CN1994304A - Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof - Google Patents
Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof Download PDFInfo
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- CN1994304A CN1994304A CN 200610167781 CN200610167781A CN1994304A CN 1994304 A CN1994304 A CN 1994304A CN 200610167781 CN200610167781 CN 200610167781 CN 200610167781 A CN200610167781 A CN 200610167781A CN 1994304 A CN1994304 A CN 1994304A
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- loratadine
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- ambroxol
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Abstract
The invention relates to a luleitadingmione oral calving tablet which can treat allergic rhinitis, etc. wherein, it has quick adsorption, high biological utilization, and simple intake method without water. It uses Loratadine and bromamine acid as materials, with some findings.
Description
Technical field
The present invention relates to a kind ofly be used to alleviate, as sneeze, watery nasal discharge, rhinocnesmus, the compound orally disintegrating tablet containing loratadine and ambroxol of shedding tears etc. and preparation method thereof with the cough of abnormal secretion thing and the relevant symptom of allergic rhinitis.
Background technology
Ambroxol hydrochloride is the respiratory mucus regulator of a new generation, also is to act on the strongest expectorant at present clinically.Have 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.
Loratadine is the long-acting tricyclic antidepressants antihistaminic of non-sedating, is the active metabolite of loratadine, can pass through optionally antagonism peripheral H1-receptor, alleviates seasonal allergic rhinitis or the urticarial related symptoms of chronic idiopathic.In addition, results of in vitro studies, this product can suppress histamine and discharge from people's mastocyte.The zooscopy prompting, this product is difficult for passing through blood brain barrier.This product oral absorption rapidly, good, 1.5 hours blood drug level peakings, most of through liver metabolism, its metabolite is still had an activity, original shape medicine and metabolite are from urine and feces discharge.
Oral cavity disintegration tablet is a kind of new pharmaceutical dosage forms, is that a kind of water that do not need in the oral cavity can disintegrate or dissolved tablet.It can be in the oral cavity rapidly disintegrate, no grittiness, good mouthfeel, swallow easily, to the oral mucosa nonirritant.The distinguishing feature of this dosage form: 1. absorption is fast, bioavailability is high; 2. instructions of taking does not need water, makes things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment; 3. intestinal is residual few, few side effects; 4. avoid the first pass effect in liver sausage road.
By retrieval, do not see the pertinent literature and the patent report of relevant compound orally disintegrating tablet containing loratadine and ambroxol.
Summary of the invention
The purpose of this invention is to provide a kind of disintegrate fast, absorb rapidly, can effectively improve the bioavailability and the blood drug level of active constituents of medicine, improve compound orally disintegrating tablet containing loratadine and ambroxol of the special bitter in the mouth of ambroxol hydrochloride, taking convenience and preparation method thereof simultaneously.
Compound orally disintegrating tablet containing loratadine and ambroxol of the present invention also contains adjuvant except principal agent.Adjuvant is any available adjuvant that is fit to make oral cavity disintegration tablet, and they can comprise filler, disintegrating agent, effervescent, correctives or odor mask, binding agent, lubricant etc.In each oral formulations unit, the amount that contains loratadine is 1.25-20mg, is preferably 2.5-10mg, and the amount that contains the active ingredient hydrochloric acid ambroxol is 10-90mg.Be preferably 20-60mg.The ratio of two kinds of active component is 1: 24-2: 3.
The amount that each preparation unit of the present invention contains the active component loratadine is 5mg more preferably, and the amount of ambroxol hydrochloride is 30mg more preferably.The ratio of two kinds of active component more preferably 1: 6.
Because oral cavity disintegration tablet requires disintegrate rapidly in the oral cavity, good mouthfeel, to the oral mucosa nonirritant.Therefore the selection to supplementary product kind and performance thereof is the key of preparation oral cavity disintegration tablet.
