CN101756947A - Compound solid preparation for treating asthma - Google Patents
Compound solid preparation for treating asthma Download PDFInfo
- Publication number
- CN101756947A CN101756947A CN200810152555A CN200810152555A CN101756947A CN 101756947 A CN101756947 A CN 101756947A CN 200810152555 A CN200810152555 A CN 200810152555A CN 200810152555 A CN200810152555 A CN 200810152555A CN 101756947 A CN101756947 A CN 101756947A
- Authority
- CN
- China
- Prior art keywords
- solid preparation
- compositions
- hydrochloride
- tablet
- starch
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Abstract
The invention discloses a compound solid preparation for treating asthma, which comprises active components of ambroxolhydrochloride and clenbuterol hydrochloride and auxiliary materials, wherein the ratio of the effective components of ambroxolhydrochloride and clenbuterol hydrochloride is 2:1-10:1 and the ratio of the effective components to the auxiliary materials is 15:100. Preferentially, the medicine-carrying content of single dose is 7.5:2mg to 30:12mg. The orally-taken solid preparation containing the effective components of ambroxolhydrochloride and clenbuterol hydrochloride has the advantages of stable placement, easy carrying, and reduced production cost and is suitable for industrialized production. The orally-taken solid preparation has obvious synergy effect on difficult breathing and other symptoms caused by airway obstructive diseases, such as 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 clenobuterol hydrochloride 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 I I type cell, 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.
Clenobuterol hydrochloride is a kind of anti-asthmatic Clenbuterol (clenbuterol), and chemical name is 42 amidos, 2 α 2 (tert-butylamine methyl), 23,52 dichlorbenzyl alcohol, and molecular formula is C
12H
18Cl
2N
20, be beta 2 receptor analeptic.The exciting beta 2-receptor of Clenbuterol energy has excitation to heart, and bronchial smooth muscle is had stronger and persistent dilating effect.Oral back is than The book of Changes gastrointestinal absorption.Do the oral adult of anti-asthmatic 20-40 μ g/ time, 3 times/day; Child 5-20 μ g/ time more than 5 years old, 3 times/day.People (women) per os TDLo:4600ng/kg.Mouse vein LD50:27600ug/kg.Clenbuterol is good absorbing in domestic animal and human body, and compares with other beta-stimulants, and its bioavailability height occurs poisoning so that eaten the Carnis Sus domestica that contains Clenbuterol.The 14C-clenobuterol hydrochloride of Zimmer (1976) confirmer 20 μ g for oral administration, during peak concentration, Clenbuterol original shape medicine accounts for 75% of total 14C-clenobuterol hydrochloride in the blood plasma.The fact that Clenbuterol bioavailability for oral administration is high has eaten the tissue that contains Clenbuterol to estimation consumer, and therefrom the amount of the Clenbuterol of Huo Deing is very important.
Indication is for alleviating the symptoms such as dyspnea that cause because of airway obstructive diseases such as bronchial asthma, chronic bronchitis and emphysema.Because these diseases partly have the appearance of expectorant usually, and the bad meeting of expectoration increases the weight of the state of an illness, therefore, both share, and singly uses one, and curative effect is more definite.Has certain synergism aspect the symptoms such as dyspnea that clinical data proof ambroxol hydrochloride and sulphuric acid clenobuterol hydrochloride cause because of airway obstructive diseases such as bronchial asthma, chronic bronchitis and emphysema in alleviation.
Summary of the invention
Consider the synergism of ambroxol hydrochloride and sulphuric acid clenobuterol hydrochloride, 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 sulphuric acid clenobuterol hydrochloride active component.
Being implemented of the technology of the present invention by following content:
A kind of compound solid preparation for the treatment of asthma is characterized in that being made up of active ingredient hydrochloric acid ambroxol and clenobuterol hydrochloride and pharmaceutic adjuvant, and the ratio of weight and number of active ingredient hydrochloric acid ambroxol and clenobuterol hydrochloride is 2: 1-10: 1.Preferred 2: 1-5: 1 best proportioning is 3.75: 1.
