CN101269000A - Oral preparation containing cefa-iskia, preparation method and application thereof - Google Patents
Oral preparation containing cefa-iskia, preparation method and application thereof Download PDFInfo
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- CN101269000A CN101269000A CNA2008100076217A CN200810007621A CN101269000A CN 101269000 A CN101269000 A CN 101269000A CN A2008100076217 A CNA2008100076217 A CN A2008100076217A CN 200810007621 A CN200810007621 A CN 200810007621A CN 101269000 A CN101269000 A CN 101269000A
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Abstract
The invention relates to a buccal preparation containing cefalexin as well as a preparation method and usage thereof. The invention aims at providing a buccal preparation taking cefalexin as ingredient, which is dissolved in saliva of oral cavity by sucking to enter the periphery of the oral cavity, the pharyngeal portion and the pharyngeal tonsils part, so as to play the role of antibacterium. The buccal preparation takes the cefalexin and ramification thereof as the raw material, and can be made into preparations such as buccal tablet, candy and pill, etc. The buccal preparation has the characteristics of rapid effect, good healing efficacy and convenient administration, etc., and can directly increase the concentration of bacteriophage drug at the parts of pathological changes, enhances the antibacterial capacity and is more suitable for the patients.
Description
Technical field
The present invention relates to a kind of medicine and its production and use, particularly contains buccal lozenge of cefalexin and its production and use.
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 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.
The oral cavity infection disease mainly comprises dental disease, the periodontal and the disease of cari oris mucosa, as dental caries, pulpitis, periapical periodontitis, periodontitis, recurrent aphtha, oral ulcer, oral leukoplakia, monilial stomatitis, the peach body region, bring into play its antibacterial action, the clinical pharyngitis that is used for the treatment of, pharyngoamygdalitis and oral cavity infection disease, particularly by prolonging preparation in intraoral melting time, it is the disintegration of preparation, prolong the action time of medicine and local lesion, and then improved the treatment pharyngitis, the drug quality of pharyngoamygdalitis and oral cavity infection disease medicament.
For achieving the above object, the present invention has adopted following technical scheme.
The buccal lozenge that contains cefalexin of the present invention is made up of ingredient that comprises cefalexin and salt derivative thereof and substrate, its Chinese medicine: substrate=1: 0.5-1: 30.0, through port intracavity buccal administration clinically is characterized in that the application of described cefalexin buccal lozenge in treatment pharyngitis, pharyngoamygdalitis and oral cavity infection disease.Select 10-100 minute the disintegration of described cefalexin buccal lozenge, preferred 15-60 minute, more preferably 20-60, preferred 20-40 minute especially, by prolonging preparation in intraoral melting time, and then improve medicine to pharyngitis, pharyngoamygdalitis and oral cavity infection treatment of diseases effect, improve drug quality.
In the comfort level that described drug quality comprises side reaction and other discomfort brought to patient in the comfort level, drug use process of medication effect, drug use, medicine stores and carry, the characteristics such as complexity of drug manufacture one or multinomial.Described raising drug quality comprises the therapeutic effect that strengthens medicine, reduce and causedly in the drug use process do not accommodate misery, conveniently use, be easy to store and carry, improve safety that medicine uses, simplify production technology, reduce in the characteristics such as toxic and side effects of medicine one or multinomial.
Wherein, selected cefalexin is chemical compound and the salt derivative thereof with following feature.
