Triptolide autolytic microneedle

A technology of triptolide and self-dissolving microneedles, which is applied in the direction of microneedles, needles, organic active ingredients, etc., to achieve the effects of stable and feasible process, improved drug safety, and good mechanical strength

Active Publication Date: 2021-09-07
GUIZHOU YANGSHENG MEDICAL INSTR
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There is no research on the combination of triptolide with microneedles

Method used

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  • Triptolide autolytic microneedle
  • Triptolide autolytic microneedle
  • Triptolide autolytic microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1, a triptolide self-dissolving microneedle, according to parts by weight, the tip matrix prescription of the triptolide self-dissolving microneedle is 24 parts of PVP, 7.8 parts of PVA, 0.45 parts of CMC-Na, 0.28 parts of triptolide, 40 parts of distilled water and 20 parts of absolute ethanol; the prescription of the backing layer matrix of the triptolide self-dissolving microneedle is 32 parts of PVP, 9 parts of PVA and 53 parts of distilled water.

[0067] Triptolide self-dissolving microneedles are prepared according to the following steps:

[0068] (1) Preparation of needles: According to the needle tip matrix prescription of triptolide self-dissolving microneedles, the needle tip materials were weighed and fully dissolved and stirred evenly, then poured into the microneedle mold, centrifuged at 3900r / min for 8min, removed and collected on the surface of the microneedle mold The drug-containing matrix solution was put into a desiccator to dry for 5 hours t...

Embodiment 2

[0070] Example 2, a triptolide self-dissolving microneedle, in parts by weight, the tip matrix prescription of the triptolide self-dissolving microneedle is 29 parts of PVP, 8.3 parts of PVA, 0.65 parts of CMC-Na, 0.42 parts of triptolide, 45 parts of distilled water and 23 parts of absolute ethanol; the prescription of the backing layer matrix of the triptolide self-dissolving microneedle is 37 parts of PVP, 12 parts of PVA and 58 parts of distilled water.

[0071] Triptolide self-dissolving microneedles are prepared according to the following steps:

[0072] (1) Preparation of needles: according to the needle tip matrix prescription of triptolide self-dissolving microneedles, the needle tip materials were weighed and fully dissolved, stirred evenly, poured into the microneedle mold, centrifuged at 4100r / min for 12min, and removed and collected on the surface of the microneedle mold. The drug-containing matrix solution was put into a desiccator to dry for 7 hours to obtain a ...

Embodiment 3

[0074] Example 3, in parts by weight, the tip matrix prescription of the triptolide self-dissolving microneedles is 26 parts of PVP, 8 parts of PVA, 0.5 parts of CMC-Na, 0.3 parts of triptolide, 42 parts of distilled water and 21 parts of absolute ethanol; the prescription of the backing layer matrix of the triptolide self-dissolving microneedle is 34 parts of PVP, 10 parts of PVA and 55 parts of distilled water.

[0075] Triptolide self-dissolving microneedles are prepared according to the following steps:

[0076] (1) Preparation of needles: according to the needle tip matrix prescription of triptolide self-dissolving microneedles, weigh the needle tip material to fully dissolve and stir evenly, inject it into the microneedle mold, centrifuge at 3950r / min for 9min, remove and collect the microneedle mold surface The drug-containing matrix solution was put into a desiccator to dry for 5.5 hours to obtain a microneedle mold with drug-containing needle tip;

[0077] (2) Prepar...

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Abstract

The invention discloses a triptolide autolytic microneedle. A prescription of a needle tip matrix of the triptolide autolytic microneedle comprises the following components of, in parts by weight, 24-29 parts of PVP (Polyvinyl Pyrrolidone), 7.8-8.3 parts of PVA (Polyvinyl Alcohol), 0.45-0.65 part of CMC-Na (Sodium Carboxymethyl Cellulose), 0.28-0.42 part of triptolide, 40-45 parts of distilled water and 20-23 parts of absolute ethyl alcohol; and a prescription of a backing layer matrix of the triptolide autolytic microneedle comprises the following components of, in parts by weight, 32-37 parts of PVP (Polyvinyl Pyrrolidone), 9-12 parts of PVA (Polyvinyl Alcohol) and 53-58 parts of distilled water. The microneedle has good microneedle formability and mechanical strength, an RSD value of a medicine loading capacity is 0.98%, a process is stable and feasible, a needle tip of a medicine-loading microneedle enables most of medicines to rapidly reach a body to take effect rapidly, and the medicine use safety of the triptolide can be improved due to a slow-release effect of a microneedle matrix; and by reducing inflammatory infiltration of cells in a synovial membrane, the expression of inflammatory factors such as TNF-alpha, IL-17, PGE2, IgG, IgM and IgA can be reduced, the expression of OPG can be increased, the expression of RANKL and an RANKL / OPG ratio can be reduced, and rheumatoid arthritis can be treated.

Description

technical field [0001] The invention belongs to the technical field of self-dissolving microneedles, in particular to a triptolide self-dissolving microneedle. Background technique [0002] Triptolide (TP), one of the main components of tripterygium glycosides, is both the main active component and the toxic component. It is the main component of the current quality control standard of Tripterygium wilfordii preparations. A number of studies have found that TP has the following properties: (1) It is almost insoluble in pure water. In clinical research, it has low bioavailability, poor absorption, and it is difficult for the blood drug concentration to reach the therapeutic concentration. (2) The elimination rate in the body is fast and non-linear, and it is mainly excreted through feces, urine, and bile; (3) The lethal dose is small and the half-lives are 31 days and 204 days, respectively, and TP is in chloroform. Good stability, while alkaline media and hydrophilic solve...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/585A61K47/32A61K47/38A61P29/00A61P19/02A61M37/00
CPCA61K9/0021A61K31/585A61K47/32A61K47/38A61P29/00A61P19/02A61M37/0015A61M2037/0046A61M2037/0053Y02A50/30
Inventor 张永萍陈鑫徐剑刘耀
Owner GUIZHOU YANGSHENG MEDICAL INSTR
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