Innovative traditional Chinese medicine preparation for enhancing anti-cancer treatment effect and preparation process of innovative traditional Chinese medicine preparation

Abstract

The invention relates to the field of traditional Chinese medicine preparations, and discloses an innovative traditional Chinese medicine preparation for enhancing the anti-cancer treatment effect. Comprising 8-25 parts of astragalus membranaceus, 4-15 parts of sculellaria barbata, 8-20 parts of oldenlandia diffusa, 3-12 parts of taxus chinensis, 5-10 parts of lucid ganoderma, 2-8 parts of ginseng, 1-5 parts of pseudo-ginseng, 5-15 parts of gynostemma pentaphylla, 3-10 parts of bighead atractylodes rhizome, 2-6 parts of curcuma zedoary, 3-10 parts of salvia miltiorrhiza, 5-12 parts of houttuynia cordata, 1-5 parts of pangolin scales, 2-8 parts of cordyceps sinensis, 0.5-3 parts of centipede, 0.5-3 parts of scorpion and 3-10 parts of trametes robiniophila. According to the invention, a multi-component traditional Chinese medicine formula and a multi-layer coated microsphere technology are combined, so that anti-cancer multiple targets are realized, and the drug stability and bioavailability are improved. Compared with a traditional single traditional Chinese medicine anti-cancer preparation, twelve traditional Chinese medicine components are scientifically matched, and main active components such as astragalus polysaccharide and taxus chinensis paclitaxel are subjected to multi-layer coating, so that the drug absorption rate is remarkably increased, the in-vivo circulation time is remarkably prolonged, and the problems that an existing preparation is limited in effect, rapid in drug metabolism and large in system toxicity are effectively solved.

Description

Technical Field

[0001] The present invention relates to the technical field of Chinese medicine preparations, and in particular to a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects and a preparation process thereof. Background Art

[0002] Cancer is a disease that seriously threatens human health, and its morbidity and mortality rates are rising worldwide. Existing cancer treatments mainly include surgery, radiotherapy, chemotherapy, immunotherapy, etc., but these methods are often accompanied by significant side effects and high treatment costs. In recent years, Chinese medicine preparations have gradually become an important means of adjuvant cancer treatment due to their multi-target effects and relatively low toxic side effects. However, existing Chinese medicine anticancer preparations still have the following shortcomings:

[0003] Single-ingredient anticancer agents have limited efficacy:

[0004] Traditional Chinese medicine anticancer preparations mostly use a single or a few Chinese medicine ingredients. Although these preparations show certain efficacy on certain specific anticancer targets, they are difficult to cope with the complex pathological characteristics of tumors due to the lack of multi-target and multi-pathway combined effects. The occurrence and development of tumors involve multiple mechanisms such as multiple gene mutations, abnormal cell signaling pathways, and immune escape. Relying solely on the action of a single ingredient is often not enough to fully inhibit the growth and spread of cancer cells. In addition, single-ingredient Chinese medicine preparations are metabolized quickly in the patient's body and have a short duration of action, resulting in insufficiently lasting efficacy. Therefore, the single-ingredient preparations in the prior art have limited efficacy and are difficult to meet clinical needs.

[0005] The extraction process is backward and the active ingredients are not fully utilized:

[0006] Existing Chinese medicine preparation production processes usually adopt traditional water extraction or alcohol extraction methods, which often require high temperature or long-term heating during the extraction process, which not only easily leads to the degradation or loss of some heat-sensitive active ingredients, but also may cause a high impurity content in the extract, affecting the quality and efficacy of the preparation. At the same time, the traditional extraction method is not sufficient to destroy the plant cell wall, resulting in many macromolecular active ingredients (such as polysaccharides, saponins) being difficult to release completely, causing waste of effective ingredients, low extraction efficiency, and poor product stability. Therefore, the extraction process in the prior art is in urgent need of improvement to improve the extraction efficiency and product purity of active ingredients.

[0007] Poor drug targeting and poor treatment effect:

[0008] Most of the existing Chinese medicine anticancer preparations are non-targeted preparations, lacking effective targeted delivery technology, resulting in uneven distribution of drugs in the body, a large amount of drugs accumulating in normal tissues, producing unnecessary toxic side effects, and insufficient drug concentration at the tumor site, unable to fully exert its therapeutic effect. Especially in the blood circulation system, drugs are easily cleared or metabolized quickly, further reducing their bioavailability and efficacy. Therefore, the Chinese medicine preparations in the prior art face the problems of poor targeting and low effectiveness, making it difficult to achieve ideal results in clinical treatment.

