CN101502656A - Composition for eliminating bitter taste of soluble and stable macrolides medicament - Google Patents
Composition for eliminating bitter taste of soluble and stable macrolides medicament Download PDFInfo
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- CN101502656A CN101502656A CN 200810154399 CN200810154399A CN101502656A CN 101502656 A CN101502656 A CN 101502656A CN 200810154399 CN200810154399 CN 200810154399 CN 200810154399 A CN200810154399 A CN 200810154399A CN 101502656 A CN101502656 A CN 101502656A
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Abstract
The invention relates to a soluble and stable composition added to macrolides medicine for removing bitterness of medicine. The composition is composed of the following components: a screening agent and a flavoring agent; the composition can obviously reduce the bitterness of the macrolides medicine or enable people to hardly feel the bitterness; in addition, the pharmaceutical preparation of the composition is stable and measurement of the medicine is not affected; furthermore, the composition can also be applied to bitter oral medicinal composition, food, cosmetics and feed.
Description
Technical field
The present invention has invented a kind of solvable and stable Macrocyclolactone lactone kind medicine composition for eliminating bitter taste, said composition can be water-soluble, and its bitterness can be covered or eliminate to the stable in properties in solution when it joins in the Macrocyclolactone lactone kind medicine of bitterness.
Background technology
In people or the poultry medication a lot of active agents are arranged, when oral, can produce undesirable bitterness, abnormal flavour immediately.The medicine that belongs to this class has tilmicosin, avilamycin, ivermectin, praziquantel, albendazole, penicillin, A Xi mycin, cimetidine, diphenhydramine, erythromycin, ibuprofen, ranitidine, theophylline etc., and covering of the Macrocyclolactone lactone kind medicine bitterness that bitterness is heavier is a great problem always.And the normally preferred route of administration of peroral dosage form administration, because oral administration is convenient, cost is low, but because the bitterness of medicine, people or poultry may not be obedient to, thus refusing to eat.Conventional way is to utilize sweeting agent and flavorant to come taste masking, overwhelm any bitterness by giving the another kind of taste of compositions with it, this method can be covered the more weak medicine of bitterness sometimes, and traditional sweeting agent does not for example often have effect during the bitterness of tilmicosin covering the medicament with strong bitterness.
CN1709513A discloses a kind of medicine production method of not having bitter taste and peculiar smell, to make solution to medicine, slowly add beta-schardinger dextrin-then, the method can be covered drug flavor and bitterness, but will make solution to medicine earlier, a lot of medicines are not diffluent, secondly, this method adds that medicine still be a liquid state behind beta-schardinger dextrin-, make the complex process of solid, shaped medicine or infeasible.CN1222316C discloses the oral preparation composition that alleviates the egg allene sodium bitterness, its bitterness screening agent is aminoalkyl methacrylate copolymer and/or glutamic acid compounds, both are chemicals, using dosage control with great difficulty not causing drug anaphylaxis.CN1065415C discloses protein-lipoid complex, the method that is used to improve the method for the sense of taste and lowers bitterness, and this method is only applicable to lower the bitterness that acid-addition salts presented of alkalescent medicine, and complex more complicated in preparation process.Given this, the present invention is primarily aimed at Macrocyclolactone lactone kind medicine, has invented a kind of compositions that can cover its bitterness, and compositions can be water-soluble, and formed pharmaceutical preparation is stable, does not influence medicine assay.
Summary of the invention
The applicant to the property research of bitterness screening agent, excipient, correctives, bitterness medicine and Macrocyclolactone lactone kind medicine, pays performing creative labour by for a long time, has developed compositions of the present invention.
Use of the present invention can significantly reduce the bitterness of Macrocyclolactone lactone kind medicine, improves the acceptability of pharmaceutical preparation.
The present invention does not contain the sucrose component that other diabetics is worried, compositions can be used for making powder, soluble powder, granule, capsule, tablet and effervescent tablet, liquid preparation etc., thereby has realized the present invention.
The characteristics of the present composition and preparation thereof are that different fully with the technology of the inclusion method solution adverse drug taste of taking in the past, only the mode by drug regimen has promptly solved specific abnormal flavour and bitterness that Macrocyclolactone lactone kind medicine has; Adopt the often numerous and diverse effort of inclusion method, the production of this preparation adopts general preparation equipment and common preparation process can realize large-scale industrialization production, need not special installation, and cost reduces, and preparation is simple.
