CN1939300A - Oral preparation containing amocillin and its making method - Google Patents
Oral preparation containing amocillin and its making method Download PDFInfo
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- CN1939300A CN1939300A CN 200610081119 CN200610081119A CN1939300A CN 1939300 A CN1939300 A CN 1939300A CN 200610081119 CN200610081119 CN 200610081119 CN 200610081119 A CN200610081119 A CN 200610081119A CN 1939300 A CN1939300 A CN 1939300A
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Abstract
An orally absorbed medicine in the form of buccal lozenge, sweets, or dripping pill dissolved by saliva features that it contains amoxicillin. Its preparing process is also disclosed.
Description
[technical field] the present invention relates to a kind of medicine and preparation method thereof, particularly contains buccal lozenge of amoxicillin and preparation method thereof.
[background technology]
Pharyngitis is the modal disease of puzzlement modern life, is pharyngeal mucous membrane, submucous tissue and adenoid diffuse inflammation, often is the part of upper respiratory tract infection.Be divided into acute and chronic two kinds clinically.Acute pharyngitis is many in autumn and winter and morbidity at the end of winter and the beginning of spring.Pathological changes ordinary wave and whole pharyngeal cavity also can limit to a place.Can cause by virus, antibacterial and physical chemical factor and high temperature, dust, fumagine, irritative gas etc.Bacterial infection is based on gram-positive coccis such as streptococcus, staphylococcus and Diplococcus pneumoniaes.Wherein serious with A group group B streptococcus causer, antibacterial or toxin enter blood, can cause the purulent lesion of organ at a distance, are called acute septic pharyngitis.Treat with oral or injection antibiotics control infection.
The chronic pharyngitis course of disease is very long, and the symptom stubbornness is often by due to the local infection or general pathological changes secondary, with chronic pathological changes repeatedly acute attack be its characteristics, in many cases, acute attack is to be caused by bacterial infection, therefore, suitable antibacterial therapy helps to control acute symptom.
Acute tonsillitis is a kind of non-specific acute inflammation of very common palatine tonsil, often with to a certain degree pharyngeal mucous membrane and swallow adenoid acute inflammation.Main pathogenic bacterium are beta hemolytic streptococcus, staphylococcus, Diplococcus pneumoniae.Adenovirus also can cause primary disease.Antibacterial and virus mixed infection are quite a few to be seen.Antibacterial may be extraneous the intrusion, also may be the antibacterial that is hidden in the tonsillar crypts, when Abwehrkraft des Koepers because of cold, humidity, overworked, have a delicate constitution, tobacco and wine are excessive, when factors such as harmful gas stimulation reduce suddenly, due to bacterial reproduction is strengthened.Acute tonsillitis is acute attack repeatedly on chronic tonsil basis often.Clinical manifestation aversion to cold, hyperpyrexia, pharyngalgia, aggravation etc. when swallowing can the concurrent rheumatic fever relevant with hemolytic streptococcal infection, multiple general diseases such as acute glome-rulonephritis, myocarditis, arthritis.Treatment adopts pain relieving to bring down a fever, oral or injection antibiotics control infection.
Treat pharyngitis, tonsillitis and oral cavity infection that bacterial infection causes, often select the antibiotics of resisting gram-positive bacteria for use, the antibiotics of the anti-gram negative bacteria of part also has therapeutical effect.The amoxicillin is the oral antibiotic of infection such as clinical widely used treatment Streptococcus hemolyticus, streptococcus pneumoniae, staphylococcus or the hemophilus influenza at present pharyngitis, pharyngoamygdalitis and the oral cavity infection that cause, is semi-synthetic penbritin class medicine.The amoxicillin can make bacterial cell become spheroplast and the dissolving of breaking rapidly by suppressing the biosynthesis of bacteria cell wall, thus the performance bactericidal effect.The preparation of having succeeded in developing of this medicine has tablet, capsule, injection, chewable tablet etc., all adopts oral or whole body administration such as injection.Be easy to cause the local pain reaction when using inconvenience, administration in view of injection.Oral absorption such as tablet and capsule is slower, and entering behind the blood distributes by whole body dilutes medicine in blood, make medicine lower at the blood drug level of diseased region, and it is also longer to reach time of effective blood drug concentration at diseased region, influences its effective antibacterial efficacy.Therefore, the buccal lozenge of development amoxicillin by the oral cavity buccal, directly acts on diseased region with high concentration medicine, is used for pharyngitis, pharyngoamygdalitis and oral cavity infection treatment of diseases, can overcome above-mentioned shortcoming, and strong auxiliary treatment means is provided.
