CN102908271B - Quick-release solid mouth care agent and preparation method thereof - Google Patents
Quick-release solid mouth care agent and preparation method thereof Download PDFInfo
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- CN102908271B CN102908271B CN201210329260.4A CN201210329260A CN102908271B CN 102908271 B CN102908271 B CN 102908271B CN 201210329260 A CN201210329260 A CN 201210329260A CN 102908271 B CN102908271 B CN 102908271B
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- oil
- quintessence oil
- natural extracts
- oleum
- release solid
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- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- 239000000284 extract Substances 0.000 claims abstract description 24
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 15
- 239000007919 dispersible tablet Substances 0.000 claims abstract description 13
- 239000003921 oil Substances 0.000 claims description 80
- 239000000203 mixture Substances 0.000 claims description 53
- 210000000214 mouth Anatomy 0.000 claims description 37
- 239000008187 granular material Substances 0.000 claims description 35
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- 239000000843 powder Substances 0.000 claims description 31
- 239000007788 liquid Substances 0.000 claims description 21
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Landscapes
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a quick-release solid mouth care agent and a preparation method thereof. The quick-release solid mouth care agent contains 5-75% of one or more than one natural product extract with anti-inflammation or bactericidal effect in percentage by weight and comprises dispersible tablets, effervescent tablets, instant tablets and xerogels. In addition, the preparation method of the quick-release solid mouth care agent disclosed by the invention is provided. The quick-release solid mouth care agent has the characteristics of wide antibacterial spectrum, efficient and rapid effect, safety and no toxicity, is capable of integrating with the advantages of mouth care products such as chewing gum, mouth wash and the like and banishing the disadvantages of the traditional mouth care products and has the advantages of good effect, convenience for carrying and simpleness in application.
Description
Technical field
The invention belongs to household chemicals field, relate to a kind of fast release solid oral cavity nursing agent and preparation method thereof.
Background technology
Oral cavity is the start-up portion of digestive tube, has a lot of important functions.In basic nursing, the nursing in oral cavity is a pith.First, healthy tooth can allow people specious, and the daily life such as speak of having a meal feels better.Secondly, for critical patient, carry out mouth care and can avoid some complication, and can observe the state of an illness according to the health condition in oral cavity.The 3rd, it is the omen that in body, pathological changes occurs at other positions that disease occurs in oral cavity.For example oral mucosa is dry is the first signal of water, salt metabolism disorder; Can there is the prolonged oral ulcer not healing, pharyngitis in anemia patient; Leukaemic can gingival hemorrhage.The 4th, internal environment of oral cavity is moistening, nutritious, is convenient to antibacterial and lives away from home, and when human body, antibacterial can excessive multiplication when due to illness resistance declines, and causes oral cavity various diseases, as dental caries, abscess, periodontitis, dental plaque etc.The various diseases that these oral cavities have itself usually becomes again the morbidity source of human body, such as the product of organizing intracellular metabolite and the oral cavity pathogen of various oral inflammations can cause by blood and lymph the infection at other positions, thereby cause the diseases such as bacterial endocarditis, rheumatic fever and nephritis, also studies have found that in the recent period oral disease and fetal weight are too low relevant.
The method of mouth care mainly contains 1 at present) brush teeth.2) chew-in technique: chew gum.3) rinsing the mouth method: with the stirring repeatedly of tongue top to bottom, left and right, front and rear, medicinal liquid is retained in 3-5min in oral cavity.4) physics rinses and mechanical scrub.In above-mentioned the whole bag of tricks, brushing can only be removed surperficial dirt, chew series products because of the not strong cleaning oral cavity comprehensively of permeability, rinsing the mouth method product is because its liquid property and Portable belt (such as the above liquid substance of aircraft forbidden band 100ml) is not used when physics flushing and mechanical scrub are generally confined to hospital surgical.The object of the present invention is to provide a kind of bactericidal effect strong, rapidly, safe, bioavailability is high, fast release solid oral cavity nursing agent and technology of preparing thereof easy to carry and use in effect.