The ratio of weight and number of active ingredient hydrochloric acid ambroxol and clenobuterol hydrochloride and pharmaceutic adjuvant is 1: 5-100, and preferred 1: 5-1: 50 wherein, and preferred every single dose medicine carrying content is 7.5: 2mg-30: 12mg, preferred 7.5: 2mg-30: 8 the bests are 7.5: 2mg.
Every single dose medicine carrying content of the present invention refers to the specification of each preparation institute pastille.
The oral solid formulation of ambroxol-hydrochloride-containing of the present invention and sulphuric acid clenobuterol hydrochloride 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 further prove compositions of the present invention alleviate aspect the symptoms such as dyspnea that cause because of airway obstructive diseases such as bronchial asthma, chronic bronchitis and emphysema by name with commodity: the disclosed therapeutic effect of compound oral solution of Flxol is suitable, and therapeutic alliance has the obvious synergistic effect.
(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 |
| Dosage form | Repeatedly freezing | 35-40 ℃ of placement | Packing Capacity | Production cost |
| 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.
Instantiation is as follows:
Example 1:(tablet) (100 amount)
Ambroxol hydrochloride 1.5g
Sulphuric acid clenobuterol hydrochloride 0.2g
Lactose 8.0g
Starch 2.0g
Polyvidone 1.0g
Carboxymethyl starch sodium 1.0g
8% starch slurry qs
Magnesium stearate qs
Pulvis Talci qs
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) (100 amounts)
Ambroxol hydrochloride 0.75g
Sulphuric acid clenobuterol hydrochloride 0.2g
Lactose 10.0g
Microcrystalline Cellulose 1.0g
Carboxymethyl starch sodium 1.5g
Aspartame 0.1g
Fructus Citri tangerinae essence 0.1g
2% hypromellose qs
Silicon dioxide qs
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) (100 amount)
Ambroxol hydrochloride 3.0g
Sulphuric acid clenobuterol hydrochloride 0.4g
Mannitol 18.0g
Microcrystalline Cellulose 2.0g
Cross-linking sodium carboxymethyl cellulose, 1.0g
Magnesium stearate qs
Silicon dioxide qs
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:(effervescent tablet) (100 amount)
Ambroxol hydrochloride 1.5g
Sulphuric acid clenobuterol hydrochloride 0.6g
Tartaric acid 5.0g
Sodium bicarbonate 5.0g
Methylcellulose 1.0g
Maltose alcohol 0.5g
Fructus Citri Limoniae essence 0.5g
Pulvis Talci qs
Preparation technology is with embodiment 1.
Example 5:(chewable tablet) (100 amount)
Ambroxol hydrochloride 1.5g
Sulphuric acid clenobuterol hydrochloride 0.4g
Mannitol 8.0g
Sorbitol 3.0g
Polyethylene glycol 6000 (50% ethanol) qs
Stevioside 0.5g
Pericarpium Citri junoris tincture 0.5g
Stearic acid qs
Preparation technology is with embodiment 3.
Example 6:(capsule) (100)
Ambroxol hydrochloride 1.5g
Sulphuric acid clenobuterol hydrochloride 0.4g
Lactose 8.0g
Starch 3.0g
Hypromellose 1.0g
Crosslinked polyvidone 1.0g
1% methylcellulose qs
Magnesium stearate qs
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.
100 bags of example 7:(granules)
Ambroxol hydrochloride 3.0g
Sulphuric acid clenobuterol hydrochloride 0.8g
Lactose 80g
Mannitol 15g
Saccharin sodium 0.5g
Essence 0.5g
2% hypromellose (water) qs
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, 14 mesh sieves are granulated, 55 ℃ of dryings, and 16 mesh sieve granulate are measured heavily packing of bag.
