CN101912613B - Taste masking preparation - Google Patents
Taste masking preparation Download PDFInfo
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- CN101912613B CN101912613B CN2010102352276A CN201010235227A CN101912613B CN 101912613 B CN101912613 B CN 101912613B CN 2010102352276 A CN2010102352276 A CN 2010102352276A CN 201010235227 A CN201010235227 A CN 201010235227A CN 101912613 B CN101912613 B CN 101912613B
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- taste masking
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- clarithromycin
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Abstract
The invention relates to an oral taste masking preparation and a preparation method thereof. The invention is characterized in that an auxiliary material which expands with water is added in the preparation process, owning to the hydro-expansiveness of the auxiliary material, a film is formed in the outer layer of a medicine, thus enabling the medicine to form a shape similar to an frog egg, delaying the contact time between the medicine and body liquid and masking the taste; and an preparation formula and an preparation process of the original product do not need to be changed, and a production spot and a device do not need to be reformed. The preparation method is simple and convenient, and industrialization can be easily achieved.
Description
Technical field
The present invention relates to the medical sci-tech field, definite saying relates to a kind of oral taste masking preparation and preparation method thereof.
Background technology
Pharmaceutical oral dosage form convenient drug administration and cost are low, be the most general present administering mode, but many medicines have hard to bear disagreeable taste, in formulation development and clinical use, have received very big restriction.
Improving constantly of Along with people's living standard, people require increasingly highly to drug quality, and " good medicine tastes bitter " no longer becomes fashion, and people hope to access good drug efficacy, mouthfeel is good and the product of taking convenience, improve the quality of living, and satisfy the body and mind demand.Especially department of pediatrics medication, taste are easy to children's and accept, and can improve the compliance of medication greatly.Therefore, effectively cover the adverse drug taste, improve the quality of products, paid attention to by pharmacy circle personage more and more.The taste masking technology is covered principal agent original disagreeable taste, especially bitterness through the preparation means exactly.
The existing oral taste masking preparation; Generally realize through interpolation correctives, paralyzant, sugar coating or film-coat; But these several kinds the technological taste masking time is relatively short, the taste masking effect is relatively poor; Especially for old man that dysphagia is arranged and child, after medicine time in mouth is long slightly, be easy to feel bitter.Therefore, in order to improve compliance of patients, need further improve the taste masking technology of medicine.
Summary of the invention
The objective of the invention is to overcome short, defective such as the taste masking effect is relatively poor of taste masking time of existing in the prior art, provide that a kind of taste masking is effective, the taste masking time is long, and have the oral formulations of good lubrication property.
The invention provides a kind of taste masking oral formulations, it is characterized in that containing the water-swellable adjuvant.Also promptly in original oral formulations prescription, add the water-swellable adjuvant.
Water-swellable adjuvant wherein is meant that the water-swellable degree is big and can be at the peripheral pharmaceutic adjuvant that forms a skim of framework, such as carbomer.
Wherein the addition of water-swellable adjuvant be the principal agent quality 0.005-4 doubly, preferred 0.03-2 is doubly.The amount that adds the water-swellable adjuvant is many more, and the taste masking time is long more, and effect is good more.Considering not change original preparation process as much as possible, consider problems such as cost simultaneously, the water-swellable adjuvant should add as far as possible less.Preparation prescription after adding the water-swellable adjuvant can keep original prescription constant, also can carry out adaptive fine setting to original prescription.
Taste masking oral formulations provided by the invention can be processed in granule, tablet, capsule, micropill, the dry suspension any.
The invention also discloses the method for preparing the taste masking oral formulations, prepare preparation, when coating, the water-swellable adjuvant is wrapped in the preparation skin with powder type with conventional method.Specifically, prepare preparation by original method exactly, during this step, add the water-swellable adjuvant, make it evenly adhere to the preparation skin with form of powder at coating.Be exactly one side jetting liquid, Yi Bian add water-swellable adjuvant powder, thus water-swellable adjuvant powder can stick on the preparation of moistening.The powder size of water-swellable adjuvant is can not ether big, about 100 orders or littler, otherwise is prone to influence homogeneity.Above coating can carry out with the coating pelletizing machine.
Adopt technical scheme of the present invention to prepare the taste masking oral formulations, can no longer add correctives.
Technical scheme provided by the present invention can be suitable for the principal agent of the principal agent that all have disagreeable taste, particularly bitterness, such as clarithromycin, chloromycetin, chloroquine, Rhizoma Coptidis, brucine, Roxithromycin, fentanyl, orbifloxacin etc.
The invention also discloses the taste masking oral formulations that contains clarithromycin.
