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Eprinomectin (EPR) emulsion gel and preparation method thereof

A technology of mycocin and emulsion, which is applied in the directions of pharmaceutical formula, aerosol delivery, emulsion delivery, etc., and can solve the problems of no commercial products

Active Publication Date: 2016-07-20
JIANGSU AGRI ANIMAL HUSBANDRY VOCATIONAL COLLEGE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Domestic research on EPR preparations has just started, and there is no commercial product yet

Method used

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  • Eprinomectin (EPR) emulsion gel and preparation method thereof
  • Eprinomectin (EPR) emulsion gel and preparation method thereof
  • Eprinomectin (EPR) emulsion gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1.1 Preparation of eprinomectin (EPR) emulsion gel:

[0039] Prescription: EPR 0.55g, Tween 800.33g, caprylic capric acid polyethylene glycol glyceride (labrasol) 0.33g, castor oil 1.19g, appropriate amount of water, appropriate amount of carbomer

[0040] Process:

[0041] ①Preparation of the oil phase: Weigh the prescribed amount of EPR into a suitable eggplant-shaped bottle, add 1ml of absolute ethanol for ultrasonic dissolution, add the prescribed amount of castor oil, mix well in a water bath at 40°C, and spin under reduced pressure at 38°C. Steam for 20 min to obtain the oil phase.

[0042] ②Preparation of the water phase: Weigh the prescribed amount of Tween 80, labrasol and 7.6 g of water, and mix them uniformly to obtain the water phase.

[0043] ③Preparation of emulsion: Slowly add the water phase into the oil phase, and carry out magnetic stirring while adding to obtain colostrum. After mixing, high-speed shearing is carried out at a speed of 8000 rpm / min ...

Embodiment 2

[0048] Embodiment 2: EPR emulsion gel adhesion determination in vitro

[0049] ① Prepare fresh mouse skin and store it in a -20°C refrigerator for future use.

[0050] ②Take out the stored skin, thaw it in normal saline, take it out, blot dry with filter paper, and stick two pieces of skin (1.8cmx1.8cm) on the surface of two glass slides a and b with 502 glue respectively.

[0051] ④ Weigh an appropriate amount of gel and apply it evenly on the skin of slide a, so that slides a and b are in close contact.

[0052] ⑤Apply 100g pressure (100g weight) on slide a and keep it for 10s. like figure 2 As shown, fix slide a, tie a plastic bag on slide b, add water to the plastic bag through the infusion bottle at a rate of 2 drops / second, stop adding water immediately when slides a and b separate.

[0053] ⑥Weigh the total mass m (g) of water and slide glass b, and press f adhesion force (g / cm 2 )f=m / r2 (r is 1.8 cm) The adhesion force per unit area is calculated. (Xiang Daxiong, ...

Embodiment 3

[0059] Example 3: In vitro transdermal experiment of EPR emulsion gel

[0060] 3.1 Preparation of mouse skin

[0061] Take the mice, kill them by decapitation, cut off the mouse hair on both sides of the midline of the abdomen, and then use a razor to shave off the fluff and quickly peel off the skin. Store in refrigerator (-20°C).

[0062] 3.2 Penetration diffusion device and test method

[0063] The prepared in vitro skin was fixed between the supply tank and the receiving tank of the Franz diffusion cell, the stratum corneum faced the supply tank, and the effective transdermal area was 2.27 cm. 2 . Weigh an appropriate amount of EPR emulsion gel (EPR suspension as a control) and apply it to the stratum corneum of mouse skin. The receiving solution was 6.50 mL of 30% methanol / physiological saline, the magnetic stirring speed was about 500 r / min, and the temperature of the water bath was 37 °C. Samples were taken at 1, 2, 4, 6, 8, 10, and 12 hours, and all the liquid in ...

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Abstract

The invention discloses eprinomectin (EPR) emulsion gel. According to the emulsion gel, EPR is prepared into an oil-in-water emulsion to improve the water solubility and effectively improve the dispersion degree and drug-loading capacity of EPR, and the EPR emulsion and gel are mixed to prepare the emulsion gel to further improve the emulsion stability. The EPR emulsion gel can be used for improving the water solubility of EPR and effectively improving the dispersion degree and drug-loading capacity of EPR, and has relatively high stability and excellent adhesive performance. Compared with an EPR suspension, the EPR emulsion gel has the advantage of constantly penetrating skin of a rat and has a relatively high percutaneous penetration rate.

Description

technical field [0001] The invention belongs to the technical field of veterinary drug preparations, and in particular relates to an eprinomectin emulsion gel and a preparation method thereof. Background technique [0002] Eprinomectin (EPR) is a new type of highly effective antiparasitic drug, which has been widely used in pesticides, veterinary drugs, sanitary drugs and human drugs. Studies have shown that EPR is well absorbed through the mouth, through the skin, and through the skin, and can be widely distributed in various tissues throughout the body, effectively killing nematodes and ectoparasites in the body. This provides the possibility for the research and development of various dosage forms of EPR (such as tablets, powders, oral liquids, injections, pouring agents, etc.). But so far, the EPR preparation that has been commercialized is only the pouring agent of Merial Company. In order to fully realize the application potential of EPR, a series of studies on the f...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/7048A61K47/32A61P33/00
CPCA61K9/0014A61K9/06A61K9/107A61K31/7048A61K47/14A61K47/32
Inventor 冒玉娟沈雁陈晓兰王莹赵丽
Owner JIANGSU AGRI ANIMAL HUSBANDRY VOCATIONAL COLLEGE
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