[summary of the invention]
The purpose of this invention is to provide a kind of is the buccal lozenge and preparation method thereof of active component with the amoxicillin, and the medicine through port is contained in the intraoral saliva and dissolves, and enters around the oral cavity, pharyngeal and pharyngeal tonsil position, brings into play its antibacterial action.
For achieving the above object, the present invention has adopted following technical scheme:.
The buccal lozenge that contains the amoxicillin of the present invention is meant by active constituents of medicine that contains the amoxicillin and substrate composed preparation, its Chinese medicine: substrate=1: 0.10-1: 20.0, through port intracavity and sublingual administration administration are used for the treatment of pharyngitis, pharyngoamygdalitis and oral cavity infection clinically.
Wherein, selected amoxicillin is chemical compound and its esters (as sodium salt, potassium salt, hydrochlorate, sulfate, hydrobromate, tartrate, the fumarate etc.) derivant with following feature: English Amoxicillin by name, molecular formula: C
16H
19N
3O
5S3H
2O, molecular weight: 419.46, chemical structural formula is:
Amoxicillin salt derivative commonly used is the amoxicillin sodium salt.。
Wherein said substrate is the preparation adjuvant that is grouped into by one or more one-tenth, comprising:
1, diluent (filler): for example Icing Sugar, gelatin, glycerol, arabic gum, starch, dextrin, lactose, glucose, mannitol, calcium sulfate, calcium hydrogen phosphate, tricalcium phosphate, gelatinized corn starch, syrup, maltose, gelatine size, cellulose, Kaolin, sodium chloride, modified starch (Sta-RX1500), microcrystalline Cellulose etc., wherein Icing Sugar has sucrose, maltose, dextrinose, dextrinose oligosaccharide, panose, cottonseed sugar, stachyose, oligofructose, fructose, inulin, protein sugar, stevioside, xylitol, maltose alcohol, sorbitol;
2, binding agent: for example water, ethanol, starch, gelatin, sucrose, glucose, dextran, syrup, lactose, arabic gum, sodium alginate, gelatine size, polyvinylpyrrolidone, Polyethylene Glycol, methylcellulose, carboxymethyl cellulose, ethyl cellulose, hydroxypropyl cellulose, maltose, sucrose dextrin copolymer;
3, disintegrating agent: for example starch (corn and potato starch), cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, pectin, carboxymethyl cellulose, microcrystalline Cellulose, tween 80, sodium laurylsulfate, stearyl alcohol sodium sulfonate, kaolin.
4, lubricant: for example stearic acid, calcium stearate, magnesium stearate, zinc stearate, hydrogenated vegetable oil, polyoxyethylene monostearate, light mineral oil, liquid paraffin, boric acid, sodium chloride, sodium benzoate, sodium acetate, enuatrol, sodium laurylsulfate (magnesium), single Laurel sucrose acid ester, adipic acid, fumaric acid, three triacetins, polyethylene glycol 1500～20000.
5, fluidizer: for example starch, purified talc, differential silica gel, pyrolytic silicon dioxide, hydrated sodium aluminosilicate.
6, slow releasing agent: for example hydroxypropyl cellulose, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, carbomer 934 P, carbomer 971P, carbomer 974P, stearic acid, hexadecanol, octadecanol, ethyl cellulose, zein etc.
7, other: conventional coloring agent, correctives, spice, as aspartame etc.
