CN102058587A - Solid preparation for treating asthma - Google Patents
Solid preparation for treating asthma Download PDFInfo
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- CN102058587A CN102058587A CN2009102285601A CN200910228560A CN102058587A CN 102058587 A CN102058587 A CN 102058587A CN 2009102285601 A CN2009102285601 A CN 2009102285601A CN 200910228560 A CN200910228560 A CN 200910228560A CN 102058587 A CN102058587 A CN 102058587A
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- oral solid
- solid formulation
- amoxicillin
- ambroxol
- solid preparation
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Abstract
The invention discloses a solid preparation for treating asthma, which is prepared from an auxiliary material and active components including ambroxol hydrochloride and amoxicillin. The ratio of the ambroxol hydrochloride to the amoxicillin is 2:1-5:1, the weight ratio of the ambroxol hydrochloride to the auxiliary material is 1:(5-50), wherein the medicine carrying content of each preparation is 6:2mg-25:12mg preferably. The oral solid preparation containing the active components of the ambroxol hydrochloride and the amoxicillin has the characteristics of stable placement, convenience for carrying, production cost reduction and more suitability for the large production. The oral solid preparation has remarkable cooperative synergism on the symptom releasing aspects of dyspnea caused by obstructive pulmonary diseases of bronchial asthma, chronic bronchitis, emphysema and the like.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, in particular, is the oral solid formulation of a kind of ambroxol-hydrochloride-containing and amoxicillin active component.
Background technology
The ambroxol hydrochloride chemistry is by name: methyl-amino trans 4-[(2-amino-3,5 two bromo-phenyl)] the Hexalin hydrochlorate.Ambroxol hydrochloride is the respiratory mucus regulator of a new generation, has the superior usefulness of eliminating the phlegm, and the synthetic and secretion of alveolar surfactant is had significant facilitation.Ambroxol hydrochloride can stimulate the bronchorrhea glandular secretion to be easier to mobile mucus to make sputum dilution, and toughness reduces, and can increase the generation and the secretion of pulmonary surfactant, thereby reduction airway resistance, reduce mucous adhesive force, activate mucociliary blanket function, promote the mucociliary transhipment.Compare with the first generation and second filial generation expelling phlegm drugs, ambroxol hydrochloride is except that having powerful mucolysis effect, and its maximum characteristics are that it can stimulate alveolar type II cells, promotes the synthetic and secretion of alveolar surfactant, thereby effectively strengthen mucus transport, promote expectoration.The main phosphatidylcholine of alveolar surfactant, its fundamental component is a palmitic acid.Ambroxol hydrochloride can impel palmitic acid to take in alveolar type II cells, thereby significantly strengthens the synthetic and secretion of alveolar surfactant.And ambroxol hydrochloride is safe in utilization, and better tolerance is reused no drug accumulation.At present, what gone on the market has ambroxol hydrochloride tablet, capsule, syrup, injection, slow releasing capsule or the like, be applicable to acute, the chronic respiratory system diseases of and expectoration dysfunction undesired, for example: the treatment of eliminating the phlegm of chronic bronchitis acute exacerbation, asthmatic bronchitis, bronchial asthma with the sputum secretion.
The amoxicillin, chemical name: amoxicillin, amoxicillin three water things, 6-[2-amino-2-(4-hydroxy phenyl) acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-formic acid three water things
The amoxicillin is a Penicillin antibiotics, to Streptococcus such as streptococcus pneumoniae, Hemolytic streptococcuss, do not produce aerobic gram positive coccus such as penicillinase staphylococcus, enterococcus faecalis, aerobic gram-negative bacterias such as escherichia coli, proteus mirabilis, Salmonella, hemophilus influenza, Diplococcus gonorrhoeae do not produce the beta lactamase bacterial strain and helicobacter pylori has good antibacterial activity.Bacteria cell wall is synthetic brings into play bactericidal action by suppressing in the amoxicillin, can make antibacterial become spheroid rapidly and dissolves, breaks.The amoxicillin is applicable to the following infection due to the sensitive organism (not producing the beta lactamase bacterial strain): 1. upper respiratory tract infection such as otitis media, sinusitis, pharyngitis, tonsillitis due to Streptococcus hemolyticus, streptococcus pneumoniae, staphylococcus or the hemophilus influenza.2. the urogenital infections due to escherichia coli, proteus mirabilis or the enterococcus faecalis.3. the skin soft-tissue infection due to Streptococcus hemolyticus, staphylococcus or the escherichia coli.4. lower respiratory infections such as acute bronchitis, pneumonia due to Streptococcus hemolyticus, streptococcus pneumoniae, staphylococcus or the hemophilus influenza.5. acute simple gonorrhea.6. this product still can be used for treating typhoid fever, typhoid carrier and leptospirosis; Stomach, duodenum helicobacter pylori also can be eradicated with clarithromycin, lansoprazole three coupling medicines in the amoxicillin, reduce the digestive tract ulcer relapse rate.
