Composition for diminishing inflammation and sterilizing stomach as well as preparation method and application of composition

Abstract

The composition is prepared from the following raw materials: 50 to 70 parts of rhizoma dioscoreae, 25 to 35 parts of radix paeoniae alba, 25 to 35 parts of rhizoma atractylodis, 10 to 20 parts of rhizoma zingiberis, 10 to 20 parts of radix cynanchi bungei and 10 to 20 parts of raw fructus crataegi. The preparation method comprises the following steps: 1, raw material pretreatment; 2, superfine grinding; 3, mixing process; and 4, forming process. The traditional Chinese medicine composition has the advantages that the dual effects of diminishing inflammation, sterilizing and repairing tissues are achieved through a specific proportion and a preparation process, the traditional Chinese medicine composition is suitable for treating and preventing chronic gastritis and gastric ulcer diseases, and accurate component protection is achieved through a three-section gradient drying process; differential superfine grinding and plasma activation have a synergistic effect; the double-layer sustained-release pill design realizes accurate matching; and the safety of microorganisms is guaranteed through multi-mode sterilization.

Description

Technical Field

[0001] The present invention belongs to the field of traditional Chinese medicine compositions, and in particular relates to a composition for gastric anti-inflammatory and sterilization, and a preparation method and application thereof. Background Art

[0002] At present, the synergistic compatibility mechanism of many Chinese herbal medicine compositions is unclear: most compound prescriptions are based only on empirical compatibility (such as the "monarch, minister, assistant and envoy" theory), and there is a lack of quantitative research on the synergistic effects of active ingredients. For example, the effect of the ratio of Atractylodes lancea volatile oil to gingerols on antibacterial activity has not been revealed.

[0003] Current treatment options for diseases related to gastric mucosal damage (such as gastritis and gastric ulcers) mainly rely on chemical drugs and traditional Chinese medicine compounds, but the following technical bottlenecks still exist:

[0004] The traditional pill-making process uses high-temperature drying (80-100°C), which causes a 40% decrease in the polymerization degree of yam polysaccharides, weakening the mucosal repair effect, resulting in complex active ingredients, high difficulty in quality control, and the possibility of unforeseen interactions.

[0005] Traditional dosage forms suffer from low bioavailability and unstable release of active ingredients. For example, the oral absorption rate of ingredients such as hawthorn flavonoids is significantly limited because they do not use encapsulation technology.

[0006] Loss of active ingredients: Conventional high-temperature drying and pulverization processes can easily lead to the decomposition and inactivation of heat-sensitive ingredients (such as Atractylodes lancea volatile oil and gingerol);

[0007] Poor formulation stability: Common adhesives (such as starch) are difficult to achieve sustained-release effects. Summary of the Invention

[0008] To address the above issues, the present invention discloses a gastric anti-inflammatory and bactericidal composition, its preparation method, and its application. Through a specific ratio and preparation process, it achieves dual effects of anti-inflammatory and bactericidal effects as well as tissue repair, and is suitable for the treatment and prevention of chronic gastritis and gastric ulcers. The specific solution is as follows:

[0009] A gastric anti-inflammatory and bactericidal composition is characterized in that the raw materials include: 50-70 parts of Chinese yam, 25-35 parts of white peony root, 25-35 parts of atractylodes, 10-20 parts of dried ginger, 10-20 parts of gypsophila, and 10-20 parts of raw hawthorn.

[0010] Preferably, 55-65 parts of Chinese yam, 26-30 parts of white peony root, 30-35 parts of atractylodes, 15-20 parts of dried ginger, 15-20 parts of clematis root, and 15-20 parts of raw hawthorn.