Described preparation type includes but not limited to buccal tablet, drop pill, confection, capsule, tablet.
The present invention relates to contain the tablet of following composition:
Described tablet is made up of active constituents of medicine that includes the amoxicillin and substrate, and wherein said substrate contains following material (accounting for the percentage by weight of substrate total amount): diluent 1-100%; Binding agent 0-30%; Disintegrating agent 0-20%; Lubricant 0-20%; Fluidizer 0-20%; Slow releasing agent 0-10% and conventional coloring agent, correctives, spice.
The present invention relates to contain the capsule of following composition:
Described capsule is made up of active constituents of medicine that includes the amoxicillin and substrate, and wherein said substrate contains following material (accounting for the percentage by weight of substrate total amount): diluent 1-100%; Binding agent 0-30%; Disintegrating agent 0-20%; Lubricant 0-20%; Fluidizer 0-20%; Slow releasing agent 0-10% and conventional coloring agent, correctives, spice.
The present invention relates to contain the drop pill of following composition:
Described drop pill is made up of active constituents of medicine that includes the amoxicillin and substrate, adopt water-bath, oil bath or other mode of heating, mixed material is heated to fusion, stir, insert on the drop pill machine with suitable speed, splash in 40 →-15 ℃ the condensing agent liquid paraffin, methyl-silicone oil, vegetable oil any one or a few, drying forms, and its mesostroma is by containing Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), one or more one-tenth in polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers and the medicinal slow release agent are grouped into.
The present invention relates to contain the buccal tablet of following composition:
Described buccal tablet is made up of active constituents of medicine that includes the amoxicillin and substrate, and wherein said substrate contains following material (accounting for the percentage by weight of substrate total amount): diluent 1-100%; Binding agent 0-30%; Disintegrating agent 0-20%; Lubricant 0-20%; Fluidizer 0-20%; Slow releasing agent 0-10% and conventional coloring agent, correctives, spice.
The present invention relates to contain the confection of following composition:
Described confection is made up of active constituents of medicine that includes the amoxicillin and substrate, and wherein said substrate contains following material (accounting for the percentage by weight of substrate total amount): diluent 1-100%; Binding agent 0-20%; Disintegrating agent 0-10%; Lubricant 0-10%; Fluidizer 0-10%; Slow releasing agent 0-10% and conventional coloring agent, correctives, spice.
Preparation method of the present invention comprises following order and step, but following be not limitation of the invention:
1. the preparation method of buccal tablet: proportionally the amoxicillin is mixed with substrate; When described substrate was Icing Sugar, described buccal tablet contained but is not limited to one or more composition in sucrose, maltose, dextrinose, dextrinose oligosaccharide, panose, cottonseed sugar, stachyose, oligofructose, glucose, fructose, lactose, inulin, protein sugar, stevioside, xylitol, maltose alcohol, sorbitol, gelatinized corn starch, syrup, the maltose etc.; When described substrate was solvent, described buccal tablet contained but is not limited to Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers one or more composition.
(1) takes by weighing an amount of Icing Sugar or other substrate, add water or binding agent, make suitable soft material, add the active constituents of medicine that contains the amoxicillin, stir, cut apart, shaping, drying.
(2) take by weighing an amount of Icing Sugar or other substrate, add the active constituents of medicine that contains the amoxicillin, add water or binding agent, stir, granulate, drying is shaped on tablet machine.
(3) take by weighing an amount of Icing Sugar or other substrate, add the active constituents of medicine that contains the amoxicillin,,, on tablet machine, be shaped then through cooled and solidified through being heated as the miscible or miscible state of semi-molten of fusion.
(4) take by weighing an amount of Icing Sugar or other substrate,, be cooled to 70-100 ℃, add the active constituents of medicine that contains the amoxicillin, stir, on tablet machine, be shaped through being heated as the miscible or miscible state of semi-molten of fusion.
