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Transdermal method and patch for nausea

A skin-to-skin contact technology, applied in medical science, bandages, etc., can solve problems such as lack of penetration enhancers

Inactive Publication Date: 2008-05-14
ABEILLE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Prolonged delivery to the blood has been reported, but with transdermal delivery devices lacking penetration enhancers

Method used

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  • Transdermal method and patch for nausea
  • Transdermal method and patch for nausea

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1: Preparation of Adhesive Mixture and Transdermal Delivery Device

[0084] Table 1:

[0085] combination

Formula A

Formula B

patch size

15.0cm 2

15.0cm 2

Estimated target daily dose

1.2mg

1.2mg

Dry%

Dry%

Styrene-butadiene rubber

pressure sensitive adhesive

44.04

--

Acrylate-vinyl ethyl

Ester Pressure Sensitive Adhesives

--

43.8

Isopropyl myristate

3.01

4.07

granisetron base

3.05

3.05

Polyester release liner

35.8

35.8

polyester mat

13.3

13.3

[0086] components

[0087] Formulation A and Formulation B were formulated using the amounts of each component in Table 1 above.

[0088]The styrene-butadiene rubber pressure sensitive adhesive used in this example was DURO-TAK(R) 87-6173 adhesive, available from National Starch and Chemica...

Embodiment 2

[0094] Example 2: Flow testing of granisetron base from a transdermal delivery device

[0095] step

[0096] Thermally isolated human cadaver skin was cut to the desired size and mounted on Franz diffusion cells. The release liner was peeled from the patch prepared according to Formulation B described in Example 1 above. Place the patch on the skin and press the patch and skin together. Add receptor solution to spreading cells and maintain assembly at 32 °C. At regular intervals (24 hours, 48 ​​hours, 72 hours, 96 hours, and 120 hours) measured amounts of receptor solution were withdrawn. The concentration of granisetron in the receptor solution was measured at each moment and the flow rates in samples A and B were calculated. The resulting data are shown in Figure 1. Similarly, the cumulative delivery of granisetron over the indicated times was calculated from the concentration of granisetron in the receptor solution at each moment and is shown in FIG. 2 .

Embodiment 3

[0097] Example 3: Stability of Granisetron in Example Examples

[0098] Table 2:

[0099] combination

[0100] Using the formulations in Table 2, patches were prepared according to the procedure described in Example 1. The patches were then tested for granisetron stability using the method described below.

[0101] Patch samples were stored at 50 °C for up to 2 months. The stability of the product is evaluated by periodically testing the granisetron content and the total amount of impurities with high performance liquid chromatography. The results are shown in Table 3 below.

[0102] table 3:

[0103] time

[0104] The data in Table 3 show that in the compositions of the examples of the present invention, granisetron remains stable at 50° C. for at least 2 months, relative to the initial time T 0 When formulated, there is only a small amount of potency loss and a small amount of impurities.

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PUM

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Abstract

Provided is a method of treating acute, delayed or anticipatory emesis for a sustained period in an individual, which involves applying to a portion of intact skin on the individual a composition of i. an antiemetically effective amount of a 5-HT3 receptor antagonist; ii. a permeation enhancing amount of permeation enhancer comprising 0.5% to 15% by weight of the skin-contacting layer; and iii. an adhesive, wherein a plasma concentration of the 5-HT3 receptor antagonist in a therapeutically effective range is provided for period of time from an onset time to 12 hours or more after the composition is removed.

Description

[0001] Related references [0002] This application claims priority to the following U.S. patent applications: 11 / 380,268 filed April 26, 2006, 60 / 682,251 filed May 18, 2005, 60 / 702,744 filed July 27, 2005, 60 / 759,381, filed January 17, 2006. technical field [0003] This application relates to transdermal devices and methods for the treatment of nausea and vomiting, and more particularly to 3 Transdermal methods, compositions and devices of receptor antagonists for the treatment of nausea and vomiting over a sustained period of time. Background technique [0004] Most patients undergoing anticancer treatment, whether with chemotherapy or radiation, suffer from treatment side effects such as nausea and vomiting, which are common complaints among patients. In order to prevent or minimize the side effects of these anticancer treatments, it is widely practiced to administer antagonists of serotonin subtype 3 (hereinafter referred to as "serotonin") in parenteral or oral form...

Claims

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Application Information

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IPC IPC(8): A61F13/00
Inventor 卡尔帕那·帕特尔苏雷什·鲍尔萨迪亚
Owner ABEILLE PHARMA