CN112451506A - Preparation method of essential oil sustained-release capsule - Google Patents
Preparation method of essential oil sustained-release capsule Download PDFInfo
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- CN112451506A CN112451506A CN202011436762.8A CN202011436762A CN112451506A CN 112451506 A CN112451506 A CN 112451506A CN 202011436762 A CN202011436762 A CN 202011436762A CN 112451506 A CN112451506 A CN 112451506A
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- China
- Prior art keywords
- essential oil
- cyclodextrin
- release capsule
- sustained
- preparation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
Abstract
The invention relates to a preparation method of an essential oil sustained-release capsule, which is characterized in that essential oil is wrapped by cyclodextrin, meanwhile, a solubilizer and a cosolvent are added to increase the solubility of the essential oil in the cyclodextrin, an inorganic powder material of the essential oil is prepared, and finally the essential oil capsule is obtained. The process is simple, the production cost is low, the obtained inclusion compound has good stability, and the requirements of production and application can be further met. The preparation method is simple and high in operability, and can further meet the requirements of production and application. The clathrate compound prepared by the invention is of a nano structure, is beneficial to the slow release and control of essential oil, and has good physical and chemical stability. The capsule prepared by the invention can reduce the volatility of the essential oil, increase the stability, and lead the essential oil to be powdered, thereby being convenient for preparing various formulations and expanding the application range.
Description
Technical Field
The invention relates to a preparation method of an essential oil sustained-release capsule, in particular to a capsule prepared by wrapping essential oil molecules with cyclodextrin to form solid-phase powder, and belongs to the field of biomedicine.
Background
Essential oil is a natural plant essence, usually extracted from roots, stems, leaves, flowers, peels or resins of plants, and is a multifunctional aromatic substance having skin-care functions. Because of their generally high volatility, many ingredients are easily lost and oxidized during manufacture, storage and transportation, resulting in changes in the sensory properties and skin care functionality of their fragrance ingredients, while low water solubility also makes it difficult to produce stable, dispersible formulations. Causing inconvenience in its storage and use.
Inclusion of essential oils is an effective means to solve the above problems. Usually, the essential oil is wrapped by a high molecular material and an inorganic powder material to form an inclusion body of the essential oil. For example, the Chinese patent 201310186523.5 discloses that liquid essential oil is wrapped in a hard shell layer of silicon dioxide, the preparation process is rapid and convenient, the liquid essential oil is clean and pollution-free, the particle size of the microcapsule of the silicon dioxide wrapped essential oil is small, the structural strength is high, the dispersibility in the water phase is good, and the adjustable range of the release performance of the essential oil wrapped by the microcapsule is large. The Chinese patent 200710160376.9 is an inorganic nano microcapsule with inorganic compound as shell and small molecular hydrocarbon as core; the preparation process is simple, the inorganic nano capsule has high thermal, chemical and mechanical stability, and the porous structure of the shell layer is favorable to the exchange between the coated matter and the outer environment. How to improve the wrapping rate is still a research hotspot.
The cyclodextrin is a barrel-shaped cavity, the inner diameter of the cavity is about 0.7-0.8 nm, the cyclodextrin is hydrophilic outside the ring and hydrophobic inside the ring, and can wrap various organic and inorganic guest molecules to form an inclusion compound, so the cyclodextrin is used as an excellent enzyme model and a molecular receptor and has extremely wide application in fields of scientific research, practical application and the like. Cyclodextrin can form inclusion compound with various physiological active substances, and can improve stability of active substances, and improve physical properties such as color, appearance, smell, solubility, etc.
Disclosure of Invention
The invention aims to provide a preparation method of an essential oil sustained-release capsule.
