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Low molecule heparin mucous membrane adhesive tablet preparations and preparation method thereof

A technology of low-molecular-weight heparin and adhesive tablets, which is applied in the direction of non-active ingredient medical preparations, pill delivery, and pharmaceutical formulations. Cholesterol-lowering effect

Inactive Publication Date: 2008-06-04
周长海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] By preparing low-molecular-weight heparin mucoadhesive tablets, the disadvantages of the current low-molecular-weight heparin injection, such as inconvenient administration, pain during injection, and possible infection at the injection site, can be overcome, and the patient's compliance with medication can be improved.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0028] The preparation method of the low molecular weight heparin mucoadhesive tablet preparation comprises the following steps:

[0029] Mix low-molecular-weight heparin, carbomer, and lactose in an appropriate amount, and directly compress the powder into tablets with a diameter of 5mm and a hardness of 4kg. Each tablet contains 20mg-80mg of low-molecular-weight heparin. Then the tablet core was put into a die with a diameter of 7mm, filled with adhesive layer auxiliary materials (Carbomer 974:HPMC K4M ratio 1:1, adhesive layer dosage: 50%) and pressed into an adhesive tablet.

example 1

[0031] The weight composition of low-molecular-weight heparin mucoadhesive tablets containing drug-containing tablet cores includes (dosage per 1000 adhesive tablets)

[0032] Lactose or fructose or sucrose 15g

[0033] Carbomer or natural hydrophilic polymer 15g

[0034] Low molecular weight heparin 20gg

[0035] The weight composition of the adhesive layer of low-molecular-weight heparin mucoadhesive tablets includes (dosage per 1000 adhesive tablets)

[0036] Carbomer or natural gum or polyvinylpyrrolidone 70g

[0037] HPMC or cellulose derivatives 70g

[0038] Magnesium stearate 0.2-25g.

example 2

[0040] The weight composition of low-molecular-weight heparin mucoadhesive tablets containing drug-containing tablet cores includes (dosage per 1000 adhesive tablets)

[0041] Lactose or fructose or sucrose 50g

[0042] Carbomer or natural hydrophilic polymer 50g

[0043] Low molecular weight heparin 80g

[0044] The weight composition of the adhesive layer of low-molecular-weight heparin mucoadhesive tablets includes (dosage per 1000 adhesive tablets)

[0045] Carbomer or natural gum or polyvinylpyrrolidone 200g

[0046] HPMC or cellulose derivatives 200g

[0047] Magnesium stearate 0.2-25g.

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Abstract

The invention relates to a preparation method of a low molecule heparin mucosal adhensive tablet preparation. The preparation method is that the low molecule heparin, carbomer and lactose are properly mixed evenly; powders are directly pressed into tablet core with the diameter of 5mm and the hardness of 4kg, and each tablet contains 20 to 80 mg low molecule heparin; then a tablet core is put into a die with the diameter of 7mm, and subsidiary substances of an adhensive layer are filled into the die to be made into the adhensive tablet. By adopting the preparation and an injection of the preparation to carry out animal experiment comparison and to do bioavailability research, distinct reduction of cholesterol, low density lipoprotein, super-low density lipoprotein caused by adhering the low molecule heparin mucosal adhensive tablet to a rabbit oral mucosa can be observed; the tablet also can reduce fibrinogen level; compared with the injection of the same dose of low molecule heparin, the effect of the tablet has no distinct difference with the effect of the injection. The bioavailability can reach 89.9 percent and has the advantages of antithrombotic function, promoting flow and reducing blood lipids, etc. The preparation has the positive curative effect, and the use is convenient. By adopting the preparation, the medicine supply times can be reduced and the effect is safe and reliable. The preparation can be used for treating hypertension, hyperlipemia and coronary heart disease, etc.

Description

technical field [0001] The invention belongs to low-molecular-weight heparin (including low-molecular-weight heparin calcium and low-molecular-weight heparin sodium) mucoadhesive tablets, oral mucosal adhesive tablet preparations and a preparation method thereof. In particular, it relates to a low-molecular-weight heparin mucoadhesive tablet preparation and a preparation method thereof. Background technique: [0002] Low molecular weight heparin (LMWH) was discovered in the 1980s when studying the molecular structure of unfractionated heparin (UFH), and it is a mixture of sulfated polysaccharides with non-uniform molecular weight. It is obtained by chemical or enzymatic depolymerization of unfractionated heparin, with a relative molecular mass of 4000~6500. LMWH is widely used clinically. It has biological activities such as anticoagulant, antithrombotic, regulating blood lipid, reducing blood viscosity, enhancing capillary permeability and improving microcirculation. It ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/32A61K47/38A61K31/727A61P3/06A61P7/02A61P9/10
Inventor 周长海
Owner 周长海
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