CN115581713B - Chinese buckeye extract colon-specific sustained-release pellets and preparation method thereof - Google Patents

Chinese buckeye extract colon-specific sustained-release pellets and preparation method thereof Download PDF

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CN115581713B
CN115581713B CN202211303070.5A CN202211303070A CN115581713B CN 115581713 B CN115581713 B CN 115581713B CN 202211303070 A CN202211303070 A CN 202211303070A CN 115581713 B CN115581713 B CN 115581713B
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pill
core
colon
extract
release
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CN115581713A (en
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施川
殷文佳
黄丽华
关小羽
刘华侨
张明
许攀
刘享平
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Hubei Lishizhen Pharmaceutical Research Co ltd
Wuhan Aimin Pharmaceutical Co ltd
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Hubei Lishizhen Pharmaceutical Research Co ltd
Wuhan Aimin Pharmaceutical Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

The invention discloses a semen aesculi extract colon-specific sustained-release pellet, which consists of a pill carrying core, an isolating layer and an enteric layer, wherein the pill carrying core comprises a blank pill core, a semen aesculi extract coated on the surface of the blank pill core and an adhesive for coating medicines; the isolating layer comprises a film forming agent, a lubricant and a targeting accelerator; the enteric layer comprises Eudragit S100, eudragit L100-55, plasticizer and anti-sticking agent. The pellets prepared by the invention can be targeted to colon release, have the characteristic of slow release, can enable the blood concentration to be more stable, reduce peak-valley fluctuation and administration frequency, improve patient compliance and are expected to play a better role in the disease treatment of colon lesions.

Description

Chinese buckeye extract colon-specific sustained-release pellets and preparation method thereof
Technical Field
The invention belongs to the field of pharmaceutical preparations, and in particular relates to a semen aesculi extract colon-specific sustained-release pellet and a preparation method thereof.
Background
The semen Aesculi is dry mature seed of Aesculus hippocastanum (Aesculus chinensis Bge.), aesculus thunbergii (Aesculus Chinensis Bge. Var. Chekiangensis (Hu et Fang) or Aesculus chinensis (Aesculus Wilso-nii Red.), and the main active ingredient is aescin, which is divided into beta configuration and alpha configuration, and has antiinflammatory, exudation preventing, cerebral edema preventing, and venous tension increasing effects. At present, the preparation is mainly applied to clinic in the form of beta-aescine sodium salt, and forms such as aescine sodium freeze-dried powder injection, aescine sodium liniment, compound aescine sodium gel, aescine sodium tablet and the like have been developed. The semen aesculi extract is a primary extract for preparing aescin, contains components such as polysaccharide, alkaloid and the like besides saponin components, and can be further purified to obtain high-purity aescin and be used for preparing aescin sodium.
Because of the short half-life period of the oral aescine, low bioavailability and large gastrointestinal side effects, the applicant has developed enteric sustained-release pellets (CN 106924222A) by utilizing the aescine active ingredient in the early stage, and the pellets are prepared and enteric-coated by using an extrusion spheronization method in the early stage of research, so that the medicament can be released in the intestinal tract to reduce the irritation of the stomach and improve the bioavailability. Because the extrusion spheronization method has higher requirements on equipment and the quality of pellets is not easy to control, the applicant intends to prepare the enteric pellets of the semen aesculi extract by using a mature and commercial blank pellet core and combining a common coating method, but the result is unexpected that the pellets prepared by the method have lower release degree in the gastrointestinal tract and higher release degree in the colon instead. On the basis, the applicant finally realizes the preparation of the buckeye extract colon-specific sustained-release pellets by further improving and exploring the preparation process.
Considering that the colon-specific drug delivery system (oral colon specific dury delivery system, ocdds) can reduce the side effects of the drug on the gastrointestinal tract and improve the bioavailability of the drug absorbed at the colon part, the method is particularly suitable for treating colon lesions (such as ulcerative colitis and colon cancer), and the pharmacological activity of aescine can be related to the treatment of colon lesions, and the application of the aescine in treating ulcerative colitis is reported in the prior literature, such as CN 111939166 a. Therefore, the colon-specific sustained-release pellets prepared by the invention are expected to play a better role in the treatment of diseases of colon lesions.
