Gastrodin nasal microspheres with bioadhesive properties and preparation method thereof

A technology of bioadhesion and gastrodin, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, and pharmaceutical formulas, can solve the problems of increasing patient pain, low drug concentration, and large dosage, and achieve drug efficacy Strong, less adhesion, high drug loading effect

Active Publication Date: 2018-09-14
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 microspheres with bioadhesive properties and preparation method thereof
  • Gastrodin nasal microspheres with bioadhesive properties and preparation method thereof
  • Gastrodin nasal microspheres with bioadhesive properties and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] (1) Preparation of water phase: 0.30 g of gastrodin was weighed and dissolved in 10 mL of 5% (volume fraction) acetic acid aqueous solution, and then 0.30 g of chitosan was added and stirred evenly to make it swell completely to obtain the water phase.

[0022] (2) Preparation of the oil phase: Weigh 1.4 g of Span80 and dissolve it in 70 mL of liquid paraffin to obtain the oil phase.

[0023] (3) Preparation of microspheres: Pre-heat the above water phase and oil phase to 40°C respectively, at a stirring speed of 1000rpm, add the water phase into the oil phase evenly and slowly, and stir and emulsify in the same direction for 30min, then add 3mL of formaldehyde, Cross-link at 40°C for 3 hours, let it stand, pour off the oil phase, wash the lower layer of microspheres with petroleum ether (50mL×3), absolute ethanol (40mL×1), filter with suction, and dry in vacuum to obtain gastrodin nasal microspheres 1.03g.

[0024] Scanning electron microscopy (SEM) was used to detect...

Embodiment 2

[0030] (1) Preparation of the water phase: Weigh 0.40 g of gastrodin and dissolve it in 100 mL of 2% (volume fraction) acetic acid aqueous solution, then add 4 g of chitosan and stir evenly to make it swell completely to obtain the water phase.

[0031] (2) Preparation of the oil phase: Weigh 24g of Span80 and dissolve it in 800mL of liquid paraffin to obtain the oil phase.

[0032] (3) Preparation of microspheres: pre-heat the above water phase and oil phase to 40°C respectively, at a stirring speed of 1000rpm, add the water phase into the oil phase evenly and slowly, and stir and emulsify in the same direction for 30min, then add 32mL of formaldehyde, Cross-link at 50°C for 3 hours, let stand, pour off the oil phase, wash the lower layer of microspheres with petroleum ether (50mL×3), absolute ethanol (40mL×1), filter with suction, and dry in vacuum to obtain gastrodin nasal microspheres 1.28g.

[0033] Scanning electron microscopy (SEM) was used to detect the microscopic ch...

Embodiment 3

[0039] (1) Preparation of water phase: 8.0 g of gastrodin was weighed and dissolved in 100 mL of 5% (volume fraction) acetic acid aqueous solution, and then 4.0 g of chitosan was added and stirred evenly to make it swell completely to obtain the water phase.

[0040] (2) Preparation of the oil phase: Weigh 20 g of Span80 and dissolve it in 1000 mL of liquid paraffin to obtain the oil phase.

[0041] (3) Preparation of microspheres: pre-heat the above water phase and oil phase to 45°C respectively, at a stirring speed of 1200rpm, add the water phase into the oil phase evenly and slowly, and stir and emulsify in the same direction for 20min, then add 40mL of formaldehyde, Cross-link at 40°C for 6 hours, let stand, pour off the oil phase, wash the lower layer of microspheres with petroleum ether (1500mL×3), absolute ethanol (1000mL×1), filter with suction, and dry in vacuum to obtain gastrodin nasal microspheres 27.57g.

[0042] Scanning electron microscopy (SEM) was used to det...

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Abstract

The invention provides nasal micro-spheres with biological adhesion characteristics and gastrodin. A method for manufacturing the nasal micro-spheres includes dissolving the gastrodin in acetic acid aqueous solution, adding chitosan into the acetic acid aqueous solution and uniformly stirring and mixing the gastrodin and the chitosan in the acetic acid aqueous solution with each other to obtain water phase; dissolving Span80 in liquid paraffin to obtain oil phase; respectively preliminarily heating the water phase and the oil phase until the temperature of the water phase and the temperature of the oil phase reach 40-50 DEG C, slowly adding the water phase into the oil phase, stirring and emulsifying the water phase and the oil phase in the same direction for 20-50min, then adding a cross-linking agent, namely, formaldehyde, into the water phase and the oil phase, carrying out cross-linking at the temperature of 40-60 DEG C for 3-6h to obtain products, allowing the products to stand still, pouring upper-layer oil phase, washing lower-layer micro-spheres by the aid of petroleum ether and absolute ethyl alcohol, drawing and filtering the micro-spheres, and drying the micro-spheres under a vacuum condition to obtain the nasal micro-spheres with the gastrodin. The nasal micro-spheres with the gastrodin and the method have the advantages that the nasal micro-spheres can remain in the nasal cavities of users for a long time and are stable in medicine release speed, medicine can be completely released, distribution of the medicine in the brains of the users, the biological availability and the efficacy can be improved, and the nasal micro-spheres are safe and nontoxic.

Description

(1) Technical field [0001] The invention relates to a gastrodin nasal 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 barrier. S...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/7034A61P25/06A61P25/20A61P25/08A61P25/00A61P9/10
Inventor 石森林张光霁李晓琦李昌煜申力施笑晖
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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