2. the preparation of drop pill: proportionally the amoxicillin is mixed with substrate; Substrate is by containing Polyethylene Glycol
(2000,4000,6000,8000,10000,20000)One or more one-tenth in polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, the polyethers are grouped into.Adopt water-bath, oil bath or other mode of heating, mixed material is heated to fusion, stir, insert on the drop pill machine, splash in 40 →-15 ℃ the condensing agent with suitable speed.Condensing agent can be any one or a few in liquid paraffin, methyl-silicone oil, the vegetable oil.
3. the preparation of confection: proportionally the amoxicillin is mixed with substrate; Matrix filler is to be grouped into by one or more the one-tenth that contains in sucrose, maltose, dextrinose, dextrinose oligosaccharide, panose, cottonseed sugar, stachyose, oligofructose, glucose, fructose, lactose, inulin, protein sugar, stevioside, xylitol, maltose alcohol, sorbitol, gelatinized corn starch, syrup, the maltose etc.
Take by weighing an amount of Icing Sugar or other substrate heat fused, be cooled to uniform temperature then after, add the active constituents of medicine contain the amoxicillin, stir, make into the plasticity magma, cut apart extrusion molding;
4. capsular preparation: proportionally the amoxicillin is mixed with substrate; Substrate is by containing Icing Sugar, gelatin, glycerol, arabic gum, starch, dextrin, lactose, glucose, mannitol, calcium sulfate, calcium hydrogen phosphate, tricalcium phosphate, gelatinized corn starch, syrup, maltose, gelatine size, polyvinylpyrrolidone, Polyethylene Glycol, methylcellulose, carboxymethyl cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, sucrose dextrin copolymer, Polyethylene Glycol
1500～20000, among stearic acid, sodium stearate, calcium stearate, sodium chloride, fumaric acid, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyoxyethylene stearate 40 esters, polyethers, carboxymethyl starch sodium, silica sol, succinic acid, xanthan gum, aspartame, mannitol, silica gel, silicon dioxide, saccharin sodium, carbomer 934 P, carbomer 971P and carbomer 974P etc. one or more become to be grouped into
Take by weighing an amount of substrate, add the active constituents of medicine that contains the amoxicillin, stir, granulate capsule charge;
5. the preparation of tablet: proportionally the amoxicillin is mixed with substrate; Substrate is by containing Icing Sugar, gelatin, glycerol, arabic gum, starch, dextrin, lactose, glucose, mannitol, calcium sulfate, calcium hydrogen phosphate, tricalcium phosphate, gelatinized corn starch, syrup, maltose, gelatine size, polyvinylpyrrolidone, Polyethylene Glycol, methylcellulose, carboxymethyl cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, sucrose dextrin copolymer, Polyethylene Glycol
1500～20000, among stearic acid, sodium stearate, calcium stearate, sodium chloride, fumaric acid, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyoxyethylene stearate 40 esters, polyethers, carboxymethyl starch sodium, silica sol, succinic acid, xanthan gum, aspartame, mannitol, silica gel, silicon dioxide, saccharin sodium, carbomer 934 P, carbomer 971P and carbomer 974P etc. one or more become to be grouped into
Take by weighing an amount of substrate, add the active constituents of medicine that contains the amoxicillin, stir, granulate, tabletting is shaped on tablet machine;
Amoxicillin of the present invention buccal lozenge is compared with existing general formulation has following benefit:
1) the amoxicillin concentration at raising position, sick limit improves its antibacterial ability.Medicine dissolves in the saliva in the oral cavity, enters around the oral cavity, pharyngeal and pharyngeal tonsil position.These medicines do not pass through hemodilution, form high local concentrations, strengthen antibacterial ability.
2) rapid-action.Medicine is behind dissolved in oral cavity, and effect and pathological tissues have saved the time limit that absorbs distribution immediately.
3) convenient drug administration.To the amoxicillin of need,, directly act on position, disease limit then by sucking the messenger drug thing at dissolved in oral cavity through the parenteral route administration.
[specific implementation method]
By following concrete embodiment, can further understand the present invention, but following example not a limitation of the invention.