The object of the present invention is to provide a kind of solvable and stable bitter taste of drug composition for eliminating, comprise in per 100 parts of compositionss: screening agent 1-30 part, correctives 0.01-15 part.Screening agent can be selected one or both in betanin, the maltodextrin, and correctives can be selected one or more in stevioside, sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, the disodium glycyrrhizinate.
Preferred compound additive comprises in per 100 parts of compositionss: stevioside 1-5 part, hydroxyproline 0.01-1 part, ethyl maltol 0.01-3 part, maltodextrin 1-30 part.
Screening agent can also be betanin, maltodextrin and various forms of derivant thereof, and correctives can also be sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, disodium glycyrrhizinate and various forms of derivant thereof.
After composition for eliminating bitter taste and the combination of solubility Macrocyclolactone lactone kind medicine, can alleviate or cover fully the bitterness of Macrocyclolactone lactone kind medicine.
After the combination of composition for eliminating bitter taste and solubility Macrocyclolactone lactone kind medicine, water soluble, properties of Aqueous Solution is stable, and interference medicament assay not.
Solvable and stable bitter taste of drug composition for eliminating can be made different dosage form, as powder, soluble powder, granule, capsule, tablet, effervescent, injection etc.
Composition for eliminating bitter taste can be used for preparing oral medication compositions, food, cosmetics or feedstuff.
The object of the present invention is to provide a kind of preparation to cover the preparation of pharmaceutical compositions method of Macrocyclolactone lactone kind medicine bitterness, thereby strengthening people or poultry is acceptable to medicine, comprise: the screening agent and the correctives that take by weighing recipe quantity respectively, screening agent and correctives are fully mixed, promptly get compositions of additives.
In contrast test, discovery is in Macrocyclolactone lactone kind medicine, only add screening agent, do not add in correctives such as stevioside, sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, the disodium glycyrrhizinate one or more, obtained medicinal mixture is through the taste taste test, the result does not cover the distinctive abnormal flavour of Macrocyclolactone lactone kind medicine, show, correctives and screening agent be used the effect of covering, correcting bitter taste and peculiar smell that can bring into play.
Compositions of additives of the present invention can be made people's medicine, the acceptable multiple dosage form of field of veterinary, comprises powder, soluble powder, granule, capsule, tablet, effervescent, injection etc.
The specific embodiment
Following examples are in order to embodiment preferred of the present invention to be described, ability technical staff should be appreciated that following description shall not be applied to restriction protection scope of the present invention.
The phosphoric acid tilmicosin bitterness shading composition that embodiment 1. is solvable and stable
Prescription: phosphoric acid tilmicosin 10kg, stevioside 2kg, hydroxyproline 0.05kg, ethyl maltol 2.5kg, maltodextrin 20kg, white shallow lake dimension powder adds to 100kg.
Method for making: earlier the 10kg maltodextrin is fully mixed with the phosphoric acid tilmicosin, remaining maltodextrin dilutes stevioside, hydroxyproline, ethyl maltol respectively once simultaneously with coubling dilution, said mixture is fully mixed promptly getting the pharmaceutical composition of covering bitter taste and peculiar smell with white shallow lake dimension powder.
The preparation of embodiment 2. medicines is that 1500g calculates with every part.Prescription: 10 parts of tylosin tartrates, 8 parts of sulfadiazine sodiums, 15 parts of maltodextrins, 1 part of betanin, 0.1 part of sorbitol, betonicine 0.1,1 part of ethyl maltol, 1 part of disodium glycyrrhizinate, 10 parts of PVP, dehydrated alcohol are an amount of, oral glucose adds to 100 parts.Carry out the preparation of granule by following technology:
(1) takes by weighing each component according to weight, adopt the equivalent dilution method with anhydrous glucose dilution each powdery components except that PVP, the supplementary material mixing, obtain mixture A after stirring;
(2) with PVP molten with dehydrated alcohol in, mix homogeneously obtains mixture B;
(3) mixture B is slowly poured among the mixture A, do and wetly to granulate with 14 mesh sieves when suitable, behind the particle drying, carry out granulate, promptly get the medicament composition granule that the solubility compound soluble does not have bitter taste and peculiar smell with 16 mesh sieves.
