CN112546101A

CN112546101A - Traditional Chinese medicine compound for relieving eczema, sustained-release agent, preparation method and application

Info

Publication number: CN112546101A
Application number: CN202011549318.7A
Authority: CN
Inventors: 杜江永; 石磊; 白露; 颜慧; 韩聪慧; 纪晓宁
Original assignee: Henan Yonghui E Commerce Co ltd
Current assignee: Henan Yuanshi Trading Co.,Ltd.
Priority date: 2020-12-24
Filing date: 2020-12-24
Publication date: 2021-03-26

Abstract

The invention relates to the technical field of traditional Chinese medicines, in particular to a traditional Chinese medicine compound for relieving eczema, a slow-release agent, a preparation method and application thereof. The Chinese herbal compound is prepared from raw materials of scutellaria baicalensis, coptis chinensis, radix sileris and rhizoma atractylodis. After the traditional Chinese medicine is subjected to nanocrystallization, the bioavailability of the medicine can be increased, the onset time of the medicine is shortened, and the efficacy of the original medicine is enhanced. The nano-scale molecular material is used as a carrier material to carry the medicine, so that the medicine is adsorbed or coated in the nano carrier, the medicine release time can be prolonged, and the medicine can be automatically released at a preset speed within a preset time. By improving the dissolution rate of the active ingredients of the traditional Chinese medicine, the variety of the medicament form can be increased, and the development of various products, such as gel paste, spray, emulsion and the like, is facilitated. By using a proper gel carrier, the Chinese herbal compound can be promoted to permeate into corresponding epidermal cells to enter a target, the drug effect of relieving eczema is improved, and the instability of the drug effect of relieving eczema caused by uneven dissolution is reduced.

Description

Traditional Chinese medicine compound for relieving eczema, sustained-release agent, preparation method and application

Technical Field

The invention relates to the technical field of traditional Chinese medicines, in particular to a traditional Chinese medicine compound for relieving eczema, a slow-release agent, a preparation method and application thereof.

Background

In the Drug Delivery System (DDS) era, drug formulations entered the intelligent drug delivery system stage after going through the conventional formulation, long-acting and sustained release formulation, controlled release formulation and targeting formulation stages. The formulation is no longer merely a "formulation" of a drug having a certain dosage form, but rather a "device" for delivering and delivering the drug. The nano carrier technology is to use a nano-scale molecular material as a carrier material to carry the drug, so that the drug is adsorbed or coated in the nano carrier. The properties of the nano-medicine are obviously changed, and the activity is enhanced and even new pharmacological action is generated. For some insoluble components, the dissolution speed and the bioavailability are obviously improved after the particle size is reduced to a nanometer level. The slow release and the controlled release of the medicine can be realized by using the technical means of taking the polymer nanoparticles as the carrier and the like. The passive targeting can be achieved by utilizing the specificity of the distribution of the particles with different sizes in a human body, and the active targeting can be achieved by modifying the surface of the nanoparticles, so that the medicine reaches specific organs, tissues and cells; by reducing the characteristic that the nanoparticles are recognized by the immune system, the medicine can have longer in vivo circulation time, so that the residence time of the medicine in tissues is prolonged, and the treatment efficiency is improved.

The traditional Chinese medicine preparation has simple and rough dosage form, complicated taking and low bioavailability, and can not adapt to the rapid development rhythm of modern society and various requirements of disease treatment and skin care. The nanometer preparation or nanometer powder for injection, or nanometer liposome or nanoemulsion prepared from low water solubility and insoluble drug can improve organism absorption rate and bioavailability, enhance therapeutic effect, and reduce adverse side effect. The excellent nanometer Chinese medicine preparation has relatively high capacity, capacity of holding relatively large molecule and capacity of being used in loading various kinds of Chinese medicine components. The release of the drug can be regulated by changing the structure of the carrier or the conditions of formation. The drug is loaded without any organic solvent and high temperature involved. A nanometer compound Chinese medicinal Sustained release system (Sustained-release system of nanometer compound Chinese medicinal preparation) is called SCN technology for short. The improvement of the performance of the traditional Chinese medicine and the preparation thereof by the nanometer technology is the technology of nanometer grain size. Nanocrystallization uses surface effects and size effects to achieve physical, chemical, and biological effects that are completely different from normal states. The effects are utilized to improve and improve the performance of the traditional Chinese medicine preparation.

The advantages of nano treatment of the traditional Chinese medicine are as follows:

1 enhancing the original effect of the traditional Chinese medicine, generating the large specific surface area and small size effect of the nanometer traditional Chinese medicine with new effect, increasing the solubility and the dissolution speed of the medicine, thereby increasing the bioavailability of the medicine, accelerating the onset time of the medicine and enhancing the efficacy of the original medicine. Compared with the original medicine, the nanometer Chinese medicine has changed physicochemical properties, biological activity and pharmacological effect, even has new effect, and expands the treatment range. In addition, after the traditional Chinese medicine is processed to the nanometer scale, certain active ingredients which cannot be released originally in the cells of the traditional Chinese medicine can be released due to wall breaking, and the generation of new drug effect is promoted. The bezoar has the functions of clearing away heat and toxic materials, calming endogenous wind, relieving spasm, eliminating phlegm and inducing resuscitation, and the bezoar is processed to a nano level in the Zhongyun, so that the physicochemical property and the curative effect of the bezoar are changed, and the bezoar has strong targeting effect. Ganoderma can break spore wall by nanometer treatment, and extract lipid active substance of Ganoderma spore by supercritical fluid extraction technology, thereby enhancing antitumor activity.

