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Granisetron hydrochloride nasal spray and preparation method thereof

A technology of granisetron hydrochloride nasal cavity and granisetron hydrochloride, applied in aerosol delivery, digestive system, drug combination, etc., can solve the problems of low proteolytic enzyme activity, low bioavailability, inconvenient use, etc., and achieve improvement Compliance, ease of administration, and improved absorption

Active Publication Date: 2012-10-03
广东同德药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

②After the drug is absorbed, it enters the systemic circulation directly, without the first-pass effect of the liver, and the activity of proteolytic enzymes in the nasal mucosa is low. It is suitable for peptide and protein drugs that are easily metabolized in the gastrointestinal fluid and gastrointestinal wall membrane or have a large first-pass effect. is an effective route of administration
In order to overcome the disadvantages of inconvenient use of injections and low bioavailability and slow onset of oral preparations, a new type of drug that can be administered quickly when the patient feels nauseated to control the occurrence of nausea and vomiting can be developed, which can reduce the pain of the patient. pain, and can reduce the labor of medical staff, and can increase the choice of another way of medication in clinical practice, so the development of such a new drug is of great significance

Method used

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  • Granisetron hydrochloride nasal spray and preparation method thereof
  • Granisetron hydrochloride nasal spray and preparation method thereof
  • Granisetron hydrochloride nasal spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] The raw materials are: 10 parts of granisetron hydrochloride, 10 parts of ethylparaben, 10 parts of polyoxyethylene-9-lauryl ether, 5 parts of thiolauryl alcohol, 10 parts of 1,2-propylene glycol, 10 parts of glycerin, purified water Right amount, right amount of fragrance.

[0069] The preparation method is as follows:

[0070] (1) Take 10 parts of granisetron hydrochloride and 10 parts of ethylparaben, pulverize them, and pass through an 80-mesh sieve; place them in a volumetric flask, add an appropriate amount of purified water, and shake fully;

[0071] (2) Add 10 parts of polyoxyethylene-9-lauryl ether, 5 parts of thiolauryl alcohol, 10 parts of 1,2-propylene glycol, 10 parts of glycerin, and an appropriate amount of essence to the solution prepared in the first step;

[0072] (3) Add purified water to the scale, shake to make the solution mix evenly;

[0073] (4) Filling, sealing and packaging to obtain granisetron hydrochloride nasal cavity spray.

Embodiment 2

[0075] The raw materials are: 10 parts of granisetron hydrochloride, 20 parts of ethylparaben, 20 parts of polyoxyethylene-9-lauryl ether, 5 parts of thiolauryl alcohol, 10 parts of 1,2-propylene glycol, 10 parts of glycerin, purified water Right amount, right amount of fragrance.

[0076] The preparation method is as follows:

[0077] (1) Take 10 parts of granisetron hydrochloride and 20 parts of ethylparaben, pulverize them, and pass through an 80-mesh sieve; place them in a volumetric flask, add an appropriate amount of purified water, and shake fully;

[0078] (2) Add 20 parts of polyoxyethylene-9-lauryl ether, 5 parts of thiolauryl alcohol, 10 parts of 1,2-propylene glycol, 10 parts of glycerin, and an appropriate amount of essence to the solution prepared in the first step;

[0079] (3) Add purified water to the scale, shake to make the solution mix evenly;

[0080] (4) Filling, sealing and packaging to obtain granisetron hydrochloride nasal cavity spray.

Embodiment 3

[0082] The raw materials are: 12 parts of granisetron hydrochloride, 15 parts of ethylparaben, 18 parts of polyoxyethylene-9-lauryl ether, 8 parts of thiolauryl alcohol, 13 parts of 1,2-propylene glycol, 15 parts of glycerin, purified water Right amount, right amount of fragrance.

[0083] The preparation method is as follows:

[0084] (1) Take 12 parts of granisetron hydrochloride and 15 parts of ethylparaben, pulverize them, and pass through an 80-mesh sieve; place them in a volumetric flask, add an appropriate amount of purified water, and shake fully;

[0085] (2) Add 18 parts of polyoxyethylene-9-lauryl ether, 8 parts of thiolauryl alcohol, 13 parts of 1,2-propylene glycol, 15 parts of glycerin, and an appropriate amount of essence to the solution prepared in the first step;

[0086] (3) Add purified water to the scale, shake to make the solution mix evenly;

[0087] (4) Filling, sealing and packaging to obtain granisetron hydrochloride nasal cavity spray.

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Abstract

The invention relates to a granisetron hydrochloride nasal spray and a preparation method thereof, wherein the granisetron hydrochloride nasal spray is prepared by granisetron hydrochloride, hydroxyphenyl ethylester, polyoxyethylene-9-laurel ether, thiolauryl alcohol, 1,2-propylene glycol, glycerin, a proper amount of purified water and essence according to weight proportions. The preparation method thereof comprises the steps: granisetron hydrochloride and hydroxyphenyl ethylester are smashed, sieved and put in a volumetric flask, the volumetric flask is added with the proper amount of purified water, sufficiently oscillated and then added with polyoxyethylene-9-laurel ether, thiolauryl alcohol, 1,2-propylene glycol, glycerin and essence in proper amount, the purified water is added onceagain to reach scales, the volumetric flask is oscillated to evenly mix the solution, and the granisetron hydrochloride nasal spray is obtained after filling, sealing and packaging; target administration of the nasal spray is realized through nose so that the nasal spray can take effect rapidly, thus the administration is convenient and compliance of patients is enhanced, and simultaneously, stimulation effect of drugs to gastrointestinal tract can also be avoided and bioavailability of the drugs is increased.

Description

technical field [0001] The invention relates to a granisetron hydrochloride nasal cavity spray and a preparation method thereof, in particular to an antiemetic drug for treating vomiting caused by cancer-granisetron hydrochloride nasal cavity spray and a preparation method thereof. Background technique [0002] Nasal drug delivery system (NDDS) refers to preparations that are used in the nasal cavity and absorbed through the nasal mucosa to exert local or systemic effects. The total volume of the human nose is 15ml, and the nasal mucosa area is 150cm 2 , There are many cilia on the nasal mucosa, which can increase the effective area for drug absorption. After the drug is absorbed through the capillary of the nasal cavity, it directly enters the systemic circulation without going through the liver system, avoiding the first-pass effect of the liver. Therefore, it is a good site for drug absorption. [0003] The nasal cavity is used as the drug administration site, and its d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/12A61K31/439A61K47/34A61P1/08A61K47/10
Inventor 夏敏林文辉蒋宇亮林柳清
Owner 广东同德药业有限公司
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