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Trans-dermal composition of anti-vomiting agent and preparation containing the same

A technology for antiemetics and ingredients, applied in the field of antiemetic ingredients delivered through the skin and formulations containing the same ingredients, can solve problems such as the effective formulation of antiemetics has not yet been developed

Inactive Publication Date: 2005-07-06
SAMYANG BIOPHARMLS CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, an effective formulation of a transdermal antiemetic has not yet been developed

Method used

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  • Trans-dermal composition of anti-vomiting agent and preparation containing the same
  • Trans-dermal composition of anti-vomiting agent and preparation containing the same
  • Trans-dermal composition of anti-vomiting agent and preparation containing the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0064] Example 1: Preparation of Composition for Transdermal Delivery

[0065] The ethanol of 30% by weight percentage, the propylene glycol of 27% by weight percentage, the oleic acid of 30% by weight percentage and the water of 40% by weight percentage mix, then add the ondansetron of 3% by weight percentage in the mixture, obtain a transdermal Passed ingredients (ingredient 1).

[0066] The skin penetration of ondansetron was determined to be 71.4 μg / cm using the procedure of the reference example 2 / h.

example 2

[0080] Example 2: Preparation of Composition for Transdermal Delivery

[0081] Ethanol containing 20% ​​by weight, 15% by weight of propylene glycol, 3% by weight of glyceryl monooleate, 2% by weight of polyoxyethylene (n=10) oleyl ether and 60% by weight of Tropisetron was added to an aqueous solution of water to a concentration of 5% by weight to obtain a transdermal component (component 2). The skin penetration rate of its tropisetron is 30.8μg / cm 2 / h.

[0082] Examples 3 to 42: Preparation of Compositions for Transdermal Delivery

[0083] Using the ingredients shown in Table 1, repeat the steps of Example 1 or 2 to obtain the medicament components (components 3 to 42) delivered through the skin, by referring to the steps of the example, determine the skin of the active ingredients in the ingredients of each medicament penetration rate.

[0084]

ingredient number

3

4

5

6

7

8...

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PUM

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Abstract

A transdermal composition of the present invention comprises (a) a matrix containing (i) 20 to 80 % by weight of an alcohol, (ii) 1 to 50 % by weight of a skin penetration enhancer selected from the group consisting of a fatty acid and a derivative thereof, a fatty alcohol and a derivative thereof, an amide, a terpene, a surfactant and a mixture thereof, and (iii) 15 to 80 % by weight of water; and (b) 1 to 15 % by weight, based on the weight of the matrix, of an antivomiting agent selected from the group consisting of tropisetron, ondansetron, granisetron and pharmaceutically acceptable salts thereof, which is capable of delivering the antivomiting agent efficiently over a period of a day or more without skin irritation.

Description

technical field [0001] This invention relates to a transdermal antiemetic composition and a formulation containing the same which is effective for transdermal delivery of an antiemetic for one or more days without irritation to the skin. Background technique [0002] Vomiting has many causes, including pathological factors, such as brain damage; physiological factors, such as pregnancy; and therapeutic factors, such as chemotherapy. Chemotherapy involving the use of anticancer agents such as cisplatin can cause severe vomiting. [0003] Vomiting is controlled by the vomiting center located in the medulla of the brain. The gag reflex is caused by abnormal activity of visceral afferent neurons in the vagus nerve located in the abdomen, which receives signals from the emetic chemoreceptive zone (CTZ) located in the vomiting center. Thus, the emesis process is transmitted by neurotransmitters such as serratonin (serotonin, 3,5-HT3 type), acetylcholine, dopamine and histamine. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/08A61F13/02A61K9/00A61K9/70A61K31/01A61K31/015A61K31/045A61K31/122A61K31/125A61K31/35A61K31/4178A61K31/439A61K31/46A61K47/10A61K47/12A61K47/14A61K47/18A61K47/20A61K47/22A61K47/24A61K47/32A61K47/38A61P1/08
CPCA61K9/0014A61K9/7084A61K31/01A61K31/015A61K31/045A61K31/122A61K31/125A61K31/35A61K31/4178A61K31/439A61K31/46A61K47/10A61K47/12A61K47/14A61P1/08
Inventor 徐宝连赵重雄崔永权黄俊硕
Owner SAMYANG BIOPHARMLS CORP
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