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Needle tip liquid, microneedle patch as well as preparation method and application of microneedle patch

A technology of microneedle sticking and needle tip, which is applied in the direction of pharmaceutical formulations, other medical devices, and medical preparations with non-active ingredients, etc. It can solve the problems of poor mechanical properties, poor mechanical properties of microneedles, and reduce the accumulation of antibacterial drugs, etc.

Pending Publication Date: 2022-07-12
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the microneedles prepared by pure ε-polylysine are brittle in texture and poor in mechanical properties, and it is difficult to pierce the stratum corneum of the skin. It is necessary to add certain polymer excipients and mix them to prepare microneedles.
If the content of excipients is high, it will occupy most of the space at the tip of the microneedle and reduce the accumulation of antibacterial drugs at the tip; if the content of excipients is too low, the mechanical properties of the microneedle will be poor

Method used

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  • Needle tip liquid, microneedle patch as well as preparation method and application of microneedle patch
  • Needle tip liquid, microneedle patch as well as preparation method and application of microneedle patch
  • Needle tip liquid, microneedle patch as well as preparation method and application of microneedle patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation and characterization of antibiotic-free ε-PLL / PVA soluble microneedle patches

[0051] 1. Preparation of the negative microneedle mold

[0052] Place the four-pyramid-shaped metal microneedle male mold (the height of the microneedles is 1200 μm, the width of the bottom is 300 μm, the distance between the tips of the needles is 800 μm, and the number of microneedles is 12×12) in absolute ethanol, ultrasonic for 20 minutes, and after repeated cleaning, the The male mold was placed at room temperature until the ethanol on its surface was completely evaporated. 9 mL of polydimethylsiloxane (PDMS) and 0.9 mL of curing agent (Dow Corning, USA) were mixed uniformly in a ratio of 10:1 (w / w) and stirred evenly, and the air bubbles were removed by vacuum for about 10 minutes. Pour the liquid PDMS containing the curing agent from the bubbles slowly into the male mold (6 g), then place it in a vacuum drying oven, connect the vacuum pump to degas for 45 minutes, until t...

Embodiment 2

[0060] Skin penetration performance of ε-PLL / PVA dissolvable microneedle patch without antibiotics

[0061] The mouse skin stratum corneum was flattened up on a flat plate, fixed with tacks, and after hair removal, the microneedle patch (ε-PLL:PVA-103=1:1) described in Example 1 was inserted into the skin, press 1 minutes, stick for 4 minutes, then remove the microneedles. Wash off the melted microneedle liquid with clean water, dip the skin surface with 4% (0.4g / 10mL) trypan blue solution for a period of time (about 2 minutes), remove the dye with clean water, dry it with tape to remove the background color , and observe the dyed pores on the skin surface and the removed microneedle tips. ( figure 2 )

[0062] figure 2 It shows that the soluble microneedle patch obtained by the prescription of ε-PLL:PVA-103=1:1 combines the hardness of ε-PLL and the toughness of macromolecular materials, and has good mechanical strength and puncture rate. reach more than 99%. image 3...

Embodiment 3

[0063] Example 3 Comparison of Microneedle Patches Constructed by Combinations of Different Excipients

[0064] ε--PLL was selected as the main needle tip matrix material, PVP, PVA or dextran (Dex 40) was used to improve the needle tip performance, and PVP K90 with an average molecular weight of 1300kDa was used as the base layer material to construct different soluble microneedle patches (for other parameters, please refer to Refer to the preparation method of Example 1). The experimental results see Figure 4 , when ε-PLL is matched with different excipients in different proportions, the quality of the prepared microneedles is different. When ε-PLL is used alone or with PVP k30 and Dex 40 alone, the prepared microneedles have uneven texture and high needle breakage rate, while when a certain proportion of PVA-103 is added to the prescription, the prepared microneedles break The needle rate is greatly reduced; the microneedles prepared by ε-PLL and PVA-103 are uniform in te...

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Abstract

The invention discloses a microneedle tip liquid, a soluble microneedle patch prepared from the microneedle tip liquid, and a preparation method and application of the soluble microneedle patch. The microneedle tip is prepared from a needle tip matrix material and a medicine, and the needle tip matrix material comprises epsilon-polylysine and polyvinyl alcohol. The prepared soluble microneedle is high in drug loading capacity (the total amount of antibacterial active ingredients reaches 2319.1 mu g / tablet), the needle tip strength of the microneedle is high, and the skin puncture rate of the microneedle can be greatly increased (the puncture rate reaches 99%). The microneedle patch can be used for skin antibiosis and can be used for treatment of skin diseases.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to needle tip liquids, microneedle patches and their preparation methods and applications. Background technique [0002] According to the latest global epidemic statistics study "Global Burden of Disease Study 2016 (GBD)", among the top 10 diseases with the highest incidence in 2016, three of them are skin diseases, including those caused by bacterial infections Pyoderma, fungal skin diseases caused by fungal infections and other skin and subcutaneous diseases. Skin diseases, especially infectious skin diseases caused by bacteria and fungi, have become an important issue affecting human health that cannot be ignored. [0003] Infectious skin diseases are mainly treated with topical drugs. The reasons are: ① Act directly on the skin target site; ② Long local stay time can better control symptoms; ③ External use has less absorption and can avoid poor systemic adm...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/198A61K47/32A61K45/06A61K47/34A61K9/00A61M37/00A61P31/02A61P17/00A61K31/65
CPCA61K9/08A61K47/34A61K47/32A61K45/06A61K31/198A61K31/65A61K9/0021A61P17/00A61P31/02A61M37/0015A61M2037/0053A61M2037/0046A61K2300/00Y02A50/30
Inventor 陆超罗芮吴传斌潘昕周桂玲权桂兰
Owner JINAN UNIVERSITY
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