CN111494334A - Method for preparing linarin microcapsule particles - Google Patents
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- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
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- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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Abstract
The invention discloses a method for preparing linarin microcapsule particles, which is to dissolve linarin in water with the weight of 8-10 times, then add tea saponin and lactic acid fatty glyceride, and stir evenly to obtain a core material solution; taking phlorizin, rhamnolipid and Arabic gum as wall materials, adding water with the weight 10-15 times of that of the wall materials, uniformly stirring, and heating to 60-70 ℃ to obtain a capsule wall material solution; adding the core material solution into the capsule wall material solution according to the mass ratio of 1:1-4, adding into a homogenizer, and homogenizing to obtain a mixed solution; and then sending the mixed solution into a granulating sprayer for spray drying, and cooling to room temperature to obtain the linarin micro-capsule particles. According to the method, the linarin is microencapsulated by selecting a proper core material and wall material, so that the high-efficiency encapsulation of the linarin can be effectively realized, the solubility is improved, the stability is improved, the storage period is prolonged, and the attachment capacity of the microcapsule on the stomach of a human body is effectively improved; can also enhance the drug effects of the linarin microcapsule such as oxidation resistance, blood sugar reduction, anti-inflammation and the like, mask the drug taste and improve the sweetness of the linarin microcapsule.
Description
Technical Field
The invention relates to the technical field of traditional Chinese medicine preparations, in particular to a method for preparing linarin micro-capsule particles.
Background
Flos Buddlejae (Buddleja officinalis Maxim) is dried bud and inflorescence of flos Buddlejae of Buddleja of Loganiaceae. It is sweet in taste, slightly cold in nature, and has effects of dispersing pathogenic wind, clearing heat, nourishing liver, improving eyesight, and eliminating nebula, and can be used for treating conjunctival congestion, swelling and pain, lacrimation, photophobia, nebula membrane, liver deficiency, dim eyesight, blurred vision, etc. The traditional Chinese medicine composition is mainly used for treating eye diseases such as xerophthalmia, diabetic retinopathy, conjunctivitis and the like in clinic, and has a remarkable curative effect.
The Mongolian flos has the advantages that one of the main drug effect components of the butterflybush flower is the Mongolian flos glycoside, the Mongolian flos glycoside is composed of robinin and one aglycone, the two isomer-form compounds α and β exist at the same time, and are one of the compounds with higher activity in a plurality of flavonoid compounds.
At present, the linarin extracted from the buddleja officinalis is only dried to obtain dry powder and then stored. However, the linarin dry powder is not protected by other media, and is easy to be oxidized and degraded under the action of light, high temperature and oxygen, so that the drug effect is reduced. The microcapsule technology is a technology of forming a microcapsule having a semipermeable or sealed capsule membrane by encapsulating a core material such as liquid, solid or gas with a natural or synthetic polymer material as a wall material. Because the microencapsulation can improve the physical properties of the encapsulated substance such as color, appearance, apparent density, solubility and the like; the stability of the core material is improved, and the reactivity, durability, heat sensitivity and photosensitivity of the coated material are improved, so that the coating material is widely applied to the industries of medicine, agriculture, chemicals, food processing, cosmetics and the like, and attracts the wide attention of the world. Therefore, microencapsulation is an effective way to improve the stability of linarin and prolong the storage period.
The above background disclosure is only for the purpose of assisting understanding of the inventive concept and technical solutions of the present invention, and does not necessarily belong to the prior art of the present patent application, and should not be used for evaluating the novelty and inventive step of the present application in the case that there is no clear evidence that the above content is disclosed at the filing date of the present patent application.
Disclosure of Invention
The invention aims to provide a method for preparing linarin microcapsule particles. The method microencapsulates the linarin powder, so that the stability of the linarin is improved, the storage period is prolonged, and the tea saponin combined with the natural nonionic surfactant is added in the preparation process, so that the compatibility of a core material and a wall material is improved, and the attachment capacity of the microcapsule on the stomach of a human body is effectively improved; the phlorizin is added, so that the sweetness of the microcapsule particles of the linarin can be improved, the medicinal taste is masked, and the phlorizin also has the effects of reducing blood sugar, improving memory, resisting oxidation, resisting cancer and the like and is synergistic with the medicinal effect of the linarin.
In order to achieve the above purpose, the technical scheme adopted by the invention is as follows:
a method for preparing linarin microcapsule granule comprises the following steps:
(1) dissolving linarin in 8-10 times of water, adding tea saponin and lactic acid fatty glyceride, and stirring to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum as wall materials, adding water with the weight 10-15 times of that of the wall materials, uniformly stirring, and heating to 60-70 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution according to the mass ratio of 1:1-4, adding into a homogenizer, and homogenizing to obtain a mixed solution;
(4) and (4) sending the mixed solution into a granulating sprayer for spray drying, and cooling to room temperature to obtain the linarin micro-capsule particles.