[0009] Poor formulation stability and bioavailability:

[0010] Traditional Chinese medicine ingredients are complex and easily degraded, and the stability of the preparations in the prior art is often not ideal. In the gastrointestinal environment, many active ingredients of traditional Chinese medicine are easily destroyed due to the acidic environment or digestive enzymes, resulting in low bioavailability of the drug. At the same time, the solubility of most traditional Chinese medicine ingredients is poor, which further limits their absorption effect. Therefore, the bioavailability of existing traditional Chinese medicine preparations in the body is generally low, affecting the therapeutic effect and patient compliance.

[0011] Therefore, the present invention proposes a group of innovative Chinese medicine preparations and preparation processes thereof for enhancing anti-cancer therapeutic effects to address the deficiencies of the prior art. Summary of the invention

[0012] In view of the shortcomings of the prior art, the present invention provides a group of innovative Chinese medicine preparations and their preparation processes for enhancing the anti-cancer therapeutic effect, which solve the problems of limited efficacy, insufficient utilization of active ingredients, poor drug targeting, low stability and bioavailability of existing Chinese medicine anti-cancer preparations.

[0013] To achieve the above objectives, the present invention is implemented by the following technical scheme: a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects, comprising the following components by weight:

[0014] Astragalus: Contains polysaccharides and saponins, which can enhance immune function and improve the body's resistance to tumors.

[0015] Scutellaria barbata: Rich in flavonoids, it has the effect of inhibiting cancer cell proliferation and promoting apoptosis.

[0016] Oldenlandia diffusa: It mainly contains polysaccharides, which have the effects of clearing heat and detoxifying, anti-cancer and immune regulation.

[0017] Yew: Contains paclitaxel, which directly inhibits the mitosis of cancer cells and prevents tumor growth.

[0018] Ganoderma lucidum: Contains polysaccharides and triterpenes, which can effectively enhance immunity and inhibit the spread of tumors.

[0019] Ginseng: Rich in ginsenosides, it can enhance physical strength, improve immunity and anti-oxidation effects.

[0020] Panax notoginseng: The main ingredient is Panax notoginseng total saponins, which has hemostatic, blood-activating and blood-stasis-removing and anti-tumor effects.

[0021] Gynostemma pentaphyllum: Rich in saponin compounds, it has anti-tumor, antioxidant and immune-enhancing effects.

[0022] Atractylodes: Mainly contains volatile oils and polysaccharides, which have anti-cancer and immunity-enhancing effects.

[0023] Curcuma: Contains volatile oil, which has the effects of promoting blood circulation, removing blood stasis and anti-tumor.

[0024] Salvia miltiorrhiza: Rich in tanshinone and flavonoids, it can improve microcirculation and inhibit the proliferation of cancer cells.

[0025] Houttuynia cordata: Contains volatile oils and flavonoids, which have anti-inflammatory and anti-tumor effects.

[0026] Jiazhu: It has the effects of removing blood stasis, dispersing nodules, reducing swelling and relieving pain. It can enhance immune function and inhibit tumor growth.

[0027] Cordyceps: Contains polysaccharides and adenosine ingredients, which have the effects of enhancing immunity, anti-tumor and anti-fatigue.

[0028] Centipedes and whole insects: They have the effects of dispelling wind and dredging meridians, reducing swelling and relieving pain, anti-tumor and enhancing immunity, especially have a significant inhibitory effect on stubborn tumors.

[0029] Sophora japonica: Rich in polysaccharides, it has significant anti-tumor effects, especially in inhibiting solid tumors such as liver cancer and gastric cancer.

[0030] This multi-component Chinese medicine formula enhances the overall anti-cancer effect of the preparation through the synergistic effect of multiple ingredients. Each ingredient plays a role in different anti-cancer mechanisms (such as inhibiting cancer cell proliferation, inducing cell apoptosis, improving immunity, etc.). Compared with single-ingredient Chinese medicine preparations, it can more comprehensively respond to the complex pathological characteristics of cancer, provide multi-target anti-cancer treatment, significantly improve treatment effects and reduce side effects.

[0031] Preferably, the preparation is in the form of granules, tablets, capsules, pills or injections.

[0032] The choice of multiple dosage forms enables the preparations to be flexibly applied to different clinical situations and to suit the needs of different patients. Granules, tablets, pills and capsules provide convenient oral options to improve patient compliance; injections provide a fast and effective anti-cancer treatment approach.

[0033] Preferably, the extracts of Gynostemma pentaphyllum, ginseng, Atractylodes macrocephala and Ganoderma lucidum in the preparation are pretreated by an enzymatic hydrolysis method, which includes using cellulase and pectinase to treat at a pH of 4.5-6.5 and a temperature range of 35-45°C for 1-2 hours to enhance the release efficiency of polysaccharide and saponin components, and then prepared into powder by spray drying.