Summary of the invention
Consider the synergism of ambroxol hydrochloride and amoxicillin, and the shortcoming of oral solution and deficiency, the invention provides to have to place and stablize, easy to carry, production cost reduces, and more is applicable to the ambroxol-hydrochloride-containing of large-scale production and the oral solid formulation of amoxicillin active component.
Being implemented by following content of the technology of the present invention: the oral solid formulation of ambroxol-hydrochloride-containing and amoxicillin active component is characterized in that being made up of active ingredient hydrochloric acid ambroxol and amoxicillin and pharmaceutic adjuvant.Active ingredient hydrochloric acid ambroxol and amoxicillin ratio of weight and number are 2: 1-5: 1, preferred 2: 1-4: 1. the ratio of weight and number of active ingredient hydrochloric acid ambroxol and amoxicillin and pharmaceutic adjuvant is 1: 5-50, preferred 1: 5-1: 30 wherein, preferred every single dose medicine carrying content is 6: 2mg-25: 12mg, preferred 6: 2mg-10: 8 the bests are 7.5: 2mg.
The oral solid formulation of ambroxol-hydrochloride-containing of the present invention and amoxicillin active component comprises: conventional tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, chewable tablet, enteric coatel tablets, capsule, granule, enteric coated capsule etc. are through the preparation of gastrointestinal tract effect.Described adjuvant comprises one or more compositions of filler, binding agent, disintegrating agent, lubricant, correctives, aromatic, gastric solubleness or enteric coating material.Described oral solid formulation preparation technology adopts wet granulation or dry granulation.Described filler comprises one or more compositions of lactose, sucrose, dextrin, starch, pregelatinized Starch, mannitol, sorbitol, calcium hydrogen phosphate, calcium sulfate, calcium carbonate, microcrystalline Cellulose.Described binding agent comprises one or more compositions of sucrose, starch, polyvidone, sodium carboxymethyl cellulose, hypromellose, hyprolose, methylcellulose, Polyethylene Glycol, medicinal alcohol, water.Described disintegrating agent comprises one or more compositions of starch, crosslinked polyvidone, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, carmethose, gas-producing disintegrant.Described lubricant comprises one or more compositions of Pulvis Talci, magnesium stearate, stearic acid, micropowder silica gel, Polyethylene Glycol (4000 or 6000), hydrogenated vegetable oil.Described correctives comprises one or more compositions of sucrose, sorbitol, saccharin sodium, maltose alcohol, steviol glycosides, aspartame etc.Described aromatic comprises that the natural aromatic agent is as Herba Menthae, Pericarpium Citri junoris tincture, Cortex cinnamomi japonici (Ramulus Cinnamomi) wet goods.Artificial fragrant spermatophore is drawn together aqueous or oiliness essence such as Fructus Citri tangerinae essence, flavoring banana essence, Fructus Citri Limoniae essence.
Oral solid formulation preparation technology of the present invention adopts wet granulation or dry granulation.Wherein said wet granulation is that principal agent and adjuvant are crossed 100 mesh sieves respectively, fully mixes, and takes by weighing the recipe quantity adjuvant then and fully mixes with principal agent.Add binding agent system soft material again, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate.Add the even tabletting of mix lubricant at last.