The present invention is through selecting, found the pharmaceutic adjuvant of suitable compound orally disintegrating tablet containing loratadine and ambroxol, wherein filler selects to be used for increasing the weight and volume of oral cavity disintegration tablet, so that the molding of preparation and divided dose, the preferred mixture of one or more in starch, lactose, dextrin, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, xylitol etc. of filler among the present invention.
The kind of disintegrating agent and the selection of consumption are for can this preparation disintegrate be most important fully at the appointed time.Disintegrating agent of the present invention selects to comprise a kind of or wherein several mixture in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, pregelatinized Starch, the carboxymethyl starch sodium.
In oral cavity disintegration tablet, can add an amount of effervescent, help the disintegrate of tablet, and an amount of acid can also be regulated taste.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the effervescent that the present invention selects, and alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.
When the percentage by weight of principal agent in preparation is higher, owing to bitterness may occur, therefore can select to add an amount of odor mask so that the patient accepts and takes, odor mask of the present invention comprises one or more the mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, hard paraffin, the Brazil wax.
The correctives that the present invention uses one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, stevioside, the acesulfame-K or wherein several mixture.
The adding of binding agent and lubricant is for the ease of the preparation of preparation and molding.Binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution.Lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci.
Oral cavity disintegration tablet of the present invention can be by freeze-drying or direct powder compression or granulating tabletting process preparation.
Adopt freeze-drying to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, correctives and odor mask (if necessary), compound recipe loratadine ambroxol can be mixed with various adjuvants, add the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization, being shaped to the material lyophilizing gets final product.
Adopt direct powder compression to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, lubricant, correctives and odor mask, and behind loratadine, ambroxol hydrochloride and various adjuvant mix homogeneously, direct powder compression gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, binding agent, lubricant, correctives and odor mask, with loratadine, ambroxol hydrochloride and partial supplementary material mix homogeneously, add binding agent system soft material, granulate dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, binding agent, lubricant, correctives and odor mask, the main method step is: acid source in the effervescent and alkali source can be separated granulation, or acid source mixed with alkali source, adopt dehydrated alcohol to granulate, dry, granulate, the disintegrating agent and the lubricant of adding surplus as binding agent, behind the mix homogeneously, tabletting gets final product.
The specific embodiment
Come compound orally disintegrating tablet containing loratadine and ambroxol of the present invention done further specifying by following example, but be not limited in following example.
Embodiment 1
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
Polyvinylpolypyrrolidone 55g
Mannitol 45g
Eudragit?L30D 15g
Aspartame 2.5g
Make 1000 altogether
Preparation method:
Loratadine, ambroxol hydrochloride are added in the Eudragit L30D suspension, add suitable quantity of water, after stirring, add polyvinylpolypyrrolidone, mannitol, aspartame, the limit edged stirs, and behind the one-tenth suspension, is poured in the suitable mould, and is freezing rapidly, drying under reduced pressure, delivery, press seal, packing.
Embodiment 2
Prescription:
Loratadine 10g
Ambroxol hydrochloride 60g
Sucrose 70g
Xanthan gum 16g
Melon glue 24g
Xylitol 80g
Stevioside 5g
Make 1000 altogether
Preparation method:
Loratadine, ambroxol hydrochloride are joined in guar gum and the xanthan gum mixed liquor, after stirring, add sucrose, xylitol, stevioside, after the limit edged stirs and makes into even suspension, be poured in the suitable mould, freezing rapidly, drying under reduced pressure, delivery, press seal, packing.
Embodiment 3
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
L-HPC 4g
PPVP 8g
Sorbitol 120g
Honey peach essence 8g
Magnesium stearate 5g
Make 1000 altogether
Preparation method:
According to the equivalent method mix homogeneously that progressively increases, other mixes with above mixture by the honey peach essence of fetching water with the loratadine, ambroxol hydrochloride, L-HPC, PPVP, sorbitol of all crossing 80 mesh sieves, adding magnesium stearate mix homogeneously, and direct powder compression gets final product.