Disclosure of Invention
The invention aims to provide a semen aesculi extract colon-specific sustained-release pellet and a preparation method thereof. To solve the problems in the prior art.
The above purpose is achieved by the following technical scheme:
a semen Aesculi extract colon-specific sustained-release pellet comprises a pill-carrying core, an isolation layer, and an enteric layer, wherein,
pill carrying core: comprises a blank pill core, semen aesculi extract coated on the surface of the blank pill core and an adhesive for coating medicines;
isolation layer: the drug-loaded pill consists of a film forming agent, a lubricant and a targeting accelerator, wherein the film forming agent accounts for 10-30% of the mass of the drug-loaded pill core; the lubricant accounts for 0.5-1.5% of the weight of the pill-carrying core; the targeted accelerator accounts for 5-12% of the mass of the pill carrying core;
enteric layer: consists of Eudragit S100, eudragit L100-55, plasticizer and anti-adhesion agent, wherein the enteric layer accounts for 40-60% of the sum of the mass of the pill-carrying core and the isolation layer,
the targeting accelerator is amylose and/or glucan; the semen Aesculi extract contains 60-80% total saponins.
Further, the blank pill core is a sucrose pill core, a microcrystalline cellulose pill core, a starch pill core or a lactose pill core. In the test, microcrystalline cellulose is less prone to degradation in the gastrointestinal tract compared with sucrose, starch and lactose, has stable property, can reduce the release of drugs in the gastrointestinal tract and enable the drugs to enter the colon more, and therefore the microcrystalline cellulose pellet core is further preferred.
Further, the adhesive is cellulose ether derivatives or polyvinylpyrrolidone, and the adhesive accounts for 1-5% of the mass of the blank pill core. The cellulose ether derivatives include, but are not limited to, methylcellulose, carboxymethylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethyl cellulose, and the like.
Further, the film forming agent is selected from one or more of carrageenan, guar gum, gelatin, acacia, chitosan and trehalose. These materials have good stability in the gastrointestinal tract and degrade well under the digestive conditions of the colon, thus facilitating colonic release of the drug.
Further, the plasticizer is triethyl citrate and/or tween 80.
Further, the lubricant is talcum powder or micro silica gel.
The invention further provides a method for preparing the buckeye extract colon-specific sustained-release pellets, which comprises the following steps:
s1: placing the blank pill core in a fluidized bed bottom spray coating device, dissolving the adhesive and the semen aesculi extract with a solvent, spraying and loading to prepare a pill-carrying core;
s2: placing the pill-carrying core in a fluidized bed bottom spray coating device, dissolving and uniformly mixing a film forming agent, a lubricant and a targeting accelerator with a solvent, and then spraying and coating to prepare an isolated layer pill-carrying core;
s3: the isolating layer pill-carrying core is placed in a fluidized bed bottom spray coating device, and the Eudragit S100, eudragit L100-55, plasticizer and anti-adhesion agent are dissolved by solvent and then spray coated.
Preferably, the spraying parameters are that the atomizing pressure is 1.5-2.0bar, the material temperature is 30-60 ℃ and the air quantity is 25-35m 3 /h。
The beneficial effects of the invention are as follows:
according to the invention, the pellets are prepared by using materials which are stable in the gastrointestinal tract and can be fully degraded in the colon, and simultaneously, the targeting accelerator is used, and the dosage of each raw material is grossly optimized, so that the colon-specific administration of the semen aesculi extract is finally realized, wherein amylose and glucan can resist the degradation of digestive enzymes and bacteria in the gastrointestinal tract, and can be digested and absorbed by colonic enzymes and bacteria, and the targeting accelerator has a certain colon targeting promoting effect.
The pellets prepared by the invention can not only target colon release, but also have slow release characteristics because the colon release accords with the first-order equation, so that the blood concentration is more stable, the peak-valley fluctuation and the administration frequency are reduced, and the patient compliance is improved. The invention also has the advantages of long drug release period, high accumulated release degree and the like.
