CN101756946A - Oral solid preparation for treating chronic bronchitis - Google Patents
Oral solid preparation for treating chronic bronchitis Download PDFInfo
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- CN101756946A CN101756946A CN200810152550A CN200810152550A CN101756946A CN 101756946 A CN101756946 A CN 101756946A CN 200810152550 A CN200810152550 A CN 200810152550A CN 200810152550 A CN200810152550 A CN 200810152550A CN 101756946 A CN101756946 A CN 101756946A
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- oral solid
- solid formulation
- hydrochloride
- ambroxol
- ephedrine hydrochloride
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Abstract
The invention discloses an oral solid preparation containing active ingredients of ambroxolhydrochloride and ephedrine hydrochloride, which comprises the active ingredients of the ambroxolhydrochloride and the ephedrine hydrochloride and auxiliary materials. The proportion of the active ingredients of the ambroxolhydrochloride to the ephedrine hydrochloride is 2:1-5:1, the proportion of the active ingredients to the auxiliary materials is 1:5-50, and preferably, the medicine carrying content in each preparation is 6:2mg-25:12mg. The oral solid preparation containing the active ingredients of the ambroxolhydrochloride and the ephedrine hydrochloride has the characteristics of stable placing, convenient carrying, production cost reduction and more suitability for big production. The oral solid preparation has remarkable synergism function on the aspects of relieving dyspnea caused by bronchial asthma, chronic bronchitis, pulmonary 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 ephedrine 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 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.
Ephedrine hydrochloride, chemical name: (1R, 2S)-2-methylamino-phenylpropyl alcohol alkane-1-alcohol hydrochloride
Ephedrine can directly act on two kinds of receptors of α, β, and the effect of performance adrenomimetic drug also can impel the adrenergic nerve tip to discharge chemical mediator, brings into play the adrenomimetic drug effect indirectly.Compare with epinephrine, the characteristics of ephedrine are stable in properties, and oral effectively effect is weak and lasting, and the central excitation effect is more remarkable.Have effects such as lax bronchial smooth muscle, excited heart, vasoconstrictive, rising blood pressure.Clinically be used for the hypotension that bronchial asthma, subarachnoid anesthesia or epidural anesthesia cause and remove nasal mucosa hyperemia, edema.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 are share, single one of using, curative effect is more definite, has certain synergism aspect the symptoms such as dyspnea that cause because of airway obstructive diseases such as bronchial asthma, chronic bronchitis and emphysema alleviating.
Summary of the invention
Consider the synergism of ambroxol hydrochloride and ephedrine hydrochloride, 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 ephedrine hydrochloride active component.
Being implemented of the technology of the present invention by following content:
The oral solid formulation of ambroxol-hydrochloride-containing and ephedrine hydrochloride active component is characterized in that being made up of active ingredient hydrochloric acid ambroxol and ephedrine hydrochloride and pharmaceutic adjuvant.Active ingredient hydrochloric acid ambroxol and ephedrine hydrochloride 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 ephedrine hydrochloride and pharmaceutic adjuvant is 1: 5-50, and preferred 1: 5-1: 30 wherein, and preferred every single dose medicine carrying content is 6: 2mg-25: 12mg, preferred 6: 2mg-10: 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 ephedrine 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 production cost is lower, and technology 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 |
| Dosage form | Repeatedly freezing | 35-40 ℃ of placement | Packing Capacity | Production cost |
| 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
Ephedrine hydrochloride 0.2g
Lactose 9.0g
Starch 3.0g
Polyvidone 2.0g
Carboxymethyl starch sodium 2.5g
8% starch slurry qs
Magnesium stearate qs
Pulvis Talci 0.5
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)
Ambroxol hydrochloride 0.6g
Ephedrine hydrochloride 0.1g
Microcrystalline Cellulose 1.0g
Carboxymethyl starch sodium 1.5
Aspartame 0.2g
Fructus Citri tangerinae essence 0.3g
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)
Ambroxol hydrochloride 3.0g
Ephedrine hydrochloride 0.4g
Microcrystalline Cellulose 1.0g
Cross-linking sodium carboxymethyl cellulose, 2.0g
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:(capsule)
Ambroxol hydrochloride 1.5g
Ephedrine hydrochloride 0.4g
Lactose 6.0g
Starch 2.0g
Hypromellose 3.0g
Crosslinked polyvidone 4.0g
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.
Example 5:(enteric coatel tablets)
Plain tablet recipe
Ambroxol hydrochloride 0.75g
Ephedrine hydrochloride 0.2g
Calcium hydrogen phosphate 8.0g
Pregelatinized Starch 2.0g
Sodium carboxymethyl cellulose 2.0g
2% hypromellose qs
Magnesium stearate qs
Preparation technology is with embodiment 1.
The coating prescription:
Plain sheet 60g
Acrylic resin L100-55 7.0g
Pulvis Talci 2.5g
Titanium dioxide 1.1g
Triethyl citrate qs
95% ethanol adds to 150ml
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 ephedrine hydrochloride (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 4 (A) | ??14.2％ | ??23.8％ | ??53.1％ | ??79.6％ | ??95.4％ | ??98.9％ | ??96.3％ |
| Example 4 (B) | ??27.8％ | ??50.1％ | ??75.2％ | ??89.9％ | ??99.2％ | ??97.4％ | ??100.1％ |
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. the oral solid formulation of ambroxol-hydrochloride-containing and ephedrine hydrochloride active component, it is characterized in that being made up of active ingredient hydrochloric acid ambroxol and ephedrine hydrochloride and pharmaceutic adjuvant, the ratio of weight and number of active ingredient hydrochloric acid ambroxol and ephedrine hydrochloride 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 |
|---|---|---|---|
| CN200810152550A CN101756946A (en) | 2008-10-29 | 2008-10-29 | Oral solid preparation for treating chronic bronchitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810152550A CN101756946A (en) | 2008-10-29 | 2008-10-29 | Oral solid preparation for treating chronic bronchitis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101756946A true CN101756946A (en) | 2010-06-30 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200810152550A Pending CN101756946A (en) | 2008-10-29 | 2008-10-29 | Oral solid preparation for treating chronic bronchitis |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105343040A (en) * | 2015-12-08 | 2016-02-24 | 青岛正大海尔制药有限公司 | Preparation method of ambroxol salbutamol powder |
| WO2017101696A1 (en) * | 2015-12-17 | 2017-06-22 | 侯丽芳 | Western medicine composition for treating acute and chronic dyspnea and preparation method thereof |
| CN108042593A (en) * | 2017-12-29 | 2018-05-18 | 广州仁恒医药科技股份有限公司 | A kind of pharmaceutical composition containing ambroxol and preparation method thereof |
-
2008
- 2008-10-29 CN CN200810152550A patent/CN101756946A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105343040A (en) * | 2015-12-08 | 2016-02-24 | 青岛正大海尔制药有限公司 | Preparation method of ambroxol salbutamol powder |
| CN105343040B (en) * | 2015-12-08 | 2018-06-05 | 青岛正大海尔制药有限公司 | The preparation method of ambroxol salbutamol powder |
| WO2017101696A1 (en) * | 2015-12-17 | 2017-06-22 | 侯丽芳 | Western medicine composition for treating acute and chronic dyspnea and preparation method thereof |
| CN108042593A (en) * | 2017-12-29 | 2018-05-18 | 广州仁恒医药科技股份有限公司 | A kind of pharmaceutical composition containing ambroxol and preparation method thereof |
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Open date: 20100630 |