Nano-fibers with drug two-phase pulse releasing function and preparation method

Abstract

The invention provides nano-fibers with a drug two-phase pulse releasing function. Each nano-fiber comprises a main fiber bundle; a parallel fiber bundle is arranged at the outer side of the main fiber bundle; the main fiber bundle and the parallel fiber bundle extend along the length direction; in a radial section, the parallel fiber bundle covers 40 percent to 70 percent of the periphery of the main fiber bundle; the main fiber bundle is composed of a drug and a pharmaceutical excipient which is easily dissolved into water; the parallel fiber bundle is composed of a drug and a polymer pharmaceutical excipient which can be dissolved under neutral and alkaline conditions. The invention further provides a preparation method of the nano-fibers; the preparation method comprises the following steps: blending the drug and the pharmaceutical excipient which is easily dissolved into the water to form a co-dissolved solution; blending the drug and the polymer pharmaceutical excipient which can be dissolved under the neutral and alkaline conditions to form a co-dissolved solution; controlling speeds of injecting the two solutions into a parallel spinning head through two sets of injection pumps respectively; preparing the nano-fibers with the drug two-phase pulse releasing function under the action of high voltage and static electricity. According to the nano-fibers with the drug two-phase pulse releasing function, the carried drug can be regulated and controlled and be released in a two-phase pulse manner.

Description

technical field

[0001] The invention belongs to the field of material science, and relates to a drug sustained and controlled release nanometer material, specifically a nanofiber with two-phase pulse release function of a drug and a preparation method thereof. Background technique

[0002] High-voltage electrospinning technology (electrospinning) is a top-down nano-manufacturing technology. The jet is formed by overcoming the liquid surface tension and viscoelastic force of the droplets at the tip of the nozzle by applying an electric field force. Under the joint action of Coulomb force and surface tension, the liquid jet is bent, stretched, and split by high frequency, and is stretched tens of millions of times within tens of milliseconds. After solvent volatilization or melt cooling, nano-scale fibers are obtained at the receiving end. This technology has the advantages of simple process, convenient operation, wide selection of materials, and strong controllability. It i...

Examples

Embodiment 1

[0030] Example 1: Parallel electrospinning process implementation and preparation of Jonas nanofibers

[0031] Dissolve 1 gram of drug ibuprofen and 7 grams of polyvinylpyrrolidone K60 in 100 ml of absolute ethanol to prepare a side working fluid.

[0032] Dissolve 1 gram of drug ibuprofen and 13 grams of fiber-forming polymer Eudragit L-100 in 100 ml of absolute ethanol to prepare the working fluid on the other side of the side-by-side electrospinning.

[0033] Put the above two working fluids into the corresponding syringes 7 and 8 respectively, install them on the respective syringe pumps 2 and 3, and connect them to the inlet of the parallel spinning head 4, and connect the high-pressure spinning head 4 and the high-pressure generator 1.

[0034] The speed at which the parallel solution is injected into the parallel spinning head is controlled respectively by two syringe pumps 2 and 3, the parallel flow rate is 1.0mL / h, the distance between the fiber receiving plate 5 and...

Embodiment 2

[0037] Example 2: Structural and Morphological Characterization of Jonas Nanofibers for Biphasic Pulse Release of Drugs

[0038] Field emission scanning electron microscopy (FESEM) was used to observe the surface of the fiber prepared in Example 1 after spraying gold, and the results were as follows image 3 shown. The prepared fiber exhibits a good linear state, no beading structure occurs, the fiber surface is smooth, and the fiber accumulation is uniform. The diameter is 670 ± 110 nm, the distribution is relatively uniform, and the diameter distribution is relatively concentrated.

[0039] The internal structure of the prepared fiber was observed by high-resolution transmission electron microscope (TEM), and the results were as follows: Figure 4 As shown, the bilateral side-by-side structural features of Jonas nanofibers are clear. The internal structure of the fiber is as Figure 5 As shown, the drug 33 is uniformly distributed among the Jonas nanofibers on the left 1...