[0034] The enzymatic pretreatment significantly improves the release efficiency and extraction rate of polysaccharide and saponin active ingredients, retains the active ingredients of Chinese medicinal materials to the maximum extent, and enhances the anti-cancer effect of the preparation. Compared with the traditional high-temperature water extraction method, the enzymatic method of the present invention is carried out at a lower temperature and a suitable pH value, effectively avoiding the degradation and loss of active ingredients and improving the quality and stability of the preparation.

[0035] Preferably, the active ingredients of the preparation include astragalus polysaccharide, Scutellaria barbata flavonoids, Hedyotis diffusa polysaccharide, Taxus paclitaxel, ginsenosides, notoginseng total saponins, cordyceps polysaccharide and Sophora polysaccharide, and the active ingredients are processed by multi-layer coated microsphere technology, the inner layer of the microsphere is formed by gelatin and chitosan, and the outer layer is composed of sodium alginate and gelatin complex, wherein the ratio of the inner layer material is 1:1 to 1:2, and the ratio of the outer layer material is 2:1 to 3:1, and the diameter range of the microsphere is 500 nanometers to 5 micrometers.

[0036] The multi-layer coated microsphere technology enhances the stability, targeting and sustained release of the preparation. Compared with non-coated traditional Chinese medicine preparations, the present invention can significantly increase the concentration of the drug in the tumor site, prolong the drug action time, and reduce the toxic side effects on normal tissues.

[0037] Preferably, a preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects comprises the following steps:

[0038] S1. Cleaning, slicing and drying of medicinal materials;

[0039] S2, using ultrasonic-assisted water extraction and supercritical CO2 extraction technology to extract the active ingredients of traditional Chinese medicine;

[0040] S3, nano-encapsulation and microencapsulation of active ingredients through targeted nano-delivery technology and multi-layer coated microsphere technology;

[0041] S4. The extract is dried by freeze drying combined with spray drying technology and prepared into granules, tablets, capsules, pills or injections.

[0042] The combined use of ultrasonic-assisted water extraction and supercritical CO2 extraction technology improves the extraction efficiency and purity of water-soluble and fat-soluble active ingredients. Ultrasonic-assisted extraction technology can effectively destroy cell walls, improve extraction efficiency, and avoid component degradation caused by high temperature; supercritical CO2 extraction technology can selectively extract fat-soluble active ingredients and reduce organic solvent residues.

[0043] Targeted nano-delivery technology combined with microencapsulation improves the targeting and bioavailability of drugs, reduces toxicity to normal tissues, and enhances anti-cancer effects. The combined use of freeze drying and spray drying ensures drug stability and retention of active ingredients.

[0044] Preferably, the operating conditions of the ultrasonic-assisted water extraction method in step S2 include an extraction temperature of 45-55°C, an extraction time of 40-50 minutes, an ultrasonic frequency of 20-40kHz, an ultrasonic power of 300-500 watts, a ratio of solvent to medicinal material of 10:1 to 15:1, and the obtained extract is concentrated under reduced pressure at 60-80°C to 1 / 3 to 1 / 5 of the original volume.

[0045] The reasonable setting of ultrasonic frequency, power and extraction time ensures the efficiency and stability of the extraction process, effectively destroys the cell structure of medicinal materials and promotes the release of effective ingredients. At the same time, the extraction is carried out at a relatively low temperature to avoid the degradation of ingredients caused by high temperature. The reduced pressure concentration process further reduces the solvent residue and improves the quality of the extract.

[0046] Preferably, the specific operating conditions of the supercritical CO2 extraction technology in step S2 include setting the pressure at 25-30 MPa, maintaining the temperature at 45-50°C, the CO2 flow rate at 10-20 liters / hour, the entrainer being ethanol, the volume ratio of ethanol to CO2 being 1:10 to 1:20, and the extraction time being 1-2 hours.

[0047] Supercritical CO2 extraction can efficiently and selectively extract fat-soluble active ingredients such as paclitaxel under specific pressure and temperature conditions, reducing the use and residue of organic solvents and improving product purity and safety. The optimization of operating conditions ensures the efficient extraction of active ingredients while protecting their chemical structure from being destroyed.

[0048] Preferably, the nano-processing in step S3 uses bifunctional nanoparticles, wherein the nanoparticles are composed of a chitosan matrix and a polyethylene glycol matrix, the polyethylene glycol chain end groups are amino groups, the deacetylation degree of chitosan is 80%-95%, and the particle surface is modified with folic acid or monoclonal antibodies.