Summary of the invention
The object of the present invention is to provide a kind of bactericidal effect strong, rapidly, safe, bioavailability is high, fast release solid oral cavity nursing agent and technology of preparing thereof easy to carry and use in effect.
Most of quintessence oils have bacteriostasis, are the fresh-keeping natural bacteriostatic agent of gourd, fruit and vegetable.Part quintessence oil has strong bactericidal action, and as Oleum Caryophylli all has stronger bactericidal action to Gram-negative and positive bacteria, Herba Origani oil all has broad-spectrum antibacterial action to fungus and bacterium.Natural essential oil series bactericidal agent is very extensive in daily use chemicals sector application, as anti-inflammatory anti-itch product contain Oleum menthae and litsea cubeba oil, the active ingredient of Lee's stirling collutory is four kinds of quintessence oils of Folium eucalypti globueli (Eucalyptus globulus Labill.) wet goods.The conventional natural essential oil series bactericidal agent of daily use chemicals industry comprises thyme oil, Mentholum, Oleum Caryophylli, wintergreen oil, eucalyptus oil, Oleum Folium Artemisiae Argyi, Oleum Cinnamomi, tea tree ethereal oil, Oleum lavandula angustifolia, Fructus Citri Limoniae oil, litsea cubeba oil, citronella oil, patchouli oil, perilla oil, Pericarpium Zanthoxyli wet goods at present.In addition, most quintessence oils have antiphlogistic effects.As Herba Schizonepetae oil all produces effect to acute and chronic animal inflammation, Oleum Bulbus Allii energy anticoagulant.And thyme oil and tea tree ethereal oil are usually used in the anti-inflammation and sterilization of oral cavity and throat and skin part.Most of quintessence oil abnormal smells from the patients are pure and fresh pleasant in addition, are applicable to preparing oral care product.
Oral dosage form refers to and in oral cavity, runs into that saliva just can be dissolved rapidly or the tablet of disintegrate.The stripping of medicine and dissolution velocity are the rate-limiting steps of drug absorption, even can affect the bioavailability of medicine.Oral cavity disintegration tablet is because disintegration rate is fast, the long-pending increase of medical surfaces makes the dissolution rate of medicine fast, is easy to be absorbed, and can reduce medicine simultaneously stimulates esophagus and gastrointestinal.The medicine of oral instant-dissolving tablet Fast Stripping can be transported to blood by oral cavity, Sublingual and lingual mucous membrane, thereby has avoided the first pass effect of liver.Therefore, taking convenience, rapid-action, bioavailability is high, toxic and side effects is little etc., and advantage makes this type of preparation in oral administration system, have unique advantage.World Ge great drugmaker is all devoted to the research of oral cavity rapid release solid preparation at present, more successful model has loratadine (Loratadine, Claritin RediTabs), ondansetron (Ondansetron, Zofran ODT), piroxicam (Piroxicam, Feldene Fast), Zolmitriptan (Zolmitriptan, Zomig) etc.But the correlation technique of this type of dosage form and drug delivery system is not yet applied in oral care product field at present.
To achieve these goals, the invention provides a kind of fast release solid oral cavity nursing agent, contain by weight percentage the natural extracts with sterilization or antiinflammatory of 5-75%.
Described natural extracts is preferably plants essential oil.
Be preferably the natural extracts with sterilization or antiinflammatory that contains 5-30%.
Described natural extracts comprises one or more in following material: thymol, Mentholum, tea polyphenols, Oleum Caryophylli, wintergreen oil, eucalyptus oil, Oleum Folium Artemisiae Argyi, Oleum Cinnamomi, tea tree ethereal oil, Oleum lavandula angustifolia, Fructus Citri Limoniae oil, litsea cubeba oil, citronella oil, patchouli oil, perilla oil, Flos Pelargonii quintessence oil, gin quintessence oil, Radix Oenotherae erythrosepalae quintessence oil, Oleum Vitis viniferae, Herba Origani oil, Flos Rosae Rugosae quintessence oil, Fructus Zanthoxyli oil, Aloe powder, rutin, hydroxyl rutin, dihydroquercetin, curcumin, bisdemethoxycurcumin, Aloe resin B, Aloe rheochrysin, ferulic acid, citric acid, tea purine and Herba Sonchi Oleracei alkali.