Embodiment 3

[0040] Example 3: Functional Analysis of Drug Controlled Release of Jonas Nanofibers in Biphasic Pulse Release of Drugs

[0041] According to the 2015 edition of Chinese Pharmacopoeia Appendix ⅩD Release Test Method 2, the RCZ-8A intelligent dissolution tester was used to conduct the in vitro dissolution test on the drug-loaded nanofibers obtained above. The control speed is 50rpm, and the temperature is 37±0.1°C. In the first 2 hours, 900 mL of artificial gastric juice without enzymes was used as the dissolution medium, followed by 900 mL of artificial intestinal juice (pH6.8 phosphate buffer solution) without enzymes as the dissolution medium to investigate the drug release properties of nanofibers in vitro. Sampling 5mL at the scheduled time, filtered through a 0.22 µm microporous membrane to obtain the eluate sample, and immediately replenished with the same volume of isothermal fresh medium. After diluting the sample appropriately, at λ=257 nm, UV-Vis spectrophotometer w...

technical field

[0001] The invention belongs to the field of material science, and relates to a drug sustained and controlled release nanometer material, specifically a nanofiber with two-phase pulse release function of a drug and a preparation method thereof. Background technique

[0002] High-voltage electrospinning technology (electrospinning) is a top-down nano-manufacturing technology. The jet is formed by overcoming the liquid surface tension and viscoelastic force of the droplets at the tip of the nozzle by applying an electric field force. Under the joint action of Coulomb force and surface tension, the liquid jet is bent, stretched, and split by high frequency, and is stretched tens of millions of times within tens of milliseconds. After solvent volatilization or melt cooling, nano-scale fibers are obtained at the receiving end. This technology has the advantages of simple process, convenient operation, wide selection of materials, and strong controllability. It i...

Examples

Embodiment 1

[0030] Example 1: Parallel electrospinning process implementation and preparation of Jonas nanofibers

[0031] Dissolve 1 gram of drug ibuprofen and 7 grams of polyvinylpyrrolidone K60 in 100 ml of absolute ethanol to prepare a side working fluid.

[0032] Dissolve 1 gram of drug ibuprofen and 13 grams of fiber-forming polymer Eudragit L-100 in 100 ml of absolute ethanol to prepare the working fluid on the other side of the side-by-side electrospinning.

[0033] Put the above two working fluids into the corresponding syringes 7 and 8 respectively, install them on the respective syringe pumps 2 and 3, and connect them to the inlet of the parallel spinning head 4, and connect the high-pressure spinning head 4 and the high-pressure generator 1.

[0034] The speed at which the parallel solution is injected into the parallel spinning head is controlled respectively by two syringe pumps 2 and 3, the parallel flow rate is 1.0mL / h, the distance between the fiber receiving plate 5 and...

Embodiment 2

[0037] Example 2: Structural and Morphological Characterization of Jonas Nanofibers for Biphasic Pulse Release of Drugs

[0038] Field emission scanning electron microscopy (FESEM) was used to observe the surface of the fiber prepared in Example 1 after spraying gold, and the results were as follows image 3 shown. The prepared fiber exhibits a good linear state, no beading structure occurs, the fiber surface is smooth, and the fiber accumulation is uniform. The diameter is 670 ± 110 nm, the distribution is relatively uniform, and the diameter distribution is relatively concentrated.

[0039] The internal structure of the prepared fiber was observed by high-resolution transmission electron microscope (TEM), and the results were as follows: Figure 4 As shown, the bilateral side-by-side structural features of Jonas nanofibers are clear. The internal structure of the fiber is as Figure 5 As shown, the drug 33 is uniformly distributed among the Jonas nanofibers on the left 1...

Embodiment 3

[0040] Example 3: Functional Analysis of Drug Controlled Release of Jonas Nanofibers in Biphasic Pulse Release of Drugs

[0041] According to the 2015 edition of Chinese Pharmacopoeia Appendix ⅩD Release Test Method 2, the RCZ-8A intelligent dissolution tester was used to conduct the in vitro dissolution test on the drug-loaded nanofibers obtained above. The control speed is 50rpm, and the temperature is 37±0.1°C. In the first 2 hours, 900 mL of artificial gastric juice without enzymes was used as the dissolution medium, followed by 900 mL of artificial intestinal juice (pH6.8 phosphate buffer solution) without enzymes as the dissolution medium to investigate the drug release properties of nanofibers in vitro. Sampling 5mL at the scheduled time, filtered through a 0.22 µm microporous membrane to obtain the eluate sample, and immediately replenished with the same volume of isothermal fresh medium. After diluting the sample appropriately, at λ=257 nm, UV-Vis spectrophotometer w...

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