CN113679749A - Preparation method of plant extract self-microemulsion sustained-release antibacterial anti-inflammatory buccal tablets - Google Patents
Preparation method of plant extract self-microemulsion sustained-release antibacterial anti-inflammatory buccal tablets Download PDFInfo
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Abstract
The invention discloses a preparation method of a plant extract self-microemulsion sustained-release bacteriostatic and anti-inflammatory buccal tablet, which is a preparation method of a chicory extract self-microemulsion buccal tablet based on rhamnolipid as an emulsifier; relates to the field of food processing and medicine production. The preparation process comprises the preparation of chicory extract, the preparation of self-microemulsion base system, the preparation of chicory extract self-microemulsion and the preparation of chicory extract self-microemulsion sustained-release buccal tablet; uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighting the filling agent, the adhesive and the flavoring agent in a grinder according to the dosage of the formula. The chicory extract self-microemulsion sustained-release buccal tablets prepared by the method and taking rhamnolipid as an emulsifier meet the quality standard of tablets in Chinese pharmacopoeia. Compared with self-microemulsion, the buccal tablet has better slow release effect and more lasting curative effect, and shows good bacteriostatic effect on escherichia coli and staphylococcus aureus. The product is stored for 12 months at room temperature, and all indexes are not changed obviously.
Description
Field of the method
The invention relates to a preparation method of a sustained-release antibacterial and anti-inflammatory buccal tablet, in particular to a preparation method of a plant extract self-microemulsion sustained-release buccal tablet which takes rhamnolipid as an emulsifier and has antibacterial and anti-inflammatory effects.
Background method
Buccal tablet is a pressed tablet slowly dissolved in oral cavity, can produce lasting drug effect on oral cavity and pharynx, and can be used for local inflammation diminishing and disinfection. In recent years, with implementation of strategic health planning in China and requirements of people on food functionality and novelty, the buccal tablet is also applied more and more in the field of food processing. The existing buccal tablets generally have the problem of short action time of the effective components after being dissolved, are not beneficial to the long-time retention of the effective components in the medicines or functional foods in the oral cavity and influence the functions of bacteriostasis, inflammation diminishing, mouth cleaning and the like. The self-microemulsion buccal tablet is adopted, so that the problem of slow release of effective components in the buccal tablet is well solved, the effective components can be slowly dissolved out in the oral cavity, and the buccal tablet can play a role for a long time. In addition, the self-microemulsion is more convenient to carry after being solidified in the form of buccal tablets.
The key factor influencing the quality of the self-microemulsion buccal tablet is the components of the self-microemulsion, which not only influences the efficacy of the product, but also influences the stability and the sustained release of the product. The key to influence the stability and sustained release of the self-microemulsion is the choice of emulsifier.
At present, the self-microemulsion is mainly used for medicine production, the used emulsifier is mainly a chemically synthesized emulsifier such as Tween 80, and the using dosage and the using range of the chemically synthesized emulsifier are limited in food production. The rhamnolipid is used as a green biosurfactant, has good emulsifying activity, and has a wider application range and higher acceptance of people. In addition, the rhamnolipid also has pharmacological actions such as antibiosis, tumor resistance, oxidation resistance and the like, and can be used as an emulsifier and a bioactive component to play double roles when a drug-loading self-microemulsion system is constructed.
The chicory contains active ingredients such as chicoric acid, chlorogenic acid, polysaccharide and the like, has biological activities of resisting bacteria and inflammation, promoting wound healing and the like, and is beneficial to the oral health of people when being used for preparing the buccal tablets. However, the chicory extract has a certain bitter and astringent taste, and the taste of the product needs to be adjusted by using a flavoring agent when the chicory extract is used as a buccal tablet ingredient, so that the chicory extract is accepted by more people.
The oleum Menthae Dementholatum has special refreshing fragrance, and can be used for refreshing, relieving itching, relieving inflammation, relieving pain, protecting liver, promoting gallbladder function, promoting transdermal absorption of various medicines, and relieving oral diseases such as aphtha of the mouth and tongue, sore throat, and toothache.