Preferred natural extracts is one or more in thymol, Mentholum, tea tree ethereal oil, eucalyptus oil.
Described fast release solid oral cavity nursing agent comprises dispersible tablet, effervescent tablet and instant.
Dispersible tablet in a kind of fast release solid oral cavity nursing agent or the preparation method of instant are provided in addition, it is characterized in that comprising:
A), when natural extracts is solid, the mixture of natural extracts or natural extracts is ground into fine powder; When natural extracts is the compound recipe of liquid or solid-liquid, make the clathrate granule of natural extracts;
B) product of step (a) is mixed to tabletting with adjuvant.
Fine powder particle diameter in described step (a) is less than 50mm.
The granularity of the clathrate granule in described step (a) is less than 100 orders.
When preparing dispersible tablet, the compression force of the tabletting step in described step (b) is 0.98-2.94 kN.
When preparing instant, the compression force of the tabletting step in described step (b) is 3-13 kN.
The preparation method that effervescent tablet in a kind of fast release solid oral cavity nursing agent is provided in addition, is characterized in that comprising the following steps:
A), when natural extracts is solid, the mixture of natural extracts or natural extracts is ground into fine powder; When natural extracts is the compound recipe of liquid or solid-liquid, make the clathrate granule of natural extracts;
B) effervescent tablet preparation process preparation routinely.
The present invention has following beneficial effect:
1. bactericidal effect is strong, and rapidly, safe, bioavailability is high, easy to carry and use in effect
2. most of quintessence oils have bacteriostasis, are the fresh-keeping natural bacteriostatic agent of gourd, fruit and vegetable, and thyme oil and tea tree ethereal oil are usually used in the anti-inflammation and sterilization of oral cavity and throat and skin part in addition, and most of quintessence oil abnormal smells from the patients are pure and fresh pleasant in addition, are applicable to preparing oral care product.
3. the medicine of oral instant-dissolving tablet Fast Stripping can be transported to blood by oral cavity, Sublingual and lingual mucous membrane, thereby has avoided the first pass effect of liver.Therefore, taking convenience, rapid-action, bioavailability is high, toxic and side effects is little etc., and advantage makes this type of preparation in oral administration system, have unique advantage.
Specific embodiment
To achieve these goals, the present invention be take one or more in thymol, Mentholum, tea tree ethereal oil, Folium eucalypti globueli (Eucalyptus globulus Labill.) wet goods natural bactericidal agent and has been prepared the oral care product of the dosage forms such as dispersible tablet, fast disintegrating tablet, instant as raw material, and its concrete preparation method is as follows:
1. the preparation of dispersible tablet type oral care product
Get one or more in the solid raw bactericidal materials such as thymol, Mentholum, tea polyphenols, according to proper ratio, by its mix homogeneously, mixture is ground into the fine powder below particle diameter 50mm.Then mixture fine powder and PVP-K30 be in 20/1～50/1 ratio, with L-HPC in 1/1～50/1 ratio, with soluble starch in 1/1～5/1 ratio, with magnesium stearate in 50/1～150/1 ratio, in compression force, be 0.98 * 10
3～2.94 * 10
3direct compression in the scope of N.The gained disintegration of tablet time is in 3min.
If selected raw bactericidal material is one or more in liquid quintessence oil (as wintergreen oil, tea tree ethereal oil etc.), or for the compound recipe of solid and liquid essential oil, first quintessence oil is made to quintessence oil-Benexate Hydrochloride with cyclodextrin inclusion compound and by above-mentioned supplementary material mass ratio, carry out tabletting processing again.The preparation method of clathrate is as follows: according to the mass ratio of quintessence oil raw material and beta-schardinger dextrin-1/3～1/10, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 40～50min and become uniform pastel, be laid on plate, be placed in 20～80 ℃ of baking oven inner drying 4～12h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
embodiment 1
Get thymol 40g, Mentholum 20g, tea polyphenols 40g(mass ratio 2/1/2) mix homogeneously, mixture is ground into the fine powder of particle diameter 20mm.Then mixture fine powder and 2.5gPVP-K30(mass ratio 40/1), with 10g L-HPC(mass ratio 10/1), with 25g soluble starch (mass ratio 4/1), with 1g magnesium stearate (mass ratio 100/1) in compression force, be 2.50 * 10
3under the pressure of N, directly prepare 1000, tablet.The gained disintegration of tablet time is about 1.4min, and other standards meets 2010 editions pharmacopeia of country about the prescription of dispersible tablet.