Chinese: cefalexin
English by name: Cephalexin Hydrate
Formal name used at school is: (6R, 7R)-the 3-methyl-7-[(R)-2-amino-2-phenylacetylamino]-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-formic acid-hydrate
Molecular formula: C
16H
17N
3O
4S
Molecular weight: 365.41
Wherein said substrate is the preparation adjuvant that is grouped into by one or more one-tenth, comprises diluent (filler), binding agent, disintegrating agent, lubricant, fluidizer, slow releasing agent, coloring agent, correctives, spice pericoronitis, necrotic stomatitis, thrush, gingivitis, membranous stomatitis, periodontal disease, herpetic stomatitis etc.Antibacterial is the important paathogenic factor that causes the oral cavity infection disease.Intraoral have a large amount of Gram-positives and a gram negative bacteria, and its value volume and range of product all occupies first of the whole body.According to the study, contain antibacterial in every milliliter of saliva and reach 1.5 hundred million.Under certain conditions, incorrect etc. when food debris accumulation, crowded dentition, method for brushing teeth, form dental plaque, tartar, when the kind of antibacterial changes, the amount of pathogenic bacterium increases or passive protective physical fitness descends, cause the generation of oral cavity infection disease.Therefore, oral cavity infection disease is caused by the various bacteria synergism.The patient often has symptoms such as toothache, gingival hemorrhage, redness, odontoseisis displacement, halitosis.Swelling and aching of gum, pyorrhea also can be used as infection focus, cause such as systemic diseases such as arthritis, the heart, cerebrovascular disease.
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.Cefalexin belongs to first generation cephalosporin, and antimicrobial spectrum and cefalotin are similar, but its antibacterial activity is poor than the latter.Except that Enterococcus, methicillin resistance staphylococcus, streptococcus pneumoniae, Hemolytic streptococcus, product or do not produce the staphylococcic most of bacterial strain of penicillinase to this product sensitivity.Cefalexin has better antibacterial action to neisseria, but hemophilus influenza is relatively poor to the sensitivity of cefalexin; Cefalexin has certain antibacterial action to part escherichia coli, proteus mirabilis, salmonella and shigella dysenteriae.All the other enterobacteriaceae lactobacteriaceaes, acinetobacter calcoaceticus, Pseudomonas aeruginosa, bacteroides fragilis all present drug resistance to this product.Fusobacterium and Wei Rong coccus are generally to the cefalexin sensitivity, and the anaerobism gram positive coccus is to the cefalexin medium sensitivity.Be mainly used in the severe infections of the respiratory tract infection of treatment due to the sensitive organism, gastrointestinal infection, urinary system, system genitale infection, skin, soft tissue etc. clinically.The preparation of having succeeded in developing of this medicine has tablet, capsule etc.Slower in view of oral absorption such as tablets, 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 mezlocillin 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 its production and use of ingredient with the cefalexin, and the medicine through port is contained in the intraoral saliva and dissolves, and enters around the oral cavity, pharyngeal and swallow flat etc.
Described preparation type includes but not limited to buccal tablet, drop pill, confection.As a kind of preparation type commonly used, buccal lozenge is meant and is contained in the oral cavity, the drug slow dissolving produces the pharmaceutical preparation of persistent local action, the main local therapeutic effects that rises, detect the whole disintegrates of planted agent in 30 minutes according to version Pharmacopoeia of People's Republic of China in 2005 detection method second disintegration.But the disintegration of present existing buccal lozenge is all below 10 minutes, as GUILIN XIGUA SHUANG buccal tablet, FUFANG CAOSHANHU HANPIAN, ribavirin buccal tablet, gluconic acid calcium tablet, ammonium iodide buccal tablet, JINSANGZIHOUBAO buccal tablet etc.Disintegration, the too fast medicine that then shows was short in partial action time, will obviously influence the topical therapeutic effect of medicine.The inventor is surprised to find by cefalexin being made buccal lozenge of the present invention by designing different pharmaceutical preparation technologies, remained on more than 10 minutes the disintegration of buccal lozenge, preferred 10-100 minute, the dissolution of insoluble drug composition reached more than 80% when making complete disintegrate simultaneously.For the preferred 20-60 minute disintegration of buccal lozenge for the purpose of the taking convenience, significant prolongation the action time of medicine and local lesion, thereby improved the topical therapeutic effect of medicine.