Embodiment 4
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
Microcrystalline Cellulose 65g
Crospolyvinylpyrrolidone 7g
Sodium bicarbonate 3g
Citric acid 5g
Pulvis Talci 2g
Aspartame 3g
Make 1000 altogether
Preparation method:
Loratadine, ambroxol hydrochloride, microcrystalline Cellulose, sodium bicarbonate, citric acid (drying is crossed) mix homogeneously of 80 mesh sieves will all be crossed, other gets crospolyvinylpyrrolidone, aspartame, Pulvis Talci and adopts the equivalent method of progressively increasing to mix with above mixture, behind the mix homogeneously, the humidity that controls environment is below 35%, direct powder compression gets final product.
Embodiment 5
Prescription:
Loratadine 2.5g
Ambroxol hydrochloride 15g
CMS-Na 10g
Microcrystalline Cellulose 60g
Pregelatinized Starch 20g
Lactose 35g
A Sipa 3g
Fructus Citri Limoniae essence 2g
Magnesium stearate 4.5g
Make 1000 altogether
Preparation method:
To all cross loratadine, ambroxol hydrochloride, aspartame, Fructus Citri Limoniae essence, microcrystalline Cellulose, pregelatinized Starch, lactose, CMS-Na, the magnesium stearate of 80 mesh sieves, mix homogeneously, tabletting gets final product.
Embodiment 6
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
Microcrystalline Cellulose 100g
Xylitol 50g
Stevioside 3.5g
Flavoring orange essence 10.5g
PPVP 16g
PVP-k30 (30% alcoholic solution) is an amount of
Magnesium stearate 7g
Make 1000 altogether
Preparation method:
To all cross loratadine, ambroxol hydrochloride, xylitol, stevioside, flavoring orange essence, the part microcrystalline Cellulose mix homogeneously of 80 mesh sieves,, granulate with PVP-k30 alcohol liquid system soft material, dry, granulate, microcrystalline Cellulose, PPVP, the magnesium stearate of adding surplus, mix homogeneously, tabletting gets final product.
Embodiment 7
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
Microcrystalline Cellulose 80g
Sorbitol 20g
Citric acid 2g
Sodium bicarbonate 4g
Sodium chloride 2g
Acesulfame-K 3g
The PVP-k30 ethanol solution is an amount of
CMS-Na 2g
PEG6000 3g
Make 1000 altogether
Preparation method:
With all crossing loratadine, ambroxol hydrochloride, sorbitol, microcrystalline Cellulose, citric acid, the sodium bicarbonate mix homogeneously of 80 mesh sieves,, granulate with PVP-K30 anhydrous alcohol solution system soft material, dry, granulate add acesulfame-K, sodium chloride, CMS-Na, PEG6000, mix homogeneously, tabletting gets final product.
Embodiment 8
Prescription:
Loratadine 5g
Ambroxol hydrochloride 30g
Lactose 25g
Mannitol 140g
L-HPC 30g
Sodium carbonate 1g
Sodium bicarbonate 4g
Tartaric acid 3g
Orange flavor 5g
Magnesium stearate 5g
Make 1000 altogether
Preparation method:
With all cross 80 mesh sieves loratadine, ambroxol hydrochloride, lactose, 35% mannitol, sodium bicarbonate, sodium carbonate, partly measure the L-HPC mix homogeneously approximately, with 50% ethanol liquid system soft material, granulation, drying, granulate; Other gets surplus 65% mannitol, adds tartaric acid, partly measures L-HPC, and mix homogeneously with 50% ethanol liquid system soft material, is granulated, and dry, granulate behind two kinds of granule mix homogeneously, add orange flavor, magnesium stearate outward, and tabletting behind the mix homogeneously gets final product.
Claims (10)
1. a compound orally disintegrating tablet containing loratadine and ambroxol is characterized in that, said preparation is made up of active component loratadine, ambroxol hydrochloride and suitable pharmaceutic adjuvant.
