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Preparation method of rhizoma acori tatarinowii volatile oil inclusion compound and vaporization inhalation type drug administration method of inclusion compound

A technology of volatile oil inclusion compound and administration method, applied in the field of traditional Chinese pharmacy, can solve the problems such as difficulty in penetrating the blood-brain barrier for drugs, unstable properties of volatile oil, intestinal toxicity and side effects, etc., and achieve prevention and adjuvant treatment of senile dementia , Improve learning and memory ability, increase the effect of stability

Inactive Publication Date: 2020-07-03
YUNNAN LVXIN BIOLOGICAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Most of the clinically used preparations of Shichangpu are traditional preparations such as compound decoctions, tablets, and pills. The dosage is large, and there are intestinal side effects. The drugs are difficult to pass through the blood-brain barrier and have low bioavailability. secondary development
[0007] Volatile oils are often irritating, which is not conducive to drug use, and volatile oils are unstable in nature, volatile in preparations, and affect the efficacy of preparations. Therefore, other technologies are used to make up for these deficiencies, such as making clathrates to increase stability and reduce irritation.

Method used

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  • Preparation method of rhizoma acori tatarinowii volatile oil inclusion compound and vaporization inhalation type drug administration method of inclusion compound
  • Preparation method of rhizoma acori tatarinowii volatile oil inclusion compound and vaporization inhalation type drug administration method of inclusion compound
  • Preparation method of rhizoma acori tatarinowii volatile oil inclusion compound and vaporization inhalation type drug administration method of inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1. Extraction of volatile oil of Shichangpu

[0027] Weigh 1.5kg of crushed Acorus calamus medicinal material, add 8 times the amount of water to soak for 2 hours, carry out according to the B method under the determination method of volatile oil in the fourth part of the "Chinese Pharmacopoeia" 2015 edition 2204, use steam distillation to extract for 6 hours, and use anhydrous sulfuric acid After sodium dehydration, (25.5 ± 1.5) mL of thick yellow oil was obtained, and the calculated volatile oil yield was (1.70 ± 0.1) %. The prepared volatile oil was stored at -18°C.

[0028] 2. Preparation of clathrate of volatile oil of Shichangpu

[0029] (1) Use the saturated aqueous solution method for clathration, weigh 100g of HP-β-CD and place it in a stoppered Erlenmeyer flask, add an appropriate amount of distilled water, heat to dissolve it completely, then lower it to 30°C, and stir at a constant temperature.

[0030] (2) Take 10mL of Acorus volatile oil, dilute it with ...

experiment example 2

[0045] Experimental example 2 inclusion process evaluation

[0046] Generally, the oil content of inclusion compound and the inclusion rate of volatile oil are used as the evaluation index of volatile oil inclusion process. The calculation formula is:

[0047] Inclusion rate of volatile oil = recovery of volatile oil in clathrate / (addition of volatile oil × blank recovery rate) × 100%. Oil content of inclusion compound = oil content of inclusion compound / weight of inclusion compound × 100%.

[0048] The specific method is as follows:

[0049] (1) Determination of tea tree essential oil blank recovery rate

[0050] In a 500mL round-bottomed flask, add 300mL of pure water and 1mL of tea tree essential oil, and operate according to Method B in 2204 Volatile Oil Determination Method in the Four General Rules of the 2015 Chinese Pharmacopoeia, read the volume of volatile oil, and calculate the blank recovery rate.

[0051]

[0052] (2) Determination of inclusion rate of vola...

experiment example 3

[0060] Experimental example 3 Stability experiment of clathrate of volatile oil of Shichangpu

[0061] β-Asarone is the main component of the volatile oil of Acorus calamus. In this experiment, the content of β-Asarone was used as a characterization index to investigate the stability of the inclusion compound and the mixture without inclusion.

[0062] The specific method is as follows:

[0063] (1) Preparation of a mixture containing Acorus volatile oil, HP-β-CD, cannabis wax, borneol, and menthol: Take the raw materials with the same feeding ratio as the inclusion compound in Example 1, put them in a mortar and grind them evenly Yes, spare.

[0064] (2) Put the clathrate prepared in Example 1 and the above mixture into a jar, place it in a constant temperature and humidity chamber with a temperature of 60°C and a humidity of 75%, and investigate for 7 days. Samples were collected on the 0th, 1st, 3rd, 5th, and 7th day, and the quantitative determination of β-asarone was ca...

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Abstract

The invention provides a preparation method of a rhizoma acori tatarinowii volatile oil inclusion compound and a vaporization inhalation drug administration method of the inclusion compound, and belongs to the technical field of traditional Chinese medicine. Rhizoma acori tatarinowii volatile oil has the functions of benefiting intelligence and invigorating the brain, and improving learning and memory ability, but the volatile oil is unstable, in the invention, the rhizoma acori tatarinowii volatile oil, hemp wax, borneol and menthol are used to prepare the hydroxypropyl-beta-cyclodextrin inclusion compound. The drug is delivered by using an electronic heater, heating is performed to a certain temperature through the electronic heater to vaporize the inclusion compound, a patient inhales the vaporized drug into a nasal cavity in a similar way as ''smoking'', and the drug can be directly absorbed into brain tissue to play a role in benefiting intelligence and invigorating the brain, andimproving learning and memory ability, and can be used to prevent and assist in the treatment of Alzheimer disease (senile dementia).

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine, and in particular relates to the preparation of a calamus volatile oil clathrate and its gasification and inhalation administration method. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a neurodegenerative disease with insidious onset and progressive development. Clinically, it is characterized by generalized dementia such as memory impairment, aphasia, apraxia, agnosia, impairment of visuospatial skills, executive dysfunction, and personality and behavior changes. Clinically, memory dysfunction and learning and cognitive decline are one of the first symptoms of AD patients. Drugs used to treat senile dementia often have side effects such as nausea, dizziness, sweating, abdominal pain, and blurred vision, and are not suitable for normal people to take for a long time. Therefore, the development of effective, safe, and non-toxic dru...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K36/888A61K47/69A61P25/28A61K36/60A61K31/045
CPCA61K9/007A61K31/045A61K36/60A61K36/888A61K47/6951A61P25/28A61K2300/00
Inventor 王钲霖刘胜贵马海悦付彬彬李智高孔令羽薛红芬蒋永昌
Owner YUNNAN LVXIN BIOLOGICAL PHARMA CO LTD
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