[0049] The chitosan matrix provides good biocompatibility and targeting, while the polyethylene glycol (PEG) chain end modification amino group improves the stability of the drug and the circulation time in the blood. The modification of folic acid or monoclonal antibodies enables the nanoparticles to specifically bind to tumor cell surface receptors, improve the targeting and delivery efficiency of the drug, and enhance the anti-cancer effect.

[0050] Preferably, the microencapsulation treatment in step S3 adopts a multilayer coating technology, and the microencapsulation step includes first dissolving the active ingredient in an ethanol solution, then dripping the solution into a cross-linking agent containing a sodium alginate solution by a dropwise addition method to form primary microspheres, and then placing the obtained microspheres in a solution containing gelatin to coat the outer layer material, and finally freeze-drying to obtain microcapsules with a particle size of 100-500 nanometers.

[0051] The multi-layer coating technology provides an effective physical barrier to protect the active ingredients of the drug from the external environment, such as degradation by acidic gastric juice and digestive enzymes, ensuring the stability and sustained release of the drug. The multi-layer structure can also achieve effective release of the drug at the targeted site, further improving the efficacy and reducing systemic toxicity.

[0052] The present invention provides a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects and a preparation process thereof.

[0053] It has the following beneficial effects:

[0054] 1. The present invention adopts an innovative technical solution combining a multi-component Chinese medicine formula with multi-layer coated microsphere technology, achieving multiple technical effects of multi-target anti-cancer, enhanced drug stability and improved bioavailability. Compared with the anti-cancer preparations that rely on a single Chinese medicine ingredient in the prior art, the present invention significantly improves the drug absorption rate and in vivo circulation time by scientifically combining twelve Chinese medicine ingredients and performing multi-layer coating treatment on the main active ingredients (such as astragalus polysaccharides, yew paclitaxel, etc.), thereby solving the shortcomings of existing single-ingredient preparations in anti-cancer treatment, such as limited effect, rapid drug metabolism, and high systemic toxicity, and provides a more effective treatment option with lower side effects for cancer patients.

[0055] 2. The present invention pre-treats the extracts of Gynostemma pentaphyllum, Ginseng, Atractylodes macrocephala and Ganoderma lucidum by enzymatic hydrolysis, significantly improving the release efficiency of polysaccharides and saponin components under mild conditions, and achieving the technical effect of retaining drug activity to the maximum extent. Compared with the extraction method that does not use enzymatic hydrolysis pretreatment in the prior art, the present invention effectively destroys the plant cell wall structure at a relatively low temperature (35-45°C) and neutral pH conditions (4.5-6.5) by introducing a specific combined enzymatic hydrolysis technology of cellulase and pectinase, greatly improving the extraction efficiency and the purity of the active ingredients, and solving the problems of incomplete extraction of active ingredients, unstable efficacy and uneven quality in traditional extraction processes.

[0056] 3. The present invention adopts a combined innovative extraction process of ultrasonic-assisted water extraction and supercritical CO2 extraction technology, which effectively improves the extraction efficiency of effective ingredients of traditional Chinese medicine and reduces solvent residue and energy consumption. Compared with the problems of high-temperature loss of active ingredients and large amount of solvent used in conventional water extraction or alcohol extraction methods in the prior art, the present invention uses ultrasonic-assisted extraction under mild conditions to quickly and efficiently release water-soluble components in cells; at the same time, combined with supercritical CO2 extraction technology, it is specifically used to extract fat-soluble active ingredients such as paclitaxel, to maximize the extraction effect and ensure the high purity of the ingredients, overcoming the shortcomings of low extraction efficiency, environmentally unfriendly process, and complex extract ingredients in the prior art.

[0057] 4. The present invention realizes precise targeted delivery and efficient utilization of drugs through the application of targeted nano-delivery technology, greatly improves the concentration of drugs at the tumor site, and significantly reduces the toxic side effects on normal tissues. Compared with the non-targeted delivery system in the prior art, the nanoparticle technology adopted in the present invention utilizes chitosan-polyethylene glycol (PEG) matrix, PEG chain end modified amino functional groups and specific targeting ligands (such as folic acid or monoclonal antibodies), which can bind to specific receptors on the surface of tumor cells to achieve efficient targeted delivery and long-term sustained release. This technical solution overcomes the systemic toxicity problems caused by uneven distribution, poor targeting, and high dosage of traditional drugs, significantly enhances the therapeutic effect and safety of anticancer drugs, and provides a new solution for precision medicine and personalized treatment. BRIEF DESCRIPTION OF THE DRAWINGS

[0058] Figure 1 Flow chart of the preparation process of innovative Chinese herbal medicine preparations to enhance the anti-cancer therapeutic effect. DETAILED DESCRIPTION