embodiment 2
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
400g quintessence oil-Benexate Hydrochloride and 10gPVP-K30, with 40g L-HPC, with 100g soluble starch, with 4g magnesium stearate in compression force, be 2.50 * 10
3under the pressure of N, directly prepare 1000, tablet.The gained disintegration of tablet time is about 1.8min, and other standards meets 2010 editions pharmacopeia of country about the prescription of dispersible tablet.
embodiment 3
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Quintessence oil-Benexate Hydrochloride and 10gPVP-K30, with 40g L-HPC, with 100g soluble starch, with 4g magnesium stearate in compression force, be 2.50 * 10
3under the pressure of N, directly prepare 1000, tablet.The gained disintegration of tablet time is about 1.6min, and other standards meets 2010 editions pharmacopeia of country about the prescription of dispersible tablet.
embodiment 4
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 20 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
600g quintessence oil-Benexate Hydrochloride and 15gPVP-K30, with 60g L-HPC, with 150g soluble starch, with 6g magnesium stearate in compression force, be 2.50 * 10
3under the pressure of N, directly prepare 1000, tablet.The gained disintegration of tablet time is about 1.8min, and other standards meets 2010 editions pharmacopeia of country about the prescription of dispersible tablet.
embodiment 5
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
600g quintessence oil-Benexate Hydrochloride and 15gPVP-K30, with 60g L-HPC, with 150g soluble starch, with 6g magnesium stearate in compression force, be 2.50 * 10
3under the pressure of N, directly prepare 1000, tablet.The gained disintegration of tablet time is about 1.6min, and other standards meets 2010 editions pharmacopeia of country about the prescription of dispersible tablet.
the preparation of instant type oral care product
Get one or more in the solid raw bactericidal materials such as thymol, Mentholum, tea polyphenols, according to proper ratio, by its mix homogeneously, the fine powder that mixture is ground into below particle diameter 50mm is standby.Get adjuvant mannitol, carboxymethyl starch sodium, microcrystalline Cellulose, (mass ratio is sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By raw bactericidal material fine powder and adjuvant fine powder, according to mass ratio 1/1～1/20 mix homogeneously, compression force is direct compression within the scope of 3-13kN, and tablet hardness is controlled at 1.5 kg/cm
2left and right.The experiment of gained tablet dissolution in vitro shows its T
50be 1.5～3min.
If selected raw bactericidal material is one or more in liquid quintessence oil (as wintergreen oil, tea tree ethereal oil etc.), or for the compound recipe of solid and liquid essential oil, first quintessence oil is made to quintessence oil-Benexate Hydrochloride with cyclodextrin inclusion compound and by above-mentioned supplementary material mass ratio, carry out tabletting processing again.The preparation method of clathrate is as follows: according to the mass ratio of quintessence oil raw material and beta-schardinger dextrin-1/3～1/10, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 40～50min and become uniform pastel, be laid on plate, be placed in 20～80 ℃ of baking oven inner drying 4～12h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
embodiment 1
Get thymol 40g, Mentholum 20g, tea polyphenols 40g(mass ratio 2/1/2) mix homogeneously, mixture is ground into the fine powder of particle diameter 20mm.Get adjuvant 120g mannitol, 30g carboxymethyl starch sodium, 30g microcrystalline Cellulose, (mass ratio is 20g sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By raw bactericidal material fine powder and adjuvant fine powder mix homogeneously, compression force is direct compression within the scope of 3～13kN, and tablet hardness is controlled at 1.5 kg/cm
2left and right.Make altogether 1000, gained tablet mouthfeel better, without sand type.Dissolution in vitro experiment shows its T
50for 2.1min, other standards meets 2010 editions pharmacopeia of country about the prescription of oral instant-dissolving tablet.