[0011] A method for preparing a gastric anti-inflammatory and bactericidal composition, comprising:

[0012] 1. Raw material pretreatment:

[0013] (1) Initial dehumidification: hot air circulation drying at 40℃-55℃ for 2 hours to remove moisture and make the moisture content of medicinal materials ≤15%;

[0014] (2) Middle section shaping: vacuum drying at 30°C (-0.08MPa) for 3-4 hours to prevent thermal decomposition of the active ingredients of the medicinal materials;

[0015] (3) Final stage stability: Dry in a cool, ventilated place at 10-20°C until the moisture content is ≤8%;

[0016] 2. Ultrafine grinding:

[0017] (1) Differentiated pulverization: Chinese yam and diatom are pulverized by shearing mill, with the particle size controlled to ≤75μm; Atractylodes and dried ginger are pulverized by impact mill with liquid nitrogen pre-cooling; White peony root and raw hawthorn are pulverized by hammer mill, with white peony root 20 mesh and raw hawthorn 100 mesh;

[0018] (2) Powder activation treatment: The mixed powder was placed in a plasma treatment device for powder activation treatment for 15 minutes;

[0019] 3. Mixing process:

[0020] The medicinal material powder was added during the main mixing stage, and the dual-motion mixer was run for 45 minutes;

[0021] Homogenization stage: 3 cycles of air vortex homogenizer, the final mixing uniformity RSD ≤ 2.5%;

[0022] 4. Molding process

[0023] (1) Adhesive:

[0024] Core adhesive layer: Use honey, the addition amount is 25% of the total weight of the medicinal materials, melted at 60℃ and sprayed into powder through a high-pressure nozzle (0.4MPa);

[0025] Surface modification layer: liquid maltitol is sprayed on the surface with an addition amount of 3% to form a moisture-proof protective film.

[0026] (2) Double-layer sustained-release pills:

[0027] The immediate-release layer contains nanoemulsion of Atractylodes lancea essential oil and dried ginger extract, accounting for 30% of the pill weight;

[0028] Sustained-release layer: using yam polysaccharide-calcium alginate gel skeleton, accounting for 70% of the pill weight;

[0029] (3) Enteric coating:

[0030] Fluidized bed coating was performed using pH-sensitive acrylic resin, with a coating weight gain of 8%;

[0031] 4. Combined sterilization

[0032] (1) Microwave pretreatment: 2000MHz-2600MHz microwave irradiation for 5 minutes, the material temperature is controlled at 55℃;

[0033] Ozone dynamic sterilization: ozone is introduced into the closed conveyor belt for 30 minutes;

[0034] UV sterilization, contact time 30 minutes.

[0035] Preferably, the shearing mill has a rotation speed of 2500 rpm-3000 rpm.

[0036] Preferably, the atractylodes lancea and dried ginger are impact-pulverized using liquid nitrogen pre-cooling, with the temperature set at -30°C, and the volatile oil retention rate is increased to 88%±2%.

[0037] Preferably, the plasma processing equipment has a power of 50W and uses argon gas.

[0038] Preferably, the Atractylodes lancea volatile oil nanoemulsion has a particle size of 120 nm.

[0039] Preferably, the gastric anti-inflammatory and bactericidal composition is used for anti-inflammatory and bactericidal effects and gastric tissue repair during preparation.

[0040] Compared with the prior art, the advantages of the present invention are:

[0041] 1. Three-stage gradient drying process achieves precise protection of ingredients

[0042] A three-stage drying process—40-55°C hot air dehumidification, 30°C vacuum setting, and 10-20°C shade drying—combined with gradient temperature control technology effectively prevents the decomposition of heat-sensitive ingredients (such as paeony glycosides and atractylodesone), increasing volatile oil retention by over 15%. 12 The vacuum drying stage uses negative pressure to lower the water evaporation temperature, preventing high temperatures from damaging the medicinal material's activity. The final shade drying stage simulates a natural drying environment, ensuring the stability of gingerols from dried ginger and organic acids from raw hawthorn. 12

[0043] 2. Synergistic effect of differentiated ultrafine grinding and plasma activation

[0044] Low-temperature pulverization technology: Atractylodes lancea and dried ginger are pulverized by impact method with liquid nitrogen pre-cooling at -30°C, and the volatile oil retention rate reaches 88%±2% (an increase of 23% compared to room temperature pulverization)13;

[0045] Targeted particle size control: yam / shan pry shear crushing (≤75μm) increases the polysaccharide dissolution rate to 92%±3%, and raw hawthorn 100 mesh crushing increases the release rate of organic acids;

[0046] Plasma activation: 50W argon plasma treatment for 15 minutes enhances the surface activity of the powder and shortens the disintegration time of the pills to 8 minutes (compared to 15 minutes with the traditional process) 1PDF.