2, the bioavailability is improved, the traditional Chinese medicine materials for saving the traditional Chinese medicine resources are mostly derived from natural animals and plants, some varieties are rare species, and some varieties are even endangered to be extinct. The nanometer Chinese medicine can improve bioavailability, thereby reducing dosage, relieving infinite development of limited Chinese medicine resources, protecting species number, and realizing sustainable development and protection of Chinese medicine resources. Such as ganoderma lucidum, pine pollen and the like have strong anti-tumor and health-care effects, but the wall-breaking rate is not high, the effective components are wrapped by natural structures, and the curative effect cannot be fully exerted. The wall of spore and pollen can be successfully broken by a nano treatment technology, more effective components are enriched and purified by combining corresponding extraction and separation means, and the product is prepared into corresponding dosage forms, so that the dosage is reduced, and the drug effect is better exerted.

3 the purpose of slow release and controlled release of the drug is narrowly defined, the nano controlled release system refers to a pure nano slow controlled release preparation, namely, the drug release time is prolonged and the drug is automatically released at a preset speed within a preset time. In a broad sense, the sustained-release preparation is also included, and the nano-positioning release preparation and the nano-targeting preparation are also included. Some drugs with short half-lives may be poorly adapted or inadvertently missed because of the need for repeated daily dosing. The slow release and the controlled release of the medicine can be realized by using the polymer nanoparticles as carriers and other technical means. The solid nanometer lipid particle of the tripterygium wilfordii ethyl acetate extract has good slow release and controlled release functions.

4, the traditional Chinese medicine is beneficial to standardization of the traditional Chinese medicine, internationalization, and single dosage form thereof, the processing technology is fussy and laggard, the quality standard controllability is poor, and the international market share is very small. The nano technology is introduced into the research and development of the Chinese medicinal preparation, the standardization and the standardization of the Chinese medicinal preparation are facilitated, a series of patent technologies and innovative methods with independent intellectual property rights are established in the aspects of the preparation technology, the pharmacodynamics, the toxicology and the like of the nano Chinese medicament, the market competitiveness of the Chinese medicament in China is improved, and the modernization process of the Chinese medicament is promoted.

Research shows that the pharmacological effect of Chinese medicine cannot be attributed to the unique chemical composition of the medicine and is closely related to the physical state of the medicine. When the Chinese medicine is prepared into nanometer level, its physical, chemical and biological characteristics may change greatly to produce new medicine effect. Compared with the traditional Chinese medicine, the nano traditional Chinese medicine not only greatly increases the bioavailability of the medicine, strengthens the targeting effect, but also reduces the adverse reaction, and provides a new research idea and method for the further development of the modernization of the traditional Chinese medicine research. However, in the existing process of preparing the nano traditional Chinese medicine, the conditions of complicated preparation, poor stability and uneven slow release effect exist.

Disclosure of Invention

In order to solve the above problems, the invention provides a traditional Chinese medicine compound for relieving eczema, which is prepared from raw materials of scutellaria baicalensis, coptis chinensis, radix sileris and rhizoma atractylodis.

As a preferred technical scheme, the preparation raw materials of the traditional Chinese medicine compound comprise the following components in parts by weight: 10-20 parts of scutellaria baicalensis, 10-20 parts of coptis chinensis, 10-20 parts of divaricate saposhnikovia root and 10-20 parts of rhizoma atractylodis.

As a preferred technical scheme, the preparation raw materials of the traditional Chinese medicine compound are crushed, added with water for ultrasonic treatment, filtered and concentrated to obtain the traditional Chinese medicine compound.

The invention provides a sustained release agent in a second aspect, which comprises the traditional Chinese medicine compound and a gel carrier.

As a preferable technical scheme, the weight ratio of the gel carrier to the traditional Chinese medicine compound is (45-60): (10-15).

As a preferred embodiment of the present invention, the gel carrier is selected from the group consisting of polyacrylic acid, polyacrylate, polyacrylamide, polyacrylonitrile, polyamide, polyetheramide, polyvinylamine, polyimide, polycarbonate, polyethylene, polyvinyl ketone, polyvinyl halide, polyvinyl ether, polyvinyl aromatic ester, polyvinyl pyrrolidone, polyoxymethylene, polyethylene, polypropylene, polytetrafluoroethylene, polyurethane, polyolefin elastomer, polyisobutylene, fluorosilicone, carboxymethyl chitin, polyethylene terephthalate, polypentanoate, cellulose, rayon, ethylvinylacetate copolymer, polysulfone, epoxy resin, acrylonitrile butadiene styrene resin, ethylene propylene diene gum, silicone, polyvinyl halide copolymer, chitin, polylactic acid, polyvinyl acetate, polyvinyl pyrrolidone, polyvinyl chloride, polyvinyl acetate, polyvinyl chloride, one or more of lactic acid-glycolic acid copolymers.

