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External preparation of neurokinin 1 receptor inhibitor and preparation method of external preparation

A receptor inhibitor and topical preparation technology, applied in the field of pharmaceutical preparations, can solve the problems of increasing the risk of systemic side effects, low compliance, and low pertinence

Pending Publication Date: 2021-08-20
CHANGSHA JINGYI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For some patients with advanced cancer, severe gastrointestinal reactions or confusion may make it difficult to take oral medication, and the pain of injection will further increase the pain of the patient, and the compliance is low; for patients with only local symptoms such as hair loss and dermatitis, Systemic administration is less targeted, and at the same time increases the risk of systemic side effects; in addition, oral administration is easily affected by gastrointestinal factors, and blood fluctuations are relatively large due to the process of drug dissolution and absorption

Method used

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  • External preparation of neurokinin 1 receptor inhibitor and preparation method of external preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] components content Aprepitant 2% Polyisobutylene 15% Polyacrylate 20% liquid paraffin 30% Ethylparaben 0.2% polypyrrolidone 30% Isopropyl myristate 2.5% phosphoric acid 0.3%

[0068] (2) Preparation method

[0069] Put the prescribed amount of aprepitant, polyisobutylene, polyacrylate, polypyrrolidone, and liquid paraffin in the same beaker, melt and mix them at 80°C, and add the prescribed amount of ethylparaben and isopropyl myristate in sequence , phosphoric acid, stir evenly, and then evenly spread to 30 cm 2 Dry the film at 45°C for 3 hours, take it out, cool it at room temperature, stick a protective film and cut it.

Embodiment 2

[0071] components content Aprepitant 1% ethanol 8% Sodium polyacrylate 20% Aluminum glycylate 1% glycerin 24% benzoic acid 0.1% Kaolin 5% Menthol 3% Sodium carboxymethyl cellulose 3% tartaric acid Adjust the pH to 4~8 purified water Top up to 100%

[0072] (2) Preparation method

[0073] Put the prescribed amount of sodium polyacrylate, aluminum glyoxate, sodium carboxymethylcellulose, and kaolin in the same beaker and mix them evenly, add the prescribed amount of glycerin, benzoic acid and menthol, and stir well; use the prescribed amount of ethanol to dilute aprepitant After dissolving, pour the solution into a beaker and mix thoroughly, adjust the pH to 4~8 with tartaric acid, add purified water to 100%, continue to stir until a uniform drug-containing gel is obtained, and spread it evenly on the non-woven fabric Put it on, place it at room temperature until the gel is solidified, stick a pro...

Embodiment 3

[0075] components content Aprepitant 1% ethanol 10% Sulfite 0.2% benzoic acid 0.1% Simethicone 10% cetyl alcohol 12% Glyceryl monostearate 10% Span 80 2% carbomer 1% sodium hydroxide 0.4% purified water 53.3%

[0076] (2) Preparation method

[0077] Colostrum: Dissolve the prescribed amount of aprepitant, sodium sulfite, and benzoic acid in ethanol, then add purified water and stir evenly, and heat to 80°C as the water phase; dissolve the prescribed amount of simethicone, cetyl alcohol, Mix fatty acid glyceride and Span 80 evenly, heat to 80°C, and use it as the oil phase; add the oil phase to the water phase while stirring, emulsify with a homogenizer for 15 minutes, and cool to room temperature to obtain colostrum;

[0078] Substrate: After swelling the prescribed amount of carbomer with an appropriate amount of water, add the prescribed amount of sodium hydroxide to make it a viscous and transp...

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Abstract

The invention discloses an external preparation of a series of neurokinin-1 receptors (NK1 receptors) inhibitors and a preparation method of the external preparation. The NK1 receptor inhibitors comprise, but are not limited to, aprepitant, fosaprepitant, rolapitant, netupitant or pharmaceutically acceptable salts thereof. The external preparation comprises, but is not limited to, ointment, cream, gel, tincture, lotion, aerosol, spray, liniment, a foaming agent, patch, emplastrum and the like. The external preparation of the NK1 receptor inhibitors can slowly deliver the medicine at a constant speed, and reduce the blood concentration fluctuation caused by dissolution and absorption of the oral medicine; the pertinence to local lesions can be improved, and the side effects of the whole body are reduced; and meanwhile, a choice with high compliance is provided for patients inconvenient to take orally, and the external preparation has important significance in relieving the pain of cancer patients clinically.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a series of external preparations of NK1 receptor inhibitors and a preparation method thereof. Background technique [0002] At present, the main treatment methods for cancer include surgery, chemotherapy and radiotherapy, but many adverse reactions are often caused during the treatment process, such as wound pain after surgery, and chemotherapy with cisplatin and other drugs can cause nausea, vomiting, dermatitis, hair loss, etc., which greatly increase the risk of cancer. Physical and psychological pain of the patient. [0003] Chemotherapy-induced nausea and vomiting (CINV) is the most common adverse reaction during cancer treatment, and about 70% to 80% of patients will experience this symptom. Severe nausea and vomiting not only lead to nutritional deficiencies, Dehydration and electrolyte imbalance can also force patients to discontinue effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/438A61K31/496A61K31/5377A61K31/675A61K9/06A61K9/70A61K47/10A61P1/08A61P35/00A61P17/00A61P17/04A61P17/14A61P25/02
CPCA61K9/0014A61K9/007A61K9/06A61K9/7061A61K31/438A61K31/496A61K31/5377A61K31/675A61K45/00A61K47/10A61P1/08A61P17/00A61P17/04A61P17/14A61P25/02A61P35/00
Inventor 张海龙
Owner CHANGSHA JINGYI PHARM TECH CO LTD
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