[0047] 3. Double-layer sustained-release pill design achieves precise matching

[0048] Immediate-release layer (30% of pill weight): Atractylodes lancea volatile oil nanoemulsion (120 nm) combined with dried ginger extract, which increases the gastric mucosal adhesion area by 3 times and reduces the Helicobacter pylori inhibition MIC value to 0.15 μg / mL (compared to 0.38 μg / mL for conventional emulsion)13;

[0049] Sustained-release layer (70% of pill weight): The yam polysaccharide-calcium alginate gel matrix has a cumulative release rate of 98% in 12 hours under gastric acid environment, continuously repairing gastric tissue damage;

[0050] pH-sensitive enteric coating: Acrylic resin coating increases weight by 8%, ensuring precise drug release in the alkaline environment of the intestine, preventing gastric acid from destroying the active ingredients, and storage stability deviation ≤2.1%6.

[0051] 4. Multimodal sterilization ensures microbial safety

[0052] The combined application of 2400MHz microwave pretreatment (55℃ temperature control) + ozone dynamic penetration + ultraviolet surface disinfection has a microbial limit of <100CFU / g, which is 40% more efficient than a single sterilization method and avoids high-temperature carbonization of honey adhesive3. DETAILED DESCRIPTION

[0053] In order to make the objects and advantages of the present invention more clearly understood, the present invention is further described below in conjunction with embodiments; it should be understood that the specific embodiments described herein are merely used to explain the present invention and are not intended to limit the present invention.

[0054] The preferred embodiments of the present invention are described below. It should be understood by those skilled in the art that these embodiments are only used to explain the technical principles of the present invention and are not intended to limit the scope of protection of the present invention.

[0055] 1. Raw material pretreatment process optimization description

[0056] Advantages of three-stage drying

[0057] Initial dehumidification (50°C hot air drying): A gradient heating strategy is used to prevent high temperatures from causing starch gelatinization in the Chinese yam. The hot air circulation design ensures uniform heating of the medicinal material. When the moisture content drops to 12%, a porous structure is formed, facilitating the release of active ingredients during subsequent pulverization.

[0058] Mid-stage setting (vacuum drying at 30°C): The boiling point of water is lowered under vacuum, reducing the loss of heat-sensitive components such as white paeony glycosides and atractylodesone (compared with conventional 60°C drying, the volatile oil retention rate is increased by more than 15%).

[0059] Terminal stability (shade drying at 15°C): Simulates a natural shade drying environment to avoid the oxidative decomposition of gingerol in dried ginger, while maintaining the stability of organic acids in raw hawthorn, in line with the Chinese Pharmacopoeia's regulations on the drying endpoint of rhizomes.

[0060] Innovations in ultrafine grinding technology

[0061] Differentiated crushing strategy:

[0062] The yam / shanqiao grinder adopts shearing crushing (2800rpm): the high speed shear force destroys the fiber structure, so that the dissolution rate of yam polysaccharides is increased to 92%±3%, which is higher than the traditional grinding method (75%±5%).

[0063] Liquid nitrogen pre-cooling and grinding of Atractylodes lancea / dried ginger (-30℃): Low temperature inhibits the volatilization of volatile oil. GC-MS detection shows that the retention rate of Atractylodes lancea volatile oil reaches 87.5%, which is 23% higher than that of grinding at room temperature.

[0064] White peony root is crushed into 20 mesh: it retains the sustained-release carrier structure of paeoniflorin; raw hawthorn is crushed into 100 mesh to increase the specific surface area and promote the rapid dissolution of organic acid.

[0065] Plasma activation treatment: Argon plasma generates hydroxyl radicals on the surface of the powder, which enhances the binding force with the honey adhesive and shortens the pill disintegration time to 8 minutes (15 minutes with the traditional process).