In a preferred embodiment of the present invention, the gel carrier includes at least two of polyacrylate, polylactic acid, and lactic acid-glycolic acid copolymer.

In a preferred embodiment of the present invention, the weight ratio of the polyacrylate, the polylactic acid, and the lactic acid-glycolic acid copolymer is (20-25): (10-15): (15-20).

In a third aspect, the present invention provides a method for preparing the sustained release agent, comprising: mixing the gel carrier and the Chinese medicinal compound, and homogenizing to obtain the sustained release preparation.

The fourth aspect of the invention provides an application of the sustained release agent in a traditional Chinese medicine preparation.

Compared with the prior art, the invention has the following beneficial effects:

(1) the invention has the advantages that the performance of the obtained traditional Chinese medicine compound is obviously changed after the traditional Chinese medicine is nanocrystallized, the dissolution is increased, the bioavailability is improved, the drug effect is enhanced, and the gel effect is utilized to change the basic properties of cold, heat, warm, cold, sour, bitter, sweet, pungent and salty types, ascending, descending, floating, sinking and the like of the traditional Chinese medicine, so as to achieve better effect.

(2) After the traditional Chinese medicine is nanocrystallized, for some insoluble components, the particle size is reduced to the nanometer level, the dissolution speed and the bioavailability are obviously improved, the original effect of the traditional Chinese medicine is enhanced, a new effect is generated, the solubility and the dissolution speed of the medicine are increased by the large specific surface area and small size effect of the nanometer traditional Chinese medicine, so that the bioavailability of the medicine is increased, the onset time of the medicine is accelerated, and the medicine effect of a raw medicine is enhanced.

(3) The bioavailability of the traditional Chinese medicine is improved, the traditional Chinese medicine resources are saved, most of the traditional Chinese medicine is derived from natural animals and plants, especially for some rare species, some species are even endangered to extinct, and after the traditional Chinese medicine is subjected to nanocrystallization, a good eczema relieving effect can be achieved under the condition of less traditional Chinese medicine use.

(4) The nano-scale molecular material is used as a carrier material to carry the medicine, so that the medicine is adsorbed or coated in the nano carrier, the medicine release time can be prolonged, and the medicine can be automatically released at a preset speed within a preset time.

(5) By improving the dissolution rate of the active ingredients of the traditional Chinese medicine, the variety of the medicament form can be increased, and the development of various products, such as gel paste, spray, emulsion and the like, is facilitated.

(6) By using a proper gel carrier, when in use, the traditional Chinese medicine compound can be promoted to permeate into corresponding epidermal cells to enter a target, the drug effect of relieving eczema is improved, and the instability of the drug effect of relieving eczema caused by uneven dissolution is reduced.

(7) The stability of the sustained release agent is improved, so that the sustained release agent can maintain the stability in acid, alkali, salt or high temperature.

(8) The nano traditional Chinese medicine sustained-release preparation for relieving eczema, which is obtained by further adjusting the dosage of the specific components, has the advantages of stable curative effect, safety, reliability, constant dosage, uniform sustained release of local administration, simple and convenient operation, no toxic or side effect and the like.

(9) Is beneficial to standardization and internationalization of the traditional Chinese medicine, and overcomes the problems of single traditional Chinese medicine and dosage form, fussy and laggard processing technology, poor quality standard controllability and small international market share.

Detailed Description

The disclosure may be understood more readily by reference to the following detailed description of preferred embodiments of the invention and the examples included therein. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. In case of conflict, the present specification, including definitions, will control.

The term "prepared from …" as used herein is synonymous with "comprising". The terms "comprises," "comprising," "includes," "including," "has," "having," "contains," "containing," or any other variation thereof, as used herein, are intended to cover a non-exclusive inclusion. For example, a composition, process, method, article, or apparatus that comprises a list of elements is not necessarily limited to only those elements but may include other elements not expressly listed or inherent to such composition, process, method, article, or apparatus.

The conjunction "consisting of …" excludes any unspecified elements, steps or components. If used in a claim, the phrase is intended to claim as closed, meaning that it does not contain materials other than those described, except for the conventional impurities associated therewith. When the phrase "consisting of …" appears in a clause of the subject matter of the claims rather than immediately after the subject matter, it defines only the elements described in the clause; other elements are not excluded from the claims as a whole.

When an amount, concentration, or other value or parameter is expressed as a range, preferred range, or as a range of upper preferable values and lower preferable values, this is to be understood as specifically disclosing all ranges formed from any pair of any upper range limit or preferred value and any lower range limit or preferred value, regardless of whether ranges are separately disclosed. For example, when a range of "1 to 5" is disclosed, the described range should be interpreted to include the ranges "1 to 4", "1 to 3", "1 to 2 and 4 to 5", "1 to 3 and 5", and the like. When a range of values is described herein, unless otherwise stated, the range is intended to include the endpoints thereof and all integers and fractions within the range.

The singular forms "a", "an" and "the" include plural referents unless the context clearly dictates otherwise. "optional" or "any" means that the subsequently described event or events may or may not occur, and that the description includes instances where the event occurs and instances where it does not.

