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Transdermal composition of antivomiting agent and preparation containing the same

A skin and ingredient technology, applied in the field of transdermal antiemetic ingredients and preparations containing the same ingredients, can solve the problem that effective antiemetic formulations have not yet been developed

Inactive Publication Date: 2002-08-14
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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  • Transdermal composition of antivomiting agent and preparation containing the same
  • Transdermal composition of antivomiting agent and preparation containing the same
  • Transdermal composition of antivomiting agent and preparation containing the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0062] Among them, Js and A have the same meaning as defined in the previous formula, and (dQ / dt)ss is the amount of drug that penetrates the skin per unit time under steady state conditions. Example 1: Preparation of Composition for Transdermal Delivery

[0063] 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).

[0064] The skin penetration of ondansetron was determined to be 71.4 μg / cm using the procedure of the reference example 2 / h. Comparative Example 1: Preparation of Comparative Components.

example 2

[0070]As we can see from the results of Example 1 and Comparative Examples 1 to 6, the composition 1 with the skin penetration enhancer is better than the comparative ingredients 1-7 without the skin penetration enhancer (sic-translation Author's note) showed higher skin penetration of ondansetron. Example 2: Preparation of Composition for Transdermal Delivery

[0071] 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. Examples 3 to 42: Preparation of Compositions for Transdermal Delivery

[0072] 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...

example 2

[0080] The skin penetration rate of tropisetron in this poultice is 47.2 μg / cm 2 / h. Preparation example 2: single-piece base material plaster

[0081] 20% by weight of ethanol, 15% by weight of polypropylene glycol, 2% by weight of oleic acid, 3% by weight of octanol, 5% by weight of octylphenoxypolyethoxyethanol and 55% The water by weight was mixed, and 8% by weight of polyvinylpyrrolidone and 4% by weight of polyvinyl alcohol dissolved in distilled water were added to the mixture. Vigorously stir the obtained solution to make it uniform, add 4% by weight hydroxyethyl cellulose and 6% by weight tropisetron to the solution, and stir the obtained mixture evenly.

[0082] The solution thus obtained was placed in a mold to a depth of 2 mm and kept at a temperature of 4°C for one day to obtain a hydrogel.

[0083] The hydrogel was placed in a layer on an impermeable protective film pre-coated with acrylate (Durotak 87-2196 National Starch Company), and then a silicone-coated ...

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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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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
CPCA61K31/125A61K31/015A61K31/46A61K9/0014A61K47/14A61K31/35A61K47/10A61K31/122A61K31/4178A61K31/01A61K9/7084A61K31/045A61K47/12A61K31/439A61P1/08
Inventor 徐宝连赵重雄崔永权黄俊硕
Owner SAMYANG BIOPHARMLS CORP
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