Change kind, the ratio of Macrocyclolactone lactone kind medicine medicine among the embodiment 1,2, change the ratio and the kind of above-mentioned correctives, can obtain different pharmaceutical compositions.Adopt these pharmaceutical compositions, according to common preparation process, requirement according to different dosage form, add different adjuvants, Macrocyclolactone lactone kind medicine powder after can making bitter taste and peculiar smell respectively and covering, soluble powder, granule, capsule, tablet, effervescent, injection etc., obtained various pharmaceutical compositions all meet the prescription of Chinese Pharmacopoeia.
Embodiment 3. taste taste tests
Test specimen: embodiment 1 pharmaceutical composition, embodiment 2 pharmaceutical compositions divide and following two kinds of compositionss.
Embodiment 1 control drug: prescription is phosphoric acid tilmicosin 10kg, and white shallow lake dimension powder adds to 100kg, and supplementary material fully mixes promptly.
Embodiment 2 control drug: prescription is that 10 parts of tylosin tartrates, 8 parts of sulfadiazine sodiums, PVP10 part, dehydrated alcohol are an amount of, oral glucose adds to 100 parts, (1), (2) among the same embodiment 2 of method for making, (3) step.
Get embodiment 1, embodiment's 2 and do not add the control drug of correctives, respectively get 1g respectively and add in 20ml20 ℃～40 ℃ water, stir evenly; 5 male and 5 women of choosing 20 to 40 age brackets carry out sensory test.By following standard bitterness is evaluated as six grades and represent by meansigma methods.
Bitterness intensity 6: extremely bitter
Bitterness intensity 5: very bitter
Bitterness intensity 4: hardship, but not strong
Bitterness intensity 3: bitter slightly
Bitterness intensity 2: can feel bitter
Bitterness intensity 1: not bitter
From the taste test result as can be seen, behind adding screening agent, the correctives, the bitterness of bitterness medicine significantly reduces, and compositions has the bridging effect of fine bitter taste and peculiar smell.
The accelerated stability test of embodiment 4. embodiment 1 pharmaceutical composition
According to the Chinese Pharmacopoeia method, the pharmaceutical composition among the embodiment 1 has been carried out accelerated stability test.Three batches of commercially available back samples, under the condition of 40 ℃ ± 2 ℃ of temperature, relative humidity 75% ± 5%, placed 6 months, detected appearance character, moisture, active constituent content respectively in the 1st, 3,6 month, the every index of result is all up to specification, compared basic no change with 0 month, show that pharmaceutical composition is more stable, correctives is to not influence of medicine.
Claims (7)
1. solvable and stable Macrocyclolactone lactone kind medicine composition for eliminating bitter taste, be mainly used in the bitterness that covers, corrects Macrocyclolactone lactone kind medicine, its screening agent comprises one or both in betanin, the maltodextrin, and correctives comprises one or more in stevioside, sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, the disodium glycyrrhizinate.
2. according to claim 1, screening agent can be betanin, maltodextrin and various forms of derivant thereof, and correctives can be inulin, sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, disodium glycyrrhizinate and various forms of derivant thereof.
3, according to claim 1, it is characterized in that comprising in per 100 parts of compositionss: screening agent 1-30 part, correctives 0.01-15 part, screening agent can be selected from one or more of betanin, maltodextrin and various forms of derivants thereof, and correctives can be selected one or more of stevioside, sorbitol, betonicine, hydroxyproline, glycogen, saccharin sodium, ethyl maltol, disodium glycyrrhizinate and various forms of derivants thereof.Comprise in preferred per 100 parts of compositionss: stevioside 1-5 part, hydroxyproline 0.01-1 part, ethyl maltol 0.01-3 part, maltodextrin 1-30 part.
4,, after composition for eliminating bitter taste and the combination of solubility Macrocyclolactone lactone kind medicine, can alleviate or cover fully the bitterness of Macrocyclolactone lactone kind medicine according to claim 1,2 described.
5, according to claim 1,2 described, after composition for eliminating bitter taste and the combination of solubility Macrocyclolactone lactone kind medicine, water soluble, properties of Aqueous Solution is stable, and interference medicament assay not.