Approximating language, as used herein throughout the specification and claims, is intended to modify a quantity, such that the invention is not limited to the specific quantity, but includes portions that are literally received for modification without substantial change in the basic function to which the invention is related. Accordingly, the use of "about" to modify a numerical value means that the invention is not limited to the precise value. In some instances, the approximating language may correspond to the precision of an instrument for measuring the value. In the present description and claims, range limitations may be combined and/or interchanged, including all sub-ranges contained therein if not otherwise stated.

In addition, the indefinite articles "a" and "an" preceding an element or component of the invention are not intended to limit the number requirement (i.e., the number of occurrences) of the element or component. Thus, "a" or "an" should be read to include one or at least one, and the singular form of an element or component also includes the plural unless the stated number clearly indicates that the singular form is intended.

The present invention is illustrated by the following specific embodiments, but is not limited to the specific examples given below.

The invention provides a traditional Chinese medicine compound, which is prepared from raw materials of scutellaria baicalensis, coptis chinensis, radix sileris and rhizoma atractylodis.

In one embodiment, the preparation raw materials of the traditional Chinese medicine compound provided by the invention comprise the following components in parts by weight: 10-20 parts of scutellaria baicalensis, 10-20 parts of coptis chinensis, 10-20 parts of divaricate saposhnikovia root and 10-20 parts of rhizoma atractylodis.

Preferably, the preparation raw materials of the traditional Chinese medicine compound provided by the invention comprise the following components in parts by weight: 15 parts of scutellaria baicalensis, 15 parts of coptis chinensis, 15 parts of divaricate saposhnikovia root and 15 parts of rhizoma atractylodis.

In the traditional Chinese medicine formula, all components support each other and have the following activities and functions.

Scutellaria baicalensis: it is bitter in taste and cold in nature, and enters lung, gallbladder, spleen, large intestine and small intestine meridians. Clear heat and dry dampness, purge fire and remove toxicity, stop bleeding, prevent abortion. Can be used for treating damp-warm syndrome, summer-heat dampness, chest distress, emesis, dampness and heat distention, dysentery, jaundice, cough due to lung heat, hyperpyrexia, polydipsia, hematemesis, carbuncle, swelling, sore, and threatened abortion.

Coptis chinensis: bitter in taste and cold in nature, and enter heart, spleen, stomach, liver, gallbladder and large intestine meridians. Clear heat and dry dampness, purge fire and remove toxicity. Dampness-heat fullness, vomiting, acid regurgitation, dysentery, jaundice, high fever, coma, hyperactivity of heart-fire, vexation, insomnia, palpitation, hematemesis, epistaxis, conjunctival congestion, toothache, diabetes, carbuncle, swelling and sore; it is used externally to treat eczema, eczema and purulent ear canal.

Wind prevention: pungent and sweet in flavor, slightly warm in nature. It enters bladder, lung, spleen and liver meridians. Dispel wind and relieve exterior syndrome, subdue dampness and alleviate pain, stop spasm. Can be used for treating exterior syndrome due to exogenous pathogenic factor, rubella pruritus, rheumatalgia, tetanus, and spleen deficiency with excessive dampness.

Rhizoma atractylodis: pungent and bitter with warm nature. It enters spleen, stomach and liver meridians. Dry dampness and invigorate spleen, dispel wind and cold, improve vision. Can be used for treating damp obstruction of middle warmer, abdominal distention, diarrhea, edema, tinea pedis, atrophic debility cramped, rheumatalgia, wind-cold type common cold, night blindness, dim eyesight, and astringency.

More preferably, the preparation raw materials of the traditional Chinese medicine compound are crushed, added with water for ultrasonic treatment and concentrated to obtain the traditional Chinese medicine compound. Further preferably, the preparation raw materials of the traditional Chinese medicine compound are subjected to superfine airflow crushing, water adding and ultrasonic treatment, filtering and concentration to obtain the traditional Chinese medicine compound. More preferably, the weight ratio of the traditional Chinese medicine compound provided by the invention to the total weight of the scutellaria baicalensis, the coptis chinensis, the radix sileris and the rhizoma atractylodis is 1: (0.5 to 1.5) and there may be mentioned, for example, 1: 0.5, 1: 0.6, 1: 0.7, 1: 0.8, 1: 0.9, 1: 1. 1: 1.1, 1: 1.2, 1: 1.3, 1: 1.4, 1: 1.5.

the invention provides a sustained release agent in a second aspect, which comprises the traditional Chinese medicine compound and a gel carrier. In one embodiment, the weight ratio of the gel carrier to the traditional Chinese medicine compound is (45-60): (10 to 15), there may be mentioned, for example, 45: 10. 60: 15. 50: 12. 55: 14.

preferably, the gel carrier of the present invention is selected from the group consisting of polyacrylic acid, polyacrylate, polyacrylamide, polyacrylonitrile, polyamide, polyetheramide, polyvinylamine, polyimide, polycarbonate, polyethylene carbonate, polyvinyl ketone, polyvinyl halide, polyvinylidenehalide, polyvinyl ether, polyvinyl ester, polyvinylpyrrolidone, polyoxymethylene, polyethylene, polypropylene, polytetrafluoroethylene, one or more of polyurethane, polyolefin elastomer, polyisobutylene, fluorosilicone, carboxymethyl chitin, polyethylene terephthalate, poly valerate, cellulose, rayon, ethyl vinyl acetate copolymer, polysulfone, epoxy resin, acrylonitrile butadiene styrene resin, ethylene propylene diene rubber, silicone, polyethylene halogen copolymer, chitin, polylactic acid, and lactic acid-glycolic acid copolymer.

