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Penetration enhancer for nasal delivery and application thereof

A nasal cavity and permeation enhancer technology, applied in non-active ingredient medical preparations, medical preparations containing active ingredients, drug combinations, etc., can solve the irreversible physiological damage of the nasal cavity, increase the solubility of insoluble drugs, and weak transmembrane ability And other issues

Pending Publication Date: 2021-01-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In terms of promoting nasal absorption of biomacromolecular drugs, adding absorption enhancers is the most common and effective method, but long-term use of surfactants can significantly irritate nasal cilia and cause irreversible damage to nasal physiology. A safe nasal absorption enhancer that can be used in multiple dosage forms is of great significance for expanding the nasal drug delivery system
[0005] Due to the low solubility of insoluble drugs in water, the dosage of nasal administration is very low, and the therapeutic effect cannot be achieved, and the addition of organic solvents will seriously damage the physiological environment of the nasal cavity. Therefore, developing a solvent that is not significantly irritating to the nasal mucosa can increase The solubility of poorly soluble drugs has important application value
For biomacromolecular drugs, due to their large molecular weight and strong hydrophilicity, they have weak transmembrane ability and less absorption after nasal administration. Therefore, it is necessary to add absorption enhancers to increase their transmembrane transport. All agents have significant irritation to cilia or nasal mucosa, and have limited ability to enhance penetration

Method used

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  • Penetration enhancer for nasal delivery and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Choline Malate System Promotes Insulin Nasal Absorption

[0030] Insulin is a biomacromolecular drug that has been widely used as a specific drug for the treatment of diabetic patients. Due to insulin's large molecular weight, strong hydrophilicity, and weak transmembrane transport ability, only injections of insulin are effective at present, and the clinical compliance is very poor. At present, many studies have attempted to make insulin into other dosage forms, such as oral, nasal, transdermal and other routes of administration. Compared with oral administration, the environment of the nasal cavity is relatively mild, the enzyme activity is low, and protein drugs are not easy to degrade; while compared with the skin, the barrier effect of the nasal mucosa is weak, and there are a large number of capillaries and lymphatic vessels under the epithelial cells, and the drug can be rapidly released. absorb. Therefore, nasal administration has been considered as ...

Embodiment 2

[0036] Example 2 Aqueous Malate Choline System Promotes Insulin Nasal Absorption

[0037] The choline malate system containing insulin was prepared, mixed with a certain amount of water, and used in the nasal administration hypoglycemic experiment. See Table 2 for detailed component descriptions.

[0038] Table 2. The mass percentages of the detailed components of the insulin-choline malate system (moisture content=40%)

[0039] DL-malic acid (Sinopharm Group) Choline Chloride (Sinopharm Group) Porcine insulin (Xuzhou Wanbang) distilled water 20％ 40％ 1％ 40％

[0040] Method: Add malic acid and choline chloride into a beaker at a weight ratio of 1:2 and mix evenly. Heat the mixture to 80°C and keep stirring for about 3 hours until the solid disappears completely. After cooling to room temperature, add 1% insulin Add to the system, add 40% distilled water, and mix well.

[0041] In this embodiment, choline malate was used to dissolve insulin, mixed wi...

Embodiment 3

[0042] Embodiment 3 choline citrate system is used to promote propranolol nasal cavity absorption

[0043] The choline citrate system containing propranolol was prepared for nasal absorption experiment, and the detailed components are shown in Table 3.

[0044] Table 3. Mass percentages of detailed components of the propranolol-choline citrate system (moisture content=0)

[0045] Citric Acid Monohydrate (Sinopharm Group) Choline bicarbonate (Sigma) Propranolol (Sinopharm Group) 29.5％ 69.5％ 1％

[0046] Method: Dissolve citric acid and choline bicarbonate in methanol at a molar ratio of 1:3, stir at room temperature for 4 hours until carbon dioxide generation stops, remove methanol and water by rotary evaporation at 60°C, and vacuum dry for 48 hours to remove residual solvent. To enhance penetration system. Add 1% propranolol into the system, stir and dissolve.

[0047] The present embodiment takes rats as the animal model, administers propranolol-chol...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a penetration enhancer for nasal delivery and application thereof. The invention relates to a penetration enhancer for promoting nasal absorption. Specifically, the penetration enhancer is a low-temperature molten salt for promoting nasal cavity absorption, and the low-temperature molten salt is an ionic liquid or eutectic solvent formed by reacting an organic acid with at least one organic base and / or a salt thereof. The penetration enhancer can dissolve active ingredients, and the active ingredients comprise indissolvable drugs and biomacromolecule drugs, for example, the penetration enhancer can significantly promote nasal absorption of insulin to achieve an ideal hypoglycemic effect. The penetration enhancer can be used alone or in combination with other carriers to promote transnasal mucosa transport of drug molecules, and has no obvious damage effect on the nasal mucosa.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and relates to a permeation enhancer for nasal cavity administration. Specifically, the invention provides a permeation enhancer for nasal cavity administration containing low-temperature molten salt. The present invention also includes the application of the penetration enhancer for nasal administration. Background technique [0002] Nasal drug delivery system refers to preparations that are used in the nasal cavity and absorbed through the nasal mucosa to exert local or systemic therapeutic effects. The respiratory area of ​​the nasal cavity is the largest part of the nasal cavity, and there are many microvilli on its mucous membrane, which greatly increases the effective surface area for drug absorption. Under the epithelial cells of the nasal cavity, there are many large and porous capillaries and a rich lymphatic network, which promote the penetration of drugs into blood ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/08A61K9/107A61K38/28A61K47/12A61K47/18A61K47/24A61P3/10
CPCA61K9/0043A61K9/08A61K9/06A61K9/107A61K47/12A61K47/183A61K47/186A61K47/24A61K38/28A61P3/10
Inventor 戚建平李洋吴伟武喜营卢懿
Owner FUDAN UNIV
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