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Gastrodin nasal starch microspheres with bioadhesive properties and preparation method thereof

A technology of starch microspheres and bioadhesion, applied in the direction of medical preparations containing active ingredients, organic active ingredients, drug combinations, etc., can solve the problems of increasing patient pain, large dosage, low drug concentration, etc., and achieve local safety Good sex, high drug loading, less adhesion effect

Active Publication Date: 2017-09-26
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Conventional route of administration, the concentration of the drug in the brain is low, and a large dosage is required to achieve the therapeutic effect
Moreover, the metabolism of gastrodin is very fast, and it is not easy to accumulate in the body. In order to maintain the curative effect, frequent administration is required clinically.
However, frequent injections will increase the suffering of patients, and nausea and other gastrointestinal side effects will occur when oral administration is large.

Method used

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  • Gastrodin nasal starch microspheres with bioadhesive properties and preparation method thereof
  • Gastrodin nasal starch microspheres with bioadhesive properties and preparation method thereof
  • Gastrodin nasal starch microspheres with bioadhesive properties and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] (1) Preparation of the water phase: Weigh 4.5 g of starch, dissolve it in 10 mL of 0.1 g / mL sodium hydroxide aqueous solution, prepare a starch solution with a starch concentration of 45 wt%, and let it stand for 30 minutes to remove air bubbles to obtain the water phase.

[0034] (2) Preparation of the oil phase: Weigh 2.0 g of gastrodin and disperse it in 1 mL of ethyl acetate to obtain the oil phase.

[0035] (3) Preparation of O / W colostrum: slowly add the oil phase into the water phase at room temperature, and stir in the same direction at a speed of 1000 rpm to obtain 9.0 mL of O / W colostrum.

[0036] (4) Preparation of microspheres: preheat 100mL liquid paraffin containing 3.5g Span80 to 40°C, add the above-mentioned colostrum into it, and stir and emulsify in the same direction at 1000rpm for 20min; then add the crosslinking agent epichlorohydrin (ECH) 5.1mL, after cross-linking at 40°C for 4h, centrifuge, pour off the upper oil phase; ) washing, drying under r...

Embodiment 2

[0043] (1) Preparation of the water phase: Weigh 3.0 g of starch, dissolve it in 10 mL of 0.05 g / mL sodium hydroxide aqueous solution, prepare a starch solution with a starch concentration of 30 wt%, and let it stand for 30 minutes to remove air bubbles to obtain the water phase.

[0044] (2) Preparation of the oil phase: weigh 2.0 g of gastrodin and disperse it in 0.8 mL of ethyl acetate to obtain the oil phase.

[0045] (3) Preparation of O / W colostrum: slowly add the oil phase into the water phase at room temperature, and stir in the same direction at a speed of 800 rpm to obtain 10.0 mL of O / W colostrum.

[0046] (4) Preparation of microspheres: Preheat 80 mL of liquid paraffin containing 2.8 g of Span80 to 40 °C, add the above-mentioned colostrum into it, and stir and emulsify in the same direction at a speed of 1400 rpm for 30 min, then add the cross-linking agent epichlorohydrin (ECH) 3mL, after cross-linking at 40°C for 4h, centrifuge and pour off the upper oil phase, ...

Embodiment 3

[0053] (1) Preparation of the water phase: Weigh 30 g of starch, dissolve it in 100 mL of 0.1 g / mL sodium hydroxide aqueous solution, prepare a starch solution with a starch concentration of 30 wt%, and let it stand for 30 minutes to remove air bubbles to obtain the water phase.

[0054] (2) Preparation of the oil phase: Weigh 30 g of gastrodin and disperse it in 15 mL of ethyl acetate to obtain the oil phase.

[0055] (3) Preparation of O / W colostrum: slowly add the oil phase into the water phase at room temperature, and stir in the same direction at a speed of 1200 rpm to obtain 100 mL of O / W colostrum.

[0056] (4) Preparation of microspheres: Preheat 1000mL liquid paraffin containing 20.0g Span80 to 40°C, add the above-mentioned colostrum into it and stir and emulsify in the same direction at a rate of 1400rpm for 40min, then add the crosslinking agent epichlorohydrin ( ECH) 51mL, after cross-linking at 40°C for 3h, centrifuge, pour off the upper oil phase, and wash the lo...

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Abstract

The invention provides a gastrodin nasal starch microsphere with bioadhesive properties. The microsphere is prepared by the following method: using starch sodium hydroxide aqueous solution as the water phase; dispersing gastrodin in ethyl acetate to obtain Oil phase; slowly add the oil phase to the water phase at room temperature, and stir in the same direction to obtain O / W colostrum; heat the liquid paraffin containing Span80 to 40-50°C, add the above colostrum into it, and stir in the same direction to emulsify After 20-40 minutes, add the cross-linking agent epichlorohydrin, cross-link at 30-50°C for 3-5 hours, centrifuge, pour off the upper oil phase, and wash the lower layer of microspheres with ethyl acetate, absolute ethanol, and acetone respectively Finally, dry under reduced pressure to obtain the described gastrodin nasal starch microspheres; the gastrodin nasal starch microspheres prepared by the present invention have a long retention time in the nasal cavity, and the drug release speed is stable and complete, which can improve the drug distribution in the brain, biological Utilization and efficacy, and safe and non-toxic.

Description

(1) Technical field [0001] The invention relates to a gastrodin nasal starch microsphere with bioadhesive properties and a preparation method thereof, belonging to the field of pharmaceutical preparations. (2) Background technology [0002] Gastrodin (p-hydroxybenzyl alcohol-β-D glucopyranoside) is the main chemical component of Gastrodia elata, and it is also the effective monomer component with the highest content in the active ingredients of Gastrodia elata. , anti-oxidation, anti-inflammation, enhancement of immunity and other pharmacological effects, widely used in the treatment of migraine, dizziness, neurasthenia, cerebral infarction and other diseases, and has low toxicity and small adverse reactions. At present, gastrodin preparations for clinical application mainly include dosage forms such as tablets and injections. [0003] The action site of gastrodin lies in the brain center, and it is a water-soluble drug, which is not easy to pass through the blood-brain bar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/7034A61K47/36A61P25/06A61P25/00
Inventor 张光霁石森林李晓琦李昌煜申力施笑晖
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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