Transdermally absorptive preparation

A technology of patch and preparation, applied in the field of transdermal absorption patch, can solve problems such as research and development

Inactive Publication Date: 2010-10-27
COSMED PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research and development of percutaneous absorption patches such as paints, ointments, creams, cataplasms, and patches is currently almost non-existent.

Method used

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  • Transdermally absorptive preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1-10、12

[0062] According to the ratio (weight ratio) shown in Table 1, after the binder A-D solution, glycerin, cholesterol, sodium lauryl sulfate and glyceryl monocaprate are mixed, add according to the ratio (weight ratio) shown in Table 1 Alendronate, incadronate, and PEG-modified alendronate dissolved in 20 parts by weight of water are then coated on a carbamate film with a thickness of 40 μm, and after drying, a film with a thickness of 200 μm of the adhesive layer is obtained. Patches for transdermal absorption.

Embodiment 11

[0064] Take 32 g of ethylene-isoprene-ethylene copolymer (manufactured by Kraton Japan, trade name [Kraton D1107]), alicyclic hydrocarbon tackifier (manufactured by Arakawa Chemical Co., trade name [Arkon P-90]) and liquid 28 g of paraffin wax (manufactured by Nacarai Desk, Chemical Reagent) was put into a mixer, and mixed at 120° C. to prepare a hot-melt adhesive (adhesive E). Lower the temperature to 90°C, add 2 g of sodium lauryl sulfate and 10 g of alendronate and mix well, then coat and dry the film on a polyethylene terephthalate film to obtain a patch with an adhesive layer thickness of 200 μm percutaneous absorption preparations.

[0065] [Table 1]

[0066] Example

[0067] Adhesives A-D are by solid content weight

Embodiment 13，14

[0069] After binder A or B, glycerin or sodium lauryl sulfate and glyceryl monocaprate are mixed by the proportioning (weight ratio) shown in Table 1, add and dissolve in the proportioning (weight ratio) shown in Table 1 Alendronate in 20% water by weight, then add dibutyl hydroxytoluene or vitamin E according to the proportion (weight ratio) shown in Table 1 and mix, then, coat a carbamate film with a thickness of 40 μm, and dry it to prepare A patch type percutaneous absorption preparation having an adhesive layer thickness of 200 μm was obtained.

[0070] The transdermal drug absorption test was carried out using the prepared patch type transdermal absorption preparation, and the results are shown in Table 2. The drug percutaneous absorption test was carried out as follows.

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Abstract

Disclosed is a tape-type transdermally absorptive preparation which has excellent transdermal absorption, high safety and high usability, and which is suitable for the treatment of a disorder of bone / calcium metabolism, such as osteoporosis, osseous Paget's disease and hypercalcemia associated with a malignant tumor. Specifically disclosed is a tape-type transdermally absorptive preparation characterized by containing a bisphosphonate or a derivative thereof. Preferably, the tape-type transdermally absorptive preparation comprises a support sheet and an adhesive layer laminated on one surface of the support sheet, wherein the adhesive sheet comprises: 100 parts by weight of an acrylic copolymer which comprises 50 to 88 wt% of acrylic acid, 8 to 40 wt% of 2-ethylhexyl acrylate and 1 to 42 wt% of a polar monomer (excluding acrylic acid); 150 to 600 parts by weight of a polyhydric alcohol; and a pharmaceutically effective amount of a bisphosphonate.

Description

technical field [0001] The invention relates to a percutaneous absorption patch, in particular to a percutaneous absorption patch for treating abnormal calcium metabolism in bones. Background technique [0002] Oral and injectable bisphosphonates are generally used for the treatment of hypercalcemia caused by osteoporosis, osteitis deformans, and malignant bone tumors. (Patent Document 1) [0003] However, the disadvantage of oral bisphosphonate pharmaceutical preparations is that the absorption rate is extremely low (1-2%) when administered orally, and the absorption rate further decreases by 80-90% when the drug is taken with food. In addition, bisphosphonate drugs have strong mucosal damage to the stomach and esophagus. In order to avoid damage to the mucosa, it is necessary to maintain an upright position for 30 minutes after taking the drug, which is very important for elderly patients who account for 70% of osteoporosis patients. Big burden. However, injections need...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/663A61K9/70A61K47/10A61K47/28A61K47/32A61P19/08A61P19/10
CPCA61K9/7061A61K31/663A61K47/10A61K47/32A61K47/28A61P19/08A61P19/10A61P3/14
Inventor 山本昌坂根稔康胜见英正神山文男权英淑
Owner COSMED PHARMA
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