The chicory extract self-microemulsion buccal tablet takes rhamnolipid as an emulsifier and peppermint oil as an oil phase and a flavoring agent, and the two components can not only play the roles of the emulsifier and the flavoring agent, but also can have the synergistic effect with the chicory extract which is the main active ingredient of the product, so that the bacteriostatic and anti-inflammatory effects of the buccal tablet are better realized. In addition, the method takes the xylitol with good caries prevention property as a sweetening agent and the curcumin with anti-inflammatory and anti-oxidation effects as a coloring agent, so that the quality and the application effect of the buccal tablet can be comprehensively improved.
Disclosure of Invention
The invention aims to provide a preparation method of a self-microemulsion sustained-release bacteriostatic and anti-inflammatory buccal tablet of a plant extract, which is characterized in that a pseudo-ternary phase diagram method is adopted to screen a medicament-carrying self-microemulsion (CE-SMEDDS) system formula of a chicory extract with rhamnolipid as an emulsifier and peppermint oil as an oil phase, and the medicament-carrying self-microemulsion is solidified by utilizing a solid carrier adsorption method, so that the prepared buccal tablet has the advantages that the hardness, friability, buccal cavity dissolution time and the like all meet the quality standard of tablets in Chinese pharmacopoeia, and the chicory extract has a good sustained-release effect and has bacteriostatic, anti-inflammatory and mouth-refreshing effects.
The purpose of the invention is realized by the following scheme:
a preparation method of a plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet comprises the following preparation processes:
(1) preparation of chicory extract: mixing chicory stem powder with 50-70% ethanol solution at a material-liquid ratio of 1:10-25, extracting under oscillation at 30-60 deg.C for 30-60min, vacuum filtering, rotary evaporating the filtrate at below 60 deg.C, drying at low temperature or vacuum freeze drying to obtain dry powder of chicory extract, and sealing for storage. When in use, the chicory extract is dissolved in sterile distilled water, filtered and prepared into an aqueous solution (CE) of the chicory extract with the mass percentage concentration of 40-50 percent
(2) Preparing a self-microemulsion base system: according to the mass ratio of rhamnolipid to tween 80 being 1-4:1, a compound emulsifier EM, a co-emulsifier polyethylene glycol (PEG-400) being 1:1-3, and peppermint oil being 1:2-4 with respect to the total amount of the emulsifier and the co-emulsifier, forming a microemulsion base system;
(3) preparation of chicory extract self-microemulsions (CE-SMEDDS): slowly dripping CE (50% chicory aqueous solution) into the microemulsion base system at a volume ratio (V/V) of 1:2 while stirring (80-150 r/min) until the mixture becomes clear and transparent. The prepared chicory drug-loaded microemulsion shows good stability in a wide acid-base range from pH more than 3 to pH less than 12 after being centrifuged for 10 minutes under the condition of 12000r/min, and the drug-loaded microemulsion has good storage stability, and a mixed system still keeps clear and transparent without layering and flocculation after being placed for 1 year at 4 ℃ and 25 ℃.
(4) The preparation method of the self-microemulsion sustained-release buccal tablet comprises the following steps: according to the formula, the solid adsorption mixture (the mass ratio of microcrystalline cellulose to CE-SMEDDS of the solid adsorbent is 1-2: 1) is 35-45%, hydroxypropyl methylcellulose (HPMC-E5) is 4.5-8.5%, xylitol is 35-45%, curcumin is 0-0.01%, and corn starch is 7-11%.
Sieving adsorbent, binder, filler, correctant and lubricant with 100 mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
The preparation method of the plant extract self-microemulsion sustained-release anti-bacterial and anti-inflammatory buccal tablet comprises the step of preparing the chicory extract from chicory leaves, chicory roots or chicory whole plants.
In the preparation process of the plant extract, ultrasonic treatment or microwave treatment is assisted before, during or after extraction, or an ultrahigh pressure extraction method and other extraction methods are adopted.
The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet comprises the steps of extracting roots, stems, leaves, flowers or whole plants of edible or medicinal plants, or directly preparing the plant extract as a raw material.