The purpose of the invention is realized by the following scheme: a preparation method of an essential oil sustained-release capsule wraps essential oil through cyclodextrin, meanwhile, a solubilizer and a cosolvent are added to increase the solubility of the essential oil in the cyclodextrin, an inorganic powder material of the essential oil is prepared, and the essential oil capsule is finally obtained, and the preparation method comprises the following steps:
(1) dissolving cyclodextrin in an alkaline aqueous solution with the pH value of 8-11 to prepare a cyclodextrin solution with the mass ratio of 1-50%, adding 50-70% of essential oil and 0-30% of fluorocarbon serving as a solubilizer and 0-10% of cosolvent, wherein the cosolvent is one of methanol, ethanol, ethyl acetate and ether, reacting for 24-48 hours at 4-10 ℃ under the stirring condition, standing the reaction solution at 4 ℃ after the reaction is finished for 24 hours, centrifugally separating after precipitation, washing the precipitated product with water and absolute ethyl alcohol, and drying the product in a vacuum drying oven at room temperature for 12 hours to obtain white solid powder;
(2) and (2) taking 100 g of the powder obtained in the step (1), adding 5-20 g of wetting agent, mixing, granulating, sieving, drying, sterilizing and encapsulating to obtain the essential oil sustained-release capsule.
On the basis of the scheme, the cyclodextrin is one or a mixture of more of alpha-cyclodextrin, beta-cyclodextrin, gamma-cyclodextrin, hydroxypropyl-beta-cyclodextrin, methyl-beta-cyclodextrin, hydroxyethyl-beta-cyclodextrin, sulfobutyl-beta-cyclodextrin and the like.
On the basis of the scheme, the alkaline aqueous solution is one or a mixture of more of sodium hydroxide, potassium hydroxide, sodium carbonate, sodium bicarbonate, sodium phosphate and urea.
On the basis of the scheme, the fluorocarbon compound is one or a mixture of more of FC-77 (perfluorocyclic ether), PFOB (perfluorooctylbromide), PFD (perfluorodecalin) or PFMHP (perfluoromethylcyclohexylpiperidine).
On the basis of the scheme, the essential oil is a mixture of one or more of lavender, sandalwood, sweet orange, rose, geranium, bergamot, eucalyptus, lemon, grapefruit and chamomile.
The invention has the advantages that:
(1) the product obtained by the invention has high encapsulation rate of essential oil and strong slow release;
(2) the product obtained by the invention is solid powder, and the dosage form of the essential oil can be changed;
(3) the invention has simple process and low production cost, and the obtained inclusion compound has good stability and can further meet the requirements of production and application.
Detailed Description
The technical solution of the present invention is further described below by specific examples. The following examples are further illustrative of the present invention and do not limit the scope of the present invention.
Example 1
A lavender essential oil sustained-release capsule is prepared by wrapping lavender essential oil by cyclodextrin, adding a solubilizer and a cosolvent at the same time, increasing the solubility of the essential oil in the cyclodextrin, preparing an inorganic powder material of the essential oil, and finally obtaining the capsule of the essential oil, and the capsule is prepared by the following steps:
(1) dissolving cyclodextrin in sodium hydroxide alkaline aqueous solution with the pH value of 11 to prepare 20% of cyclodextrin solution, adding 50% of lavender essential oil, 10% of fluorocarbon FC-77 and 1% of cosolvent in mass ratio, reacting at 4 ℃ for 24 hours under the stirring condition, standing the reaction liquid at 4 ℃ for 24 hours, performing centrifugal separation after precipitation, washing the precipitated product with water and absolute ethyl alcohol, and drying the product in a vacuum drying oven at room temperature for 12 hours to obtain white solid powder;
(2) and (2) taking 100 g of the powder obtained in the step (1), adding 5 g of wetting agent, mixing to prepare a soft material, granulating, sieving, drying, sterilizing and encapsulating to obtain the lavender essential oil sustained-release capsule.
The slow release rate of the essential oil is 45 percent released in 24 hours.
Example 2
A rose essential oil sustained-release capsule is similar to the step of the example 1, and is prepared by the following steps:
(1) dissolving cyclodextrin in an alkaline aqueous solution of sodium carbonate with the pH value of 8 to prepare a cyclodextrin solution with the mass ratio of 30%, adding 70% of rose essential oil, 15% of a solubilizer PFOB and 10% of cosolvent ethyl acetate, reacting for 24 hours at 4 ℃ under the stirring condition, standing for 24 hours after the reaction is finished, standing for 8 ℃, performing centrifugal separation after precipitation, washing the precipitated product with water and absolute ethyl alcohol, and drying the product in a vacuum drying oven at room temperature for 12 hours to obtain white solid powder;
(2) and (2) taking 100 g of the powder obtained in the step (1), adding 5-20 g of wetting agent, mixing to prepare a soft material, granulating, sieving, drying, sterilizing and encapsulating to obtain the rose essential oil sustained-release capsule.
