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Self-micro emulsion solft capsule of dihydropyridine type calcium ion agonist, and its prepn. method

A technology of calcium ion antagonists and dihydropyridines, which is applied in the field of self-microemulsifying soft capsules of dihydropyridine calcium ion antagonists and its preparation, can solve the problems of poor water solubility, low dissolution rate, and low bioavailability, etc. Achieve high dissolution rate, increase dissolution rate, and good water solubility

Inactive Publication Date: 2005-01-05
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Existing oral preparations of nitrendipine and nimodipine include preparations such as tablets, common hard capsules and soft capsules, which cause low dissolution rate and low bioavailability because of their poor water solubility.

Method used

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  • Self-micro emulsion solft capsule of dihydropyridine type calcium ion agonist, and its prepn. method
  • Self-micro emulsion solft capsule of dihydropyridine type calcium ion agonist, and its prepn. method
  • Self-micro emulsion solft capsule of dihydropyridine type calcium ion agonist, and its prepn. method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The composition of the prescription is as follows: (g)

[0039] Nitrindipine 10

[0040] Dimethylisosorbide 115

[0041] Ethyl oleate 65

[0042] Tween80 150

[0043] Vitamin E 10

[0044] Made 1000 softgels in total

[0045] Preparation process: Weigh an appropriate amount of nitrendipine, add the prescribed amount of dimethyl isosorbide, Tween80, shake it in a constant temperature shaking bath at 40°C and 100 rpm for about 1 hour to dissolve it, and then add the prescribed amount of oil Ethyl acetate and vitamin E were stirred evenly, and pressed into capsules after the liquid medicine dropped to room temperature.

Embodiment 2

[0047] The composition of the prescription is as follows: (g)

[0048] Nitrindipine 10

[0049] Dimethylisosorbide 100

[0050] Miglyol 812 50

[0051] Tween80 185

[0052] Vitamin E 10

[0053] Made 1000 softgels in total

[0054] The preparation process is the same as in Example 1.

Embodiment 3

[0056] The composition of the prescription is as follows: (g)

[0057] Nitrindipine 10

[0058] Laborosol 120

[0059] Ethyl oleate 65

[0060] Tween80 145

[0061] Vitamin E 10

[0062] Made 1000 softgels in total

[0063] The preparation process is the same as in Example 1.

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PUM

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Abstract

A self-microemulsified softcapsule of nimodipine or nitrendipine is prepared from nimodipine or nitrendipine, coemulsifier, self emulsifier, oil and antioxidizing agent through proportionally mixing nimodipine or nitrendipine, coemulsifier and self emulsifier, constant-temp oscillating, adding oil and antioxidizing agent, stirring, cooling, and shaping.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a self-microemulsifying soft capsule of nitrendipine or a dihydropyridine calcium ion antagonist of nimodipine and a preparation method thereof. Background technique: [0002] Nitrendipine (nitrendipine) is a dihydropyridine calcium antagonist, which has strong selectivity to vascular smooth muscle, but has a weak effect on cardiac muscle, so it can cause blood vessels around the body, including coronary arteries and renal arterioles, to expand , produces a hypotensive effect, but has little effect on normal blood pressure. It is mainly used to treat various types of hypertension, and the antihypertensive effect is significant and long-lasting, especially suitable for elderly hypertensive patients, and can improve the blood supply and myocardial function of the heart, kidney, and brain while reducing blood pressure. [0003] Nitrendipine has low oral bioavailability, t 1 / 2 fo...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/4422A61P9/10A61P9/12A61P25/06A61P25/28
Inventor 何仲贵殷静唐星张天虹
Owner SHENYANG PHARMA UNIVERSITY
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