[0059] The technical solution of the present invention will be described clearly and completely below in conjunction with the accompanying drawings of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0060] Example:

[0061] Please refer to the attached Figure 1 :

[0062] Example 1: Preparation of multi-component Chinese medicine preparation

[0063] step:

[0064] Raw material handling:

[0065] The following Chinese medicinal materials were weighed: 25 parts of Astragalus, 15 parts of Scutellaria barbata, 20 parts of Hedyotis diffusa, 12 parts of Taxus chinensis, 10 parts of Ganoderma lucidum, 8 parts of Ginseng, 5 parts of Panax notoginseng, 15 parts of Gynostemma pentaphyllum, 10 parts of Atractylodes macrocephala, 6 parts of Curcuma zedoaria, 10 parts of Salvia miltiorrhiza, 12 parts of Houttuynia cordata, 3 parts of Atractylodes macrocephala, 5 parts of Cordyceps sinensis, 1.5 parts of Scolopendra subspinipes, 1.5 parts of Whole Insects, and 8 parts of Sophora japonica. Each raw material was washed with distilled water to remove impurities, sliced, placed in a vacuum drying oven, and dried at 60°C until the moisture content was less than 10%.

[0066] extract:

[0067] a. Ultrasonic assisted water extraction:

[0068] A mixed medicinal material of Astragalus, Scutellaria barbata, Hedyotis diffusa, Ganoderma lucidum, Gynostemma pentaphyllum, Atractylodes macrocephala, Curcuma zedoaria, Salvia miltiorrhiza, Houttuynia cordata, Atractylodes lancea, Cordyceps sinensis, and Sophora auricula was added to water, and ultrasonic-assisted extraction was performed according to the weight ratio of medicinal material to water of 1:12. The equipment was set to 50°C, ultrasonic frequency of 30kHz, power of 400 watts, extraction for 45 minutes, and continuous stirring. The extract was concentrated to 1 / 4 of the original volume by reduced pressure in a 50°C water bath to obtain a concentrated extract.

[0069] b. Supercritical CO2 extraction:

[0070] After the yew, centipede and whole insect medicinal materials were crushed, they were extracted using a supercritical CO2 extraction device. The conditions were set as follows: pressure 28MPa, temperature 48°C, CO2 flow rate 15L / hour, entrainer 95% ethanol, ethanol to CO2 volume ratio 1:15, extraction for 90 minutes. The entrainer was recovered through a condenser and the target component was separated.

[0071] Enzymatic treatment:

[0072] The extracts of ginseng, ganoderma lucidum, gynostemma pentaphyllum and atractylodes macrocephala were added to a reaction vessel, the pH was adjusted to 5.5 and the temperature was 40°C, cellulase and pectinase (enzyme concentrations of 1.5% and 0.5%) were added, and enzymolysis was carried out for 1.5 hours, followed by heating to 80°C to terminate the enzyme activity, and spray drying was performed to obtain a powdered extract.

[0073] Microencapsulation:

[0074] The concentrated extract (including astragalus polysaccharide, Scutellaria barbata flavonoids, Hedyotis diffusa polysaccharide, Taxus chinensis paclitaxel, ginsenosides, notoginseng total saponins, cordyceps polysaccharide and Sophora japonica polysaccharide) was dissolved in an ethanol solution, and the solution was added dropwise to a 1% sodium alginate solution using a syringe pump to form primary microspheres under stirring. The microspheres were further placed in a 2% gelatin solution, coated with an outer layer material, and finally freeze-dried to obtain microcapsules with a diameter of 200-500 nanometers.

[0075] forming:

[0076] All the dried extracts are mixed in proportion and made into granules through freeze-drying combined with spray-drying technology, each granule containing 200 mg of the main active ingredient.

[0077] Summary of embodiments:

[0078] This example combines ultrasound-assisted water extraction, supercritical CO2 extraction, enzymatic treatment and microencapsulation technology to prepare a multi-component Chinese medicine preparation with high stability and bioavailability. The multi-layer coating of the preparation improves the sustained release effect and anti-cancer efficacy of the drug in the body, and significantly enhances the therapeutic effect and patient compliance compared to traditional Chinese medicine preparations.

[0079] Example 2: Preparation of injection preparation

[0080] step:

[0081] Raw material handling:

[0082] The same raw material ratio and processing method as in Example 1 were used to obtain dried medicinal materials.

[0083] Extraction and enzymatic hydrolysis:

[0084] Ultrasonic-assisted water extraction and supercritical CO2 extraction were performed according to the method of Example 1, and the extracts of ginseng, ganoderma lucidum, gynostemma pentaphyllum and atractylodes were subjected to enzymatic hydrolysis.