The oil phase is peppermint oil, edible vegetable oil, essential oil (such as tea tree essential oil and lemon essential oil) or mixed oil.
The microcrystalline cellulose and the corn starch are substances with the functions of resisting bacteria, embedding and the like, such as methyl-beta-cyclodextrin and deacetylated chitin.
According to the preparation method of the plant extract self-microemulsion sustained-release anti-bacterial and anti-inflammatory buccal tablet, the curcumin is anthocyanin, carotenoid, chlorophyll, sorghum red pigment functional natural pigment or edible artificial synthetic pigment, and the color of the product is changed according to the use or non-use of the pigment and the color of the pigment.
In the preparation method of the plant extract self-microemulsion sustained-release antibacterial anti-inflammatory buccal tablet, the xylitol is sorbitol and erythritol which have low calorie and anti-caries property.
In the preparation method of the plant extract self-microemulsion sustained-release anti-inflammatory buccal tablet, the filler and the adsorbent are common materials for buccal tablets.
The invention has the advantages and effects that:
the invention provides a method for preparing a plant extract self-microemulsion sustained-release buccal tablet based on rhamnolipid as an emulsifier, which is characterized in that various components of the plant extract, the rhamnolipid, an oil phase, an adsorbent, a pigment and the like of the buccal tablet synergistically play antibacterial and anti-inflammatory effects. The product has good surface gloss, fine taste and moderate sweetness, and has the effects of refreshing breath, inhibiting bacteria reproduction in the oral cavity, assisting in eliminating oral inflammation and the like.
The buccal tablets prepared by the method have the weight difference range of-3.3-3.8%, the average hardness of 11.22kg, the friability of 0.36% and buccal cavity buccal time of about 15-18 min, and all meet the quality standard of tablets in Chinese pharmacopoeia. By the detection of dissolution rate by a small cup method, the accumulative release rate of the chicory extract in the CE-SMEDDS preparation and the CE-SMEDDS oral buccal tablet is up to 90% in 15min and 30min respectively, which shows that the oral buccal tablet has better sustained-release effect and more lasting curative effect compared with self-microemulsion. In a filter paper method bacteriostatic activity test, buccal tablet solutions with the concentrations of 0.2, 0.5, 0.8 and 1.0g/mL respectively show good bacteriostatic effects on escherichia coli and staphylococcus aureus. The product is stored for 12 months at room temperature, and all indexes are not changed obviously.
Drawings
FIG. 1 is a photograph of a CE-SMEDDS buccal tablet;
FIG. 2 is a graph showing the bacteriostatic effect of the CE-SMEDDS buccal tablets (mass concentration 1 g/mL) on bacteria;
wherein panel a is a Staphylococcus aureus panel; FIG. b is a diagram of Escherichia coli.
Detailed Description
The present invention will be described in detail with reference to examples.
Example 1
Mixing chicory stem powder with 70% ethanol solution at a mass percentage concentration of 1:20, oscillating and extracting at 50 ℃ for 50min, filtering, performing rotary evaporation on the filtrate at a temperature below 60 ℃, performing vacuum freeze drying to obtain dry powder of chicory extract, and sealing for storage. The application method comprises weighing herba Cichorii extract, dissolving with sterile distilled water, filtering, and making into 50% herba Cichorii extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:1 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1 to prepare a self-microemulsion base system;
slowly dripping CE (chicory aqueous solution) into a microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain a medicament-carrying microemulsion (CE-SMEDDS) of the chicory extract with good stability;
preparing the sustained-release buccal tablets according to a formula (45% of microcrystalline cellulose and CE-SMEDDS mixture Ma (mass ratio of 1: 1), 5% of hydroxypropyl methylcellulose (HPMC-E5), 40% of xylitol, 0.01% of curcumin and 10% of corn starch): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Example 2