In addition, buccal lozenge is after containing of intraoral disintegration, and ingredient wherein should mainly be present in dissolved state just can bring into play its due therapeutical effect in the saliva.Cefalexin prototype compound slightly soluble in water; do not carry out hydrotropy as preparation process and handle the then medicine purpose that very difficult realization mainly exists with dissolved state in saliva; therefore; the present invention utilizes surfactant polyethylene; polyoxyethylene stearate 40 esters; beta cyclodextrin; poloxamer; carboxymethyl starch sodium; substrate such as stearic acid and medicine material are made solid dispersion or sucrose; maltose; dextrinose; the dextrinose oligosaccharide; panose; cottonseed sugar; stachyose; oligofructose; glucose; fructose; lactose; inulin; protein sugar; stevioside; xylitol; maltose alcohol; sorbitol; gelatinized corn starch; syrup; Icing Sugar such as maltose and medicine material are made solid dispersion; make medicine be molecule; colloid or microcrystalline state are scattered in the substrate; the total surface area of medicine increases; and substrate is hydrophilic; medicine had wetting action; can make medicine molten microgranule or the solution of loosing into rapidly; thereby make the dissolving of medicine and absorb quickening; thereby improved bioavailability, reached the purpose that significantly improves medicine topical therapeutic effect.
The present invention relates to contain the drop pill of following composition:
Described drop pill is made up of ingredient that includes cefalexin 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, beta cyclodextrin, 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 ingredient that includes cefalexin and substrate, and wherein said substrate contains following material: diluent 1-100%; Binding agent 0-30%; Disintegrating agent 0-10%; Lubricant 0-20%; Fluidizer 0-20%; Slow releasing agent 0-30% and conventional coloring agent, correctives, spice.
The present invention relates to contain the confection of following composition:
Described confection is made up of ingredient that includes cefalexin and substrate, and wherein said substrate contains following material: diluent 1-100%; Binding agent 0-20%; Disintegrating agent 0-10%; Lubricant 0-10%; Fluidizer 0-10%; Slow releasing agent 0-30% 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 cefalexin is mixed with substrate; When described substrate was Icing Sugar, substrate 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 solid dispersion, substrate contained but is not limited to Polyethylene Glycol
(2000,4000,6000,8000,10000, 20000), polyoxyethylene stearate 40 esters, beta cyclodextrin, 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 ingredient that contains cefalexin, stir, cut apart, shaping, drying.
(2) take by weighing an amount of Icing Sugar or other substrate, add the ingredient that contains cefalexin, 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 ingredient that contains cefalexin,,, 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 ingredient that contains cefalexin, 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 cefalexin 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, beta cyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, 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 cefalexin 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 ingredient contain cefalexin, stir, make into the plasticity magma, cut apart extrusion molding;
Cefalexin buccal lozenge of the present invention is compared with existing general formulation has following benefit:
1) the cefalexin concentration of raising diseased region 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 acts on pathological tissues immediately behind dissolved in oral cavity, saved to absorb the time limit that distributes.
3) convenient drug administration.
4) preparation of buccal lozenge of the present invention and prior art for preparing is relatively: matched group disintegration 13 ± 5 (minute), the dissolution of cefalexin only is 36 ± 5 (%) during disintegrate fully.And be 17 ± 5 the disintegration of buccal lozenge of the present invention (minute), the cefalexin dissolution is 89 ± 11 (%) during disintegrate fully.The result shows that buccal lozenge of the present invention has significantly improved the dissolution of medicine.
4) production technology is simple.
Specific implementation method
By following concrete embodiment, can further understand the present invention, but following example not a limitation of the invention.
Embodiment 1-cefalexin confection
Prescription: cefalexin 125g, sucrose 818.5g, citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 36.5g, 1000 of amount of formulation.
Method: preparation cefalexin 125g, citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 36.5g mixture grind, and cross 20 purpose sieves.Get sucrose 818.5 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 cefalexin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 28-35 minute disintegration, and fully the dissolution during disintegrate is 84%-89%.