Compared with the existing extrusion spheronization method, the method has the advantages of stable property, controllable quality, high yield (more than 95%), short production period, low cost and the like.
The micropill prepared by the invention is expected to play a better role in the treatment of diseases of colon lesions (such as ulcerative colitis).
Drawings
Fig. 1: graph of particle size distribution of pellets.
Fig. 2: micropellet surface and cross-sectional micrograph.
Fig. 3: in vitro release profile of pellets (example 1).
Fig. 4: in vitro release profile of pellets (example 2).
Fig. 5: in vitro release profile of pellets (example 3).
Fig. 6: in vitro release profile of pellets (example 4).
Fig. 7: in vitro release profile of pellets (comparative).
Detailed Description
The present invention will be described in detail with reference to specific examples.
Key raw materials and instruments: buckeye extract (lot 211001, purity of total saponins 76%, pharmaceutical stock company of martial arts); sodium aescinate control (lot number 100376-2017.3, purity 96.9%, national food and drug verification institute); blank pill core (Anhui mountain river pharmaceutic adjuvant Co., ltd.).
Agilent 1260 type high performance liquid chromatograph (Agilent corporation, USA); XSE 205DU electronic balance [ mertrel-tolidox instruments (Shanghai) limited ]; easy Diss-T×8 type elution apparatus (RIG GTEK); FE28-standard pH meter (Sichuan Donghua measuring and detecting technology Co., ltd.); FLZB-1.5 bottom spouted bed (Shanghai Co., ltd. For developing the technology of the Critical machine); MYP2011-100 electric stirrer (Shanghai Mei Ying Hunan instruments and meters Co., ltd.).
EXAMPLE 1 preparation of colon-specific sustained-release pellets of semen Aesculi extract
1. Preparation of pill-carrying cores
Raw and auxiliary materials Action Dosage of
Microcrystalline cellulose pill core Blank pill core 100g
HPC-EF Adhesive agent 2.5g
Semen aesculi extract Active ingredient 12g
60% ethanol Solvent(s) 200ml
Placing microcrystalline cellulose pill core in fluidized bed bottom spray coating device, dissolving HPC-EF and semen Aesculi extract in 60% ethanol until it is clear, and spraying for application. The spraying parameters are as follows: atomization pressure is 1.5bar, material temperature is 40-45 ℃ and air quantity is 25m 3 And/h. Drying after spraying, discharging, and sieving the micropill with 40-60 mesh sieve to obtain the pill-carrying core.
2. Micropill coating process
(1) Isolation layer coating
Raw and auxiliary materials Action Dosage of
Pill carrying core —— 100g
Guar gum Film forming agent 15g
Talc powder Lubricant 0.7g
Amylose starch Targeting accelerators 8g
Dextran Targeting accelerators 2.5g
Purified water Solvent(s) 300ml
Placing the pill-carrying core into a fluidized bed bottom spray coating device, dissolving guar gum, talcum powder, amylose and dextran into purified water, and spraying liquid for coating. The coating parameters are atomization pressure 1.8bar, material temperature 55-60 ℃, air quantity 28m 3 And/h. Discharging after spraying, and sieving the micropill with 40-60 mesh sieve to obtain the isolating layer pill-carrying core.
(2) Enteric coating
Raw and auxiliary materials Action Dosage of
Pill carrying core with isolation layer —— 100g
Eudragit S100 Coating agent 35g
Eudragit L100-55 Coating agent 6.5g
Citric acid triethyl ester Plasticizer(s) 3.3g
Tween 80 Plasticizer(s) 0.3g
Glycerol monostearate Anti-sticking agent 0.6g
Water and its preparation method Solvent(s) 70ml
Placing the pill-carrying core of the isolation layer in a fluidized bed bottom spray coating device, dissolving Eudragit S100, eudragit L100-55, triethyl citrate, tween 80 and glycerol monostearate with water to obtain coating liquid, and spraying liquid for coating. The coating parameters are atomization pressure 1.8bar, material temperature 30-35 ℃, air quantity 35m 3 And/h. Drying and discharging after spraying the liquid, and sieving the pellets with a 20-40 mesh sieve.
