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Bulleyaconitine A dissoluble microneedle patch and preparation method thereof

A technology of aconitin and microneedle paste, which is applied in the direction of microneedle, needle, sheet delivery, etc., can solve the problems of skin discomfort symptoms, allergies, and restrictions on wide application, and achieve easy promotion, good compliance, and preparation method simple effect

Pending Publication Date: 2020-08-25
YUNNAN INST OF MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, reactions such as oral numbness are common in oral administration, which to some extent limits the wide application of the drug in clinical practice.
Compared with oral administration preparations, injection administration has a quick onset of action and significant curative effect. However, due to the narrow therapeutic index of aconitin, the difference between the toxic dose and the effective dose is not large. Therefore, the peak plasma concentration of injection administration is higher Not conducive to the control of side effects
[0009] There are also some researchers who have developed a transdermal patch of aconitin to avoid the disadvantages of oral administration and injection. However, due to the hindrance of the stratum corneum, the aconitin in the transdermal patch is not easy to penetrate the skin. Absorbed by the human body, it usually takes a long time to apply, which often leads to skin discomfort and even allergies. In addition, its absorption is not ideal

Method used

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  • Bulleyaconitine A dissoluble microneedle patch and preparation method thereof
  • Bulleyaconitine A dissoluble microneedle patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A kind of aconitin dissolvable microneedle patch, its structure is as follows figure 1 As shown, it includes a needle body 4 and a matrix layer 3, the needle body 4 includes a support layer 2 and a needle tip drug-loaded layer 1 above the support layer 2, the support layer 2 is bonded on the base layer 3, The drug composition in the drug-loaded layer 1 of the needle tip includes a high molecular polymer, aconitin and ethanol. The specific preparation method is as follows:

[0037] (1) Preparation of needle tip drug-loaded layer solution: according to the mass ratio of 20% aconitin, 3% PVP K30, 17% Gantrez S-97, 60% ethanol, aconitin, PVP K30, Gantrez S -97 is dissolved in 60% ethanol (v / v) to obtain the product.

[0038] (2) Preparation of support layer and base layer solution: dissolve hyaluronic acid in water to obtain a 50% (w / w) hyaluronic acid solution.

[0039] (3) Weigh 0.5 g of the needle tip drug-loaded layer solution, add it to the microneedle mold, and cen...

Embodiment 2

[0046] According to the preparation process of Example 1, the preparation structure is as follows figure 1 The shown aconitin dissolvable microneedle patch, the specific preparation method is as follows:

[0047] (1) Preparation of the needle tip drug-loaded layer solution: according to the mass ratio of 40% aconitin, 7% PEG10000, 13% Gantrez S-97, 40% ethanol, the aconitin, PEG10000, Gantrez S-97 Soluble in 60% ethanol (v / v), that is.

[0048] (2) Preparation of support layer and base layer solution: dissolving sodium hyaluronate in water to prepare a 50% (w / w) hyaluronic acid solution.

[0049] (3) Weigh 0.5 g of the needle-tip drug-loaded layer solution, add it into the microneedle mold, and evacuate until the vacuum degree is 0.06 MPa-0.1 MPa.

[0050] (4) Weigh 0.4 g of the solution of the support layer and the base layer, add it into the microneedle mold, evacuate to a vacuum degree of 0.06MPa-0.1MPa, and gently scrape off the excess solution.

[0051] (5) Dry the mic...

Embodiment 3

[0055] A kind of aconitin dissolvable microneedle patch such as figure 1 As shown, the drug loading amount of quincetin is 200μg, and the microneedle density is 100 needles / cm 2 , the length of the needle is 700 μm, and the length of the drug-loaded layer at the needle tip is 500 μm. The preparation method comprises the following steps:

[0056] (1) Preparation of needle tip drug-loaded layer solution: according to the mass ratio of 40% aconitin, 3% PVP K30, 17% Gantrez S-97, 40% ethanol, aconitin, PEG10000, Gantrez S- 97 was dissolved in 60% ethanol (v / v) to obtain the product.

[0057] (2) Preparation of support layer solution: Dissolve PVP K90 in water to obtain a 30% (w / w) aqueous solution.

[0058] (3) Preparation of the base layer solution: dissolving sodium hyaluronate in water to obtain a 50% (w / w) hyaluronic acid solution.

[0059] (4) Weigh 0.5 g of the needle-tip drug-loaded layer solution, add it into the microneedle mold, and evacuate until the vacuum degree is...

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Abstract

The invention relates to the technical field of traditional Chinese medicine, and concretely discloses a Bulleyaconitine A dissoluble microneedle patch and a preparation method thereof. The Bulleyaconitine A dissoluble microneedle patch disclosed by the invention comprises needle bodies and a substrate layer, wherein each needle body comprises a support layer and a needle point medicine carrying layer on the support layer; the support layers are bonded on the substrate layer; the composition of medicine in the needle point medicine carrying layers includes high-molecular polymers, Bulleyaconitine A and ethanol; and the high-molecular polymers are one or more of polyvinylpyrrolidone, methyl vinyl ether-cis-butenedioic anhydride copolymers and polyethylene glycol. The microneedle patch disclosed by the invention has the advantages that the Bulleyaconitine A indissoluble in water can be made into a dissoluble microneedle patch by combining with a microneedle technology, the efficient transdermal administration of the Bulleyaconitine A is realized; the administration mode is minimally invasive administration; the compliance of a patient is good; and the autonomous administration can berealized.

Description

technical field [0001] The invention relates to the technical field of traditional Chinese medicines, in particular to an aconitin soluble microneedle patch and a preparation method thereof. Background technique [0002] Microneedle (microneedle) is a new type of transdermal drug delivery method, which can solve the problem of low delivery efficiency of transdermal patches. Solid needle-like structure, the length generally does not exceed 1.0mm. After the microneedle pierces the stratum corneum of the skin, tiny channels can be formed to allow the drug to enter the body efficiently, which can improve the bioavailability of the drug and reduce the dosage. However, the depth of its penetration into the skin is shallow and basically does not trigger pain receptors, and there is no pain when used. The pores formed by microneedle puncture usually heal within 2 hours. [0003] Microneedles include solid microneedles, hollow microneedles, and dissolvable microneedles. Among them,...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/439A61K47/32A61K47/10A61P29/00A61P25/04A61P19/02A61M37/00
CPCA61K9/0021A61K9/7023A61K31/439A61K47/32A61K47/10A61P29/00A61P25/04A61P19/02A61M37/0015A61M2037/0023A61M2037/0053
Inventor 董汛丁江生王京昆孙思颖孙文强周云龙张天财
Owner YUNNAN INST OF MATERIA MEDICA
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