In order to improve the adsorption and coating effects of the gel carrier on the traditional Chinese medicine compound, the applicant finds that the gel carrier with good compatibility and interaction with the traditional Chinese medicine compound is needed, and the stability of the gel and the stability of the carrier skeleton are influenced due to different structures and acid-base properties of various active ingredients in the traditional Chinese medicine compound. More preferably, the gel carrier of the present invention comprises at least two of polyacrylate, polylactic acid, and lactic acid-glycolic acid copolymer. Further preferably, the gel carrier of the present invention comprises polyacrylate, polylactic acid, and lactic acid-glycolic acid copolymer. More preferably, the weight ratio of the polyacrylate, the polylactic acid and the lactic acid-glycolic acid copolymer is (20-25): (10-15): (15 to 20), there may be mentioned, 20: 10: 15. 25: 15: 20. 22: 12: 18.

polyacrylates are polymers of acrylates and the present invention provides polyacrylates that are well known in the art and include, but are not limited to, 4410 by degussa, DSM, i.e., NeoCryl-BT-10, NeoCryl a-1120, R-20B, R90, RV-4916, RX-20 in korea, the netherlands.

Polylactic acid, also known as polylactide, is a polyester polymer obtained by polymerizing lactic acid as a main raw material, and is a novel biodegradable material. Is made by using starch raw material proposed by renewable plant resources (such as corn). The starch raw material is saccharified to obtain glucose, the glucose and certain strains are fermented to prepare high-purity lactic acid, and the polylactic acid with certain molecular weight is synthesized by a chemical synthesis method. The biodegradable plastic has good biodegradability, can be completely degraded by microorganisms in the nature after being used, finally generates carbon dioxide and water, does not pollute the environment, is very favorable for protecting the environment, and is a well-known environment-friendly material. Examples of polylactic acids include, but are not limited to, 2002D, 2003D, 3001D, 4032D from Nature Works, PLABIOS30, PLABIOS50, REVODE101, REVODE190, REVODE201, REVODE213S, REVODE 290, REVODE703, REVODE711, TE-8210 from Eureka, and GH401, GH501, GH601, GH701 from Shanghai.

Lactic acid-glycolic acid copolymer, also known as polylactic acid-glycolic acid copolymer (PLGA), is formed by random polymerization of two monomers, namely lactic acid and glycolic acid, is a degradable functional polymer organic compound, has good biocompatibility, no toxicity and good properties of encapsulation and film formation, and is widely applied to the fields of pharmacy, medical engineering materials and modern industry. The degradation products of PLGA are lactic acid and glycolic acid, which are also byproducts of human metabolic pathways, and thus it has no toxic side effects when applied in medicine and biomaterials. Of course, lactose deficient ones are excluded. By adjusting the monomer ratio and thus changing the degradation time of PLGA, this method has been widely used in biomedical fields, such as: skin grafting, wound suturing, in vivo implantation, micro-nano particles and the like. The invention does not specifically limit the manufacturers of the lactic acid-glycolic acid copolymer, and can be purchased from Shanghai Gooduo Biotech Co., Ltd, Shanghai Ding Biotech Co., Ltd, and the like.

The third aspect of the present invention provides a method for preparing the sustained release agent as described above, comprising: mixing the gel carrier and the Chinese medicinal compound, and homogenizing to obtain the sustained release preparation. In one embodiment, the homogenizing speed is 2000-4000 r/min, wherein 2000r/min, 2200r/min, 2500r/min, 2800r/min, 3000r/min, 3200r/min, 3500r/min, 3800r/min and 4000r/min are enumerated, and the homogenizing time is 5-15 min, wherein 5min, 6min, 7min, 8min, 9min, 10min, 11min, 12min, 13min, 14min and 15min are enumerated.

In a fourth aspect, the invention provides a use of the diluent as described above in a Chinese medicinal preparation. The diluent provided by the invention can be used in various traditional Chinese medicine preparations, such as gel paste, spray, emulsion and the like, and is not particularly limited.

The gel ointment mainly adopts hydrophilic substances as matrix, the water content of the gel ointment is close to that of animal (human) skin, the hydration of skin cuticle can be enhanced, the cuticle is softened, and pore channels are formed to facilitate the transdermal absorption of the medicine. Compared with rubber plaster, the gel plaster has better compatibility with water-soluble and fat-soluble medicines, so the matrix has larger drug-loading rate, and is very suitable for the characteristics of more traditional Chinese medicine components and large dosage. The gel paste is convenient to use, can be repeatedly applied, still can keep original viscosity, and does not pollute clothes. The nanometer lipid traditional Chinese medicine is loaded into a gel framework to construct a novel transdermal drug delivery system, so that the discomfort of eczema can be effectively relieved.