Embodiment 1-amoxicillin confection
Prescription: amoxicillin 12.5g, sucrose 965.5g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, carbomer 934 P 2g, 500 of amount of formulation.
Method: preparation amoxicillin 12.5g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, carbomer 934 P 2g mixture grind, and cross 20 purpose sieves.Get sucrose 965.5 grams, be heated to 140 ℃ of fusings, be cooled to 85 ℃, add the mixture after sieving, stirred fast 10 minutes, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of amoxicillin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 7-9 minute disintegration, and fully the dissolution during disintegrate is 92%-95%.
Embodiment 2-low sugar amoxicillin confection
Prescription: amoxicillin 12.5g, sucrose 315.5g, oligofructose 300g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-400.1g, mannitol 10g, carbomer 934 P 2g, 500 of amount of formulation.
Method: preparation amoxicillin 12.5g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, carbomer 934 P 2g mixture grind, and cross 20 purpose sieves.Get sucrose 315.5g, oligofructose 300g, xylitol 300g, inulin 50g, mix, be heated to 140 ℃ of fusings, be cooled to 85 ℃, add the mixture after sieving, stirred fast 10 minutes, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of amoxicillin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 8-10 minute disintegration, and fully the dissolution during disintegrate is 91%-95%.
Embodiment 3-low sugar amoxicillin buccal tablet
Prescription: Amoxicillin Sodium 25g, gelatin 240g, glycerol 60g, water 60g, oligofructose 293g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-400.1g, mannitol 10g, magnesium stearate 10g, carbomer 934 P 2g, 1000 of amount of formulation.
Method: preparation gelatin 240g, glycerol 60g, water 60g mixed-matrix, drying adds Amoxicillin Sodium 12.5g, oligofructose 293g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-400.1g again, mannitol 10g, carbomer 934 P 2g mixture, grind, cross 20 purpose sieves, granulate 60 ℃ of dryings with the second alcohol and water, add 10 gram magnesium stearate then, mixing places extrusion molding on the tablet machine, and every buccal tablet weighs 1 gram.Measure the disintegration of amoxicillin buccal tablet in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 6-9 minute disintegration, and fully the dissolution during disintegrate is 93%-96%.
Embodiment 4-amoxicillin buccal tablet
Prescription: amoxicillin 250 grams, hypromellose 88 grams, Polyethylene Glycol
6000350 grams, aspartame 1 gram, 1000 of amount of formulation.
Method: preparation hypromellose 88 grams, Polyethylene Glycol
6000350 grams, aspartame 1 gram mixed-matrix, heat fused is cooled to 80 ℃, adds amoxicillin 250 grams, stirring and evenly mixing, room temperature is cooled to solidifies, and granulates, and places extrusion molding on the tablet machine, and every buccal tablet weighs 1 gram.Measure the disintegration of amoxicillin sodium lozenge in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 24-27 minute disintegration, and fully the dissolution during disintegrate is 98%-99%.
Embodiment 5-low sugar Amoxicillin Sodium confection
Prescription: amoxicillin 12.5g, sucrose 315.5g, oligofructose 300g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, carbomer 934 P 2g, 500 of amount of formulation.
Method: preparation amoxicillin 12.5g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, carbomer 934 P 2g mixture grind, and cross 20 purpose sieves.Get sucrose 315.5g, oligofructose 300g, xylitol 300g, inulin 50g, mix, be heated to 140 ℃ of fusings, be cooled to 85 ℃, add the mixture after sieving, stirred fast 10 minutes, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of amoxicillin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 8-11 minute disintegration, and fully the dissolution during disintegrate is 90%-93%.
