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Triamcinolone acetonide soluble micro-needle and preparation method thereof

A soluble, microneedle technology, applied in microneedles, needles, pharmaceutical formulations, etc., can solve the problems of insufficient skin puncture efficiency, low solubility of triamcinolone acetonide, and reduced drug delivery efficacy, so as to reduce the difficult to control and improve the dosage of drug delivery. Needle tip drug loading rate and risk reduction effect

Inactive Publication Date: 2018-08-17
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dose of triamcinolone acetonide used in the treatment of scars is relatively large, and the current microneedles generally have low drug loading, and the drug migration is relatively serious, resulting in most of the drugs being concentrated at the base of the microneedle patch, greatly Reduced drug efficacy
In addition, the solubility of triamcinolone acetonide in water is extremely low, and when it is prepared into soluble microneedles using the existing microneedle excipient prescription, the drug loading capacity of the microneedles is lower. Therefore, triamcinolone acetonide is prepared into soluble microneedles To treat hypertrophic scars or keloids, the drug loading capacity and tip drug loading rate of the microneedles need to be improved urgently
In addition, the mechanical strength of current soluble microneedles is still lower than that of solid microneedles made of metal or silicon, and the puncture efficiency of the skin is insufficient.

Method used

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  • Triamcinolone acetonide soluble micro-needle and preparation method thereof
  • Triamcinolone acetonide soluble micro-needle and preparation method thereof
  • Triamcinolone acetonide soluble micro-needle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Example 1 Preparation of triamcinolone acetonide soluble microneedles

[0048] In this embodiment, triamcinolone acetonide soluble microneedles (referred to as TA-DMNA-1) are prepared. The shape of the needle tip is bullet-shaped, the height of the cylindrical support structure of the needle tip is 700 μm, and the height of the conical needle tip structure is 500 μm. The diameter of the bottom of the cone is 300 μm, the distance between the tops of the cones of two adjacent needle points is 900 μm, and the base is a circle with a diameter of 2 cm. The preparation of the soluble microneedle comprises the following steps:

[0049] 1. Preparation of drug inclusion complex solution (TA-HP-β-CD-IC)

[0050] Accurately weigh 0.4345 g (0.001 mol) of triamcinolone acetonide (TA) and 12.8427 (0.009 mol) of hydroxypropyl-β-cyclodextrin (HP-β-CD), add 10 mL of water, stir to dissolve, and use magnetic stirring Stir at 200rpm for 4 hours, centrifuge at 4000rpm for 10min to take t...

Embodiment 2

[0060] Example 2 Preparation of triamcinolone acetonide soluble microneedles

[0061] In this example, the preparation of triamcinolone acetonide soluble microneedles (TA-DMNA-2) is carried out. The shape of the needle tip is bullet-shaped, the height of the cylindrical support structure of the needle tip is 700 μm, and the height of the conical needle tip structure is 500 μm. The diameter of the bottom is 300 μm, the distance between the tops of the cones of two adjacent needle tips is 900 μm, and the base is a circle with a diameter of 2 cm. The preparation of the soluble microneedle comprises the following steps:

[0062] 1. Preparation of TA-HP-β-CD-IC aqueous solution

[0063] Accurately weigh 0.4345 g (0.001 mol) of triamcinolone acetonide raw material, 12.8427 g (0.009 mol) of HP-β-CD, add water 10 mL, stir to dissolve, and use a magnetic stirrer to stir at 200 rpm for 4 hours, and centrifuge at 4000 rpm for 10 min Take the supernatant to obtain the TA-HP-β-CD-IC aque...

Embodiment 3

[0073] Example 3 Preparation of triamcinolone acetonide soluble microneedles

[0074] In this example, the preparation of triamcinolone acetonide soluble microneedles (TA-DMNA-3) is carried out. The shape of the needle tip is bullet-shaped, the height of the cylindrical support structure of the needle tip is 700 μm, and the height of the conical needle tip structure is 500 μm. The diameter of the bottom is 300 μm, the distance between the tops of the cones of two adjacent needle tips is 900 μm, and the base is a circle with a diameter of 2 cm. The preparation of the soluble microneedle comprises the following steps:

[0075] 1. Preparation of TA-HP-β-CD-IC aqueous solution

[0076]Accurately weigh 0.4345g (0.001mol) of triamcinolone acetonide raw material, 12.8427g (0.009mol) of HP-β-CD, add 10mL of water, stir to dissolve, and use a magnetic stirrer to stir at a speed of 200rpm for 4 hours, and centrifuge at 4000rpm for 10min Take the supernatant to obtain the TA-HP-β-CD-IC...

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Abstract

The invention relates to a triamcinolone acetonide soluble micro-needle and a preparation method thereof. The soluble micro-needle comprises a needle tip and a substrate, the needle tip comprises sodium hyaluronate, triamcinolone acetonide and beta-cyclodextrin, the molar ratio of triamcinolone acetonide to the beta-cyclodextrin is 1:5-10, the weight ratio of the sodium hyaluronate to the triamcinolone acetonide is 15-70:1, and the substrate comprises high-molecular polymers. According to the triamcinolone acetonide soluble micro-needle, the medicine content of the needle tip is high, the needle tip has excellent mechanical strength and can penetrate scar tissues harder and more compact than common skins, a medicine delivery channel is formed, medicines are released, the micro-needle can effectively replace a current mode that the medicines are delivered by a medical syringe, pain caused by injection of the syringe is greatly reduced, and the medicines are efficiently delivered. The soluble micro-needle is prepared by a three-step centrifugation forming method, and the medicine loading ratio of the needle tip can be greatly increased.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a triamcinolone acetonide soluble microneedle and a preparation method thereof. Background technique [0002] The skin is the largest organ of the human body. When the skin is damaged, the skin will undergo tissue repair according to the degree, nature and scope of the damage, including complete regeneration and incomplete regeneration. When the skin damage reaches a certain level, such as full-thickness skin damage, it is difficult for the skin to restore its original structure and function, and microscopic tissue hyperplasia replaces the defective tissue, eventually forming a scar, which is incomplete regeneration, or scar repair. Excessive scarring is the formation of hypertrophic scars or keloids, also known as pathological scars. Both hypertrophic scars and keloids protrude significantly on normal skin, with redness and congestion; hypertrophic scars are...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/58A61K47/69A61K47/36A61P17/02A61M37/00
CPCA61K31/58A61K9/0021A61K47/36A61K47/6951A61M37/0015A61M2037/0053A61P17/02
Inventor 吴传斌林师麒侯嫒琳杨佩佩顾宇琨权桂兰
Owner SUN YAT SEN UNIV
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