Wherein said dry granulation is meant crosses 100 mesh sieves respectively with principal agent and adjuvant, fully mixes, and adopts the roll squeezer cake of press, and 18 mesh sieve granulate are crossed in the agent of reuse granulate, add the even tabletting of mix lubricant or encapsulated at last.
It is as follows that compositions of the present invention and compound oral solution are compared the advantage that is had:
(1) compositions placement of the present invention is stable, easy to carry, and the low technology of production cost is simpler.
(2) pharmacodynamic experiment proves that further therapeutic alliance has the obvious synergistic effect to compositions of the present invention aspect the symptoms such as dyspnea that cause because of airway obstructive diseases such as bronchial asthma, chronic bronchitis and emphysema alleviating.
(3) compositions of the present invention has overcome solution and has separated out precipitation easily winter in the north, and the easy moldy metamorphism in south is seen photolysis or the like defective.
| Dosage form | Repeatedly freezing | 35-40 ℃ of placement | Packing Capacity | Production cost |
| Solution | Precipitation appears | Change easily | Easily broken | High |
| Conventional tablet | No change | No change | No change | Low |
| Dispersible tablet | No change | No change | No change | Low |
| Capsule | No change | No change | No change | Low |
| Granule | No change | No change | No change | Low |
The specific embodiment
The present invention is described further below in conjunction with embodiment, and embodiment only is indicative content, means that never it limits the scope of the invention by any way.
Example 1:(tablet) (100 amount)
Principal agent and adjuvant are crossed 100 mesh sieves respectively, fully mix, take by weighing the recipe quantity adjuvant then and fully mix with principal agent.Add starch slurry system soft material again, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate.Add the even tabletting of mix lubricant at last.
Example 2 (dispersible tablet)
Principal agent and adjuvant are crossed 100 mesh sieves respectively, fully mix, take by weighing the recipe quantity adjuvant then and fully mix with principal agent.Add binding agent system soft material again, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate.Add lubricant and remaining carboxymethylstach sodium mix homogeneously tabletting at last.
Example 3:(oral cavity disintegration tablet)
Principal agent and adjuvant are crossed 100 mesh sieves respectively, fully mix, adopt the roll squeezer cake of press, 18 mesh sieve granulate are crossed in the agent of reuse granulate, add the even tabletting of mix lubricant at last.
Example 4:(capsule)
Principal agent and adjuvant are crossed 100 mesh sieves respectively, fully mix, take by weighing the recipe quantity adjuvant then and fully mix with principal agent.Add binding agent system soft material again, 20 mesh sieves are granulated, 55 ℃ of dryings, 18 mesh sieve granulate.It is evenly encapsulated to add mix lubricant.
Example 5:(enteric coatel tablets)
Preparation technology is with embodiment 1.
The coating prescription:
Art for coating:
A, acrylic resin L100-55, titanium dioxide, Pulvis Talci, the triethyl citrate of recipe quantity be dissolved in 95% the ethanol, fully mixing.
B, the plain sheet of recipe quantity is placed coating pan, start air blast, making the sheet temperature is about 40 ℃, sprays into enteric coating with spray gun, and spray speed is 5ml/ minute, sprayed to enteric coating, and dry 1h, packing gets final product.
Pack into enteric coated capsule or enteric coated back dress conventional capsule of the granule of embodiment 9, treating excess syndrome example 6 can be realized.
Ambroxol-hydrochloride-containing of the present invention (A) has carried out dissolution in vitro and release comparative experiments with the oral solid formulation dispersible tablet and the enteric coatel tablets of amoxicillin (B) active component, and experimental result is as follows:
Embodiment 10, as follows with the dispersible tablet dissolution in vitro experiment of the embodiment 2 of the inventive method preparation:
A. dissolution determination condition: instrument: the ZRS-4 medicament dissolution instrument, rotating speed: 50 rev/mins, respectively at 2,5,10,15,20,30,45 minutes sampling and measuring.