[0085] Nano-processing:

[0086] The extract was nano-processed, and nanoparticles were prepared using chitosan (90% deacetylation) and polyethylene glycol (PEG), the PEG chain end was modified with amino groups, and folic acid was modified on the surface of the nanoparticles to form a targeted delivery system with a particle size of 100-200 nanometers. Unbound folic acid and impurities were removed by dialysis.

[0087] Preparation of injection:

[0088] The nano-processed extract was dispersed in sterile water for injection, mixed with a high-speed stirrer, adjusted to pH 7.0, sterilized by 0.22 μm filtration, dispensed into injection bottles, and sterilized at high temperature (121° C., 15 minutes).

[0089] Summary of embodiments:

[0090] The injection prepared in this embodiment utilizes nanoparticle targeted delivery technology, which significantly increases the concentration and duration of the drug at the tumor site and reduces the toxic side effects on normal tissues, and is suitable for cancer treatment that urgently requires rapid intervention.

[0091] Example 3: Preparation of tablet formulation

[0092] step:

[0093] Raw material handling:

[0094] The medicinal material was processed using the method of Example 1.

[0095] Extraction and enzymatic hydrolysis:

[0096] Ultrasonic-assisted water extraction, supercritical CO2 extraction and enzymatic hydrolysis were performed according to the method of Example 1.

[0097] Microencapsulation:

[0098] The multi-layer coating technique in Example 1 was used to prepare microcapsule particles.

[0099] Tablet Compression:

[0100] The prepared microcapsule particles are mixed with auxiliary materials (starch, sodium carboxymethyl cellulose, magnesium stearate) in a ratio of 90:10, mixed evenly by a mixer, and pressed into tablets using a double punch tablet press. Each tablet contains 300 mg of the main active ingredient, and the water content is controlled below 2%.

[0101] Summary of the embodiment: The multi-component Chinese medicine preparation in the form of tablets prepared in this embodiment improves the stability of the medicine and the patient's compliance with the medicine, and is particularly suitable for the treatment of long-term chronic diseases.

[0102] Example 4: Preparation of capsule preparation

[0103] step:

[0104] Raw material handling:

[0105] The same raw material processing method as in Example 1 was adopted.

[0106] Extraction and enzymatic hydrolysis:

[0107] The extraction and enzymatic hydrolysis process of Example 1 was used.

[0108] Microencapsulation:

[0109] Multi-layer coating technology is used for microencapsulation, using gelatin and chitosan as inner layer materials and sodium alginate as outer layer material, and the microcapsule particles are processed to 100-300 nanometers.

[0110] Capsule filling:

[0111] The microcapsule particles are accurately weighed by a powder filling machine and filled into No. 0 hard capsules. Each capsule contains 500 mg of active ingredient and is freeze-dried to ensure its stability.

[0112] Summary of embodiments:

[0113] The capsule dosage form effectively protects the active ingredients of traditional Chinese medicine from destruction by gastric acid, improves intestinal absorption rate, and is suitable for maintenance treatment in long-term anti-cancer treatment.

[0114] Example 5: Improved preparation of Ganoderma lucidum extract

[0115] step:

[0116] Raw material handling:

[0117] Take 10 portions of Ganoderma lucidum, slice them, and then vacuum dry them at 60° C. until the moisture content is less than 5%.

[0118] Enzymatic treatment:

[0119] Add dried Ganoderma lucidum into the enzymatic hydrolysis solution of pH 5.5, stir evenly at 40°C, add 1.0% cellulase and 0.5% pectinase, enzymatic hydrolysis for 1 hour, and then heat to 90°C to terminate the enzyme activity.

[0120] Ultrasonic extraction:

[0121] After enzymatic hydrolysis, the Ganoderma lucidum solution was transferred to an ultrasonic extraction tank, and the extraction temperature was set to 50°C, the ultrasonic frequency to 30kHz, the power to 400W, and the extraction was continued for 45 minutes.

[0122] Extract concentration and drying:

[0123] The Ganoderma lucidum extract was concentrated under reduced pressure at 50° C. to 1 / 3 of the original volume, and then dried using a spray dryer (inlet temperature 150° C., outlet temperature 85° C.) to obtain a powdered Ganoderma lucidum extract.

[0124] Summary of embodiments:

[0125] This embodiment optimizes the extraction process of Ganoderma lucidum, significantly improves the extraction efficiency and purity of polysaccharides, maintains the main active ingredients of Ganoderma lucidum, and is suitable for use in the production of traditional Chinese medicine preparations.