Further, the mass ratio of the linarin to the tea saponin to the lactic acid fatty acid glyceride is 100:1-5: 3-7.
Further, the mass ratio of the phlorizin, the rhamnolipid and the Arabic gum in the wall material is 1-3:3-5: 10-20.
Further, the homogenization is carried out for 2-3 times under the pressure of 40-60 MPa.
Further, the spray drying process comprises the steps of atomizing at 0.08-0.10MPa, flowing at 10-15m L/min, introducing air at 140 ℃ and 70-90 ℃ and drying at 40-60m3/h。
Further, the drying is carried out until the water content is 4.0-5.5%.
Compared with the prior art, the invention has the advantages and beneficial effects that:
1. according to the method, the linarin is microencapsulated by selecting a proper core material and wall material, so that the high-efficiency encapsulation of the linarin can be effectively realized, the solubility is improved, the stability is improved, the storage period is prolonged, and the attachment capacity of the microcapsule on the stomach of a human body is effectively improved; can also enhance the drug effects of the linarin microcapsule such as oxidation resistance, blood sugar reduction, anti-inflammation and the like, mask the drug taste and improve the sweetness of the linarin microcapsule.
2. According to the invention, tea saponin and lactic acid fatty glyceride core material are added, and the tea saponin is used as a natural nonionic surfactant, so that the tea saponin has good functions of emulsification, dispersion, foaming, wetting and the like, improves the compatibility among the raw materials, has pharmacological actions of diminishing inflammation, easing pain, resisting permeation and the like, and is synergistic with the drug effect of linarin; the lactic acid fatty glyceride can improve the compatibility of oil and water, and the prepared linarin microcapsule is stable and uniform.
3. The phlorizin, rhamnolipid and arabic gum are used as wall materials, so that the compactness of the microcapsule is improved, the core material is easier to coat, and the property of the microcapsule product is more stable. The phlorizin can also improve the sweetness of the microcapsule particles of the linarin and mask the medicinal taste, and has the effects of reducing blood sugar, improving memory, resisting oxidation, resisting cancer and the like and is synergistic with the medicinal effect of the linarin.
Detailed Description
The present invention will be described in further detail with reference to specific embodiments. It should be emphasized that the following description is merely exemplary in nature and is not intended to limit the scope of the invention or its application.
Example 1
A method for preparing linarin microcapsule granule comprises the following steps:
(1) dissolving linarin in 10 times of water, adding tea saponin 3.5 wt% and fatty glyceride lactate 5 wt% of linarin, heating to 70 deg.C, stirring, and dissolving completely to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum in a mass ratio of 2:3:15 as wall materials, adding water in an amount which is 12 times of the weight of the wall materials, uniformly stirring, and heating to 70 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution while the solution is hot, adding the capsule wall material solution into a homogenizer according to the mass ratio of 1:3, and homogenizing for 30min each time for 3 times under the pressure of 40MPa to obtain a mixed solution;
(4) will be provided withThe mixed solution is sent to a granulating sprayer for spray drying until the water content is 4.3 percent, and the mixed solution is cooled to room temperature to obtain the linarin micro-capsule particles, wherein the spray drying process comprises the steps of atomizing at 0.08MPa, flowing at 15m L/min, feeding air at 130 ℃, discharging air at 80 ℃ and drying at 50m3/h。
The detection shows that the encapsulation rate of the linarin reaches 97.43 percent, and the solubility is 98.04 percent.
The encapsulation efficiency is detected by adopting a high performance liquid chromatography, the encapsulation efficiency is × 100% of the mass of the linarin encapsulated in the microcapsule per the content of the linarin encapsulated in the microcapsule and unencapsulated in the microcapsule, taking linarin as a reference substance, adding 95% ethanol solution to prepare solution containing 50 mu g of linarin per 1ml, taking 0.1 g of each linarin microcapsule particle, precisely weighing, adding 20ml of 95% ethanol, shaking up, filtering, taking filtrate, and detecting the wavelength of 313 nm.
Example 2
A method for preparing linarin microcapsule granule comprises the following steps:
(1) dissolving linarin in 8 times of water, adding tea saponin 2 wt% and fatty glyceride lactate 6 wt% of linarin, heating to 65 deg.C, stirring, and dissolving completely to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum in a mass ratio of 1:4:10 as wall materials, adding water in an amount which is 10 times of the weight of the wall materials, uniformly stirring, and heating to 70 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution while the solution is hot, adding the capsule wall material solution into a homogenizer according to the mass ratio of 1:2, and homogenizing for 2 times under the pressure of 50MPa for 30min each time to obtain a mixed solution;
(4) sending the mixed solution into a granulating sprayer for spray drying until the water content is 4.6%, and cooling to room temperature to obtain linarin microcapsule particles, wherein the spray drying process comprises atomizing at 0.09MPa and at 12m L/min, air inlet at 120 deg.C and air exhaust at 75 deg.C, and drying air at 40m3/h。
The detection shows that the encapsulation rate of the linarin reaches 95.37 percent, and the solubility is 98.72 percent.