embodiment 2
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Get adjuvant 480g mannitol, 120g carboxymethyl starch sodium, 120g microcrystalline Cellulose, (mass ratio is 80g sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By quintessence oil-Benexate Hydrochloride and adjuvant fine powder mix homogeneously, compression force is direct compression within the scope of 3-13kN, makes altogether 1000.Gained tablet hardness is controlled at 1.5 kg/cm
2left and right, mouthfeel better, without sand type.Dissolution in vitro experiment shows its T
50for 3.0min, other standards meets 2010 editions pharmacopeia of country about the prescription of oral instant-dissolving tablet.
embodiment 3
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Get adjuvant 480g mannitol, 120g carboxymethyl starch sodium, 120g microcrystalline Cellulose, (mass ratio is 80g sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By quintessence oil-Benexate Hydrochloride and adjuvant fine powder mix homogeneously, compression force is direct compression within the scope of 3-13kN, makes altogether 1000.Gained tablet hardness is controlled at 1.5 kg/cm
2left and right, mouthfeel better, without sand type.Dissolution in vitro experiment shows its T
50for 2.8min, other standards meets 2010 editions pharmacopeia of country about the prescription of oral instant-dissolving tablet.
embodiment 4
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 20 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Get adjuvant 720g mannitol, 180g carboxymethyl starch sodium, 180g microcrystalline Cellulose, (mass ratio is 120g sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By 600g quintessence oil-Benexate Hydrochloride and adjuvant fine powder mix homogeneously, compression force is direct compression within the scope of 3-13kN, makes altogether 1000.Gained tablet hardness is controlled at 1.5 kg/cm
2left and right, mouthfeel better, without sand type.Dissolution in vitro experiment shows its T
50for 3.0min, other standards meets 2010 editions pharmacopeia of country about the prescription of oral instant-dissolving tablet.
embodiment 5
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 20 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Get adjuvant 720g mannitol, 180g carboxymethyl starch sodium, 180g microcrystalline Cellulose, (mass ratio is 120g sal glauberi: mannitol/CMS-Na/ MCC/ Na
2sO
4.10H
2o=6/1.5/1.5/1) grind to form fine powder mix homogeneously standby.By 600g quintessence oil-Benexate Hydrochloride and adjuvant fine powder mix homogeneously, compression force is direct compression within the scope of 3-13kN, makes altogether 1000.Gained tablet hardness is controlled at 1.5 kg/cm
2left and right, mouthfeel better, without sand type.Dissolution in vitro experiment shows its T
50for 2.8min, other standards meets 2010 editions pharmacopeia of country about the prescription of oral instant-dissolving tablet.
the preparation of effervescent tablet type oral care product
(1) get one or more in the solid raw bactericidal materials such as thymol, Mentholum, tea polyphenols, according to proper ratio, by its mix homogeneously, the fine powder that mixture is ground into below particle diameter 50mm is standby.Weighting raw materials fine powder and appropriate tartaric acid (antibacterial and tartaric acid mass ratio are 10/1-3/1), add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens after mix homogeneously.45 ℃ dry after, 14 mesh sieve granulate.(2) take sodium bicarbonate, mannitol, PVP-K30 (NaHCO
3/ mannitol/PVP-K30=50/50/1-10/10/1) pulverize, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 mesh sieve granulate.(1) and (2) made granule is taken in proportion, add appropriate PEG4000 as lubricant tabletting.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.
