Dapsone compound suspension as well as preparation method and application thereof

A technology of suspension and dapsone, which is applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem that the drug with transdermal rate cannot reach the effective drug therapeutic dose, release rate and transdermal rate change, and skin delivery target. Troubles such as tropism instability, to achieve the effect of reducing the drug penetration rate, reducing the skin retention, and maintaining a stable drug particle size

Active 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

[0004] However, the following problems and deficiencies exist in the use of the prior art or marketed drugs: 1. The quality of the preparation is not stable
After long-term storage, the accumulation of dapsone in the gel causes the particle size of the product to continuously increase, and the particle size of the gel directly affects the quality of the product, and its particle size does not meet the requirements of the "Chinese Pharmacopoeia" (≤180μm ), while the gel applied to the affected area will produce an obvious sandy feeling and discomfort; 2. The skin delivery targeting of the prior art dapsone preparation is unstable
Due to the unstable particle size, the release rate and transdermal rate of external preparations vary significantly during the application process, which is not conducive to the concentrated targeting of the drug to the skin lesion to exert its drug effect
For example, excessive drug release or transdermal rate leads to the rapid absorption of the drug through the skin into the systemic circulation, resulting in systemic adverse reactions such as blood system, gastrointestinal system and neurotoxicity, and there is a greater safety risk
Too slow drug release or transdermal rate will lead to the infiltration of the drug into the cortical tissue will not reach the effective drug therapeutic dose

Method used

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  • Dapsone compound suspension as well as preparation method and application thereof
  • Dapsone compound suspension as well as preparation method and application thereof
  • Dapsone compound suspension as well as preparation method and application thereof

Examples

Experimental program
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preparation example Construction

[0059] One, the preparation research of embodiment

[0060] Nanosuspension and Gel Prescription Form

[0061]

[0062] Examples 1-4 prepared drug nanosuspension by wet grinding method. The suspension prescription contains 10% dapsone and 1.5% polymer. Dapsone is crushed through a 150-mesh sieve, dispersed in 10 times the amount of pure water to prepare the initial mixture, and put into the inner cavity of a wet circulation grinder. The mixture is mixed with equal volumes of zirconia grinding beads (Ф0.5 mm), and ground at 3000 rpm for 40 minutes, and the average particle diameter of dapsone in the obtained suspension is 300-400 nm.

Embodiment 5

[0063]Example 5 is similar to Example 1, but the suspension formulation contains 10% dapsone, 1.6% PVP-K30, 0.6% HPMC-K4M, and wet grinding for 50 minutes. The average particle size of dapsone in the resulting suspension was 296.3 nm. The film-spraying agent is prepared by adding appropriate amount of auxiliary materials into the suspension. Preparation prescription: 5% dapsone, 2% PVP-K30, 0.3% HPMC-K4M, 5% HPβCD, 30% ethanol, 3% glycerin, 0.05% ethylparaben, 0.1% disodium edetate , make up pure water to 100%. Preparation process: Dissolve the remaining auxiliary materials in ethanol or pure water according to the prescription of the preparation, add the drug suspension while stirring successively, make up the pure water to 100%, and stir thoroughly at 100-200r / min to obtain the product. The dapsone content in the obtained spray film agent is 4.98%, and the average drug particle diameter is 246.3nm.

Embodiment 6

[0064] Example 6 is similar to Example 1, but the suspension formulation contains 15% dapsone, 2% PVP-K30, and 1% PEG4000. Dapsone was crushed through a 150-mesh sieve, dispersed in 7 times the amount of pure water to prepare an initial mixture, and ground with zirconia beads (Ф0.5 mm) at 3500 rpm for 40 minutes to obtain a drug nanosuspension. The dapsone content in the obtained suspension was 14.95%, and the average drug particle diameter was 393.7nm.

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Abstract

The invention discloses a dapsone compound suspension as well as a preparation method and application thereof, the suspension comprises a dapsone compound and a polymer, and the polymer is selected from one or more of the following components: polyvinylpyrrolidone, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, PVP / VA, Soluplus and polyethylene glycol. Compared with the prior art, the suspension disclosed by the invention has the advantages of large drug loading capacity, narrow particle size distribution, good stability, easiness in production and preparation, industrial applicability and the like.

Description

technical field [0001] The invention belongs to the technical field of suspensions, in particular to a suspension of dapsone compounds and its preparation method and application. Background technique [0002] Dapsone (4,4'-diaminodiphenylsulfone, dapsone) was once a classic drug for the treatment of leprosy and herpetic dermatitis. In recent years, it has been found that dapsone has antibacterial and immunosuppressive effects on Corynebacterium acnes. There are currently several studies or products involving topical dermal formulations of dapsone for the topical treatment of acne. [0003] There are currently several studies or products involving topical dermal formulations of dapsone for the topical treatment of acne. For example, Invention Patent 1 (Application No. 2016108453526) discloses a gel preparation containing dapsone and its preparation method, and Invention Patent 2 (Application No. 2011103242193) provides a dapsone gel with stable quality and its preparation m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/145A61K47/22A61K47/10A61K47/32A61K47/38A61P17/00A61P17/10A61P31/04A61P37/06
CPCA61K31/145A61K9/10A61K47/32A61K47/38A61K47/10A61K9/0014A61K47/22A61P17/10A61P31/04A61P37/06A61P17/00
Inventor 杨星昊
Owner NANJING XINTONG RUIYI MEDICINE SCI & TECH
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