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Tetrahydropalmatine intra-gastric floating oral microsphere

A technology of tetrahydropalmatine and gastric floating, applied in the field of gastric floating microspheres, which can solve the problems of large dose of dripping pills, inconvenient administration, low bioavailability, etc., achieve stable drug release speed, reduce the number of administrations, and improve the preparation process simple effect

Active Publication Date: 2014-04-30
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dropping pills have a large dose and low bioavailability, while injections are inconvenient to administer

Method used

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  • Tetrahydropalmatine intra-gastric floating oral microsphere
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  • Tetrahydropalmatine intra-gastric floating oral microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Weigh 0.6g THP and 0.8g ethyl cellulose (EC), mix well, dissolve in 20mL ethyl acetate to form an organic phase. In addition, 100 mL of PVA aqueous solution with a mass fraction of 0.5% was prepared as the water phase. Under the condition of a stirring speed of 50rpm, slowly add the organic phase to the water phase, and continue to stir at 35°C until the organic solvent is evaporated, let it stand for a certain period of time, filter, discard the filtrate, and wash the filter cake with distilled water (50mL× 3) Vacuum drying at 50°C for 8.5 hours to obtain 1.2 g of light yellow microspheres. The average particle size of the microspheres is 518.5 μm, the drug loading capacity is 40.3%, and the encapsulation efficiency is 92%. The microspheres have a round appearance, a hollow structure, and a bulk density of 0.44. meet the requirements.

Embodiment 2

[0032] Weigh 1g THP and 1.2g Eugragit S100 (a kind of acrylic resin) respectively, mix them evenly, and dissolve them in 120mL ethanol to form an organic phase. Another 150 mL of PVA aqueous solution with a mass fraction of 0.5% was prepared as the water phase. Under the condition of 200rpm stirring speed, slowly add the organic phase to the water phase, and continue to stir at 30°C until the organic solvent evaporates, let it stand for a certain period of time, filter, discard the filtrate, and wash the filter cake with distilled water (100mL×2) , and vacuum-dried at 35°C for 12 hours to obtain 1.7 g of pale yellow microspheres. The average particle size of the microspheres is 480.1 μm, the drug loading capacity is 35.2%, and the encapsulation efficiency is 89.3%. The microspheres have a round appearance, a hollow structure, and a bulk density of 0.48. meet the requirements.

Embodiment 3

[0034] Weigh 6g THP and 8g Eugragit L100 respectively, mix well, dissolve in 80mL dichloromethane to form an organic phase. Another 600 mL of PVA aqueous solution with a mass fraction of 0.5% was prepared as the water phase. Under the condition of 150rpm stirring speed, slowly drop the organic phase into the water phase, keep stirring at 38°C until the organic solvent evaporates, let it stand for a certain period of time, filter, discard the filtrate, and wash the filter cake with distilled water (150mL×4) , and vacuum-dried at 52°C for 7 hours to obtain 10.5 g of pale yellow microspheres. The average particle size of the microspheres was measured to be 523.9 μm, the drug loading capacity was 34.1%, and the encapsulation efficiency was 86.7%. The appearance of the microspheres was round, with a hollow structure, and the bulk density was 0.51. All meet the requirements.

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Abstract

The invention provides a tetrahydropalmatine intra-gastric floating oral microsphere. The microsphere is prepared by the method comprising the following steps: uniformly mixing the tetrahydropalmatine and pharmaceutically acceptable carrier materials, dissolving in a pharmaceutically acceptable organic solvent to form an organic phase; preparing a pharmaceutically acceptable hydrophilic emulsifier aqueous solution as an aqueous solution; slowly dripping the organic phase into the aqueous phase under a stirring state, constantly stirring until the organic solvent is volatized, standing, filtering, removing the filtrate, washing the filter cake with distilled water, and drying in vacuum to obtain the tetrahydropalmatine intra-gastric floating oral microsphere. The tetrahydropalmatine intra-gastric floating oral microsphere is simple in preparation process, good in reproducibility, high in drug-loading capacity and encapsulation efficiency, good in intra-gastric floating and sustained-releasing performance and can constantly float and slowly release drugs at constant speed in 12 hours, and the drug can be released over 90 percent in accumulation of 12 hours, so that the drug can be released stably, slowly and directionally.

Description

(1) Technical field [0001] The invention relates to a gastric floating microsphere, in particular to a gastric floating microsphere with tetrahydropalmatine as a medicinal active ingredient. (2) Background technology [0002] Corydalis yanhusuo, also known as Yuanhu, is the dry tuber of Corydalis yanhusuo W.T.Wang, a plant of the poppy family, with pungent, bitter, and warm nature. It has the effects of promoting blood circulation and dispelling blood stasis, promoting qi and relieving pain, and is mainly used to treat various pains such as chest and hypochondrium pain, epigastric pain, tumbling and swelling pain. Modern studies have shown that Corydalis has the effects of analgesia, inhibition of gastric juice secretion and anti-ulcer effects. Its main active ingredients are alkaloids, and tetrahydropalmatine (THP) has the strongest effect. THP is insoluble in water and alkaline solutions. Soluble in organic solvents such as methanol. It has a good effect on chronic persi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4375A61P1/04
Inventor 石森林何三民熊雪丰李昌煜吴瑾瑾
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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