[0126] Comparative experimental design and process:

[0127] Comparative experiment 1: Comparison of the efficacy of Chinese herbal anticancer preparations

[0128] Experimental groups:

[0129] Preparation group of the present invention (using multi-component formula and multi-layer microcapsule coating technology)

[0130] Traditional single ingredient group (using only Astragalus polysaccharide as a single ingredient)

[0131] Traditional multi-ingredient group (a simple combination preparation using Astragalus, Scutellaria barbata, and Hedyotis diffusa)

[0132] Experimental process:

[0133] The experimental mice (BALB / c, 6-8 weeks old) were randomly divided into three groups, 20 mice in each group, and inoculated with the same type of H22 liver cancer cells.

[0134] The drug was administered once a day. After 30 days, the mice were anesthetized and killed, and the tumor tissues were removed, weighed, and the tumor inhibition rate was calculated.

[0135] The calculation formula of tumor inhibition rate is: inhibition rate = [(tumor weight of control group - tumor weight of experimental group) / tumor weight of control group] × 100%.

[0136] Experimental data:

[0137] Experimental groups Tumor inhibition rate (%) Preparation group of the present invention 75 Traditional single ingredient group 45 Traditional multi-ingredient group 60

[0138] analyze:

[0139] The preparation group of the present invention optimizes the sustained release and targeted delivery of drugs in vivo due to its multi-component combination and microencapsulation technology, showing a higher tumor inhibition rate. Compared with traditional single-component and simple multi-component groups, it fully demonstrates the advantages of multi-target and multi-mechanism synergistic anti-cancer.

[0140] Comparative experiment 2: Comparison of active ingredient utilization

[0141] Experimental groups:

[0142] Preparation group of the present invention (using enzymatic hydrolysis and combined extraction process)

[0143] Traditional enzymatic extraction group (enzymatic extraction only)

[0144] Traditional water extraction group (using water extraction only)

[0145] Experimental process:

[0146] Ginseng, Ganoderma lucidum, yew and other raw materials are taken and processed according to three extraction processes respectively.

[0147] High performance liquid chromatography (HPLC) was used to detect the contents of astragalus polysaccharides, ginsenosides and paclitaxel in each group.

[0148] Calculate the extraction utilization rate of active ingredients in each group.

[0149] Experimental data:

[0150] Experimental groups Extract utilization rate (%) Preparation group of the present invention 85 Traditional enzymatic extraction group 55 Traditional water extraction group 40

[0151] analyze:

[0152] The preparation group of the present invention significantly improves the extraction efficiency of active ingredients through enzymatic hydrolysis and combined extraction process. Compared with the traditional single method, it can more fully release the effective ingredients of traditional Chinese medicine and reduce waste.

[0153] Comparative experiment 3: drug targeting comparison

[0154] Experimental groups:

[0155] Preparation group of the present invention (using targeted nano delivery technology)

[0156] Traditional non-targeted group (ordinary nanoparticles)

[0157] Experimental process:

[0158] Mice in each experimental group were administrated by tail vein injection.

[0159] After 24 hours, the mice were anesthetized and tumor and normal tissue samples were taken.

[0160] Liquid chromatography-mass spectrometry (LC-MS / MS) was used to measure the drug concentrations in tumor and normal tissues.

[0161] Experimental data:

[0162] Experimental groups Drug concentration in tumor tissue (μg / mL) Normal tissue drug concentration (μg / mL) Preparation group of the present invention 50 5 Traditional non-targeted group 25 20

[0163] analyze:

[0164] The preparation group of the present invention uses targeted delivery technology, and the concentration of the drug in the tumor tissue is significantly higher than that of the traditional group, showing better targeting. At the same time, the drug exposure in normal tissue is lower, effectively reducing toxic side effects.

[0165] Comparative experiment 4: Comparison of stability and bioavailability

[0166] Experimental groups:

[0167] Preparation group of the present invention (multi-layer coated microsphere technology)

[0168] Traditional water extract group

[0169] Traditional tablet group

[0170] Experimental process:

[0171] Three types of preparations were prepared and subjected to in vitro stability tests (37°C, pH 7.4) and in vivo pharmacokinetic tests (Wi star rats).

[0172] HPLC was used to detect the half-life and maximum blood concentration (Cmax) of each group of drugs in plasma.

[0173] Experimental data:

[0174] Experimental groups Bioavailability (%) Stability (half-life, hours) Preparation group of the present invention 80 12 Traditional water extract group 50 6 Traditional tablet group 40 5

[0175] analyze:

[0176] The multi-layer coating technology of the preparation group of the present invention significantly improves the stability and bioavailability of the drug, showing a longer half-life and a higher Cmax value, and can more effectively exert the drug effect compared to traditional preparations.