If selected raw bactericidal material is one or more in liquid quintessence oil (as wintergreen oil, tea tree ethereal oil etc.), or for the compound recipe of solid and liquid essential oil, first with cyclodextrin inclusion compound, makes quintessence oil-Benexate Hydrochloride and by above-mentioned supplementary material mass ratio, carry out tabletting processing again.The preparation method of clathrate is as follows: according to the mass ratio of quintessence oil raw material and beta-schardinger dextrin-1/3～1/10, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 40～50min and become uniform pastel, be laid on plate, be placed in 20～80 ℃ of baking oven inner drying 4～12h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
embodiment 1
Get thymol 40g, Mentholum 20g, tea polyphenols 40g(mass ratio 2/1/2) mix homogeneously, mixture is ground into the fine powder of particle diameter 20mm.Take the crude drug fine powder 100g and the 18g tartaric acid that have been pulverized and mixed, after mix homogeneously, add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(2) take 50g sodium bicarbonate, 50g mannitol, 1g PVP-K30 pulverizing, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(1) and (2) made granule 1.2/1 is taken in mass ratio, add the PEG4000 of 2g as lubricant tabletting, make 1000.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.Gained tablet standard meets 2010 editions pharmacopeia of country about the prescription of oral cavity effervescent tablet.
embodiment 2
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Take the quintessence oil-Benexate Hydrochloride 400g and the 72g tartaric acid that have prepared, after mix homogeneously, add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(2) take 200g sodium bicarbonate, 200g mannitol, 4g PVP-K30 pulverizing, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(1) and (2) made granule 1.2/1 is taken in mass ratio, add the PEG4000 of 8g as lubricant tabletting, make 1000.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.Gained tablet standard meets 2010 editions pharmacopeia of country about the prescription of oral cavity effervescent tablet.
embodiment 3
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/3, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 40 ℃ of baking oven inner drying 6h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Take the quintessence oil-Benexate Hydrochloride 400g and the 72g tartaric acid that have prepared, after mix homogeneously, add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(2) claim 200g sodium bicarbonate, 200g mannitol, 4g PVP-K30 to pulverize, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(1) and (2) made granule 1.2/1 is taken in mass ratio, add the PEG4000 of 8g as lubricant tabletting, make 1000.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.Gained tablet standard meets 2010 editions pharmacopeia of country about the prescription of oral cavity effervescent tablet.
embodiment 4
Get 12.5g wintergreen oil, 37.5g eucalyptus oil, 25g Oleum Folium Artemisiae Argyi, 25g Oleum Caryophylli (according to mass ratio 1/3/2/2) mix homogeneously and make " total quintessence oil ".According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 20 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Take the quintessence oil-Benexate Hydrochloride 600g and the 108g tartaric acid that have prepared, after mix homogeneously, add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(2) take 300g sodium bicarbonate, 300g mannitol, 6g PVP-K30 pulverizing, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(1) and (2) made granule 1.2/1 is taken in mass ratio, add the PEG4000 of 12g as lubricant tabletting, make 1000.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.Gained tablet standard meets 2010 editions pharmacopeia of country about the prescription of oral cavity effervescent tablet.
embodiment 5
Get 12.5g thymol, 37.5g eucalyptus oil, 37.5g Oleum Folium Artemisiae Argyi, 12.5g Oleum menthae (according to mass ratio 1/3/3/1) mix homogeneously and make " total quintessence oil " (solid bactericide dissolves in liquid sterilization quintessence oil).According to the mass ratio of total quintessence oil and beta-schardinger dextrin-1/5, weigh.First get beta-schardinger dextrin-and appropriate water and be placed in mortar and fully grind, after mixing, add quintessence oil raw material, grind 45min and become uniform pastel, be laid on plate, be placed in 20 ℃ of baking oven inner drying 10h, make quintessence oil-Benexate Hydrochloride.To on clathrate slave plate, scrape, cross 100 mesh sieves, standby.
Take the quintessence oil-Benexate Hydrochloride 400g and the 72g tartaric acid that have prepared, after mix homogeneously, add the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(2) claim 300g sodium bicarbonate, 300g mannitol, 6g PVP-K30 to pulverize, mix homogeneously, adds the dehydrated alcohol that contains 5%PVP-K30 to prepare in right amount granule, 18 order nylon screens.45 ℃ dry after, 14 order granulate.(1) and (2) made granule 1.2/1 is taken in mass ratio, add the PEG4000 of 12g as lubricant tabletting, make 1000.During tabletting, temperature is less than 18 ℃, and air humidity is less than or equal to 40%.Gained tablet standard meets 2010 editions pharmacopeia of country about the prescription of oral cavity effervescent tablet.
