Dihydroergotoxine methanesulfonate sustained release tablet and preparation method thereof
A technology of dihydroergot alkaloid methanesulfonate and slow-release tablets, which is applied in the field of medicine, can solve the problems of reduced bioavailability, difficulty in dissolving and absorbing, and troubles, and achieves the effects of convenient application, low cost, and simple process
Inactive Publication Date: 2014-06-18
珠海天翼医药技术开发有限公司
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- Application Information
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Problems solved by technology
[0003] Dihydroergot alkaloid mesylate sustained-release preparations have stable blood drug concentration, less toxic and side effects, and better safety and effectiveness compared with common preparations. However, due to the influence of the release speed of traditional sustained-release preparations, they are relatively fast Thereby it needs to be taken orally once every morning and evening, which brings certain troubles to the crowd who often eat. Patent CN200810118871.8 and patent 200810239715.7 have announced a kind of preparation method of dihydroergot alkaloid methanesulfonate tablet, which adopts the conventional slow-release tablet preparation method Sustained release formulation
However, dihydroergot alkaloid mesylate does not dissolve at all in artificial intestinal juice (pH6.8), so the above-mentioned slow-release preparations only release a part in the stomach of the human body, and then reach the small intestine, it is difficult to dissolve and absorb, and bioavailability degree will decrease
Method used
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Comparison scheme
Effect test
Embodiment 1
[0017] Raw materials
[0018] hypromellose
[0019] After the raw and auxiliary materials are evenly mixed, they are directly compressed into tablets, and the tablet weight ranges from 0.237 to 0.263 g to obtain the finished product 1.
Embodiment 2
[0021] Raw materials
[0022] After the raw and auxiliary materials are evenly mixed, they are directly compressed into tablets with a weight range of 0.237-0.263g to obtain the finished product 2.
Embodiment 3
[0024] Raw materials
[0025] After the raw and auxiliary materials are evenly mixed, they are directly compressed into tablets with a weight range of 0.237-0.263g to obtain the finished product 3.
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The invention provides a dihydroergotoxine methanesulfonate sustained release tablet. The dihydroergotoxine methanesulfonate sustained release tablet comprises the following components in parts by weight: 1%-1.5% of dihydroergotoxine methanesulfonate, 70%-90% of sustained release agent, 8%-28% of expanding agent and 0.5%-1% of lubricating agent, wherein in the product obtained according to the formula, the sustained release agent can form a gel in water, the expanding agent can expand rapidly in water to ensure that the tablet is finally expanded to 10-20 times of the size of an original tablet; the volume of the tablet produces buoyancy to enable the tablet to float on a gastric fluid; with slow dissolution of the gel, a main drug releases slowly in vivo to achieve the sustained release effect. Besides, the main drug can be dissolved and absorbed in medicine liquid to achieve good bioavailability. The invention also provides a preparation method of the dihydroergotoxine methanesulfonate sustained release tablet. The preparation method is simple in process and suitable for popularization.
Description
technical field [0001] The invention relates to the field of medicine, in particular to a dihydroergot alkaloid mesylate sustained-release tablet, and also relates to a preparation method of a dihydroergot alkaloid mesylate sustained-release tablet. Background technique [0002] Dihydroergot alkaloid methanesulfonate is a kind of medicine, which is suitable for mental degeneration symptoms caused by age, Alzheimer's disease, cerebrovascular accident, peripheral vascular disease, and conscious vascular symptoms caused by arterial hypertension. [0003] Dihydroergot alkaloid mesylate sustained-release preparations have stable blood drug concentration, less toxic and side effects, and better safety and effectiveness compared with common preparations. However, due to the influence of the release speed of traditional sustained-release preparations, they are relatively fast Thereby it needs to be taken orally once every morning and evening, which brings certain troubles to the cro...
Claims
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Patent Timeline
Login to View More IPC IPC(8): A61K9/22A61K31/48A61K47/32A61K47/36A61K47/38A61P25/28A61P9/10A61P9/12A61P9/00
Inventor 张晓明麦耀权
Owner 珠海天翼医药技术开发有限公司