Embodiment 2-low sugar cefalexin confection
Prescription: cefalexin 125g, sucrose 168.5g, oligofructose 300g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 36.5g, 1000 of amount of formulation.
Method: preparation citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 36.5g mixture grind, and cross 20 purpose sieves.Get sucrose 168.5g, oligofructose 300g, xylitol 300g, inulin 50g, mix, be heated to 140 ℃ of fusings, add the mixture after sieving, stirred fast 10 minutes, be cooled to 85 ℃, add cefalexin 125g, stirred 10 minutes fast, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of cefalexin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 28-36 minute disintegration, and fully the dissolution during disintegrate is 85%-91%.
Embodiment 3-cefalexin buccal tablet
Prescription: cefalexin 125 grams, hypromellose 128 grams, Polyethylene Glycol
6000746 grams, aspartame 1 gram.
Method: preparation hypromellose 128 grams, Polyethylene Glycol
6000746 grams, aspartame 1 gram mixed-matrix, heat fused is cooled to 80 ℃, adds cefalexin 125 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 cefalexin buccal tablet in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 24-31 minute disintegration, and fully the dissolution during disintegrate is 85%-92%.
The preparation of embodiment 4-cefalexin buccal drop pills
Method: taking polyethylene glycol 40008.8 restrains respectively, polyethylene glycol 6000 25 grams, polyoxyethylene stearate 40 esters 1 gram, hypromellose 4 grams, beta cyclodextrin 1 gram, poloxamer 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 cefalexin raw material powder 30 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 cefalexin 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 74% as a result, and dissolve scattered time limit 11-16 minute, the ball method of double differences was different from 10%, hardness is qualified, and fully the dissolution during disintegrate is 83%-90%.
Embodiment 5-cefalexin confection
Prescription: cefalexin 125g, sucrose 170.5g, oligofructose 82.5g, xylitol 300g, inulin 50g, citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 252 grams, 1000 of amount of formulation.
Method: preparation citric acid 10g, food pigment-400.1g, mannitol 10g, hypromellose 252 gram mixture grind, and cross 20 purpose sieves.Get sucrose 170.5g, oligofructose 82.5g, xylitol 300g, inulin 50g, mix, be heated to 140 ℃ of fusings, add the mixture after sieving, stirring and evenly mixing is cooled to 85 ℃ fast, add cefalexin 125g, stirred 10 minutes fast, place extrusion molding on the product shaping machine, every buccal tablet weighs 2 grams.Measure the disintegration of cefalexin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The result: be 81-91 minute disintegration, and fully the dissolution during disintegrate is 85%-94%.
Embodiment 6-buccal lozenge of the present invention and existing tablet are to the contrast test of the influence of cefalexin dissolution
1. technology one is substrate with the Icing Sugar
The control formulation preparation method: preparation cefalexin 125g, sucrose 855 grams, citric acid 10g, food pigment-400.1g, mannitol 10g mixture grinds, and crosses 20 purpose sieves, places extrusion molding on the product shaping machine, and every buccal tablet weighs 2 grams.Measure the disintegration of cefalexin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The preparation method of buccal lozenge of the present invention: preparation citric acid 10g, food pigment-400.1g, mannitol 10g mixture grinds, and crosses 20 purpose sieves.Get sucrose 855 grams, be heated to 140 ℃ of fusings, add the mixture after sieving, stirring and evenly mixing is cooled to 85 ℃ fast, adds cefalexin 125g, stirs fast 10 minutes, places extrusion molding on the product shaping machine, and every buccal tablet weighs 2 grams.Measure the disintegration of cefalexin confection in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The results are shown in Table 1, the present invention is the dissolution that the solid dispersion preparation technology of substrate can significantly improve cefalexin with the Icing Sugar.