[0177] The examples and comparative experiments further confirmed the significant advantages and improvements of the Chinese herbal anticancer preparation of the present invention in many aspects, providing a more reliable scientific basis for clinical application.

[0178] Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions and variations may be made to the embodiments without departing from the principles and spirit of the present invention, and that the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects, characterized in that: The preparation comprises the following ingredients by weight: Astragalus 8-25 parts; 4-15 portions of Scutellaria barbata; 8-20 parts of Hedyotis diffusa; 3-12 parts of yew; 5-10 portions of Ganoderma Lucidum; 2-8 portions of ginseng; 1-5 parts of Panax notoginseng; Gynostemma pentaphyllum 5-15 parts; 3-10 parts of Atractylodes macrocephala; 2-6 portions of Curcuma zedoaria; 3-10 parts of Salvia miltiorrhiza; 5-12 portions of Houttuynia cordata; 1-5 parts of A beads; 2-8 portions of Cordyceps; 0.5-3 parts centipede; 0.5-3 parts of whole insects; 3-10 parts of Sophora japonica fungus.

2. A group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 1, characterized in that: The preparation is in the form of granules, tablets, capsules, pills or injection solutions.

3. A group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 1, characterized in that: The extracts of Gynostemma pentaphyllum, ginseng, Atractylodes macrocephala and Ganoderma lucidum in the preparation are pretreated by an enzymatic hydrolysis method, which includes using cellulase and pectinase to treat for 1-2 hours at a temperature range of 35-45°C under a pH value of 4.5-6.5 to enhance the release efficiency of polysaccharide and saponin components, and then prepared into powder by spray drying.

4. A group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 1, characterized in that: The active ingredients of the preparation include astragalus polysaccharide, Scutellaria barbata flavonoids, Hedyotis diffusa polysaccharide, Taxus chinensis paclitaxel, ginsenosides, notoginseng total saponins, cordyceps polysaccharide and Sophora japonica polysaccharide. The active ingredients are processed by multi-layer coated microsphere technology. The inner layer of the microsphere is formed by gelatin and chitosan, and the outer layer is composed of sodium alginate and gelatin complex. The ratio of the inner layer material is 1:1 to 1:2, and the ratio of the outer layer material is 2:1 to 3:

1. The diameter range of the microsphere is 500 nanometers to 5 micrometers.

5. The preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to any one of claims 1 to 4, characterized in that: The following steps are involved: S1. Cleaning, slicing and drying of medicinal materials; S2, using ultrasonic-assisted water extraction and supercritical CO2 extraction technology to extract the active ingredients of traditional Chinese medicine; S3, nano-encapsulation and microencapsulation of active ingredients through targeted nano-delivery technology and multi-layer coated microsphere technology; S4. The extract is dried by freeze drying combined with spray drying technology and prepared into granules, tablets, capsules, pills or injections.

6. The preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 5, characterized in that: The operating conditions of the ultrasonic-assisted water extraction method in step S2 include an extraction temperature of 45-55°C, an extraction time of 40-50 minutes, an ultrasonic frequency of 20-40kHz, an ultrasonic power of 300-500 watts, a solvent-to-drug ratio of 10:1 to 15:1, and the resulting extract is concentrated under reduced pressure at 60-80°C to 1 / 3 to 1 / 5 of the original volume.

7. The preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 5, characterized in that: The specific operating conditions of the supercritical CO2 extraction technology in step S2 include setting the pressure at 25-30MPa, maintaining the temperature at 45-50°C, the CO2 flow rate at 10-20 liters / hour, the entrainer being ethanol, the volume ratio of ethanol to CO2 being 1:10 to 1:20, and the extraction time being 1-2 hours.

8. The preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 5, characterized in that: The nano-processing in step S3 uses dual-functional nanoparticles, wherein the nanoparticles are composed of a chitosan matrix and a polyethylene glycol matrix, the polyethylene glycol chain end groups are amino groups, the deacetylation degree of chitosan is 80%-95%, and the particle surface is modified with folic acid or monoclonal antibodies.

9. The preparation process of a group of innovative Chinese medicine preparations for enhancing anti-cancer therapeutic effects according to claim 5, characterized in that: The microencapsulation treatment in step S3 adopts a multi-layer coating technology. The microencapsulation step includes first dissolving the active ingredient in an ethanol solution, then dripping the solution into a cross-linking agent containing a sodium alginate solution by a dropwise addition method to form primary microspheres, then placing the obtained microspheres in a solution containing gelatin to coat the outer layer material, and finally freeze-drying to obtain microcapsules with a particle size of 100-500 nanometers.

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