Assay method: adopt the HPLC method, detect wavelength 220nm
| Time (branch) | 2 | 5 | 10 | 15 | 20 | 30 | 45 |
| Example 2 (A) | 15.2％ | 23.8％ | 54.1％ | 78.6％ | 92.4％ | 97.9％ | 98.3％ |
| Example 2 (B) | 26.8％ | 50.1％ | 79.2％ | 86.9％ | 95.2％ | 98.4％ | 100.2％ |
B. as follows with the release in vitro degree test of embodiment 8 enteric coatel tablets of the inventive method preparation:
Drug release determination condition: instrument: ZRS-4 medicament dissolution instrument, rotating speed: 50 rev/mins,, discard above-mentioned acid solution respectively at 2 hours sampling and measuring of running in the hydrochloric acid solution of 0.1mol/L, add phosphate buffer running 60 minutes immediately, 10,20,30,45,60 minutes sampling and measuring.
Assay method: adopt the HPLC method, detect wavelength 220nm
Measurement result is as follows:
Claims (7)
1. a solid preparation for the treatment of asthma is characterized in that being made up of active ingredient hydrochloric acid ambroxol and amoxicillin and pharmaceutic adjuvant, and the ratio of weight and number of active ingredient hydrochloric acid ambroxol and amoxicillin is 2: 1-5: 1.
2. the described oral solid formulation of claim 1, the ratio of weight and number that it is characterized in that described active component and pharmaceutic adjuvant is 1: 5-50.
3. the described oral solid formulation of claim 1 is characterized in that every single dose medicine carrying content of described ambroxol-hydrochloride-containing and salbutamol active components is 6: 2mg-25: 12mg.
4. the described oral solid formulation of claim 1 is characterized in that described preparation comprises conventional tablet, dispersible tablet, oral cavity disintegration tablet, capsule, granule or enteric coated capsule.
5. the described oral solid formulation of claim 1 is characterized in that described pharmaceutic adjuvant adjuvant comprises one or more compositions of filler, binding agent, disintegrating agent, lubricant, correctives, aromatic, gastric solubleness or enteric coating material.
6. according to the described oral solid formulation of claim 1-4, it is characterized in that described oral solid formulation preparation technology adopts wet granulation or dry granulation.
7. oral solid formulation according to claim 5 is characterized in that described filler is lactose, sucrose or microcrystalline Cellulose; Described binding agent is sodium carboxymethyl cellulose, hypromellose, hyprolose, methylcellulose or Polyethylene Glycol; Described disintegrating agent is starch, crosslinked polyvidone, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose or carmethose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102285601A CN102058587A (en) | 2009-11-13 | 2009-11-13 | Solid preparation for treating asthma |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102285601A CN102058587A (en) | 2009-11-13 | 2009-11-13 | Solid preparation for treating asthma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102058587A true CN102058587A (en) | 2011-05-18 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009102285601A Pending CN102058587A (en) | 2009-11-13 | 2009-11-13 | Solid preparation for treating asthma |
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| CN (1) | CN102058587A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102716128A (en) * | 2012-07-03 | 2012-10-10 | 王学军 | Pharmaceutical composition for treating asthma |
| CN102784141A (en) * | 2012-07-24 | 2012-11-21 | 宋金春 | Solid preparation of ambroxol hydrochloride and amoxicillin, and prescription and preparation method thereof |
| CN106474122A (en) * | 2016-09-07 | 2017-03-08 | 湘北威尔曼制药股份有限公司 | A kind of pharmaceutical composition of amoxicillin and clavulanate potassium and its application |
-
2009
- 2009-11-13 CN CN2009102285601A patent/CN102058587A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102716128A (en) * | 2012-07-03 | 2012-10-10 | 王学军 | Pharmaceutical composition for treating asthma |
| CN102784141A (en) * | 2012-07-24 | 2012-11-21 | 宋金春 | Solid preparation of ambroxol hydrochloride and amoxicillin, and prescription and preparation method thereof |
| CN106474122A (en) * | 2016-09-07 | 2017-03-08 | 湘北威尔曼制药股份有限公司 | A kind of pharmaceutical composition of amoxicillin and clavulanate potassium and its application |
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| C06 | Publication | ||
| PB01 | Publication | ||
| DD01 | Delivery of document by public notice |
Addressee: Sun Shengzeng Document name: Notification of Publication of the Application for Invention |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20110518 |