Example 3
A method for preparing linarin microcapsule granule comprises the following steps:
(1) dissolving linarin in 10 times of water, adding tea saponin 4 wt% and fatty glyceride lactate 5 wt% of linarin, heating to 70 deg.C, stirring, and dissolving completely to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum in a mass ratio of 3:5:20 as wall materials, adding 14 times of water by weight of the wall materials, uniformly stirring, and heating to 65 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution while the solution is hot, adding the capsule wall material solution into a homogenizer according to the mass ratio of 1:1, and homogenizing for 3 times under the pressure of 60MPa for 20min each time to obtain a mixed solution;
(4) sending the mixed solution into a granulating sprayer for spray drying until the water content is 4.8%, and cooling to room temperature to obtain linarin microcapsule particles, wherein the spray drying process comprises atomizing at 0.10MPa and at 15m L/min, air inlet at 130 deg.C and air outlet at 80 deg.C, and drying air at 50m3/h。
The detection shows that the encapsulation rate of the linarin reaches 96.49 percent, and the solubility is 97.23 percent.
Example 4
A method for preparing linarin microcapsule granule comprises the following steps:
(1) dissolving linarin in 10 times of water, adding tea saponin 5 wt% and fatty glyceride lactate 6 wt% of linarin, heating to 60 deg.C, stirring, and dissolving completely to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum in a mass ratio of 2:3:15 as wall materials, adding water in an amount which is 15 times of the weight of the wall materials, uniformly stirring, and heating to 65 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution while the solution is hot, adding the capsule wall material solution into a homogenizer according to the mass ratio of 1:4, and homogenizing for 2 times under the pressure of 40MPa for 40min each time to obtain a mixed solution;
(4) sending the mixed solution into a granulating sprayer for spray drying until the water content is reduced5.2 percent, cooling to room temperature to obtain the linarin microcapsule particles, wherein the spray drying process comprises the steps of atomizing at 0.08MPa, flowing at 10m L/min, feeding air at 140 ℃, discharging air at 75 ℃ and drying air at 40m3/h。
The detection shows that the encapsulation rate of the linarin reaches 97.04 percent, and the solubility is 98.13 percent.
The foregoing is a more detailed description of the invention in connection with specific/preferred embodiments and is not intended to limit the practice of the invention to those descriptions. It will be apparent to those skilled in the art that various substitutions and modifications can be made to the described embodiments without departing from the spirit of the invention, and such substitutions and modifications are to be considered as within the scope of the invention.
Claims (6)
1. A method for preparing linarin microcapsule particles is characterized by comprising the following steps: the method comprises the following steps:
(1) dissolving linarin in 8-10 times of water, adding tea saponin and lactic acid fatty glyceride, and stirring to obtain core material solution;
(2) taking phlorizin, rhamnolipid and Arabic gum as wall materials, adding water with the weight 10-15 times of that of the wall materials, uniformly stirring, and heating to 60-70 ℃ to obtain a capsule wall material solution;
(3) adding the core material solution into the capsule wall material solution according to the mass ratio of 1:1-4, adding into a homogenizer, and homogenizing to obtain a mixed solution;
(4) and (4) sending the mixed solution into a granulating sprayer for spray drying, and cooling to room temperature to obtain the linarin micro-capsule particles.
2. The process for the preparation of the linarin microcapsule granules according to claim 1, characterized in that: the mass ratio of the linarin to the tea saponin to the lactic acid fatty glyceride is 100:1-5: 3-7.
3. The process for the preparation of the linarin microcapsule granules according to claim 1, characterized in that: the mass ratio of the phlorizin to the rhamnolipid to the arabic gum in the wall material is 1-3:3-5: 10-20.
4. The process for the preparation of the linarin microcapsule granules according to claim 1, characterized in that: the homogenizing is carried out for 2-3 times under the pressure of 40-60 MPa.
5. The method for preparing the linarin microcapsule particles as claimed in claim 1, wherein the spray drying process comprises the steps of atomizing at 0.08-0.10MPa, flowing at 10-15m L/min, introducing air at 120-140 ℃, exhausting at 70-90 ℃, and drying at 40-60m3/h。
6. The method for preparing the linarin microcapsule particles according to claim 5, wherein: the drying is carried out until the water content is 4.0-5.5%.
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