Test examples
1. Particle size
Detecting particle size by a laser particle size analyzer, wherein the set parameters are as follows: the light shielding degree is 0.26%, the refractive index of the particles is 1.500, the absorptivity is 0.1, the obtained particle size distribution curve is in normal distribution (figure 1), and d (0.1), d (0.5) and d (0.9) are 539.34um, 664.749 and 921.826 respectively.
2. Scanning electron microscopy image (SEM) morphology analysis
The surface and cross section of the pellets were observed using a Scanning Electron Microscope (SEM). The results show that: the microsphere is solid sphere, the surface is compact and smooth, and the medicine carrying layer, the isolation layer and the enteric layer can be clearly distinguished by the fracture surface (figure 2).
3. Drug release performance detection
Taking 0.1mol/L hydrochloric acid solution, pH6.8 phosphate buffer solution and pH7.6 phosphate buffer solution as dissolution media, simulating in vivo digestive tract conditions, and examining the dissolution performance of the medicine by detecting the total saponin content. Referring to the second method of the second appendix XD of Chinese pharmacopoeia, hydrochloric acid solution is taken as a dissolution medium, phosphate buffer with pH value of 6.8 is replaced after 2 hours, and phosphate buffer with pH value of 7.6 is replaced after 6 hours. The rotating speed is 100r/min, the temperature is 37+/-0.5 ℃, 5mL of solution is taken at regular time, 0.45 mu m is filtered, 5mL of dissolution medium is added, the content of total saponins is measured by an HPLC method, the total saponins are measured every 1h, and the cumulative release degree is calculated according to the measurement result.
Chromatographic conditions: agilent ZORBAX SB-C18 chromatographic column (250 mm. Times.4.6 mm,5 μm); the mobile phase is acetonitrile-0.2% phosphoric acid (40:60, v/v); the flow rate is 1.0mL/min; the column temperature is 30 ℃; the detection wavelength is 220nm; the sample loading was 20. Mu.l. The total saponin peak area is represented by aescin A, B, C, D peak area, and the total saponin content is calculated according to an external standard method.
The prepared pellets have cumulative release rates of 0.85% and 1.73% in simulated gastric fluid (2 h) and intestinal fluid (4 h) respectively, and a cumulative release rate of 91.50% in simulated intestinal fluid for 6h and a drug release after 5h approaching the peak (figure 3), which indicates that the majority of the drug is released in the colon.
And the fitting analysis is carried out on the release curve in the simulated colon, the fitting effect of the zero-order equation and the Higuchi equation is poor, the first-order equation R2 is 0.99911, and the fitting effect is good. Therefore, the in-vitro drug release rule of the pellets prepared by the invention accords with a first-order equation, and the result shows that the release of the pellets in the colon has the slow release characteristic.
EXAMPLE 2 preparation of colon-specific sustained-release pellets of semen Aesculi extract
1. Preparation of pill-carrying cores
Raw and auxiliary materials Action Dosage of
Sucrose pill core Blank pill core 100g
HPC-EF Adhesive agent 3g
Semen aesculi extract Active ingredient 12g
60% ethanol Solvent(s) 300ml
Placing sucrose pill core in fluidized bed bottom spray coating device, dissolving HPC-EF and semen Aesculi extract in 60% ethanol until it is clear, and spraying for application.
2. Micropill coating process
(1) Isolation layer
Raw and auxiliary materials Action Dosage of
Pill carrying core —— 100g
Gelatin Film forming agent 25g
Micro powder silica gel Lubricant 0.5g
Amylose starch Targeting accelerators 8g
Purified water Solvent(s) 450ml
Placing the pill-carrying core into a fluidized bed bottom spray coating device, dissolving gelatin, aerosil and amylose into purified water, spraying liquid and coating.
(2) Enteric layer
Placing the pill-carrying core of the isolation layer in a fluidized bed bottom spray coating device, dissolving Eudragit S100, eudragit L100-55, triethyl citrate and glycerol monostearate with water to obtain coating liquid, and spraying liquid for coating.
