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Bisoprolol Fumarate drop pills, and preparation method

A technology of bisoprolol fumarate and fumaric acid, applied in the field of bisoprolol fumarate drop pills and its preparation, can solve problems such as difficulty in adapting to swallowing, affecting full efficacy of the drug, and low bioavailability , to achieve the effect of being beneficial to labor protection and environmental protection, beneficial to human body absorption, and high bioavailability

Inactive Publication Date: 2007-10-10
陈茜
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the characteristics of such conventional preparation technology, such oral preparations have disadvantages such as long disintegration time, poor absorption, slow onset of action, and low bioavailability, which affect the full play of the drug effect.
During storage, it is easy to split, change color, absorb moisture, etc., and the quality is unstable
It is also difficult to accommodate patients who have difficulty swallowing

Method used

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  • Bisoprolol Fumarate drop pills, and preparation method
  • Bisoprolol Fumarate drop pills, and preparation method
  • Bisoprolol Fumarate drop pills, and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: In this example, the formulation of bisoprolol fumarate and a single matrix is ​​used to operate according to the preparation method in the [specific implementation method]. The coolant is simethicone oil, and dripping pills are made, and the roundness and pills are selected. Weight difference, hardness, dissolution time, etc. are used as indicators to observe the influence of the weight ratio of the drug to the single matrix on the product involved in the present invention. The test results are shown in Table 1.

[0027] Table 1 Tests of drug and single matrix formulation (all drugs are 1 part)

[0028]

[0029] 2

Polyethylene glycol 4000 (5 parts)

+++

<10

+++

<15

+++

3

Polyethylene glycol 4000 (15 parts)

+++

<10

+++

<15

+++

4

Polyethylene glycol 4000 (30 parts)

+++

<10

+++

<15

+++

5

Polyethylene glyco...

Embodiment 2

[0032] Example 2: In this example, through the formula of bisoprolol fumarate and mixed matrix, operate according to the preparation method in the [specific implementation method], the coolant is simethicone oil, and drop pills are made, and the roundness and pills are selected. Weight difference, hardness, dissolution time, etc. were used as investigation indicators to determine the weight ratio of the drug to the mixed matrix. The test results are shown in Table 2.

[0033] Table 2 Drug and mixed matrix formulation test (1 part of drug)

[0034]

[0035] 6

Polyethylene glycol 6000: carboxymethyl starch

Sodium = 1:0.3 (15 parts)

+++

<10

+++

<15

+++

7

Polyethylene glycol 6000: poloxamer = 1:

0.2 (1 part)

+++

<10

++

<15

++

8

Polyethylene glycol 6000: poloxamer = 1:

0.2 (5 parts)

+++

<10

...

Embodiment 3

[0038] Embodiment 3: In this embodiment, different coolants are selected, and the coolant is simethicone, liquid paraffin, vegetable oil, and polyethylene glycol is selected as a single matrix 6000 , the mixed matrix chooses polyethylene glycol 6000 : the formula of poloxamer=1:0.2, operate according to the preparation method in [the specific embodiment], drip dripping pill, select roundness, pill weight difference, hardness, dissolving time etc. as investigation index, observe different The impact of coolant on the products involved in the present invention, the test results are shown in Table 3.

[0039] Table 3 Experiments using different coolants (drug: matrix = 1:5)

[0040]

[0041] 3

liquid paraffin

single

++

<10

+++

<15

++

4

liquid paraffin

mix

++

<10

+++

<15

++

5

vegetable oil

single

++

<10

+++

<15

++

...

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Abstract

A dripping pill of bisoprolol fumarate for treating primary hypertension and angina pectoris is prepared from bisoprolol fumarate and the matrix of dripping pill. Its preparing process is also disclosed.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, in particular to a bisoprolol fumarate drop pill prepared from bisoprolol fumarate and a drop pill base for the treatment of patients with essential hypertension and angina pectoris and its preparation method. Background technique [0002] Hypertension and angina pectoris are the most common cardiovascular diseases in the world today, and are the leading causes of death and disability in adults. In recent years, with the progress of society, the improvement of people's living standards and the continuous acceleration of the pace of work, the number of patients with hypertension has increased significantly. The prevalence of hypertension in my country has increased significantly. According to statistics in China, the incidence of hypertension among people aged 35 to 74 in China is as high as 27%, and the number of patients is close to 130 million. , and with an annual growth rate of more than 30...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/138A61K9/20A61P9/10A61P9/12
Inventor 陈茜滕慧丽
Owner 陈茜
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