The slow release rate of the essential oil is 53 percent after 24 hours.
Example 3
The grapefruit essential oil sustained-release capsule is similar to the step of the example 1, and is prepared by the following steps:
(1) dissolving cyclodextrin in an alkaline aqueous solution with the pH value of 11 to prepare a cyclodextrin solution with the mass ratio of 50%, adding 70% of grapefruit essential oil, 20% of solubilizer FC-77 and 10% of cosolvent ethyl ether, reacting at 4 ℃ for 24 hours under the stirring condition, standing the reaction solution at 4 ℃ for 24 hours after the reaction is finished, carrying out centrifugal separation after precipitation, washing the precipitated product with water and absolute ethyl alcohol, and drying the product in a vacuum drying oven at room temperature for 12 hours to obtain white solid powder;
(2) and (2) taking 100 g of the powder obtained in the step (1), adding 20 g of wetting agent, mixing to prepare a soft material, granulating, sieving, drying, sterilizing and encapsulating to obtain the essential oil sustained-release capsule.
(2) And (2) taking 100 g of the powder obtained in the step (1), adding 20 g of wetting agent, granulating, sieving, drying, sterilizing and encapsulating to obtain the grapefruit essential oil sustained-release capsule.
The slow release rate of the grapefruit essential oil is 37% after 24 hours.
Claims (5)
1. A preparation method of an essential oil sustained-release capsule is characterized in that essential oil is wrapped by cyclodextrin, meanwhile, a solubilizer and a cosolvent are added to increase the solubility of the essential oil in the cyclodextrin, an inorganic powder material of the essential oil is prepared, and the essential oil capsule is finally obtained, and the preparation method comprises the following steps:
(1) dissolving cyclodextrin in an alkaline aqueous solution with the pH value of 8-11 to prepare a cyclodextrin solution with the mass ratio of 1-50%, adding 50-70% of essential oil and 0-30% of fluorocarbon serving as a solubilizer and 0-10% of cosolvent, wherein the cosolvent is one of methanol, ethanol, ethyl acetate and ether, reacting for 24-48 hours at 4-10 ℃ under the stirring condition, standing the reaction solution for 24 hours at 4-8 ℃ after the reaction is finished, centrifugally separating after precipitation, washing the precipitated product with water and absolute ethanol, and drying the product in a vacuum drying oven at room temperature for 12 hours to obtain white solid powder;
(2) and (2) taking 100 g of the powder obtained in the step (1), adding 5-20 g of wetting agent, mixing, granulating, sieving, drying, sterilizing and encapsulating to obtain the essential oil sustained-release capsule.
2. The preparation method of the essential oil sustained-release capsule according to claim 1, wherein the cyclodextrin is one or a mixture of more of alpha-cyclodextrin, beta-cyclodextrin, gamma-cyclodextrin, hydroxypropyl-beta-cyclodextrin, methyl-beta-cyclodextrin, hydroxyethyl-beta-cyclodextrin and sulfobutyl-beta-cyclodextrin.
3. The method for preparing the essential oil sustained-release capsule according to claim 1, wherein the alkaline aqueous solution is one or a mixture of sodium hydroxide, potassium hydroxide, sodium carbonate, sodium bicarbonate, sodium phosphate and urea.
4. The method for preparing the essential oil sustained-release capsule according to claim 1, wherein the fluorocarbon compound is one or a mixture of more of perfluorocyclic ether, perfluorooctyl bromide, perfluorodecalin and perfluoromethylcyclohexylpiperidine.
5. The method for preparing the essential oil sustained-release capsule according to claim 1, wherein the essential oil is one or a mixture of more of lavender, sandalwood, sweet orange, rose, geranium, bergamot, eucalyptus, lemon, grapefruit and chamomile.
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| Application Number | Priority Date | Filing Date | Title |
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| CN202011436762.8A CN112451506A (en) | 2020-12-10 | 2020-12-10 | Preparation method of essential oil sustained-release capsule |
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| CN202011436762.8A CN112451506A (en) | 2020-12-10 | 2020-12-10 | Preparation method of essential oil sustained-release capsule |
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Patent Citations (12)
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Application publication date: 20210309 |