The pellets prepared had cumulative release levels of 1.17% in simulated gastric fluid (2 h) and 3.55% in intestinal fluid (4 h), respectively, 85.65% in simulated colon and near peak after 3h (fig. 4).
EXAMPLE 3 preparation of colon-specific sustained-release pellets of semen Aesculi extract
1. Preparation of pill-carrying cores
Raw and auxiliary materials Action Dosage of
Starch pellet core Blank pill core 100g
PVP K90 Adhesive agent 1.5g
Semen aesculi extract Active ingredient 12g
60% ethanol Solvent(s) 200ml
Placing starch pellet core into fluidized bed bottom spray coating device, dissolving PVP K90 and semen Aesculi extract into 60% ethanol until it is clear, and spraying for application.
2. Micropill coating process
(1) Isolation layer
Raw and auxiliary materials Action Dosage of
Pill carrying core —— 100g
Trehalose Film forming agent 20g
Talc powder Lubricant 1.1g
Dextran Targeting accelerators 5g
Purified water Solvent(s) 300ml
Placing the pill-carrying core in a fluidized bed bottom spray coating device, dissolving trehalose, talcum powder and dextran into purified water, and spraying liquid for coating.
(2) Enteric layer
Raw and auxiliary materials Action Dosage of
Pill carrying core with isolation layer —— 100g
Eudragit S100 Coating agent 26g
Eudragit L100-55 Coating agent 12.5g
Citric acid triethyl ester Plasticizer(s) 3.5g
Tween 80 Plasticizer(s) 0.6g
Glycerol monostearate Anti-sticking agent 0.9g
Water and its preparation method Solvent(s) 50ml
Placing the pill-carrying core of the isolation layer in a fluidized bed bottom spray coating device, dissolving Eudragit S100, eudragit L100-55, triethyl citrate, tween 80 and glycerol monostearate with water to obtain coating liquid, and spraying liquid for coating.
The pellets prepared had cumulative release of 3.37% and 5.13% in simulated gastric fluid (2 h) and intestinal fluid (4 h), respectively, and 6h in simulated colon had cumulative release of 95.15% and after 4h were near peak (fig. 5).
EXAMPLE 4 preparation of colon-specific sustained-release pellets of semen Aesculi extract
1. Preparation of pill-carrying cores
Raw and auxiliary materials Action Dosage of
Lactosucrose pellet core Blank pill core 100g
CMC Adhesive agent 5g
Semen aesculi extract Active ingredient 12g
60% ethanol Solvent(s) 350ml
Placing lactose pellet core in fluidized bed bottom spray coating device, dissolving CMC and semen Aesculi extract in 60% ethanol until it is clear, and spraying for application.
2. Micropill coating process
(1) Isolation layer
Placing the pill-carrying core into a fluidized bed bottom spray coating device, dissolving chitosan, talcum powder, amylose and dextran into purified water, and spraying liquid for coating.
(2) Enteric layer
Raw and auxiliary materials Action Dosage of
Pill carrying core with isolation layer —— 100g
Eudragit S100 Coating agent 30g
Uttky L100-55 Coating agent 6g
Citric acid triethyl ester Plasticizer(s) 3.3g
Tween 80 Plasticizer(s) 0.5g
Glycerol monostearate Anti-sticking agent 1.2g
Water and its preparation method Solvent(s) 50ml
Placing the pill-carrying core of the isolation layer in a fluidized bed bottom spray coating device, dissolving Eudragit S100, eudragit L100-55, triethyl citrate, tween 80 and glycerol monostearate with water to obtain coating liquid, and spraying liquid for coating.
The prepared pellets had cumulative release of 0.57% and 6.81% in simulated gastric fluid (2 h) and intestinal fluid (4 h), respectively, and 89.23% in simulated colon for 6h (fig. 6).
Comparative example enteric micropill was prepared according to the conventional method
1. Preparation of pill-carrying cores
Placing sucrose pill core in fluidized bed bottom spray coating device, dissolving CMC and semen Aesculi extract in 60% ethanol until it is clear, and spraying for application.
