solution is added to a 5mL disposable plastic syringe, a 9 gauge needle is selected, the solution advancing rate is adjusted to 0.8ml / h, the applied voltage is 15kv, and the grounded aluminum foil is used to receive the fiber filament at the level of the needle tip. The distance is 10cm;

[0027] (3) The average diameter of the obtained drug-loaded fiber is 500nm, see Figure 2A , See the diameter distribution Figure 2D , See the cumulative release of drugs image 3 .

Embodiment 2

[0029] (1) Prepare a solution with a polyglycolic acid (PLGA) concentration of 20wt%, and the solvent is N,N-dimethylformamide;

[0030] (2) The concentration of captopril in the formulated drug-loading polymer is 15%;

[0031] (3) In (1) the solution is added to a 5mL disposable plastic syringe, a 9-gauge needle is selected, the solution advance rate is adjusted to 0.6mL / h, the applied voltage is 10kv, and the grounded aluminum foil is used to receive the fiber filament at the level of the needle tip. The distance is 20cm.

[0032] The average diameter of the obtained drug-loaded fiber is 200nm, see Figure 2B .

Embodiment 3

[0034] (1) Prepare a solution with a concentration of 20wt% of the copolymer of lactide and caprolactone (PLCL), and the solvent is N,N-dimethylformamide;

[0035] (2) In the formulated drug-loading polymer, the concentration of captopril is 12%;

[0036] (3) In (1) the solution was added to a 5mL disposable plastic syringe, a 9-gauge needle was selected, the solution advancing rate was adjusted to 0.4mL / h, the applied voltage was 10kv, and the grounded aluminum foil was used to receive the fiber filament at the level directly in front of the needle tip. The distance is 40cm.

[0037] The average diameter of the obtained drug-loaded fiber is 600nm, see Figure 2C .

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Abstract

The invention relates to a captopril-carrying nano-grade fiber sustained-release system and a preparation method thereof. The sustained-release system comprises the components of: a biodegradable high-molecular material and captopril. The drug-loading rate of the system is 8-80wt%, and the diameter of the nano-grade fiber is 80nm-1.20mum. The preparation method comprises the steps that: (1) the biodegradable high-molecular material is dissolved in an organic solvent; the mixture is stirred until the material is completely dissolved; captopril is added and the mixture is stirred; the mixture is subjected to ultrasonic deaeration, such that a spinning liquid is obtained; (2) the spinning liquid is added into an injector, and electrostatic spinning is carried out, such that the captopril-carrying nano-grade fiber sustained-release system is obtained. According to the invention, with the nano-grade sustained-release system composed of the drug-carrying nano-grade fiber, drug release is effectively controlled. The biodegradable high-molecular material can be automatically degraded with human metabolism, such that an effect of sustained-release is achieved. The process is simple, an equipment cost is low, the conditions are easy to control, and drug availability is improved.

Description

Technical field [0001] The invention belongs to the field of captopril carriers and their preparation, and particularly relates to a slow-release body containing captopril nanofibers and a preparation method thereof. Background technique [0002] Hypertension is the most common cardiovascular and cerebrovascular disease. Due to its frequency and impact on the heart, kidneys and other organs, it has become a major public health problem worldwide. [0003] Angiotensin converting enzyme (ACE) inhibitors have become the first choice for the treatment of hypertension. Captopril (Cpl) is the first angiotensin converting enzyme inhibitor to be used clinically, and is mainly used for the treatment of hypertension, heart failure and other diseases. Its chemical name is 1-[(2S)-3-mercapto-2-methylpropionyl]-Lproline (C9H15NO3S). The antihypertensive mechanism is to inhibit the activity of angiotensin converting enzyme, reduce the level of angiotensin II, Diastolic arterioles and so on. Ho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/401A61K47/34A61K47/32A61P9/12A61P9/04
Inventor 朱利民张婳权静娄少峰田利强
Owner DONGHUA UNIV
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