Skin flap infection and avascular necrosis prevention and treatment transdermal preparation and preparation method thereof

A technology of transdermal preparation and skin flap infection, which is applied in the field of medicine, can solve the problems of limited skin penetration area and affect the penetration effect of drugs, and achieve the effect of no systemic effect, reduction of toxic and side effects, and improvement of curative effect

Inactive Publication Date: 2015-07-22
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The stratum corneum of the skin is the main rate-limiting barrier for transdermal drug delivery, so there are certain limitations in transdermal drug delivery: 1. Drugs with a relative molecular weight below 800 Da can easily pass through, while drugs such as LMWH-Na with a molecular weight of more than 800 Da 2. Because the skin penetration area is limited, the combined use of multiple drugs will inevitably compete for skin penetration channels, affecting the drug penetration effect

Method used

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  • Skin flap infection and avascular necrosis prevention and treatment transdermal preparation and preparation method thereof
  • Skin flap infection and avascular necrosis prevention and treatment transdermal preparation and preparation method thereof
  • Skin flap infection and avascular necrosis prevention and treatment transdermal preparation and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0032] The preparation of embodiment one gel

[0033] Prepare the gel as follows:

[0034] 1. Preparation of sodium carboxymethyl cellulose gel matrix: Weigh 5.0 g of sodium carboxymethyl cellulose raw material, disperse it with 10.0 g of 95% ethanol, add 65.0 g of distilled water, stir evenly, seal it, place it overnight, and make it fully Swell to form a hydrogel matrix.

[0035] 2. Preparation of gel:

[0036] Main drug formula:

[0037] 1.00% AZM Gel Formula 100.0mg AZM

[0038] 0.50% AB gel formula 50.0mg AB

[0039] 0.16% LMWH-Na gel formula 16.0mg LMWH-Na

[0040] Transdermal formulation for prevention and treatment of flap infection ischemic necrosis 100.0mg AZM+50.0mg AB+16.0mg LMWH-Na

[0041]Accurately weigh the main ingredients according to the above formula, measure 300.0mg of azone and 200.0mg of propylene glycol, put them in a 25ml beaker, add absolute ethanol until 2g is dissolved, add them into 8g of gel matrix, stir well, and make 1.00% AZM gel respecti...

Embodiment 2

[0042] Example 2 Preparation of Infected Flap Model of Random Ischemia

[0043] Three days before the operation, the back of the mice was depilated with 8% sodium sulfide. After anesthesia by intraperitoneal injection of pentobarbital sodium (0.3ml / 100g body weight), the rat was fixed on the operating table in a prone position, and a random flap of 10.0mm×70.0mm was designed with a pedicle of 20.0mm from the tail end. Routine disinfection with povidone iodine, incision of the skin along the designed line, the meat membrane reaching the superficial layer of the back sarcolemma, sharp separation along this layer to the pedicle of the flap, and in situ intermittent sutures with 3 / 0 silk sutures after thorough hemostasis.

[0044] After the standard strains of Staphylococcus aureus and pathogenic Escherichia coli were revived in a 4°C incubator, two colonies were picked in a sterile operating table and placed in LB liquid medium, and slowly oscillated in a constant temperature sha...

Embodiment 3

[0046] Example 3 Detection of AZM and AB Contents in Rat Plasma and Flap Tissue

[0047] 1. Construction of AZM and AB content determination methods

[0048] (1) Chromatographic conditions Chromatographic column: Luna C 18 Column (250×4.60mm, 5μm); mobile phase: acetonitrile-phosphate buffer (0.02mol L -1 Potassium dihydrogen phosphate, use 1mol L -1 Sodium hydroxide to adjust to PH8.0) (55:45); flow rate: 1.0mL min -1 ; Column temperature: 30° C.; Detection wavelength: 210 nm; Injection volume: 20 μL.

[0049] (2) Preparation of reference substance solution Accurately weigh 30.0mg of AZM and 20.0mg of AB respectively, dissolve them in acetonitrile and dilute to volume in a 10.0mL volumetric flask to obtain a concentration of 2000μg·mL -1 standard solution, ready for use.

[0050] (3) System suitability test Under the specified chromatographic conditions, accurately draw the reference solution, the sample solution, and 20.0 μL of physiological saline, respectively, and in...

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Abstract

The invention belongs to the field of medicine, and relates to a skin flap infection and avascular necrosis prevention and treatment transdermal preparation and a preparation method thereof. The skin flap infection and avascular necrosis prevention and treatment transdermal preparation contains azithromycin (AZM), amlodipine (AB), low molecular weight heparin (LMWH-Na), a hydrogel matrix and other components. According to the present invention, the rational formula and the optimized preparation method are adopted to preferably select the optimal concentrations of the three main drugs, such that the problem that the three main drugs compete the kin penetration channel and the macromolecule LMWH-Na is not easily subjected to percutaneous penetration are solved; and with the prepared transdermal preparation, the disadvantages that the drugs of the oral administration or intravenous injection and other systemic administration, and intubation intermittent administration under the skin flap or one time injection and other topical administrations difficultly reach the ischemic local skin flap while the plasma concentration is relatively high so as to easily produce systemic adverse reactions and the like are overcome, the stable effective drug concentration at the local skin flap can be maintained, the skin flap survival area can be improved, the systemic effect is low, and the defects of the existing treatment method in the field of skin flap infection and avascular necrosis are overcome.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a transdermal preparation for preventing and treating ischemic necrosis of skin flap infection and a preparation method thereof. Background technique [0002] Flap transfer or replantation of avulsed skin flaps is an important means of repairing skin defects and reconstructing organs in plastic surgery and other surgeries. Incomplete debridement of the wound before flap transplantation, or avulsion of the flap, or repair of infected wounds such as chronic osteomyelitis often lead to flap infection; flap formation surgery or avulsion trauma and flap infection can cause skin The spasm and thrombosis of the blood supply vessels of the flap further aggravate the infection of the flap, and the infection will inevitably affect the local blood supply of the flap. Animal experiments and clinical applications of anti-infective drugs, vasodilators and anticoagulants have achieved good resu...

Claims

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Application Information

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IPC IPC(8): A61K31/727A61K9/06A61K47/38A61P17/02A61P9/10A61P31/04A61K31/4422A61K31/7052
Inventor 张选奋秦永红张曈焦阳
Owner LANZHOU UNIVERSITY
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