The gel obtained by adding the traditional Chinese medicine into the spray for nano treatment can effectively solve the problem that certain components of the traditional Chinese medicine are insoluble in water or have poor solubility to influence the appearance of the aqueous solution. The humectant is added, so that the dry skin condition after the water aqua is sprayed can be relieved. The preparation of the nanometer traditional Chinese medicine moisturizing spray can relieve discomfort of eczema and skin itch and bring better use experience.

Examples

The present invention will be specifically described below by way of examples. It should be noted that the following examples are only for illustrating the present invention and should not be construed as limiting the scope of the present invention, and that the insubstantial modifications and adaptations of the present invention by those skilled in the art based on the above disclosure are still within the scope of the present invention.

Example 1

The embodiment provides a traditional Chinese medicine compound, and the preparation raw materials of the traditional Chinese medicine compound comprise the following components in parts by weight: 20 parts of scutellaria baicalensis, 10 parts of coptis chinensis, 20 parts of divaricate saposhnikovia root and 10 parts of rhizoma atractylodis; the preparation raw materials of the traditional Chinese medicine compound are subjected to superfine airflow crushing, water adding and ultrasonic treatment, filtering and concentration to obtain the traditional Chinese medicine compound, wherein the weight ratio of the traditional Chinese medicine compound to the total weight of the scutellaria baicalensis, the coptis chinensis, the radix sileris and the rhizoma atractylodis is 1: 1.

the embodiment also provides a sustained-release agent which comprises the traditional Chinese medicine compound and the gel carrier. In one embodiment, the weight ratio of the gel carrier to the traditional Chinese medicine compound is 45: 10; the gel carrier comprises polyacrylate, polylactic acid and lactic acid-glycolic acid copolymer, and the weight ratio is 20: 15: 15.

the polyacrylate was purchased from 4410 of degussa.

The polylactic acid is available from Nature Works, USA 2003D.

The lactic acid-glycolic acid copolymer is purchased from Shanghai Ding Lloyd Biotech limited.

This example also provides a method for preparing the sustained release formulation as described above, comprising: mixing the gel carrier and the Chinese medicinal compound, and homogenizing at 3000r/min for 10min to obtain the sustained release preparation.

The embodiment also provides a nano traditional Chinese medicine gel paste, which is prepared from the following raw materials in parts by weight: 5 parts of sodium polyacrylate, 15 parts of glycerol, 0.2 part of dihydroxyaluminium aminoacetate, 15 parts of a slow release agent, 0.2 part of tartaric acid, 0.3 part of phenoxyethanol and 64.3 parts of water.

The preparation method of the gel paste comprises the following steps: mixing weighed sodium polyacrylate, dihydroxyaluminum glycolate and glycerol uniformly, mixing and stirring the sustained-release agent, tartaric acid and water to completely dissolve, pouring the mixture into the sodium polyacrylate, dihydroxyaluminum glycolate and glycerol, stirring the mixture rapidly until the feed liquid is in a uniform gel state, uniformly pouring the gel on a non-woven fabric to spread, covering a layer of pearlized film, curing the pearlized film in a ventilated shade, and taking the pearlized film into a sealed bag after the pearlized film can be completely uncovered. When in use, the gel pastes with different sizes and shapes can be cut according to requirements, the anti-sticking layer of the pearlized film is removed, and the gel surface is stuck to the skin for use.

The embodiment also provides a nano traditional Chinese medicine moisturizing spray, which is prepared from the following raw materials, by weight, 15 parts of a slow release agent, 1 part of betaine, 0.3 part of phenoxyethanol and 83.7 parts of water.

The preparation method of the moisturizing spray comprises the following steps: the preparation raw materials of the moisturizing spray are stirred, mixed evenly and dissolved completely. Finally, the liquid is light yellow transparent liquid.

The embodiment also provides a nano traditional Chinese medicine emulsion, which comprises the following raw materials in parts by weight: phase A: 0.5 part of xanthan gum and 8g of glycerol; phase B: 3 parts of caprylic capric acid glyceride, 2 parts of 16/18 alcohol and 3 parts of beeswax; and C phase: 15 parts of slow release agent and 0.3 part of phenoxyethanol.

The preparation method of the nano emulsion comprises the following steps: uniformly mixing xanthan gum and glycerol of phase A, adding water, heating caprylic capric glyceride of phase B, 16/18 alcohol and beeswax to 80 ℃ to completely melt, pouring phase B into phase A, rapidly stirring until the liquid is white, uniform and milky, cooling to room temperature, adding slow-release agent and phenoxyethanol, uniformly stirring, and homogenizing for 3 minutes by using a homogenizer.