2. Micropill coating process
(1) Isolation layer
Raw and auxiliary materials Action Dosage of
Pill carrying core —— 100g
HPLC Film forming agent 25g
Purified water Solvent(s) 400ml
The pellet-carrying cores were placed in a fluid bed bottom spray coating apparatus, HPLC was dissolved in purified water, and spray coated.
(2) Enteric layer
Raw and auxiliary materials Action Dosage of
Pill carrying core with isolation layer —— 100g
Eudragit L100-55 Coating agent 45g
Citric acid triethyl ester Plasticizer(s) 3.3g
Glycerol monostearate Anti-sticking agent 0.6g
Purified water Solvent(s) 50ml
The pill-carrying core of the isolation layer is placed in a fluidized bed bottom spray coating device, and the Eudragit L100-55, triethyl citrate and glycerol monostearate are dissolved with water to prepare coating liquid, and the coating liquid is sprayed for coating.
The pellets prepared had cumulative release of 2.56% and 30.51% in simulated gastric fluid (2 h) and intestinal fluid (4 h), respectively, and 75.65% in 6h in simulated colon (fig. 7). The release amount of the drug in the intestinal tract is small, and a large amount of drug is released after entering intestinal juice.

Claims (8)

1. A colon-specific sustained-release pellet of semen Aesculi extract comprises a pill-carrying core, an isolation layer and an enteric layer, and is characterized in that,
pill carrying core: comprises a blank pill core, semen aesculi extract coated on the surface of the blank pill core and an adhesive for coating medicines;
isolation layer: the drug-loaded pill consists of a film forming agent, a lubricant and a targeting accelerator, wherein the film forming agent accounts for 10-30% of the mass of the drug-loaded pill core; the lubricant accounts for 0.5-1.5% of the weight of the pill-carrying core; the targeted accelerator accounts for 5-12% of the mass of the pill carrying core;
enteric layer: consists of Eudragit S100, eudragit L100-55, plasticizer and anti-adhesion agent, wherein the enteric layer accounts for 40-60% of the sum of the mass of the pill-carrying core and the isolation layer,
the targeting accelerator is amylose and/or glucan; the semen Aesculi extract contains 60-80% total saponins.
2. The buckeye extract colon-specific sustained-release pellet of claim 1, wherein: the blank pill core is sucrose pill core, microcrystalline cellulose pill core, starch pill core or lactose pill core.
3. The buckeye extract colon-specific sustained-release pellet of claim 1, wherein: the adhesive is cellulose ether derivatives or polyvinylpyrrolidone, and accounts for 1-5% of the mass of the blank pill core.
4. The buckeye extract colon-specific sustained-release pellet of claim 1, wherein: the film forming agent is selected from one or more of carrageenan, guar gum, gelatin, acacia, chitosan and trehalose.
5. The buckeye extract colon-specific sustained-release pellet of claim 1, wherein: the plasticizer is triethyl citrate and/or tween 80.
6. The buckeye extract colon-specific sustained-release pellet of claim 1, wherein: the lubricant is talcum powder or micro silica gel.
7. A method for preparing the buckeye extract colon-specific sustained-release pellets according to any one of claims 1 to 6, characterized by comprising the following steps:
s1: placing the blank pill core in a fluidized bed bottom spray coating device, dissolving the adhesive and the semen aesculi extract with a solvent, spraying and loading to prepare a pill-carrying core;
s2: placing the pill-carrying core in a fluidized bed bottom spray coating device, dissolving and uniformly mixing a film forming agent, a lubricant and a targeting accelerator with a solvent, and then spraying and coating to prepare an isolated layer pill-carrying core;
s3: the isolating layer pill-carrying core is placed in a fluidized bed bottom spray coating device, and the Eudragit S100, eudragit L100-55, plasticizer and anti-adhesion agent are dissolved by solvent and then spray coated.
8. The method for preparing the colon-specific sustained-release pellets of semen aesculi extract according to claim 7, which is characterized in that: the spraying parameters are that the atomization pressure is 1.5-2.0bar, the material temperature is 30-60 ℃ and the air quantity is 25-35m 3 /h。
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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113527379A (en) * 2021-08-19 2021-10-22 海南师范大学 Method for extracting, separating and purifying aescine from semen Veronicae

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