Slow-releasing microball with nimoldipine and its preparing method

A technology of nimodide-loaded and sustained-release microspheres, which is applied in the directions of drug combinations, pharmaceutical formulations, and non-active ingredients medical preparations, etc., to achieve the effects of mild conditions, improved stability, improved strength and acid resistance

Inactive Publication Date: 2005-12-28
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it is mainly used as a primary food raw material at home and abroad, and there are few studies on it as a drug carrier.

Method used

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  • Slow-releasing microball with nimoldipine and its preparing method
  • Slow-releasing microball with nimoldipine and its preparing method
  • Slow-releasing microball with nimoldipine and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0019] 2g sodium alginate and 0.5g konjac glucomannan are dissolved in 100ml deionized water, add 2.2g nimodipine solid dispersion, the weight ratio of nimodipine and molecular weight 6000 polyethylene glycol in this solid dispersion is 1: 1. Prepare konjac glucomannan-sodium alginate mixed solution containing nimodipine solid dispersion. Using the capillary breaking method, the vibration frequency is 50Hz, and the flow rate is 138cm / s. The above mixed solution is dropped into CaCl in the form of tiny droplets. 2 Concentration is 0.2M, chitosan concentration is 0.25% (w / v), chitosan molecular weight is 8.55×10 6 In the chitosan calcium chloride solution, gel 30 minutes, filter washing, 50 ℃ of dryings, can obtain the nimodipine slow-release microsphere ( figure 1 ). The average particle size of the microspheres is 0.91mm, the particle size deviation is 10.7%, and the sphericity is good.

example 2

[0021] 2g sodium alginate and 0.5g konjac glucomannan are dissolved in 100ml deionized water, add 2.2g nimodipine solid dispersion, the weight ratio of nimodipine and molecular weight 6000 polyethylene glycol in this solid dispersion is 1: 1. Or add 1.1 g of nimodipine plain medicine to the above-mentioned mixed sol to prepare a konjac glucomannan-sodium alginate mixed solution containing nimodipine solid dispersion or nimodipine plain medicine. According to Example 1, the sustained-release microspheres loaded with nimodipine original drug and nimodipine solid dispersion were prepared by capillary crushing method. After being treated in simulated gastric juice for 4 hours, the gastric release rates of microspheres loaded with nimodipine original drug and nimodipine solid dispersion were 3.75% and 4.56%, respectively. The microspheres were placed in the simulated intestinal fluid again, and the drug release was shown in figure 2 . figure 2 It can be seen that the release ra...

example 3

[0023] 2g of sodium alginate was dissolved in 100ml of deionized water with 0, 0.25, 0.375, and 0.5g of konjac glucomannan respectively, and 2.2g of nimodipine solid dispersion was added respectively. The weight ratio of polyethylene glycol is 1:1, and nimodipine solid dispersion-konjac glucomannan-sodium alginate mixed solutions with different contents of konjac glucomannan are prepared. According to Example 1, the drug-loaded konjac glucomannan-calcium alginate-chitosan microspheres with different contents of konjac glucomannan were prepared by capillary crushing method. After being treated in simulated gastric juice for 4 hours, the release rates of the microspheres in gastric juice are all lower than 5%. The microparticles were again placed in the simulated intestinal fluid, and the release of the drug was shown in image 3 . Depend on image 3 It can be seen that the microspheres containing higher concentration of konjac glucomannan have lower drug release rate.

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Abstract

The invention discloses a sustained-release microsphere loaded with nimodipine and a preparation method thereof. The microsphere has a single core structure or a core-shell structure, the core material is composed of nimodipine solid dispersion and konjac glucomannan-calcium alginate, and the shell material is a chitosan-calcium alginate polyelectrolyte membrane. The preparation process mixes the nimodipine solid dispersion with konjac glucomannan-calcium alginate hydrosol, and uses the capillary breaking method to add CaCl dropwise 2 Aqueous solution or Chitosan-CaCl 2 In the aqueous solution, the obtained spheres are washed and dried to obtain drug-loaded konjac glucomannan-calcium alginate microspheres or drug-loaded konjac glucomannan-calcium alginate-chitosan microspheres. The present invention has the advantages of improving the bioavailability and slow-release effect of nimodipine; by changing conditions such as konjac glucomannan content, gel ion concentration, chitosan molecular weight and chitosan concentration, it is easy to realize drug control. Explanation; the preparation process is simple, the production cost is low, and it is easy to produce on a large scale.

Description

technical field [0001] The invention relates to a slow-release microsphere loaded with nimodipine medicine, which belongs to the improvement of oral nimodipine preparation dosage form. Background technique [0002] Nimodipine (NMP for short) is a second-generation pyridine calcium antagonist that preferentially acts on small arteries and selectively acts on cerebral blood vessels. Clinically, it is mainly used for the treatment of diseases such as ischemic cerebrovascular disease, migraine, sudden deafness, senile dementia, subarachnoid hemorrhage and hypertension (especially for essential hypertension), and has achieved good results. At the same time, it also has the effect of protecting or promoting memory. However, the solubility of the drug is small, and the bioavailability of oral tablets is low, which is only 3% to 28% of that of intravenous injection. Ordinary tablets need to be taken 3 to 4 times a day, not only the number of times of taking the medicine is high, b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4422A61K47/36A61P9/12
Inventor 何明霞王康何志敏
Owner TIANJIN UNIV
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