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Nitrendipine self-emulsification soft capsules and preparation method thereof

A technology of nitrendipine and self-microemulsification, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and drug delivery. Effects of low bioavailability, increased bioavailability, and reduced disparity

Inactive Publication Date: 2009-04-29
贾祥波 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Nitrendipine, which is widely used clinically at present, is mostly ordinary tablets. Tablet is one of the most widely used oral solid dosage forms in the field of medicine. It has the advantages of convenient storage and drug stability. However, due to its extremely low solubility of nitrendipine , often due to disintegration and slow dissolution of the drug, the full absorption of the drug is affected, that is, after taking the ordinary tablet, there are long dissolution time, low dissolution rate, poor absorption, strong intestinal first-pass effect, short half-life, and low bioavailability and other problems affect the therapeutic effect, so it is necessary to develop a new nitrendipine preparation

Method used

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  • Nitrendipine self-emulsification soft capsules and preparation method thereof
  • Nitrendipine self-emulsification soft capsules and preparation method thereof
  • Nitrendipine self-emulsification soft capsules and preparation method thereof

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Embodiment 1

[0028] Embodiment one: a kind of nitrendipine self-microemulsifying soft capsule of the present invention and preparation method thereof, adopt following processing steps: its component (prescription amount) ratio is by weight:

[0029] Preparation of the shell fluid:

[0030] First, weigh 900 parts of gelatin in the prescribed amount; add 200 parts of glycerin; 200 parts of sorbitol; 15 parts of titanium dioxide, 1.0 part of pigment, after stirring evenly, filter (70 mesh), vacuum defoaming, vacuum degree -0.07MPa, keep warm at 68°C (holding time), and obtain the capsule shell liquid, the rotational viscosity of the capsule shell liquid It is 260mPa.s, put it into the barrel for standby.

[0031] Preparation of content solution:

[0032]Then weigh 2 parts of nitrendipine, 12 parts of ethanol, 20 parts of propylene glycol, 80 parts of hydrogenated castor oil, and 6 parts of medium-chain fatty acid triacylglycerol in the homogeneous emulsification pot, heat to 40 °C, and heat...

Embodiment 2

[0040] A kind of nitrendipine self-microemulsifying soft capsule of the present invention and preparation method thereof, adopt following process step: its component (recipe quantity) ratio is by weight:

[0041] Preparation of the shell fluid:

[0042] First, weigh 1000 parts of gelatin in the prescribed amount; place 220 parts of glycerin; 220 parts of sorbitol; 18 parts of titanium dioxide, 1.2 parts of pigment, after stirring evenly, filter (80 mesh), vacuum defoaming, vacuum degree -0.08MPa, heat preservation at 60°C, (holding time), and obtain the capsule shell liquid, the rotation of the capsule shell liquid The viscosity is 250mPa.s, put it into the barrel for standby.

[0043] Preparation of content solution:

[0044] Then weigh 3 parts of nitrendipine, 18 parts of ethanol, 30 parts of polyethylene glycol (400), 100 parts of phospholipids, and 20 parts of ethyl linoleate in the homogeneous emulsification pot, and heat to 45 ° C. Heating time: 1.5h, stirring to diss...

Embodiment 3

[0052] A kind of nitrendipine self-microemulsifying soft capsule of the present invention and preparation method thereof, adopt following process step: its component (recipe quantity) ratio is by weight:

[0053] Preparation of the shell fluid:

[0054] First, weigh 1200 parts of gelatin in the prescribed amount; place 240 parts of glycerin; 260 parts of sorbitol; 20 parts of titanium dioxide, 1.5 parts of pigment, after stirring evenly, filter (75 mesh), vacuum defoaming, vacuum degree -0.06MPa, heat preservation (holding time) at 72°C, and obtain the capsule shell liquid, the rotational viscosity of the capsule shell liquid If it is greater than 280mPa.s, put it into a barrel for use.

[0055] Preparation of content solution:

[0056] Then weigh 4 parts of nitrendipine, 25 parts of ethanol, 35 parts of propylene glycol, 120 parts of phospholipids, and 35 parts of ethyl linoleate in the homogeneous emulsification pot, heat to 47°C, heating time: 2.0h, Stir to dissolve the ...

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Abstract

The invention relates to a nitrendipine self-microemulsifying soft capsule used for treating hypertension, and a preparation method thereof. The preparation method comprises the steps of: taking gelatin, putting the gelatin in a mixed solution of glycerin, sorbic alcohol and water for swelling, adding ethylparaben, heating the mixed solution till the gelatin is dissolved, adding titanium dioxide and a pigment into the mixed solution, resting the mixed solution for defoaming after being evenly stirred and sieved, screening the mixed solution for standby; evenly mixing nitrendipine, an emulsification auxiliary agent, an oil phase and an emulsifier and heating and stirring to form a clear solution of contents of the capsule; pressing the capsule shell fluid and the contents into soft capsules by a rotational mold pill press; and after the steps of drying and surface processing, obtaining the finished products of the soft capsules. The nitrendipine self-microemulsifying soft capsule can improve the bioavailability of the nitrendipine and perform clinical effects more safely and effectively. The preparation method is relatively simple, has no special requirements for equipment, can be realized on most production lines of the soft capsules, is easy to be accepted by production departments and manufacturers and has low manufacturing cost, thus having broad prospect of clinical application.

Description

technical field [0001] The invention relates to a nitrendipine self-microemulsifying soft capsule and a preparation method thereof, in particular to a self-microemulsifying soft capsule containing nitrendipine for treating hypertension. Background technique [0002] Nitrendipine, English name: Nitrendipine; chemical name 2,6-dimethyl-4-(3-nitrophenyl)1,4-dihydro-3, nitrophenyl)-1,4-di Methylethyl Hydrogen-3,5-pyridinedicarboxylate. Molecular formula: C18H20N2O6; molecular weight: 360.37. [0003] Nitrendipine is a second-generation dihydropyridine calcium channel blocker, developed by the Federal Republic of Germany in 1972, registered in Europe in 1985 and approved for clinical antihypertensive treatment of hypertension, Nitrendipine is nifedipine Nitrendipine is a calcium antagonist that selectively acts on vascular smooth muscle, and its main pharmacological effect is to antagonize the calcium flow of the slow channel, thereby reducing the calcium current correspondingl...

Claims

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Application Information

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IPC IPC(8): A61K9/66A61K31/435A61P9/12
Inventor 贾祥波陆继好
Owner 贾祥波
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