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Pharmaceutical composition containing butyphthalide and solubilizer

A composition and technology of butylphthalide, which is applied in the field of pharmaceutical compositions containing butylphthalide and docusate sodium, can solve the problems of difficult operation, increased difficulty of taking patients, complicated process, etc., and achieve reduction of raw material loss, animal biological Effects of improved utilization and simplified operation procedures

Active Publication Date: 2018-09-21
田普森
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Problems in this tablet patent: butylphthalide is used in a large amount clinically. In order to increase its solubility, a large amount of cyclodextrin or its analogues must be added to completely include butylphthalide. The implementation of this patent Example 1 and Example 2, the ratio of butylphthalide to β-CD is 1:9, which leads to 600 mg per tablet, which increases the difficulty of taking it for patients; in the process, the inclusion complex is dried and crushed, then added with other excipients and then compressed into tablets. Complicated and difficult to operate, especially the problem of clathrate drying
In Example 5 of CN02123000.5 patent, the prescription and process of butylphthalide sodium chloride injection are disclosed, 32.38g (0.021mol) of hydroxypropyl beta cyclodextrin and 1g (0.0052mol) NBP are included to solubilize NBP, NBP: hydroxypropyl β-cyclodextrin = 1 mol: 4 mol, a large amount of hydroxypropyl β-cyclodextrin used in the commercially available butylphthalide sodium chloride injection will increase nephrotoxicity, leaving hidden dangers for clinical medication
The amount of N,N-dimethylacetamide used in Example 3 of CN201610361174.X patent is at least 8 times the amount of butylphthalide, which has potential safety hazards

Method used

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  • Pharmaceutical composition containing butyphthalide and solubilizer
  • Pharmaceutical composition containing butyphthalide and solubilizer
  • Pharmaceutical composition containing butyphthalide and solubilizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: injection and preparation method thereof

[0047] 1. Prescription: See Table 1

[0048] Table 1: 100 prescriptions for butylphthalide injection

[0049]

[0050] 2. Preparation process:

[0051] Weigh API and docusate sodium according to the prescription, add 100ml of water for injection and stir for 15 minutes, add PEG400 and ultrasonically stir until a clear solution, replenish water for injection to the full amount, add osmotic pressure regulator and stir for 15 minutes; use 0.1N hydrochloric acid or 0.1N hydrogen Sodium oxide is used to adjust the pH, and the pH is controlled between 4 and 7. Measure the content and pH value, filter with a 0.22 μm microporous membrane after passing the inspection, fill it after passing the clarity inspection, and sterilize at 121°C for 20 minutes.

Embodiment 2

[0052] Embodiment 2: tablet and preparation method thereof

[0053] 1. Prescription: See Table 2

[0054] Table 2: Prescription of 1,000 butylphthalide tablets

[0055] components

2-1

2-2

2-3

2-4

Butylphthalide

100

100

100

100

Z1

3.07

2.81

4.02

4.50

water

24.0

22.5

25

26

Povidone K30

100.0

125.0

90

80

β-cyclodextrin

80.0

100

90

lactose monohydrate

160.0

150

180

Low-substituted hydroxypropyl cellulose

80.0

Crospovidone

20.5

30

sucrose

140.0

pregelatinized starch

30

100

corn starch

100.0

Microcrystalline Cellulose PH302

55.0

talcum powder

12.0

24.5

16

Magnesium stearate

8.0

7.2

7.5

6

colloidal silica

2.2

2.0

5.0

10

gross weight

565.77

556.51

516...

Embodiment 3

[0061] Embodiment 3: Capsule and preparation method thereof

[0062] 1. Prescription: see Table 3

[0063] Table 3: Prescription of Butylphthalide Soft Capsules 1000 Capsules

[0064]

[0065]

[0066] 2. Preparation process:

[0067] 1) Preparation of medicinal liquid oil: Take 4-1 as an example, weigh 50g of soybean oil and heat at 40°C, add docusate sodium, stir evenly, continue to stir butylphthalide and remaining soybean oil, and place medicinal liquid oil at room temperature. Compressed capsules.

[0068] 2) Preparation of gelatin solution: weigh 100g of gelatin, 35g of glycerin, 120g of water, and 180mg of ethylparaben, put them into a plastic tank, heat to 60-70°C, add gelatin, stir to dissolve, defoam, filter, Filter the 50-55 ℃ thermal insulation glue tank for later use; put the material into the interlayer tank and stir, heat the steam interlayer to make it melt, keep it warm for 1 to 2 hours, let it stand until the foam floats up, keep it warm and filter, ...

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Abstract

The invention relates to a pharmaceutical composition containing butyphthalide and solubilizer. The composition contains the butyphthalide and solubilizer, wherein a weight ratio of the two ingredients is 1:(0.005-1). The butyphthalide is an oil micromolecule, and clinical dosage is high. In order to increase solubility of the composition and enable the composition to be well absorbed by the humanbody, many inventors conduct researches in the past. For example, the composition is encapsulated by cyclodextrin, or N,N-dimethyl-acetamide is used for improving the water solubility, however, various defects exist. On the basis of the solubilizer, corresponding excipients are matched, and the composition is prepared into various dosage forms, such as injection, tablets and soft capsules.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing butylphthalide and docusate sodium. Background technique [0002] Butylphthalide (dl-3-n-butylphthalide, NBP) is one of the chemical components in celery oil, which can improve the damage of central nervous system function in patients with acute ischemic stroke, and can promote the functional recovery of patients. Animal pharmacodynamic studies have shown that butylphthalide can block multiple pathological links of brain damage caused by ischemic stroke, has a strong anti-ischemic effect, and can significantly reduce the infarct size of regional cerebral ischemia in rats. Reduce cerebral edema, improve brain energy metabolism and microcirculation and blood flow in ischemic brain regions, inhibit nerve cell apoptosis, and have anti-thrombotic and anti-platelet aggregation effects. Butylphthalide may reduce the content of arachidon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/28A61K9/48A61K47/20A61K47/10A61K47/32A61K31/365A61P9/10A61P25/00A61P7/10A61P7/02
CPCA61K9/0019A61K9/08A61K9/2013A61K9/2027A61K9/2806A61K9/4858A61K31/365A61K47/10A61K47/20A61P7/02A61P7/10A61P9/10A61P25/00
Inventor 田普森
Owner 田普森