CN113425692A

CN113425692A - Laburnine orally disintegrating tablet and preparation method thereof

Info

Publication number: CN113425692A
Application number: CN202010207569.0A
Authority: CN
Inventors: 董玉娇; 王宇杰
Original assignee: Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
Current assignee: Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
Priority date: 2020-03-23
Filing date: 2020-03-23
Publication date: 2021-09-24

Abstract

The invention relates to the technical field of medicines, and relates to a laburnine orally disintegrating tablet and a preparation method thereof, which are characterized in that: contains cytisine, filler, disintegrant, lubricant and correctant. In addition, the preparation method adopts wet granulation, has stable and mature technical process and simple preparation process, and is suitable for large-scale production. The laburnine orally disintegrating tablet provided by the invention has the advantages of rapid disintegration, excellent taste, no gravel feeling, good compliance and the like.

Description

Laburnine orally disintegrating tablet and preparation method thereof

Technical Field

The invention belongs to the field of pharmaceutical preparations, relates to a cytisine orally disintegrating tablet and a preparation method thereof, and is a novel smoking cessation drug with remarkable curative effect.

Background

Cytisine (Cytisine) is a kind of alkaloid with alpha-pyridone tricyclic structure, and is mostly distributed in leguminous and berberidaceae plants. The cytisine can be clinically used for intramuscular or intravenous injection, and can be used for rescuing reflex apnea, shock, neonatal asphyxia and the like caused by operations and various wounds. Some recent studies show that the alkaloid also has various biological activities such as arrhythmia resistance, infection resistance and the like. In recent years, the cytisine as a curative effect obviously attracts the attention of the international medical community.

Disclosure of Invention

The invention aims to provide a method for preparing a high-purity zinc oxide,The orally disintegrating tablet has the advantages of high dissolution speed, good patient compliance and high drug bioavailability. In order to overcome the defects that the common cytisine tablet has poor compliance to dysphagia patients, low bioavailability and difficulty in preparing oral preparations from bitter taste, the inventor of the invention selects and selects a large number of experiments to effectively improve the taste of cytisine and provides a cytisine orally disintegrating tablet with quicker dissolution, stable quality and strong patient compliance. Meanwhile, the preparation method of the orally disintegrating tablet, which has simple and stable process and is suitable for mass production, is also provided. The application provides a sparteine orally disintegrating tablet which characterized in that: contains cytisine, filler, disintegrant, lubricant and correctant. The filler is one or more of mannitol, silicified microcrystalline (90), silicified microcrystalline (50), and microcrystalline cellulose PH 101; wherein the laburnine is pulverized and sieved with 200 mesh sieve, and has particle diameter less than 30um。

The disintegrating agent is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose and croscarmellose sodium; the internal filling amount is 20-60%, the disintegrating amount is 3-10%, the flavoring amount is 0.4-3%, and the lubricating amount is 1-2%. Adding wetting agent which is one or more of ethanol and water, sieving with 30 mesh sieve, and granulating. And (4) drying by blowing at 40 ℃ until the water content is 1-3%. Weighing the dried granules, adding in a reduced yield, wherein the added disintegrating agent is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose and croscarmellose sodium, preferably sodium croscarmellose; the correctant is one or more of aspartame, Mentholum, acesulfame potassium, stevioside, herba Menthae essence, and vanilla essence, preferably Mentholum and acesulfame potassium. The additional lubricant is one or more of magnesium stearate, magnesium aluminum silicate, sodium stearyl fumarate, sucrose fatty acid ester, glyceryl monostearate and talcum powder, preferably magnesium stearate;

example 1

The laburnine orally disintegrating tablet is prepared from the following components in percentage by weight:

a method for preparing the laburnine orally disintegrating tablet by adopting wet granulation comprises the following steps:

the preparation method comprises the steps of crushing the sparteine, sieving the crushed sparteine with a 200-mesh sieve, adding auxiliary materials according to the prescription amount, taking 20% of purified water as a wetting agent, granulating with a 40-mesh sieve, carrying out air blast drying at 40 ℃, drying the water to 1-3%, sieving the dried granules with a 30-mesh sieve, grading, weighing, converting the yield, adding silicified microcrystal (90), menthol, acesulfame and magnesium stearate, and carrying out phi 6 flat punching on the tablets, wherein the weight of the tablets is 150 mg, and the hardness is 20-40N.

Example 2

the preparation method comprises the steps of crushing the sparteine, sieving the crushed sparteine with a 200-mesh sieve, adding auxiliary materials according to the prescription amount, taking 20% of purified water as a wetting agent, granulating the obtained product with a 30-mesh sieve, carrying out air blast drying at 40 ℃, drying the obtained product until the water content is 1-3%, sieving the dried granules with the 30-mesh sieve, carrying out size stabilization, weighing, converting the obtained product into yield, adding silicified microcrystal (90), menthol, acesulfame and magnesium stearate, and carrying out phi 6 flat punching on the obtained product, wherein the weight of the.

Example 3

the preparation method comprises the steps of crushing the sparteine, sieving the crushed sparteine with a 200-mesh sieve, adding auxiliary materials according to the prescription amount, taking 20% of purified water as a wetting agent, granulating the obtained product with a 30-mesh sieve, carrying out air blast drying at 40 ℃, drying the obtained product until the water content is 1-3%, sieving the dried granules with the 30-mesh sieve, carrying out size stabilization, weighing, converting the obtained product into yield, adding silicified microcrystal (50), menthol, acesulfame and magnesium stearate, and carrying out phi 6 flat punching on the obtained product, wherein the weight of the obtained product is 150 mg, and the hardness of the obtained product is 20-40N.