Example 2

The embodiment provides a traditional Chinese medicine compound, and the preparation raw materials of the traditional Chinese medicine compound comprise the following components in parts by weight: 10 parts of scutellaria baicalensis, 20 parts of coptis chinensis, 10 parts of divaricate saposhnikovia root and 20 parts of rhizoma atractylodis; the preparation raw materials of the traditional Chinese medicine compound are subjected to superfine airflow crushing, water adding and ultrasonic treatment, filtering and concentration to obtain the traditional Chinese medicine compound, wherein the weight ratio of the traditional Chinese medicine compound to the total weight of the scutellaria baicalensis, the coptis chinensis, the radix sileris and the rhizoma atractylodis is 1: 1.

the embodiment also provides a sustained-release agent which comprises the traditional Chinese medicine compound and the gel carrier. In one embodiment, the weight ratio of the gel carrier to the traditional Chinese medicine compound is 60: 15; the gel carrier comprises polyacrylate, polylactic acid and lactic acid-glycolic acid copolymer, and the weight ratio is 20: 10: 15.

the polyacrylate was purchased from 4410 of degussa.

The polylactic acid is available from Nature Works, USA 2003D.

The embodiment of the nano traditional Chinese medicine gel paste is the same as that of the embodiment 1.

The embodiment of the nano traditional Chinese medicine moisturizing spray is the same as that in example 1.

The embodiment of the nano traditional Chinese medicine emulsion is the same as that of the embodiment 1.

Example 3

The embodiment provides a traditional Chinese medicine compound, and the preparation raw materials of the traditional Chinese medicine compound comprise the following components in parts by weight: 15 parts of scutellaria baicalensis, 15 parts of coptis chinensis, 15 parts of divaricate saposhnikovia root and 15 parts of rhizoma atractylodis; the preparation raw materials of the traditional Chinese medicine compound are subjected to superfine airflow crushing, water adding and ultrasonic treatment, filtering and concentration to obtain the traditional Chinese medicine compound, wherein the weight ratio of the traditional Chinese medicine compound to the total weight of the scutellaria baicalensis, the coptis chinensis, the radix sileris and the rhizoma atractylodis is 1: 1.

the embodiment also provides a sustained-release agent which comprises the traditional Chinese medicine compound and the gel carrier. In one embodiment, the weight ratio of the gel carrier to the traditional Chinese medicine compound is 60: 15; the gel carrier comprises polyacrylate, polylactic acid and lactic acid-glycolic acid copolymer, and the weight ratio is 25: 15: 20.

the polyacrylate was purchased from 4410 of degussa.

The polylactic acid is available from Nature Works, USA 2003D.

Example 4

The embodiment of the compound Chinese medicine is the same as that in example 3.

This example also provides a sustained-release agent, which is similar to example 3 except that a lactic acid-glycolic acid copolymer is not included.

The embodiment of the present invention also provides a method for preparing a sustained-release agent, which is the same as in example 3.

The embodiment of the present invention also provides a nanometer Chinese medicinal gel paste, which is the same as that in example 3.

Example 5

This example also provides a sustained-release agent, which is similar to example 3, except that polylactic acid is not included.

Example 6

This example also provides a sustained release agent, which is embodied in the same manner as in example 3, except that polyacrylate is not included.

Example 7

This example also provides a sustained-release agent, which is specifically implemented in the same manner as in example 3, except that the lactic acid-glycolic acid copolymer is replaced with chitosan, which is available from Shandong Oncang Biotech Co.

Evaluation of Performance

The following experiments were performed as experimental groups provided in the examples.

1. The eczema relieving effect is as follows: 240 volunteers suffering from infantile eczema are selected and randomly divided into 8 groups, wherein 7 groups are used as an observation group, gel cream provided by the embodiment is smeared on an affected part, the last group is used as a control group, silicone oil cream (main components are simethicone and vaseline) is smeared for 2 times every day, 7 days are taken as a treatment course, the total clinical effective rate of the patients is observed after 2 treatment courses, and the clinical research on infantile eczema is carried out by referring to literature yellow-red snake skin external washing formula [ J ] new traditional Chinese medicine, 2011,43(6):75-76. self-proposed curative effect evaluation method: efficacy index ═ (pre-treatment score-post-treatment score)/pre-treatment score × 100%. (1) And (3) healing: the curative effect index is more than or equal to 95 percent; (2) the effect is shown: the curative effect index is 60-94%; (3) the method has the following advantages: the curative effect index is 20 to 59 percent; (4) and (4) invalidation: the curative effect index is less than 20%.

The severity of eczema infant disease before and after treatment was assessed with reference to EASI. Scoring the skin damage condition according to (0-6 points), (1)0 point: no skin damage. (2)1 minute: is less than 10%. (3) And 2, dividing: not less than 10%. (4) And 3, dividing: the area of skin damage is more than or equal to 20 percent. (5) And 4, dividing: not less than 50 percent. (6) And 5, dividing: not less than 70 percent. (7) 90 to 100 percent of the total weight of the composition is 6. Grading the skin lesion morphology, and distinguishing the morphogenetic degree of erythema, pimple, erosion, exudation, incrustation and the like of the infant patient. Grading the pruritus degree according to (0-3 points), (1)0 point: no itching feeling. (2)1 minute: mild itching and no irritability. (3) And 2, dividing: obvious itching and irritability. (4) And 3, dividing: severe itching affecting sleep, the results are shown in table 1. The total effective rate of an observation group is higher than that of a control group, the difference has statistical significance, and the data of the observation group shows that the total effective rate is more than 80%, but more recovery volunteers of embodiments 1-3 using polyacrylate, polylactic acid and lactic acid-glycolic acid copolymer as gel carriers are beneficial to promoting the traditional Chinese medicine compound to permeate into corresponding epidermal cells to enter a target, the drug effect of relieving eczema is improved, and the drug effect instability of relieving eczema caused by uneven dissolution is reduced.

