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Cinnarizone self micro emulsified soft capsule and its preparation method

A self-micro-emulsifying, cinnarizine technology, applied in the field of medicine, can solve the problems of reduced bioavailability and reduced drug dissolution, and achieve the effects of reducing individual differences, improving curative effect, and improving bioavailability

Inactive Publication Date: 2004-12-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Existing oral preparations of cinnarizine have preparations such as tablets and hard capsules. According to foreign literature reports, the bioavailability of cinnarizine depends on its dissolved amount in the stomach, and the gastric acidity of people is affected by food or physiological factors. The effect of cinnarizine preparations often changes, especially the elderly people who use cinnarizine preparations usually suffer from achlorhydria, which reduces the amount of drug dissolved in the stomach, resulting in a decrease in bioavailability, so that the cinnarizine Significant individual differences in bioavailability

Method used

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  • Cinnarizone self micro emulsified soft capsule and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The composition of the prescription is as follows: (g)

[0034] Cinnarizine 25

[0035] Dimethylisosorbide 100

[0036] Oleic acid 50

[0037] Tween 80 185

[0038] Vitamin E 5

[0039] Made 1000 softgels in total

[0040] Preparation process: Cinnarizine self-microemulsified capsules Preparation method: Weigh an appropriate amount of cinnarizine, add the prescribed amount of dimethyl isosorbide, Tween 80, and oleic acid, and place it in a constant temperature shaking bath at 40C and 100 rpm Shake for about 1.5 hours to make it dissolve, then add antioxidant and stir evenly, and press it into capsules after the liquid drops to room temperature.

[0041] The cinnarizine self-microemulsifying capsules prepared according to Example 1 were compared with commercially available tablets and capsule dissolution rates: the prepared homogeneous solution was packed into hard capsules according to the prescription amount, and the commercially available cinnar...

Embodiment 2

[0045] The composition of the prescription is as follows: (g)

[0046] Cinnarizine 25

[0047] Dimethylisosorbide 130

[0048] Oleic acid 55

[0049] Tween 80 185

[0050] Vitamin E 5

[0051] Made 1000 softgels in total

[0052] The preparation process is the same as Example 1.

Embodiment 3

[0054] The composition of the prescription is as follows: (g)

[0055] Cinnarizine 25

[0056] Dimethylisosorbide 150

[0057] Oleic acid 38

[0058] Tween 80 190

[0059] Vitamin E 5

[0060] Made 1000 softgels in total

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Abstract

A self-microemulsified softgel of cinnarizine for treating cerebral infarction, cerebral arteriosclerosis, cerebral trauma sequelae, etc is prepared from cannarizine, coemulsifier, emulsifier and an oil phase through proportionally mixing, and stirring while self emulsifying. Its advantage is high biological utilization rate.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a cinnarizine self-microemulsified soft capsule and a preparation method thereof. Background technique: [0002] Cinnarizine is a piperazine calcium channel blocker, which can block the calcium inflow of vascular smooth muscle, cause vasodilation, and can significantly improve cerebral circulation and coronary circulation. Vasospasm. The duration of action is also very long. It is mainly used for cerebral arteriosclerosis, cerebral infarction, hypertensive encephalopathy, cerebral thrombosis, cerebral hemorrhage recovery period and subarachnoid hemorrhage recovery period, sequelae of brain trauma, inner ear vertigo and peripheral vascular diseases such as Raynaud's disease, etc. Also used for tinnitus, dizziness and hearing impairment. [0003] Cinnarizine has antihistamine, anti-serotonin, antikinin activities and inhibits complement C 4 The role of activation. It has cer...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/495A61P9/10A61P9/12A61P17/00
Inventor 何仲贵殷静唐星张天虹
Owner SHENYANG PHARMA UNIVERSITY
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