[0066] 2. Scientific Basis for Drug Formulation Design

[0067] Rationality of the structure of double-layer sustained-release pills

[0068] Immediate-release layer (30% of pellet weight):

[0069] Atractylodes lancea volatile oil nanoemulsion (120nm): Nanoparticle size increases the gastric mucosal adhesion area. In vitro antibacterial experiments show that the MIC value against Helicobacter pylori is reduced to 0.15μg / mL (the ordinary emulsion is 0.38μg / mL).

[0070] Dried ginger extract (6-gingerol ≥8%): synergistically exerts local antibacterial effects on the gastric mucosa with atractylodes oil, reducing the damage of gastric acid to drugs.

[0071] Sustained-release layer (70% of pellet weight):

[0072] Chinese yam polysaccharide-calcium alginate gel: slowly swells in a gastric fluid pH 1.2 environment, with a cumulative release rate of 98% in 12 hours, achieving a continuous supply of gastric tissue repair components.

[0073] Necessity of enteric coating

[0074] Acrylic resin (EUDRAGIT L100-55) dissolves at a pH ≥ 5.5, ensuring precise drug release in the duodenum and preventing gastric acid from damaging the polysaccharide structure of Chinese yam. Accelerated testing showed that at an 8% coating weight gain, drug dissolution deviation was ≤ 2.1% over a six-month storage period.

[0075] 3. Key points for controlling key process parameters

[0076] Mixing and homogenization stage

[0077] The dual motion mixer adopts three-dimensional motion + forced shear mode, and the uniformity of RSD≤2.5% ensures that the difference in drug content per pill is less than 5% (Pharmacopoeia requirement is less than 10%).

[0078] Three cycles of air vortex homogenization: the first cycle removes particles with a diameter of >150 μm, and the second cycle adjusts the bulk density to 0.45 g / cm 3 , three times to eliminate the agglomeration caused by electrostatic adsorption.

[0079] Advantages of sterilization process combination

[0080] Microwave pretreatment (2400MHz): Selectively heats water molecules, killing >99.9% of heat-resistant spores and preventing carbonization of honey caused by high temperatures.

[0081] Ozone + UV combination: Ozone penetrates the gaps between powders to kill internal microorganisms, while UV rays treat residual bacteria on the surface. The final microbial limit is <100 CFU / g (enterprise internal control standard).

[0082] 4. Additional Notes

[0083] Raw material quality control

[0084] The allantoin content of Chinese yam needs to be tested (≥0.25%), the white peony root should use the first-class product produced in Bozhou with ≥3.5% paeoniflorin, and the atractylodes lancea needs to be identified by TLC atractylodes ketone spot colorimetric reaction.

[0085] Production environment requirements

[0086] The humidity in the ultrafine grinding workshop is controlled at 40%±5% to prevent the drug powder from absorbing moisture and agglomerating; the enteric coating operation room needs to maintain a constant temperature of 25℃ to avoid fluctuations in the viscosity of the resin solution.

[0087] Storage conditions

[0088] Double-layer aluminum-plastic blister packaging with built-in silica gel desiccant (moisture content indicator card). The recommended long-term storage temperature is ≤25°C and humidity ≤60%. Accelerated testing shows no significant degradation during the 36-month shelf life.

[0089] Example 2:

[0090] Rationality of ratio adjustment

[0091] 55 parts of Chinese yam: reduces the polysaccharide content to the median value to avoid high viscosity affecting the disintegration of pills. It is suitable for patients with excessive gastric acid secretion.

[0092] 15 parts of dried ginger: reduces the stimulation of gingerol and is combined with liquid maltitol moisture barrier, making it more suitable for erosive gastric mucosal inflammation 2PDF.

[0093] Process fine-tuning verification data

[0094] When the shearing crushing speed is 2500rpm, the particle size distribution of Chinese yam is D90=68μm, and the dissolution rate is increased by 7% compared with 3000rpm (because excessive crushing leads to increased surface energy of particles, which is not conducive to dispersion).

[0095] When the ozone sterilization time is shortened to 25 minutes, the UV dose needs to be increased to 45mJ / cm 2 Otherwise, the mold detection rate will rise to 0.3% (exceeding the upper limit of 0.1%).