The preparation of embodiment 6-amoxicillin buccal drop pills
Method: get Hard Macrogol 16.3 grams respectively, polyethylene glycol 6000 13 grams, polyoxyethylene stearate 40 esters 1 gram, carbomer 2 grams, betacyclodextrin 1 gram, poloxamer 0.5 gram, carboxymethyl starch sodium 0.5 gram, stearic acid 0.1 gram, sodium stearate 0.1 gram, glycerin gelatine 0.1 gram, glyceryl monostearate 0.1 gram, Lac 0.1 gram, polyoxyethylene monostearate 0.1 gram, polyethers 0.1 gram, mix homogeneously, add amoxicillin raw material powder 15 grams again, fully mix, adopt electrically heated mode with the supplementary material mixture heated that makes to molten condition, adopt homemade special drilling pill machine, regulate its water dropper temperature and make it remain on 85 ℃ (error＜2%); With the methyl-silicone oil is condensing agent, the refrigeration control system of regulating the drop pill machine makes the temperature of condensing agent remain on 20 →-5 ℃ (error＜5%), the system of dripping, wait to take out behind the type of being shrunk to, remove the surface condensation agent, dry, make the drop pill that contains amoxicillin 30mg/ grain, carry out then rounding rate (%), dissolve scattered time limit (minute), the mensuration of the ball method of double differences different (%) and hardness, the rounding rate is 73% as a result, and dissolve scattered time limit 5-7 minute, the ball method of double differences was different from 10%, hardness is qualified, and fully the dissolution during disintegrate is 95%-99%.
Embodiment 7-low sugar amoxicillin buccal tablet
Prescription: Amoxicillin Sodium 25g, gelatin 240g, glycerol 60g, water 60g, oligofructose 207g, xylitol 212g, inulin 50g, citric acid 10g, food pigment-400.1g, mannitol 10g, magnesium stearate 10g, hypromellose 176 grams, 1000 of amount of formulation.
Method: preparation gelatin 240g, glycerol 60g, water 60g mixed-matrix, drying adds Amoxicillin Sodium 25g, oligofructose 207g, xylitol 212g, inulin 50g, citric acid 10g, food pigment-40 0.1g again, mannitol 10g, hypromellose 88 gram mixture, grind, cross 20 purpose sieves, granulate 60 ℃ of dryings with the second alcohol and water, add 10 gram magnesium stearate then, mixing places extrusion molding on the tablet machine, and every buccal tablet weighs 1 gram.Measure the disintegration of amoxicillin buccal tablet in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 29-35 minute disintegration, and fully the dissolution during disintegrate is 94%-96%.
Embodiment 8-low sugar Amoxicillin Sodium confection
Prescription: amoxicillin 12.5g, sucrose 141.5g, oligofructose 300g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, hypromellose 176 grams, 500 of amount of formulation.
Method: preparation amoxicillin 12.5g, citric acid 10g, food pigment-40 0.1g, mannitol 10g, hypromellose 176 gram mixture grind, and cross 20 purpose sieves.Get sucrose 141.5g, oligofructose 214g, xylitol 300g, inulin 50g, mix, be heated to 140 ℃ of fusings, be cooled to 85 ℃, add the mixture after sieving, stirred fast 10 minutes, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of amoxicillin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 28-31 minute disintegration, and fully the dissolution during disintegrate is 92%-93%.
The efficacy test of the embodiment 9-embodiment of the invention 4 amoxicillin buccal tablets
Medicine: trial target: the embodiment of the invention 4 amoxicillin buccal tablet 0.25g/ sheets, reference substance: the Amoxicillin Capsules 0.25g/ grain that middle promise Pharmaceutical (Shijiazhuang) company limited is produced
Method: choose acute pharyngitis and acute pharyngoamygdalitis patient medical history, be divided into oral group of Amoxicillin Capsules, the amoxicillin buccal tablet is sucked group.Each group all awards 8/day of 8 slices/day of amoxicillin buccal tablets or Amoxicillin Capsules.Oral group with per 6 hours once, each 2, through water delivery service.Suck group with per 6 hours once, 2 of each buccal continuously, every tablet of medicine time of oral cavity including reservation with greater than 20 minutes.Each is organized case and all observed 24 hours, improves situation respectively at observation in 4,8,16,24,48 hours and record clinical symptoms and sign after the administration.By writing down the case load that each time point clinical symptoms and sign are improved, analyze the therapeutic effect of buccal lozenge to acute pharyngitis and acute pharyngoamygdalitis.Clinical symptoms and sign be improved as that heating is disappeared, pharyngalgia disappears, pharyngeal or tonsil is congested alleviates three indexs and occurs one at least.