Example 8:(enteric coatel tablets)
Plain tablet recipe
Ambroxol hydrochloride 0.75g
Sulphuric acid clenobuterol hydrochloride 0.2g
Calcium hydrogen phosphate 8.0g
Pregelatinized Starch 2.0g
Sodium carboxymethyl cellulose 1.0g
Carboxymethyl starch sodium 1.0g
2% hypromellose qs
Magnesium stearate qs
Preparation technology is with embodiment 1.
The coating prescription:
Plain sheet 80g
Acrylic resin L100-55 8.0g
Pulvis Talci 2.0g
Titanium dioxide 1.6g
Triethyl citrate qs
95% ethanol adds to 145ml
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.
Claims (8)
1. a compound solid preparation for the treatment of asthma is characterized in that being made up of active ingredient hydrochloric acid ambroxol and clenobuterol hydrochloride and pharmaceutic adjuvant, and the ratio of weight and number of active ingredient hydrochloric acid ambroxol and clenobuterol hydrochloride is 2: 1-10: 1.
2. solid preparation according to claim 1, the ratio of weight and number that it is characterized in that described active component and pharmaceutic adjuvant is 1: 5-100.
3. solid preparation according to claim 1 is characterized in that every single dose medicine carrying content of described ambroxol-hydrochloride-containing and clenobuterol hydrochloride active component is 7.5: 2mg-30: 12mg.
4. solid preparation according to claim 1 is characterized in that described preparation comprises conventional tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, chewable tablet, enteric coatel tablets, capsule, granule or enteric coated capsule.
5. solid preparation according to 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 solid preparation of claim 1-4, it is characterized in that described oral solid formulation preparation technology adopts wet granulation or dry granulation.
7. solid preparation according to claim 5 is characterized in that 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.
8. solid preparation according to claim 5 is characterized in that described lubricant comprises one or more compositions of Pulvis Talci, magnesium stearate, stearic acid, micropowder silica gel, hydrogenated vegetable oil, Polyethylene Glycol-4000 or Polyethylene Glycol-6000; Described correctives comprises one or more compositions of sucrose, sorbitol, saccharin sodium, maltose alcohol, steviol glycosides, aspartame; Described aromatic comprises natural aromatic agent, Herba Menthae, Pericarpium Citri junoris tincture or Oleum Cinnamomi; Artificial fragrant spermatophore is drawn together Fructus Citri tangerinae essence, flavoring banana essence or Fructus Citri Limoniae essence.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810152555A CN101756947A (en) | 2008-10-29 | 2008-10-29 | Compound solid preparation for treating asthma |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810152555A CN101756947A (en) | 2008-10-29 | 2008-10-29 | Compound solid preparation for treating asthma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101756947A true CN101756947A (en) | 2010-06-30 |
Family
ID=42488431
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200810152555A Pending CN101756947A (en) | 2008-10-29 | 2008-10-29 | Compound solid preparation for treating asthma |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101756947A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101961307A (en) * | 2010-09-14 | 2011-02-02 | 武汉人福药业有限责任公司 | Oral liquid for treating respiratory disease and preparation method thereof |
| CN102772395A (en) * | 2011-05-09 | 2012-11-14 | 中国人民解放军军事医学科学院毒物药物研究所 | Sustained release preparation containing ambroxol hydrochloride and clenbuterol hydrochloride, and preparation method thereof |
| CN111346063A (en) * | 2020-03-13 | 2020-06-30 | 南京嘉晨医药科技有限公司 | Chewable tablet containing ambroxol hydrochloride and clenbuterol hydrochloride and preparation method thereof |
| CN113975259A (en) * | 2021-09-14 | 2022-01-28 | 南京海纳医药科技股份有限公司 | Ambroxol hydrochloride compound effervescent tablet and preparation method thereof |
