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Adrenaline sublingual spray for allergic shock as well as preparation method and application of adrenaline sublingual spray

An anaphylactic shock and epinephrine technology, applied in allergic diseases, aerosol delivery, medical preparations with inactive ingredients, etc. The effect of avoiding potential allergic reactions, simple preparation process, and reducing industrial costs

Active Publication Date: 2021-12-07
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent US20070202163A and patent CN109310646A respectively relate to a sublingual epinephrine tablet and a sublingual film. Only after sublingual administration of 40 mg can achieve the similar blood concentration of epinephrine after intramuscular injection of 0.3 mg, and the bioavailability is low. big security risk

Method used

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  • Adrenaline sublingual spray for allergic shock as well as preparation method and application of adrenaline sublingual spray
  • Adrenaline sublingual spray for allergic shock as well as preparation method and application of adrenaline sublingual spray
  • Adrenaline sublingual spray for allergic shock as well as preparation method and application of adrenaline sublingual spray

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0051] 1. Preparation of epinephrine sublingual spray

[0052] 1. Preparation of epinephrine sublingual sprays with different dosages of polysorbate 80

[0053] Accurately weigh 10 mg of epinephrine into an eggplant-shaped bottle, add 0.3 mL of 0.2M hydrochloric acid solution, and stir until the epinephrine is completely dissolved to obtain an epinephrine stock solution (Product 1). This process is completed in the dark.

[0054] Precisely weigh the absorption enhancer polysorbate 80 and the metal ion chelating agent ethylenediaminetetraacetic acid disodium (EDTA2Na) of the prescribed amount, add 0.7mL of pure water, so that the total volume of product 2 and product 1 in this step is the full amount of 1mL, Adjust temperature to 25°C, rotor speed 100r / min, stop heating after stirring for 2 hours, cool to room temperature naturally, add pH regulator citric acid and sodium citrate to adjust pH value to 3-4, and obtain excipient dilution (product 2).

[0055] Combine product 1 a...

Embodiment 21

[0084] Embodiment 21 does not add the stability of the adrenaline target concentration solution (10mg / mL) of other auxiliary materials

[0085] Accurately weigh 10mg of epinephrine and add it to an eggplant-shaped bottle, add 0.3mL of 0.2M hydrochloric acid solution, stir until the epinephrine is completely dissolved, add 0.7mL of pure water until the total volume is 1mL, add pH regulators citric acid and sodium citrate respectively Adjust the final pH value to 2.5, 3.5, 4.5, 5.5, and 6.5 to obtain 10 mg / mL target concentration solutions of adrenaline with different pH values.

[0086] After placing the 10 mg / mL target concentration solutions of adrenaline with different pH values ​​for one month, the content of adrenaline solutions with pH 4 and above significantly decreased, the color of the solutions changed significantly, and the impurity content increased significantly; the content of adrenaline solutions below pH 4 did not Significant changes occurred, and the solution h...

Embodiment 22

[0087] Sublingual mucosal permeability in vitro of embodiment 22 epinephrine sublingual spray

[0088] The oral mucosa of pigs was selected as the experimental model, and divided into a control group (blank adrenaline sublingual spray without absorption enhancer in Comparative Examples 1-4), and a preparation group (different prescriptions in Examples 1-20). The Franz diffusion cell was selected for in vitro permeation experiments. After administration, samples were taken at 0, 5, 10, 15, 20, 30, 40, 60, 90, 120, and 180 minutes, and the adrenaline content was detected by high performance liquid chromatography, and compared with the control Groups were compared to evaluate the in vitro mucosal permeability of adrenaline spray prepared by different prescriptions ( figure 2 , 3 , 4, 5, 6). The results are shown in the table below.

[0089] Table 5 Parameters of mucosal penetration of epinephrine within 30 minutes under different polysorbate 80 dosages (mean±SEM, n=3)

[009...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses an epinephrine sublingual spray for allergic shock and a preparation method thereof. The invention solves the problems of poor stability and delayed absorption of the existing adrenaline preparation. A patient can take the medicine at the first time when the allergic shock disease occurs, the medicine can rapidly penetrate through sublingual mucosa and enter blood circulation, the medicine effect can be achieved within 15 min, and the medicine can be used as a standing emergency medicine to replace an injection and has good clinical application prospects in the field of allergic shock treatment.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an epinephrine sublingual spray for anaphylactic shock, a preparation method and application thereof. Background technique [0002] Epinephrine is an adrenergic receptor agonist, which can reverse the bronchospasm, asthma, dyspnea, syncope, shock, urticaria, edema and other symptoms caused by anaphylactic shock in a few minutes. the only drug of choice. However, adrenaline is unstable in neutral or alkaline aqueous solution, and is easily oxidized and racemized when exposed to air or exposed to sunlight, and its activity is reduced, which limits its formulation development. [0003] Epinephrine products listed in the domestic market are mainly epinephrine hydrochloride or epinephrine tartrate injection. In addition to conventional injections, there is also an epinephrine pen that can be self-injected (such as ), but are expensive and single-use only. Epi...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/137A61K47/12A61K47/26A61K47/20A61K47/44A61P37/08
CPCA61K9/12A61K9/006A61K31/137A61K47/12A61K47/26A61K47/20A61K47/44A61P37/08
Inventor 丁杨周建平施徐王佳惠
Owner CHINA PHARM UNIV
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