Claims (1)
1. a preparation method for fast release solid oral cavity nursing agent dispersible tablet, is characterized in that,
Described fast release solid oral cavity nursing agent contains the natural extracts with sterilization or antiinflammation of the 5%-75% that accounts for described fast release solid oral cavity nursing agent by weight percentage,
Described natural extracts is preferably plants essential oil,
Described natural extracts comprises one or more in following material: thymol, Mentholum, tea polyphenols, Oleum Caryophylli, wintergreen oil, eucalyptus oil, Oleum Folium Artemisiae Argyi, Oleum Cinnamomi, tea tree ethereal oil, Oleum lavandula angustifolia, Fructus Citri Limoniae oil, litsea cubeba oil, citronella oil, patchouli oil, perilla oil, Fructus Zanthoxyli oil, Flos Pelargonii quintessence oil, gin quintessence oil, Radix Oenotherae erythrosepalae quintessence oil, Oleum Vitis viniferae, Herba Origani oil, Flos Rosae Rugosae quintessence oil, Aloe powder, rutin, hydroxyl rutin, dihydroquercetin, curcumin, bisdemethoxycurcumin, Aloe resin B, Aloe rheochrysin, ferulic acid, citric acid, tea purine and Herba Sonchi Oleracei alkali,
Comprise:
A), when natural extracts is solid, the mixture of natural extracts or natural extracts is ground into fine powder; When natural extracts is the compound recipe of liquid or solid-liquid, make the clathrate granule of natural extracts;
B) product of step (a) is mixed to tabletting with adjuvant;
Fine powder particle diameter in step (a) is less than 50mm;
The granularity of the clathrate granule in step (a) is less than 100 orders;
When preparing dispersible tablet, the compression force of the tabletting step in step (b) is 0.98-2.94kN.
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| CN104434829B (en) * | 2014-11-26 | 2018-08-31 | 黑龙江八一农垦大学 | A kind of Essential Oil of Acorus tatarinowii oral quick disintegrating tablet and preparation method thereof |
| CN104367767B (en) * | 2014-11-26 | 2018-04-10 | 黑龙江八一农垦大学 | A kind of oral quick disintegrating tablet of garlic oil and preparation method thereof |
| CN105125425A (en) * | 2015-09-23 | 2015-12-09 | 北京水木中天植物科学研究院 | Oral anti-inflammation collutory |
| CN106491452A (en) * | 2016-12-15 | 2017-03-15 | 钦州市钦南区科学技术情报研究所 | A kind of oral cavity nursing agent and preparation method thereof |
| CN108042387A (en) * | 2017-12-11 | 2018-05-18 | 陕西瑞凯生物科技有限公司 | A kind of antibacterial mouthwash of bioprotein and preparation method thereof |
| WO2022093568A1 (en) * | 2020-10-29 | 2022-05-05 | One Home Brands, Inc. | Stable anhydrous disinfectant concentrate formulation and method of making the same |
| CN113368193B (en) * | 2021-06-09 | 2022-10-04 | 海而思（郑州）科技有限公司 | Skin bacteriostatic gel and preparation method thereof |
| CN114009457B (en) * | 2021-10-26 | 2022-09-23 | 国家粮食和物资储备局科学研究院 | A kind of essential oil composition and application thereof |
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| CN1552312A (en) * | 2003-11-27 | 2004-12-08 | 李 东 | Oral solid quick releasing agent |
| CN101321560B (en) * | 2005-12-02 | 2012-10-31 | Gic创新公司 | Chewable compositions with fast release magnolia bark extract |
| CN101439048B (en) * | 2007-11-22 | 2012-06-20 | 何煜 | Chinese medicine glue rapid-release preparation for oral cavity and method for producing the same |
| CN101194916B (en) * | 2007-11-22 | 2010-09-29 | 何煜 | Oral cavity rapid release preparation and method for preparing the same |
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