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Silver sulfadiazine thermosensitive gel as well as preparation method and application thereof

A technology of silver thermosensitive gel and silver sulfadiazine, which is used in medical science, bandages, etc., can solve problems such as unfavorable gel form transformation, fibroblast toxicity, transient pain, etc. The effect of medication pain and reducing the number of medication changes

Active Publication Date: 2018-06-08
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently commercially available silver sulfadiazine is mostly ointment applied to the affected area. The concentration of silver sulfadiazine is 1.0%. , requiring an increase in the number of administrations (2 to 4 times a day), however, multiple administrations will cause the accumulation of silver ions, which will lead to problems such as vascular toxicity, keratinocyte and fibroblast toxicity (Sandri et al., 2014; Brandt et al., 2012; Muller et al., 2003 and Tsipouras et al., 1995)
At the same time, repeated administration will cause problems such as transient pain, uneven application, difficulty in contacting the wound, and poor patient compliance.
[0004] In the literature about silver sulfadiazine preparations, there are obvious defects in the preparations. For example, the patent application with publication number CN104013574A discloses a suspension preparation of temperature-variable painless nanometer sulfadiazine metal compound hyaluronic acid. The phase transition temperature is set at 37°C, which fails to fully consider the human skin temperature (32°C), which is obviously not conducive to the transition to the gel form, and the sulfadiazine metal compound in the suspension state is prone to drug burst release
At present, there are no relevant reports on the market of sulfadiazine silver thermosensitive gel products at home and abroad

Method used

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  • Silver sulfadiazine thermosensitive gel as well as preparation method and application thereof
  • Silver sulfadiazine thermosensitive gel as well as preparation method and application thereof
  • Silver sulfadiazine thermosensitive gel as well as preparation method and application thereof

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preparation example Construction

[0038] 2) Preparation of silver sulfadiazine nanosuspension: take silver sulfadiazine (crude drug) and join in the aqueous solution containing stabilizer (stabilizer can be selected from Poloxamer 407), so that the final concentration of silver sulfadiazine is 20mg / ml~100mg / ml, adopt wet grinding method (2500rpm, 30min) or high-pressure homogeneous method (pressure 1400bar, 50 cycles) to prepare silver sulfadiazine nanosuspension.

[0039] 3) Preparation of silver sulfadiazine-loaded poloxamer thermosensitive gel: add the silver sulfadiazine nanosuspension obtained in step 2) into the gel solution obtained in step 1), and mix evenly to obtain a concentration of silver sulfadiazine nanocrystals The sulfadiazine silver thermosensitive gel is 0.5wt%-1.5wt%. Store at 4°C or below, and spray on the affected area to form a gel when in use.

Embodiment 1

[0042] Example 1: Preparation of thermosensitive gel loaded with 10mg / ml silver sulfadiazine

[0043] 1) Preparation of gel solution: 17.5 g of poloxamer 407 was precisely weighed, and 10 g of glycerol solution was added to 100 ml of distilled water to obtain a gel solution.

[0044] 2) Preparation of silver sulfadiazine nanosuspension: 6g poloxamer 407 was dissolved and dispersed in 194ml deionized water to obtain a 3wt% poloxamer 407 solution; 20g sulfadiazine silver was dispersed in 180ml 3wt% poloxa In the M407 solution, add a ball mill to adjust the rotating speed to 2500rpm and process for 30min to obtain a 100mg / ml silver sulfadiazine nanosuspension.

[0045] 3) Preparation of drug-loaded temperature-sensitive gel: add the sulfadiazine silver nanosuspension in step 2) into the gel solution in a ratio of 10:90 to obtain the sulfadiazine-loaded silver temperature-sensitive gel, sulfadiazine The final concentration of silver in the temperature-sensitive gel is 10mg / ml (in...

Embodiment 2

[0047] Example 2: Preparation of thermosensitive gel loaded with 10mg / ml silver sulfadiazine

[0048] 1) Preparation of gel solution: 25 g of poloxamer 407 powder, 2 g of poloxamer 188 powder and 10 g of glycerol were accurately weighed and added to 100 ml of distilled water to obtain a gel solution.

[0049] 2) Preparation of silver sulfadiazine nanosuspension: 6g poloxamer 407 was dissolved and dispersed in 194ml deionized water to obtain a 3wt% poloxamer 407 solution; 20g sulfadiazine silver was dispersed in 180ml 3wt% poloxa In the M407 solution, use high-pressure homogeneous method (pressure 1400bar, 50 circulations), obtain sulfadiazine silver nano-suspension.

[0050] 3) Preparation of drug-loaded temperature-sensitive gel: add the silver sulfadiazine nanosuspension in step 2) into the gel solution in step 1) according to the volume ratio of 10:90 to obtain the silver-sulfadiazine-loaded temperature-sensitive gel. Glue, the final concentration of silver sulfadiazine in...

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Abstract

The invention discloses silver sulfadiazine thermosensitive gel as well as a preparation method and application thereof. The silver sulfadiazine thermosensitive gel is prepared from the following rawmaterials: silver sulfadiazine nanocrystalline, 11 to 20 weight percent of poloxamer 407, 0 to 4 weight percent of temperature regulator, 3 to 13 weight percent of humectant and the balance of water.The gel nanocrystallizes silver sulfadiazine so as to increase the surface area of the silver sulfadiazine and enhance the antibacterial effects; by taking the poloxamer as a gel substrate and utilizing the thermosensitive gelling properties, effective fitting and easiness in removal of wound are realized; meanwhile, the gel can be used as a drug reservoir, and further slow release and long-term effects of antibacterial drugs are achieved. The gel can be directly used on the surfaces suffering from trauma, bedsore and ulceration so as to realize the effects of isolating, resisting bacteria, promoting wound healing and the like. The gel provided by the invention has the advantages that a substrate and components of the gel are both safe and non-toxic biomaterials and can be widely used in treatment and repair of clinical acute and chronic wound infection.

Description

technical field [0001] The invention relates to the technical field of temperature-sensitive in-situ gels, in particular to a silver sulfadiazine temperature-sensitive gel and a preparation method and application thereof. Background technique [0002] Trauma often leads to complications such as infection, excessive inflammation, and diabetic ulcers. Ordinary gel dressings are difficult to fight against more stubborn complications, especially infection. Because the wound exudate is rich in protein and other nutrients, it provides good conditions for the growth of microorganisms, so the wound surface is very easy to be infected. When infection occurs, microorganisms can decompose wound collagen and granular tissue, destroy new matrix, and cause excessive accumulation of macrophages and inflammatory cells, delay wound healing, and even lead to wound deterioration and systemic sepsis. In order to control wound infection, especially when the wound tissue is necrotic, lacks blood...

Claims

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Application Information

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IPC IPC(8): A61L26/00
CPCA61L26/0019A61L26/0066A61L26/008A61L2300/216A61L2300/404A61L2300/602C08L71/02
Inventor 窦桂芳刘晓亚甘慧孟志云朱晓霞顾若兰吴卓娜李俭郑颖孙文种
Owner ACADEMY OF MILITARY MEDICAL SCI
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