Mixing chicory powder and 70% ethanol solution in a material-liquid ratio of 1:25, performing ultrasonic treatment on the mixed solution for 10min at 200W, performing oscillation extraction at 35 ℃ for 60min, performing suction filtration, performing rotary evaporation on the filtrate at below 60 ℃, drying in an oven at 60 ℃ to obtain dry powder of the chicory extract, and performing sealed storage. The application method comprises weighing herba Cichorii extract, dissolving with sterile distilled water, filtering, and making into 50% herba Cichorii extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:1.5 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture, almond oil and tea tree essential oil in a mass ratio of 3:1:0.01, and preparing a self-microemulsion basic system;
slowly dripping CE (chicory aqueous solution) into a microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain a medicament-carrying microemulsion (CE-SMEDDS) of the chicory extract with good stability;
preparing the sustained-release buccal tablets according to a formula (40% of microcrystalline cellulose and CE-SMEDDS mixture Ma (mass ratio of 1: 1), 7.5% of hydroxypropyl methylcellulose (HPMC-E5), 45% of xylitol, 0-0.01% of curcumin and 7.5% of corn starch): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Example 3
Mixing chicory powder with 50% ethanol solution in a mass percentage concentration at a material-liquid ratio of 1:15, performing oscillation extraction at 50 ℃ for 50min, and performing suction filtration; adding 5 times volume of 50% ethanol solution into the residue, and extracting at 50 deg.C for 30min under oscillation; mixing the filtrates, rotary evaporating at 55 deg.C, vacuum freeze drying to obtain dry powder of herba Cichorii extract, and sealing for storage. The application method comprises weighing herba Cichorii extract, dissolving with sterile distilled water, filtering, and making into 45% herba Cichorii extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:2 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1 to prepare a self-microemulsion base system;
slowly dripping CE (chicory aqueous solution) into a microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain a medicament-carrying microemulsion (CE-SMEDDS) of the chicory extract with good stability;
preparing the sustained-release buccal tablets according to a formula (45% of microcrystalline cellulose and CE-SMEDDS mixture Ma (mass ratio of 1: 1), 5% of hydroxypropyl methylcellulose (HPMC-E5), 40% of xylitol, 0.01% of curcumin and 10% of corn starch): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
The embodiments described above describe the basic principles and main features of the present invention, but those skilled in the relevant art will understand that the scope of the present invention is not limited by the above embodiments. The foregoing examples and description have been given for the purpose of illustrating the principles of the present invention and are therefore to be understood as being within the scope of the appended claims. The scope of the invention is defined by the appended claims and equivalents thereof.
Example 4
Mixing chicory stem powder with 70% ethanol solution at a mass percent concentration ratio of 1:20, treating at 400MPa and room temperature for 5min, filtering, rotary evaporating the filtrate at below 60 ℃, freeze-drying under vacuum to obtain dry powder of chicory extract, and sealing for storage. The application method comprises weighing herba Cichorii extract, dissolving with sterile distilled water, filtering, and making into 50% herba Cichorii extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:1 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1 to prepare a self-microemulsion base system;
slowly dripping CE (chicory aqueous solution) into a microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain a medicament-carrying microemulsion (CE-SMEDDS) of the chicory extract with good stability;
preparing the sustained-release buccal tablets according to a formula (microcrystalline cellulose, methyl-beta-cyclodextrin and CE-SMEDDS mixture Ma (the mass ratio is 0.5:0.5: 1) 45%, hydroxypropyl methylcellulose (HPMC-E5) 5%, xylitol 20%, sorbitol 20%, sorghum red pigment 0.001%, corn starch 5% and deacetylated chitin 5%): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and sorghum red pigment, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Example 5
Mixing citronella powder and 70% ethanol solution in a material-liquid ratio of 1:20, treating at 400MPa and room temperature for 5min, and performing suction filtration; adding 5 times of 50% ethanol solution into the filter residue, treating at 300MPa and room temperature for 5min, and filtering; mixing the filtrates, rotary evaporating at 55 deg.C, drying at 60 deg.C to obtain dry powder of herba Cymbopogonis Citrari extract, and sealing for storage. Vacuum freeze drying to obtain dry powder of herba Cymbopogonis Citrari extract, and sealing for storage. The application method comprises weighing herba Cymbopogonis Citrari extract, dissolving with sterile distilled water, filtering, and making into 50% water solution (CE) of herba Cymbopogonis Citrari extract;