6, according to claim 1,2,3 described, solvable and stable bitter taste of drug composition for eliminating can be made different dosage form, as powder, soluble powder, granule, capsule, tablet, effervescent, injection etc.
7, according to claim 1,2,3 described, composition for eliminating bitter taste can be used for preparing oral medication compositions, food, cosmetics or feedstuff.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200810154399 CN101502656B (en) | 2008-12-24 | 2008-12-24 | Composition for eliminating bitter taste of soluble and stable macrolides medicament |
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| CN 200810154399 CN101502656B (en) | 2008-12-24 | 2008-12-24 | Composition for eliminating bitter taste of soluble and stable macrolides medicament |
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| CN101502656A true CN101502656A (en) | 2009-08-12 |
| CN101502656B CN101502656B (en) | 2013-05-29 |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028098A (en) * | 2010-11-19 | 2011-04-27 | 重庆民泰香料化工有限责任公司 | Feed sweetener |
| EP2641477A1 (en) * | 2012-03-19 | 2013-09-25 | Symrise AG | Compositions of matter |
| CN108719321A (en) * | 2018-08-06 | 2018-11-02 | 山东华实药业有限公司 | A kind of stability disinfection tablet and its manufacture craft |
| CN109985054A (en) * | 2017-12-29 | 2019-07-09 | 瑞普（天津）生物药业有限公司 | A kind of band regulation layer gel skeleton type ivermectin sustained release tablets |
| CN109999201A (en) * | 2019-04-19 | 2019-07-12 | 成都中医药大学 | A kind of novel taste masking companion agent and application thereof |
| CN111248369A (en) * | 2020-01-22 | 2020-06-09 | 北京千菌方菌物科学研究院 | Preparation method of hericium erinaceus beverage |
| CN112618492A (en) * | 2020-12-15 | 2021-04-09 | 四川乾通动物药业有限公司 | Albendazole ivermectin powder and preparation method thereof |
| US11700870B2 (en) | 2016-09-02 | 2023-07-18 | Tate & Lyle Solutions Usa Llc | Use of tri- and tetra-saccharides as taste modulators |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1631371A (en) * | 2004-12-20 | 2005-06-29 | 李�杰 | Oral administered bitter free powder of macrolide antibiotic, its prescription and preparation process |
| CN101084890A (en) * | 2007-07-02 | 2007-12-12 | 北京因科瑞斯生物制品研究所 | Ginkgo flavone and lactone dispersion tablet and preparation method thereof |
-
2008
- 2008-12-24 CN CN 200810154399 patent/CN101502656B/en active Active
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028098A (en) * | 2010-11-19 | 2011-04-27 | 重庆民泰香料化工有限责任公司 | Feed sweetener |
| CN102028098B (en) * | 2010-11-19 | 2012-10-17 | 重庆民泰香料化工有限责任公司 | Feed sweetener |
| EP2641477A1 (en) * | 2012-03-19 | 2013-09-25 | Symrise AG | Compositions of matter |
| US8828473B2 (en) | 2012-03-19 | 2014-09-09 | Symrise Ag | Substance mixtures |
| US11700870B2 (en) | 2016-09-02 | 2023-07-18 | Tate & Lyle Solutions Usa Llc | Use of tri- and tetra-saccharides as taste modulators |
| CN109985054A (en) * | 2017-12-29 | 2019-07-09 | 瑞普（天津）生物药业有限公司 | A kind of band regulation layer gel skeleton type ivermectin sustained release tablets |
| CN108719321A (en) * | 2018-08-06 | 2018-11-02 | 山东华实药业有限公司 | A kind of stability disinfection tablet and its manufacture craft |
| CN109999201A (en) * | 2019-04-19 | 2019-07-12 | 成都中医药大学 | A kind of novel taste masking companion agent and application thereof |
| CN109999201B (en) * | 2019-04-19 | 2023-02-17 | 成都中医药大学 | Taste-masking mate agent and application thereof |
| CN111248369A (en) * | 2020-01-22 | 2020-06-09 | 北京千菌方菌物科学研究院 | Preparation method of hericium erinaceus beverage |
| CN112618492A (en) * | 2020-12-15 | 2021-04-09 | 四川乾通动物药业有限公司 | Albendazole ivermectin powder and preparation method thereof |
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|---|---|
| CN101502656B (en) | 2013-05-29 |
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