The result: by table 1 as seen, by the laboratory observation to 69 routine cases, it is amoxicillin buccal tablet group 82% that 24 hours clinical symptoms of taking medicine and sign are improved percentage rate, and oral group 53% of Amoxicillin Capsules illustrates that the curative effect of sucking administration is better than oral administration.
The efficacy test result of study of table 1, buccal lozenge of the present invention
| Group | Case load | Accumulative total is improved case load | ||||
| 4 hours | 8 hours | 16 hours | 24 hours | 48 hours | ||
| Amoxicillin buccal tablet group *Oral group of Amoxicillin Capsules | 39 30 | 6 0 | 15 3 | 22 9 | 29 14 | 31 16 |
*p＜0.05
Claims (10)
1. one kind is the buccal lozenge of main active with the amoxicillin, is made of its Chinese medicine active constituents of medicine that includes the amoxicillin and substrate: substrate=1: 0.10-1: 20.0.
2. the buccal lozenge of amoxicillin according to claim 1, it is characterized in that: described buccal lozenge is used for through port intracavity and sublingual administration administration.
3. the buccal lozenge of amoxicillin according to claim 1 is characterized in that: described buccal lozenge is clinical to be used for but to be not limited to treat pharyngitis, pharyngoamygdalitis and oral cavity infection.
4. the buccal lozenge of antibiotics according to claim 1, it is characterized in that: described amoxicillin is Utimox and salt derivative thereof.
5. the buccal lozenge of amoxicillin according to claim 1, it is characterized in that: described preparation type includes but not limited to buccal tablet, drop pill, confection, capsule, tablet.
6. the described a kind of preparation method that contains the buccal tablet of amoxicillin of claim 5, it is characterized in that: described buccal tablet is through being heated as the miscible or miscible state of semi-molten of fusion by the active component that contains the amoxicillin and substrate, then through cooled and solidified, and then make described buccal tablet.
7. preparation method according to claim 6 is characterized in that: described substrate is by containing Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers one or more one-tenth be grouped into.
8. the described a kind of preparation method that contains the confection of amoxicillin of claim 5, it is characterized in that: described confection be earlier with substrate through being heated as the miscible state of fusion, then through being cooled to semi-solid, add the active constituents of medicine that contains the amoxicillin then, stirring and evenly mixing, make into the plasticity magma, cut apart, extrusion molding.
9. preparation method according to claim 8, it is characterized in that: described substrate is Icing Sugar, contains but is not limited to one or more composition of sucrose, maltose, dextrinose, dextrinose oligosaccharide, panose, cottonseed sugar, stachyose, oligofructose, fructose, inulin, protein sugar, stevioside, xylitol, maltose alcohol, sorbitol, gelatinized corn starch, syrup, maltose.
10. according to claim 6 and 8 described preparation methoies, it is characterized in that: described substrate contains one or more medicinal slow releasing agent and conventional coloring agent, correctives, spice.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610081119 CN1939300A (en) | 2005-09-26 | 2006-05-22 | Oral preparation containing amocillin and its making method |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200510104990 | 2005-09-26 | ||
| CN200510104990.4 | 2005-09-26 | ||
| CN 200610081119 CN1939300A (en) | 2005-09-26 | 2006-05-22 | Oral preparation containing amocillin and its making method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1939300A true CN1939300A (en) | 2007-04-04 |
Family
ID=37958008
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610081119 Pending CN1939300A (en) | 2005-09-26 | 2006-05-22 | Oral preparation containing amocillin and its making method |
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| Country | Link |
|---|---|
| CN (1) | CN1939300A (en) |
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2006
- 2006-05-22 CN CN 200610081119 patent/CN1939300A/en active Pending
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