Table 1, the present invention are the influence of the solid dispersion preparation technology of substrate to the cefalexin dissolution with the Icing Sugar
＊p＜0.05
2. technology two is substrate with the surfactant
Control formulation preparation method: preparation cefalexin 125g, hypromellose 100 grams, Polyethylene Glycol
6000775 grams, aspartame 0.1 gram mixed-matrix, stirring and evenly mixing is granulated, and places extrusion molding on the tablet machine, and every buccal tablet weighs 2 grams.Measure the disintegration of cefalexin sodium lozenge in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The preparation method of buccal lozenge of the present invention: preparation hypromellose 100 grams, Polyethylene Glycol
6000775 grams, aspartame 0.1 gram mixed-matrix, heat fused is cooled to 80 ℃, adds cefalexin 125g, 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 2 grams.Measure the disintegration of cefalexin sodium lozenge in 37 ℃ of 900ml water and the dissolution during complete disintegrate then.
The results are shown in Table 2, the present invention is the dissolution that the solid dispersion preparation technology of substrate can significantly improve cefalexin with the surfactant.
Table 2, the present invention are the influence of the solid dispersion preparation technology of substrate to the cefalexin dissolution with the surfactant
＊p＜0.05
Claims (10)
1. a drug quality that improves treatment pharyngitis, pharyngoamygdalitis and oral cavity infection disease is the buccal lozenge of main ingredient with cefalexin, it is characterized in that described buccal lozenge is made up of ingredient that includes cefalexin and salt derivative thereof and substrate.
2. buccal lozenge according to claim 1, be 10-100 minute the disintegration of described cefalexin buccal lozenge.
3. buccal lozenge according to claim 2, be 20-60 minute the disintegration of described cefalexin buccal lozenge.
4. the buccal lozenge of cefalexin according to claim 1, it is characterized in that: described buccal lozenge type comprises buccal tablet, drop pill, confection.
5. the preparation method of the buccal tablet in the described buccal lozenge that contains cefalexin of claim 4, 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 ingredient that contains cefalexin and substrate, then through cooled and solidified, and then make described buccal tablet.
6. the preparation method of the drop pill in the described buccal lozenge that contains cefalexin of claim 4, it is characterized in that: proportionally cefalexin is mixed with 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 and be shaped.
7. the preparation method of the confection in the described buccal lozenge that contains cefalexin of claim 4, 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 ingredient that contains cefalexin then, stirring and evenly mixing, make into the plasticity magma, cut apart, extrusion molding.
8. claim 5 or 6 or 7 preparation method, wherein said substrate is one or more compositions that comprise in Polyethylene Glycol, polyoxyethylene stearate 40 esters, beta cyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers, the Icing Sugar.
9. according to claim 5,6,7 described preparation methoies, it is characterized in that: described substrate comprises one or more medicinal slow releasing agent and coloring agent, correctives, spice and other pharmaceutic adjuvant.
10. the application of the buccal lozenge of claim 1 in preparing the medicine that can improve treatment pharyngitis, pharyngoamygdalitis and oral cavity infection disease drug quality.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100076217A CN101269000A (en) | 2007-03-21 | 2008-03-03 | Oral preparation containing cefa-iskia, preparation method and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200710087109.3 | 2007-03-21 | ||
| CN200710087109 | 2007-03-21 | ||
| CNA2008100076217A CN101269000A (en) | 2007-03-21 | 2008-03-03 | Oral preparation containing cefa-iskia, preparation method and application thereof |
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| CN101269000A true CN101269000A (en) | 2008-09-24 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102846568A (en) * | 2012-08-27 | 2013-01-02 | 辽宁王牌速效制药有限公司 | Preparation method of cephalexin layering digestion tablet |
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2008
- 2008-03-03 CN CNA2008100076217A patent/CN101269000A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102846568A (en) * | 2012-08-27 | 2013-01-02 | 辽宁王牌速效制药有限公司 | Preparation method of cephalexin layering digestion tablet |
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