2. the compositions of claim 1, the amount that described each preparation unit contains the active component loratadine is 1.25-20mg, is preferably 2.5-10mg, the amount that contains the active ingredient hydrochloric acid ambroxol is 10-90mg.Be preferably 20-60mg.The ratio of two kinds of active component is 1: 24-2: 3.
3. the compositions of claim 1, the amount that described each preparation unit contains the active component loratadine is 5mg more preferably, and the amount that contains the active ingredient hydrochloric acid ambroxol is 30mg more preferably.The ratio of two kinds of active component more preferably 1: 6.
4. the described oral cavity disintegration tablet of claim 1 is characterized in that, the described excipient substance that is fit to make oral cavity disintegration tablet comprises one or more in filler, disintegrating agent, effervescent, correctives, odor mask, binding agent or the lubricant etc.
5. the described oral cavity disintegration tablet of claim 3 is characterized in that described filler is selected from one or more the mixture in starch, lactose, dextrin, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, the xylitol.Described disintegrating agent is selected from a kind of or wherein several mixture in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, pregelatinized Starch, the carboxymethyl starch sodium.Acid source is selected from citric acid, tartaric acid, four mixture of one or more in acid, lysine, the arginine in the described effervescent, and alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.Described odor mask is selected from one or more the mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, hard paraffin, the Brazil wax.Described binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution; Described lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci.Described correctives one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside, the acesulfame-K or wherein several mixture.
6. the preparation method of the oral cavity disintegration tablet of claim 1 is characterized in that, adopts the preparation of freeze-drying or direct powder compression or granulating tabletting process.
7. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the preparation process of freeze-drying is: active constituents of medicine loratadine, ambroxol hydrochloride and other adjuvant are added the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization to material lyophilizing is shaped.
8. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the direct powder compression preparation process is: behind mix homogeneously such as loratadine, ambroxol hydrochloride and filler, disintegrating agent, effervescent, lubricant, correctives and odor mask, adopt direct powder compression to be prepared.
9. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the granulating tabletting process preparation process is: with compound recipe loratadine, ambroxol hydrochloride and part disintegrating agent, effervescent, filler, correctives and odor mask, add binding agent system soft material, granulate, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
10. the described preparation method of claim 9, it is characterized in that, the step that wherein adds effervescent is, acid source in the effervescent and alkali source are separated granulation, or acid source is mixed with alkali source, adopt dehydrated alcohol to granulate as binding agent, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610167781 CN1994304A (en) | 2006-11-21 | 2006-12-21 | Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610114672.0 | 2006-11-21 | ||
| CN200610114672 | 2006-11-21 | ||
| CN 200610167781 CN1994304A (en) | 2006-11-21 | 2006-12-21 | Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1994304A true CN1994304A (en) | 2007-07-11 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610167781 Pending CN1994304A (en) | 2006-11-21 | 2006-12-21 | Compound orally disintegrating tablet containing loratadine and ambroxol and preparation process thereof |
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| CN (1) | CN1994304A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324383A (en) * | 2014-09-28 | 2015-02-04 | 南京泽恒医药技术开发有限公司 | Diphenhydramine hydrochloride drug composition and preparation method thereof |
| CN107296800A (en) * | 2017-06-01 | 2017-10-27 | 江苏黄河药业股份有限公司 | A kind of Loratadine effervescent tablet and preparation method thereof |
-
2006
- 2006-12-21 CN CN 200610167781 patent/CN1994304A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324383A (en) * | 2014-09-28 | 2015-02-04 | 南京泽恒医药技术开发有限公司 | Diphenhydramine hydrochloride drug composition and preparation method thereof |
| CN107296800A (en) * | 2017-06-01 | 2017-10-27 | 江苏黄河药业股份有限公司 | A kind of Loratadine effervescent tablet and preparation method thereof |
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| 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: 20070711 |