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:0.75 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1, and preparing a self-microemulsion base system;
slowly dripping CE (citronella water solution) into a microemulsion base system at a volume ratio (V/V) of 1:2, and stirring while adding until the mixture becomes clear and transparent to obtain a citronella extract drug-loaded microemulsion (CE-SMEDDS) with good stability;
preparing the sustained-release buccal tablets according to a formula (microcrystalline cellulose, methyl-beta-cyclodextrin and CE-SMEDDS mixture Ma (the mass ratio is 0.5:0.5: 1) 45%, hydroxypropyl methylcellulose (HPMC-E5) 5%, xylitol 20%, sorbitol 20%, sodium copper chlorophyllin 0.001%, corn starch 5%, and deacetylated chitin 5%): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and sodium copper chlorophyllin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Example 6
Dissolving green tea or other tea extract with sterile distilled water, filtering, and making into 50% tea extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:0.75 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1, and preparing a self-microemulsion base system;
slowly dripping CE (tea aqueous solution) into the microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain tea extract drug-loaded microemulsion (CE-SMEDDS) with good stability;
preparing the sustained-release buccal tablets according to a formula (microcrystalline cellulose, methyl-beta-cyclodextrin and CE-SMEDDS mixture Ma (the mass ratio is 0.5:0.5: 1) 45%, hydroxypropyl methylcellulose (HPMC-E5) 5%, xylitol 20%, sorbitol 20%, sodium copper chlorophyllin 0.001%, corn starch 5%, and deacetylated chitin 5%): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and sodium copper chlorophyllin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Example 7
Mixing Angelica keiskei powder with 70% ethanol solution at a material-liquid ratio of 1:20, extracting at 50 deg.C under oscillation for 50min, vacuum filtering, rotary evaporating the filtrate at below 60 deg.C, vacuum freeze drying to obtain Angelica keiskei extract dry powder, and sealing for storage. The application method comprises weighing Angelica keiskei Koidz extract, dissolving with sterile distilled water, filtering, and making into 50% Angelica keiskei Koidz extract water solution (CE);
uniformly mixing rhamnolipid and tween 80 in a mass ratio of 1:1 to form a compound Emulsifier (EM), uniformly mixing the EM and polyethylene glycol (PEG-400) in a mass ratio of 1:2, uniformly mixing the mixture and peppermint oil in a mass ratio of 3:1 to prepare a self-microemulsion base system;
slowly dripping CE (water solution of Angelica keiskei Koidz) into the microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent to obtain the microemulsion (CE-SMEDDS) carrying medicine of Angelica keiskei Koidz extract with good stability;
preparing the sustained-release buccal tablets according to a formula (45% of microcrystalline cellulose and CE-SMEDDS mixture Ma (mass ratio of 1: 1), 5% of hydroxypropyl methylcellulose (HPMC-E5), 40% of erythritol, 0.01% of curcumin and 10% of pregelatinized starch): the adsorbent, the adhesive, the filler, the flavoring agent and the lubricant in the formula are respectively ground and sieved by a 100-mesh sieve. Uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting with automatic tabletting machine. And finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
Claims (8)
1. A preparation method of a plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet is characterized by comprising the following preparation processes:
(1) preparation of chicory extract: mixing chicory stem powder with 50-70% ethanol solution at a material-liquid ratio of 1:10-25, extracting under oscillation at 30-60 deg.C for 30-60min, vacuum filtering, rotary evaporating the filtrate at below 60 deg.C, drying at low temperature or vacuum freeze drying to obtain dry powder of chicory extract, and sealing for storage; when in use, the chicory is dissolved in sterile distilled water, filtered and prepared into chicory extract water solution (CE) with the mass percentage concentration of 40-50%;
(2) preparing a self-microemulsion base system: according to the mass ratio of rhamnolipid to tween 80 being 1-4:1, a compound emulsifier EM, a co-emulsifier polyethylene glycol (PEG-400) being 1:1-3, and peppermint oil being 1:2-4 with respect to the total amount of the emulsifier and the co-emulsifier, forming a microemulsion base system;