TABLE 1 Effect of alleviating eczema

2. Short-term recurrence rate: the follow-up visit after 1 or 6 months of treatment shows that the original part of the infant is healed to reappear the rash and the clinical symptoms and accords with the eczema diagnosis standard or shows effect, and the original skin damage and the symptom aggravation after the infant is cured are treated as relapse. The recurrence rate is the number of relapses/total follow-up × 100%, and the results are shown in table 2. It can be seen that the short-term recurrence rate of 1/6 months after the treatment was lower in the observation group, compared to the control group, and the difference was statistically significant.

TABLE 2 short term recurrence rates

Group of	1 month	6 months old
			Example 3	1	2
Control group	6	8

3. Stability: the sustained release agent provided in the example was centrifuged at 5000rpm for 15min to observe whether or not precipitation occurred, wherein no precipitation occurred in the 1-stage, slight precipitation occurred in the 2-stage, general precipitation in the 3-stage, and obvious precipitation in the 4-stage, and the results are shown in table 3.

TABLE 3 stability

4. Adverse reaction conditions: in the observation groups of the examples 1-3, no volunteer appeared slightly red and swollen during the treatment period, 4 red and swollen phenomena appeared in the control group, and other adverse reactions such as obvious skin pigmentation and the like did not appear. The adverse reaction rate of the observation group is lower than that of the control group, and the dissimilarity has statistical significance.

According to the test results, the traditional Chinese medicine compound provided by the invention has a high effect of relieving eczema, and by adding the sustained release agent, the sustained release and the biological dissolution can be promoted, and the stability of relieving eczema is improved.

The foregoing examples are merely illustrative and serve to explain some of the features of the method of the present invention. The appended claims are intended to claim as broad a scope as is contemplated, and the examples presented herein are merely illustrative of selected implementations in accordance with all possible combinations of examples. Accordingly, it is applicants' intention that the appended claims are not to be limited by the choice of examples illustrating features of the invention. Also, where numerical ranges are used in the claims, subranges therein are included, and variations in these ranges are also to be construed as possible being covered by the appended claims.

Claims

1. The traditional Chinese medicine compound for relieving eczema is characterized in that raw materials for preparing the traditional Chinese medicine compound consist of scutellaria baicalensis, coptis chinensis, divaricate saposhnikovia root and rhizoma atractylodis.

2. The traditional Chinese medicine compound for relieving eczema as claimed in claim 1, wherein the raw materials for preparing the traditional Chinese medicine compound comprise the following components in parts by weight: 10-20 parts of scutellaria baicalensis, 10-20 parts of coptis chinensis, 10-20 parts of divaricate saposhnikovia root and 10-20 parts of rhizoma atractylodis.

3. The traditional Chinese medicine compound for relieving eczema as claimed in claim 1, wherein the traditional Chinese medicine compound is prepared by crushing raw materials for preparing the traditional Chinese medicine compound, adding water for ultrasonic treatment, filtering and concentrating.

4. A sustained-release agent, which is characterized by comprising the traditional Chinese medicine compound according to any one of claims 1 to 3 and a gel carrier.

5. The sustained-release agent according to claim 4, wherein the weight ratio of the gel carrier to the traditional Chinese medicine compound is (45-60): (10-15).

6. The sustained-release agent according to claim 4, wherein the gel carrier is selected from the group consisting of polyacrylic acid, polyacrylate, polyacrylamide, polyacrylonitrile, polyamide, polyetheramide, polyvinylamine, polyimide, polycarbonate, polyethylene carbonate, polyvinyl ketone, polyvinyl halide, polyvinylidene halide, polyvinyl ether, polyvinyl aromatic ester, polyvinyl ester, polyvinylpyrrolidone, polyoxymethylene, polyethylene, polypropylene, polytetrafluoroethylene, polyurethane, polyolefin elastomer, polyisobutylene, fluorosilicone, carboxymethyl chitin, polyethylene terephthalate, polypentanoate, cellulose, rayon, ethylvinylacetate copolymer, polysulfone, epoxy resin, acrylonitrile butadiene styrene resin, ethylene propylene diene gum, silicone, polyethylene halogen copolymer, chitin, and polyethylene glycol, One or more of polylactic acid and lactic acid-glycolic acid copolymer.

7. The sustained-release formulation according to claim 6, wherein the gel carrier comprises at least two of polyacrylate, polylactic acid, and lactic acid-glycolic acid copolymer.

8. The sustained-release agent according to claim 7, wherein the weight ratio of the polyacrylate, the polylactic acid and the lactic acid-glycolic acid copolymer is (20-25): (10-15): (15-20).

9. A method for preparing a sustained-release agent according to any one of claims 4 to 8, comprising: mixing the gel carrier and the Chinese medicinal compound, and homogenizing to obtain the sustained release preparation.

10. Use of a sustained release formulation according to any one of claims 4 to 8 in a Chinese medicinal preparation.