Transdermal patch comprising rasagiline mesylate and preparation method therefor
AssigneeShanghai World Leader Pharmaceutical Co., Ltd.
InventorsJinkang Gong, Zhihui Xu, Changlei Sun
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Abstract
A transdermal patch comprising rasagiline mesylate and a preparation method therefor. A hydrogen bond complex is formed by means of the combined action of rasagiline mesylate, crospovidone and a crystallization inhibitor, so that rasagiline mesylate is present in a drug carrier in an amorphous state, thereby avoiding an unstable form of a free base. The transdermal patch further comprises a release-promoting agent selected from one or more of levulinic acid, octanoic acid and undecylenic acid.
Claims28
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A transdermal patch comprising rasagiline mesylate, comprising a backing layer, a matrix layer and a protective layer, wherein the matrix layer comprises following components in mass percentage:
- 0.5-5.0% of rasagiline mesylate, 40-80% of a binder, 3-25% of crospovidone, 0.1-5.0% of a release promoter, 1-15% of a penetration enhancer, 0.5-10% of a plasticizer, and 0.001-0.5% of an antioxidant, wherein a mass ratio of rasagiline mesylate to crospovidone is 1:5 to 1:15, and a content of the binder is finally adjusted to formulate a mass percentage of 100%, and the release promoter is selected from one or a combination of several of levulinic acid, octanoic acid, and undecanoic acid.
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A preparation method for a transdermal patch comprising rasagiline mesylate, comprising:
- step 1:
- preparing a drug-containing matrix layer, wherein 0.5-5.0% of rasagiline mesylate, 0.1-5.0% of a release promoter, 1-15% of a penetration enhancer, 0.5-10% of a plasticizer, and 0.001-0.5% of an antioxidant are weighed, dissolved in a solvent, and mixed and stirred until all solids are completely dissolved to provide a homogeneous solution;
- 3-25% of crospovidone is added into the homogeneous solution, followed by pre-mixing and swelling sufficiently and then homogenizing, to provide a white emulsion liquid;
- and 40-80% of a binder is added to the white emulsion liquid, followed by mixing and stirring uniformly to provide an intermediate solution;
- step 2:
- coating and drying to remove the solvent, wherein the intermediate solution is coated on a protective layer, with a wet film thickness of 100-500 μm, and then dried to provide a dried matrix, with a dried film thickness of 20-250 μm;
- and
- step 3:
- laminating, compounding and cutting, wherein the backing layer is laminated and compounded with the dried matrix, and then cut into patches,
- wherein the release promoter is selected from one or a combination of several of levulinic acid, octanoic acid, and undecanoic acid, a mass ratio of rasagiline mesylate to crospovidone is 1:5 to 1:15, and a content of the binder is finally adjusted to formulate a mass percentage of 100%.
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A matrix mixture, for preparing a transdermal patch comprising rasagiline mesylate, comprising following components in mass percentage:
- 0.5-5.0% of rasagiline mesylate, 40-80% of a binder, 3-25% of crospovidone, 0.1-5.0% of a release promoter, 1-15% of a penetration enhancer, 0.5-10% of a plasticizer, and 0.001-0.5% of an antioxidant, with a mass ratio of rasagiline mesylate to crospovidone being 1:5 to 1:15, and a content of the binder being finally adjusted to formulate a mass percentage of 100%, wherein the release promoter is selected from one or a combination of several of levulinic acid, octanoic acid, and undecanoic acid.
Dependencies are inferred from the claim text.