(3) preparation of chicory extract self-microemulsions (CE-SMEDDS): slowly dripping CE (50% chicory aqueous solution) into the microemulsion base system at a volume ratio (V/V) of 1:2 while stirring until the mixture becomes clear and transparent; the prepared chicory drug-loaded microemulsion shows good stability in a wide acid-base range from pH more than 3 to pH less than 12 after being centrifuged for 10 minutes under the condition of 12000r/min, and the drug-loaded microemulsion has good storage stability, and a mixed system still keeps clear and transparent without layering and flocculation after being placed for 1 year at 4 ℃ and 25 ℃;
(4) the preparation method of the self-microemulsion sustained-release buccal tablet comprises the following steps: according to the formula, 35-45% of a solid adsorption mixture (the mass ratio of microcrystalline cellulose to CE-SMEDDS of a solid adsorbent is 1-2: 1), 4.5-8.5% of hydroxypropyl methylcellulose (HPMC-E5), 35-45% of xylitol, 0-0.01% of curcumin and 7-11% of corn starch are adopted;
sieving adsorbent, adhesive, filler, correctant and lubricant with 100 mesh sieve; uniformly mixing the CE-SMEDDS and an adsorbent to obtain a solid adsorption mixture Ma; weighing the filler, the adhesive and the flavoring agent according to the formula dosage, adding a small amount of Ma into a grinder for multiple times, and uniformly mixing; mixing the above materials, adding magnesium stearate and curcumin, mixing, sieving with 80 mesh sieve, and tabletting; and finally, putting the pressed buccal tablets into an ultraviolet sterilization chamber, sterilizing for 30min, and storing in a sealed lightproof container.
2. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet according to claim 1, wherein the chicory extract is prepared from chicory leaves, chicory roots or chicory whole plants.
3. The method for preparing the plant extract self-microemulsion sustained-release bacteriostatic and anti-inflammatory buccal tablets as claimed in claim 1, wherein in the preparation process of the chicory extract, ultrasonic treatment or microwave treatment is assisted before, during or after oscillation extraction.
4. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet according to claim 1, wherein the chicory comprises roots, stems, leaves, flowers or whole plants of edible or medicinal plants.
5. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic and anti-inflammatory buccal tablet according to claim 1, wherein the oil phase is peppermint oil which is replaced by edible plant oil, essential oil (such as tea tree essential oil and lemon essential oil) or mixed oil with bacteriostatic action.
6. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic and anti-inflammatory buccal tablet according to claim 1, wherein the microcrystalline cellulose and the corn starch are partially or completely replaced by methyl-beta-cyclodextrin and deacetylated chitin which have antibacterial and embedding effects.
7. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet according to claim 1, wherein the curcumin is anthocyanin, carotenoid, chlorophyll, sorghum red pigment functional natural pigment or edible artificial synthetic pigment, and the color of the product is changed according to the use or non-use of the pigment and the color of the pigment.
8. The preparation method of the plant extract self-microemulsion sustained-release bacteriostatic anti-inflammatory buccal tablet according to claim 1, wherein the xylitol is sorbitol, erythritol low-calorie sugar alcohol with anticaries property.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101869299A (en) * | 2010-06-25 | 2010-10-27 | 王爱平 | Cichorium endivia L. extract and application thereof |
| CN102727446A (en) * | 2011-04-06 | 2012-10-17 | 复旦大学 | Solid preparation containing poorly soluble drug and preparation method thereof |
| CN103536632A (en) * | 2012-07-17 | 2014-01-29 | 陕西省中医药研究院 | Self-microemulsifying brucea javanica oil oral granules and preparation method thereof |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101869299A (en) * | 2010-06-25 | 2010-10-27 | 王爱平 | Cichorium endivia L. extract and application thereof |
| CN102727446A (en) * | 2011-04-06 | 2012-10-17 | 复旦大学 | Solid preparation containing poorly soluble drug and preparation method thereof |
| CN103536632A (en) * | 2012-07-17 | 2014-01-29 | 陕西省中医药研究院 | Self-microemulsifying brucea javanica oil oral granules and preparation method thereof |
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