Example 4

Example 5

Comparative example 1

crushing the cytisine, sieving with a 200-mesh sieve, adding auxiliary materials in the formula amount, taking 20% of purified water as a wetting agent, granulating with a 40-mesh sieve, drying by blowing at 40 ℃, drying to 1-3% of water, sieving the dried granules with a 30-mesh sieve, grading, weighing, converting into yield, adding silicified microcrystal (90), menthol, acesulfame and magnesium stearate, pressing into tablets with phi 6, the tablet weight is 150 mg, and the hardness is 20-40N

Comparative example 2

the preparation method comprises the steps of crushing the sparteine, sieving the crushed sparteine with a 200-mesh sieve, adding auxiliary materials according to the prescription amount, taking 20% of purified water as a wetting agent, granulating with a 40-mesh sieve, carrying out air blast drying at 40 ℃, drying the water to 1-3%, sieving the dried granules with a 30-mesh sieve, carrying out size stabilization, weighing, converting the yield, adding microcrystalline cellulose (PH 101), menthol, acesulfame and magnesium stearate, and carrying out phi 6 flat punching on the tablets, wherein the tablet weight is 150 mg, and the hardness is 20-40N.

Comparative example 3

the preparation method comprises the steps of crushing the sparteine, sieving the crushed sparteine with a 200-mesh sieve, adding auxiliary materials according to the prescription amount, taking 20% of purified water as a wetting agent, granulating with a 40-mesh sieve, carrying out air blast drying at 40 ℃, drying the water to 1-3%, sieving the dried granules with a 30-mesh sieve, grading, weighing, converting the yield, adding microcrystalline cellulose (PH 102), menthol, acesulfame and magnesium stearate, and carrying out phi 6 flat punching on the tablets, wherein the tablet weight is 150 mg, and the hardness is 20-40N.

The disintegration time measuring method comprises the following steps: taking the samples of the examples and the comparative examples, the disintegration time and mouth feel of the laburnine orally disintegrating tablets prepared in the examples and the comparative examples are shown in table 1, referring to the disintegration time limit inspection method (0921, second part of chinese pharmacopoeia 2015 edition), which is an operation according to the method, and the time from when the tablets were contacted with water until the granules completely passed through the sieve is taken as the disintegration time.

Table 1 disintegration time and mouth feel of laburnine orally disintegrating tablets prepared in examples and comparative examples

Name (R)	Disintegration time(s)	Taste of the product
			Example 1	27 s	Cool feeling is strong, sweetness is general, and no gravel feeling is caused
Example 2	25 s	Cool feeling is strong, sweetness is general, and no gravel feeling is caused
			Example 3	30 s	Cool feeling is strong, sweetness is general, and no gravel feeling is caused
Example 4	29 s	Cool feeling is strong, sweetness is general, and no gravel feeling is caused
			Comparative example 1	59 s	Strong cooling feeling, pseudo-tingling feeling, and no gravel feeling
Comparative example 2	132 s	Strong cooling feeling, pseudo-tingling feeling, and no gravel feeling
			Comparative example 3	128 s	Strong cooling feeling, pseudo-tingling feeling, and no gravel feeling

Through the investigation and analysis of the aspects of disintegration time, appearance, taste and the like of the samples prepared in the embodiments, the laburnine orally disintegrating tablet prepared by the invention is quick in disintegration, can be completely disintegrated within 40 seconds, has good taste, does not have gravel feeling and uncomfortable feeling, and meets the requirements of patients. And the preparation process is simple and is suitable for large-scale production.

Claims

1. A laburnine orally disintegrating tablet is characterized in that: contains cytisine, filler, disintegrant, lubricant and correctant.

2. The method of claim 1, further comprising: the filler is one or more of mannitol, silicified microcrystalline (90), silicified microcrystalline (50), and microcrystalline cellulose PH 101.

3. According to claim 2, characterized in that: the internal filling amount is 20% -60%.

4. The method of claim 1, further comprising: the disintegrant is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, and croscarmellose sodium.

5. According to claim 4, characterized in that: the disintegrating dosage is 3% -10%.

6. The method of claim 1, further comprising: the lubricant is one or more of magnesium stearate, magnesium aluminum silicate, sodium stearyl fumarate, sucrose fatty acid ester, glyceryl monostearate, pulvis Talci, stearic acid, and silicon dioxide.

7. According to claim 6, characterized in that: the amount of the lubricant is 1% -2%.

8. The method of claim 1, further comprising: the correctant is one or more of aspartame, Mentholum, acesulfame potassium, stevioside, herba Menthae essence, and vanilla essence.

9. The method of claim 8, further comprising: the flavoring agent is 0.4-3%.

10. The method of claim 1, which is prepared by:

(1) pulverizing the raw material laburnine, sieving with 200 mesh sieve, adding filler and disintegrating agent, mixing, adding wetting agent to make soft material, sieving with 30 mesh sieve, and granulating; wherein the particle diameter of the raw material medicine is less than 30μm；

(2) Drying the mixture in a baking oven at 40 ℃ by blast air until the water content is 1-3%;

(3) taking out the dried particles, and finishing the particles by a 30-mesh sieve;

(4) and (4) weighing the dried particles in the step (3), and adding the conversion yield.