[0096] Thus far, the technical solutions of the present invention have been described in conjunction with preferred embodiments. However, it will be readily understood by those skilled in the art that the scope of protection of the present invention is clearly not limited to these specific embodiments. Without departing from the principles of the present invention, those skilled in the art may make equivalent changes or substitutions to the relevant technical features, and the technical solutions after such changes or substitutions will fall within the scope of protection of the present invention.

Claims

1. A gastric anti-inflammatory and bactericidal composition, characterized in that: The raw materials include: 50-70 parts of Chinese yam, 25-35 parts of white peony root, 25-35 parts of atractylodes, 10-20 parts of dried ginger, 10-20 parts of gypsophila, and 10-20 parts of raw hawthorn.

2. The anti-inflammatory and bactericidal composition for the stomach according to claim 1, characterized in that: The raw materials include: 55-65 parts of Chinese yam, 26-30 parts of white peony root, 30-35 parts of atractylodes, 15-20 parts of dried ginger, 15-20 parts of gypsophila, and 15-20 parts of raw hawthorn.

3. A method for preparing a gastric anti-inflammatory and bactericidal composition, characterized in that: include:

1. Raw material pretreatment: (1) Initial dehumidification: hot air circulation drying at 40℃-55℃ for 2 hours to remove moisture and make the moisture content of medicinal materials ≤15%; (2) Middle section shaping: vacuum drying at 30°C (-0.08MPa) for 3-4 hours to prevent thermal decomposition of the active ingredients of the medicinal materials; (3) Final stage stability: Dry in a cool, ventilated place at 10-20°C until the moisture content is ≤8%; 2. Ultrafine grinding: (1) Differentiated pulverization: Chinese yam and diatom are pulverized by shearing mill, with the particle size controlled to ≤75μm; Atractylodes and dried ginger are pulverized by impact mill with liquid nitrogen pre-cooling; White peony root and raw hawthorn are pulverized by hammer mill, with white peony root 20 mesh and raw hawthorn 100 mesh; (2) Powder activation treatment: The mixed powder was placed in a plasma treatment device for powder activation treatment for 15 minutes; 3. Mixing process: The medicinal material powder was added during the main mixing stage, and the dual-motion mixer was run for 45 minutes; Homogenization stage: 3 cycles of air vortex homogenizer, the final mixing uniformity RSD ≤ 2.5%; 4. Molding process: (1) Adhesive: Core adhesive layer: Use honey, the addition amount is 25% of the total weight of the medicinal materials, melted at 60℃ and sprayed into powder through a high-pressure nozzle (0.4MPa); Surface modification layer: liquid maltitol is sprayed on the surface with an addition amount of 3% to form a moisture-proof protective film. (2) Double-layer sustained-release pills: The immediate-release layer contains nanoemulsion of Atractylodes lancea essential oil and dried ginger extract, accounting for 30% of the pill weight; Sustained-release layer: using yam polysaccharide-calcium alginate gel skeleton, accounting for 70% of the pill weight; (3) Enteric coating: Fluidized bed coating was performed using pH-sensitive acrylic resin, with a coating weight gain of 8%; 4. Combined sterilization (1) Microwave pretreatment: 2000MHz-2600MHz microwave irradiation for 5 minutes, the material temperature is controlled at 55℃; Ozone dynamic sterilization: ozone is introduced into the closed conveyor belt for 30 minutes; UV sterilization, contact time 30 minutes.

4. The method according to claim 3, characterized in that The shearing pulverizer has a rotation speed of 2500 rpm-3000 rpm.

5. The method according to claim 3, characterized in that The atractylodes lancea and dried ginger are crushed by impact method with liquid nitrogen pre-cooling, and the temperature is set to -30°C, and the volatile oil retention rate is increased to 88%±2%.

6. The method according to claim 3, characterized in that The plasma processing equipment has a power of 50W and uses argon gas.

7. The method according to claim 3, characterized in that The particle size of the Atractylodes lancea volatile oil nanoemulsion is 120 nm.

8. The gastric anti-inflammatory and bactericidal composition according to any one of claims 1 to 7 is used for anti-inflammatory and bactericidal purposes and gastric tissue repair during preparation.