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Nitroglycerin sublingual tablet and preparation method thereof

A technology for nitroglycerin and sublingual tablets, which is applied in directions such as pharmaceutical formulations, medical preparations of inactive ingredients, and pill delivery, can solve problems such as unfavorable carrying, low hardness, and brittleness easily.

Inactive Publication Date: 2021-02-05
南京斯泰尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the addition of these stabilizers may cause prolongation of disintegration time
At the same time, since the nitroglycerin sublingual tablet needs to disintegrate quickly under the tongue to take effect quickly, its hardness is very low, basically less than 5N, and it is prone to brittleness, which is not conducive to carrying

Method used

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  • Nitroglycerin sublingual tablet and preparation method thereof
  • Nitroglycerin sublingual tablet and preparation method thereof
  • Nitroglycerin sublingual tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1 Nitroglycerin sublingual tablet (specification: 0.3mg)

[0021]

[0022]

[0023] Step a: pretreatment: (1) part of lactose monohydrate and stearic acid macrogol glyceride are mixed through a 100 mesh sieve (2) part of lactose monohydrate and colloidal silicon dioxide are mixed through a 100 mesh sieve (3) micro Crystalline cellulose crosses 100 mesh sieves (4) magnesium stearate crosses 80 mesh sieves; (5) raw materials cross 100 mesh sieves;

[0024] Step b: Mixing: Add about half of the lactose monohydrate and macrogol glyceride stearate into the three-dimensional mixer, add the raw materials, add the remaining lactose monohydrate and macrogol glycerol stearate mixture, Mix for 5 minutes at 12 rpm; add the mixture of lactose monohydrate and colloidal silicon dioxide and mix for 5 minutes; add microcrystalline cellulose and mix for 5 minutes; add magnesium stearate and mix for 5 minutes.

[0025] Step c: Tablet compression: This product is a white ...

Embodiment 2

[0026] Example 2 Nitroglycerin Sublingual Tablet (Specification: 0.6mg)

[0027]

[0028] Step a: pretreatment: (1) part of lactose monohydrate and stearic acid macrogol glyceride are mixed through a 100 mesh sieve (2) part of lactose monohydrate and colloidal silicon dioxide are mixed through a 100 mesh sieve (3) micro Crystalline cellulose crosses 100 mesh sieves (4) magnesium stearate crosses 80 mesh sieves; (5) raw materials cross 100 mesh sieves;

[0029] Step b: Mixing: Add about half of the lactose monohydrate and macrogol glyceride stearate into the three-dimensional mixer, add the raw materials, add the remaining lactose monohydrate and macrogol glycerol stearate mixture, Mix for 5 minutes at 12 rpm; add the mixture of lactose monohydrate and colloidal silicon dioxide and mix for 5 minutes; add microcrystalline cellulose and mix for 5 minutes; add magnesium stearate and mix for 5 minutes.

[0030] Step c: Tablet compression: This product is a white compressed tabl...

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Abstract

The invention relates to a nitroglycerin sublingual tablet for treating angina pectoris. According to the nitroglycerin sublingual tablet for treating the angina pectoris, a novel surfactant polyethyleneglycol stearate is utilized to increase the stability of the prepared nitroglycerin sublingual tablet and shorten disintegration time of the tablet in the oral cavity; and moreover, the nitroglycerin sublingual tablet has the advantages of being capable of avoiding first pass effect and convenient to store.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, in particular, the invention relates to a sublingual nitroglycerin tablet and a preparation method thereof. Background technique [0002] Because nitroglycerin has an obvious first-pass effect, and its oral bioavailability is only 8%, nitroglycerin sublingual tablets can quickly relieve the attack of angina pectoris caused by coronary artery disease. Its mechanism of action is the formation of free radical nitric oxide (NO), which activates guanylate cyclase, leading to an increase in guanosine 3'5' monophosphate (cyclic GMP) in smooth muscle and other tissues, which in turn leads to myosin Dephosphorylation of light chains, thereby regulating the contractile state of smooth muscle and causing vasodilation. [0003] Although nitroglycerin tablets have been used clinically for decades, due to the strong volatility of nitroglycerin, it is easy to cause instability of tablet content, including mig...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/26A61K47/38A61K47/14A61K31/21A61P9/10
CPCA61K9/2054A61K9/2031A61K9/2018A61K9/006A61K31/21A61P9/10
Inventor 张自强孙军娣周国才
Owner 南京斯泰尔医药科技有限公司
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