| CN115137695A (en) * | 2021-03-29 | 2022-10-04 | 成都倍特药业股份有限公司 | Ammoniumbromoterio liquid preparation and preparation method thereof |
-
2008
- 2008-10-29 CN CN200810152555A patent/CN101756947A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101961307A (en) * | 2010-09-14 | 2011-02-02 | 武汉人福药业有限责任公司 | Oral liquid for treating respiratory disease and preparation method thereof |
| CN101961307B (en) * | 2010-09-14 | 2012-07-25 | 武汉人福药业有限责任公司 | Oral liquid for treating respiratory disease and preparation method thereof |
| CN102772395A (en) * | 2011-05-09 | 2012-11-14 | 中国人民解放军军事医学科学院毒物药物研究所 | Sustained release preparation containing ambroxol hydrochloride and clenbuterol hydrochloride, and preparation method thereof |
| CN111346063A (en) * | 2020-03-13 | 2020-06-30 | 南京嘉晨医药科技有限公司 | Chewable tablet containing ambroxol hydrochloride and clenbuterol hydrochloride and preparation method thereof |
| CN115137695A (en) * | 2021-03-29 | 2022-10-04 | 成都倍特药业股份有限公司 | Ammoniumbromoterio liquid preparation and preparation method thereof |
| CN113975259A (en) * | 2021-09-14 | 2022-01-28 | 南京海纳医药科技股份有限公司 | Ambroxol hydrochloride compound effervescent tablet and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101099729B (en) | Oral solid preparation containing ambroxol hydrochloride and salbutamol active components | |
| CN101129346B (en) | Ambroxol hydrochloride oral cavity disintegrating tablet and method of producing the same | |
| CN103446450A (en) | Composition capable of relieving physical fatigue and preparation method of composition | |
| CN101756947A (en) | Compound solid preparation for treating asthma | |
| CN107913256A (en) | A kind of macitentan oral disnitegration tablet for treating pulmonary hypertension and preparation method thereof | |
| CN101099730A (en) | Oral solid preparation containing ambroxol hydrochloride and guaifenesin active components | |
| CN103070865A (en) | Oral solid preparation taking prucalopride succinate as active ingredient and application of oral solid preparation | |
| CN101904827A (en) | Orally disintegrating tablet of ambroxol hydrochloride and preparation method thereof | |
| CN101167723B (en) | Valsartan dispersible tablet and preparation method thereof | |
| CN102727456B (en) | Drug port cavity disintegrating tablet and preparation method thereof | |
| CN101401796A (en) | Pramipexole orally disintegrating tablets and preparation method thereof | |
| CN101756946A (en) | Oral solid preparation for treating chronic bronchitis | |
| CN101642461B (en) | Drug composition of iguratimod and glucosamine, preparation method and drug application thereof | |
| CN101982174A (en) | Formula of compound medicine preparation for relieving cough and preventing asthma and preparation method thereof | |
| CN102846555A (en) | Solid preparation comprising pirfenidone as active component and application thereof | |
| CN101352440B (en) | Guaifenesin, pseudoephedrine hydrochloride and dextromethorphan hydrobromide sustained-release preparation and preparation method thereof | |
| CN103800290A (en) | Glucosamine hydrochloride pellet preparation and preparation method thereof | |
| CN103040835B (en) | A kind of Pharmaceutical composition containing sildenafil citrate and preparation method thereof | |
| CN102058587A (en) | Solid preparation for treating asthma | |
| CN100386086C (en) | Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process | |
| CN1985807A (en) | Compound Desloratadine-Ambroxol oral disintegrated tablet and its preparing method | |
| CN102772455A (en) | Seabuckthorn flavone dispersible tablets | |
| CN101176730A (en) | Pharmaceutical composition and technique of preparing the same | |
| CN110755521B (en) | Weisu effervescent tablet and preparation method thereof | |
| CN102058611A (en) | Compound solid preparation for treating asthma |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20100630 |