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Transdermal drug delivery composition containing dapsone compound and preparation method of transdermal drug delivery composition

A composition and the technology of dapsone, applied in the direction of medical preparations containing active ingredients, drug combinations, active ingredients of peroxygen compounds, etc., can solve the problem of poor targeting of dapsone drug delivery and affect patients' medication compliance , unfavorable continuous application of drugs and other issues, to achieve the effect of improving the transdermal transfer effect, stabilizing drug content and properties, and reducing adverse reactions and toxic reactions

Pending Publication Date: 2021-11-02
NANJING XINTONG RUIYI MEDICINE SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, there are the following problems and deficiencies in the use of existing technologies or marketed drugs: 1. Poor targeting of dapsone drug delivery
The above problems not only affect the quality of drugs, but also affect the compliance of patients with medication, which is not conducive to the continuous application of drugs

Method used

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  • Transdermal drug delivery composition containing dapsone compound and preparation method of transdermal drug delivery composition
  • Transdermal drug delivery composition containing dapsone compound and preparation method of transdermal drug delivery composition
  • Transdermal drug delivery composition containing dapsone compound and preparation method of transdermal drug delivery composition

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preparation example Construction

[0076] (1) preparation example of gel

[0077] Drug Solution Gel Prescription Form

[0078]

[0079] Preparation method of G11, G21 and control RG11:

[0080] The dapsone is crushed through a 100-mesh sieve and set aside; the drug solution is prepared by stirring and dispersing. Weigh the prescribed amount of dapsone, HP-β-CD and / or diethylene glycol monoethyl ether, add 1 / 3 of the prescribed amount of pure water, and stir to completely dissolve; evenly disperse the carbomer in an appropriate amount of pure water Let stand in water to make it fully swell, add dropwise 20% triethanolamine solution to adjust the pH to 7.0 to form a semi-solid gel matrix, add drug solution and other excipients, make up pure water to 100%, 100-200r / min Stir well to make it into a gel, degas, and pack, that is.

[0081] Example G12 is similar to Example G11, but the cyclodextrin is sulfobutyl-β-cyclodextrin (SBE-β-CD), and the content is 25%;

[0082] Example G13 is similar to Example G11, b...

Embodiment N11

[0112] Embodiment N11, N12, N21, N22 and contrast gel RN0, RN1, RN2, RN22 preparation method:

[0113] Drug nanosuspensions were prepared using a wet circulation mill. Dapsone was crushed through a 150-mesh sieve, 1 / 2 of the prescription amount of pure water and 0.8% hydroxyethyl cellulose were added, and the same volume of zirconia grinding beads (Ф0.5mm) was used to grind at 3000rpm for 120 minutes, and HP-β-CD was added Or / mix with diethylene glycol monoethyl ether evenly to obtain a drug nanosuspension; evenly disperse the carbomer in an appropriate amount of pure water and let it stand to make it fully swell, add dropwise 20% triethanolamine solution to adjust the pH to 7.0 , to form a semi-solid gel matrix, add drug nanosuspension and other auxiliary materials, make up pure water to 100%, stir at 100-200r / min to make it into a gel, degas, and pack, to get final product. The average particle diameter of dapsone in the obtained suspension gel is 316.2-335.4 nm.

[0114] ...

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Abstract

The invention discloses a transdermal drug delivery composition containing dapsone compounds and a preparation method of the transdermal drug delivery composition. The composition is mainly prepared from the following raw materials: dapsone compounds and cyclodextrin. The preparation method comprises the following steps: micronizing the dapsone compound, then fully mixing and dispersing the micronized dapsone compound and cyclodextrin in a water-soluble medium to prepare a solution, a micron suspension or a nano suspension, and finally mixing the solution, the micron suspension or the nano suspension with pharmaceutically acceptable auxiliary materials and / or matrixes to obtain the medicine. The external preparation of the composition disclosed by the invention has the characteristics of remarkable skin targeted delivery effect, improved preparation stability, reduced skin irritation and good industrialization feasibility of the preparation process, and shows better application potential.

Description

technical field [0001] The invention belongs to the technical field of transdermal drug delivery, in particular to a transdermal drug composition containing dapsone compounds and a preparation method thereof. Background technique [0002] Acne is a common skin disease that mostly occurs during adolescence. The acne can be contaminated with bacteria, such as Propionibacterium acnes, and can also be characterized by inflammation. Acne tends to occur on areas of the skin where the sebaceous glands are most active, such as the face. Acne is associated with psychological trauma and, if left untreated, can lead to scarring and disfigurement and can cause associated skin disorders such as: folliculitis, perioral dermatitis, photodamage, skin aging, psoriasis, atopic dermatitis, keratosis Lesions, scars (including surgical scars and acne scars), sebaceous cysts, inflammatory skin diseases, post-inflammatory hyperpigmentation, etc. There are various factors that cause acne, but th...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/08A61K9/10A61K31/145A61K31/192A61K31/327A61K47/10A61K47/40A61P17/10A61P31/04A61P33/02A61P33/06A61P33/08A61P37/06A61P17/00
CPCA61K9/10A61K9/06A61K9/08A61K31/145A61K31/192A61K31/327A61K47/40A61K47/10A61K9/0014A61P17/10A61P31/04A61P33/02A61P33/06A61P33/08A61P37/06A61P17/00
Inventor 杨星昊
Owner NANJING XINTONG RUIYI MEDICINE SCI & TECH
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