Clarithromycin is semisynthetic erythromycin derivatives, and its mechanism of action is through combining the synthetic of impede protein matter with cytoribosome 50 subunits of sensitive organism, and then produces bacteriostasis.Clinically, clarithromycin is widely used in treatment such as upper respiratory tract infection, comprises nasopharynx infection, tonsillitis, pharyngitis, nasal sinusitis etc.; Lower respiratory infection comprises bronchitis, bacterial pneumonia, atypical pneumonia etc.; Skin infection, erysipelas, folliculitis and wound infection, particularly effective to legionella pneumophilia and the caused pneumonia of mycoplasma pneumoniae, be one of first-selected oral antibiotic of clinicist.
At present, clarithromycin has tablet, capsule, dry suspension etc.Because clarithromycin flavor is extremely bitter, existing dosage form to cover the bitter time shorter, cause that to cover bitter effect relatively poor relatively, patient's compliance is not good in clinical practice uses.The present invention has improved its taste masking effect widely through when coating, adding the water-swellable adjuvant.Specifically in Biaxin, contain the water-swellable adjuvant, like card pool nurse.Water-swellable adjuvant quality is 0.005-4 a times of clarithromycin, is preferably 0.03-2 doubly.
When the preparation Biaxin, elder generation is by original prescription, according to existing equipment, and preparation technology prepares, one side jetting liquid when coating, Yi Bian add water-swellable adjuvant powder, thus water-swellable adjuvant powder can stick on the preparation of moistening.The powder size of water-swellable adjuvant is can not ether big, about 100 orders or littler, otherwise is prone to influence homogeneity.
The taste masking oral formulations that contains clarithromycin can be prepared as in granule, tablet, capsule, micropill, the dry suspension any, is particularly suitable for processing tablet and dry suspension.
Taste masking oral formulations provided by the present invention; A kind of new approaches of oral formulations taste masking are provided, promptly in preparation, have added the adjuvant of water-swellable, make preparation meet water after; Stone becomes a skim because of imbibition; Thereby make medicine form the shape of similar Rana ovum, thereby can delay the time of contact of medicine and body fluid, play the taste masking effect.And such adjuvant has good lubricity, helps to swallow, and also played the effect of taste masking indirectly.And it needn't change the preparation prescription and the preparation technology of existing product; Only need on last coating operation, to do one changes slightly; Both guaranteed excellent taste masking effect, guaranteed the pharmacy characteristic of product and the continuity of production again, need not do transformation production site, equipment.Its preparation method is simple, convenient, is easy to industrialization.
The specific embodiment
Below further specify the present invention through embodiment.
Embodiment 1
Embodiment 1 clarithromycin dry suspension
Clamycin 2 5.0g
Icing Sugar 35.0g
Starch 15.0g
Polyvinylpyrrolidone 2.3g
Eudragit E 100 11.2g
Pulvis Talci 5.6g
Carbomer 12.5g
Triethyl citrate 0.6g
Preparation technology: Icing Sugar, starch are processed celphere, are adhesive with the ethanol/water solution of polyvinylpyrrolidone, with the medicine-feeding form clarithromycin are wrapped on the celphere; Use acrylic resin, triethyl citrate and talcous suspension coating then; Spray coating solution on one side, Yi Bian add the carbomer powder, thus the carbomer powder can stick on the ball of moistening; Formation contains the coatings of carbomer, and packing promptly gets.
Embodiment 2 clarithromycin tablets
Clamycin 2 5.0g
Microcrystalline Cellulose 4.7g
Lactose 3.0g
Starch 2.1g
Carboxymethyl starch sodium 2.4g
10% starch slurry 20.0g
Magnesium stearate 0.3g
Opadry 1.2g
Carbomer 25.0g
Preparation technology: at first clarithromycin is placed wet granulator; Add starch, microcrystalline Cellulose, lactose, in add the carboxymethyl starch sodium mix homogeneously, reuse 10% starch slurry wet granulation is after dry, the arrangement; Add magnesium stearate, add carboxymethyl starch sodium mix homogeneously, tabletting; Use the ethanol/water solution coating of Opadry then, parcel one deck carbomer promptly gets in coating.
Embodiment 3 CM-particles
Chloromycetin 25.0g
Lactose 100g
Microcrystalline Cellulose 200g
10% starch slurry 100g
Carbomer 50.0g
Hypromellose 6.0g
Magnesium stearate 1.0g
Preparation technology: with chloromycetin, lactose, microcrystalline Cellulose mix homogeneously, 10% starch slurry is that binding agent is granulated, dry, granulate, and with hypromellose, carbomer coating, dry back adds the magnesium stearate mix homogeneously, and packing promptly gets.
Embodiment 4 Arechin (Polfa) micropills
Arechin (Polfa) 25.0g
Icing Sugar 300g
Microcrystalline Cellulose 100g
Polyvinylpyrrolidone 5.0g
Acrylic resin 50.0g
Carbomer 0.75g
Triethyl citrate 3.0g
Pulvis Talci 4.0g
Preparation technology: Icing Sugar, microcrystalline Cellulose are processed celphere, Arechin (Polfa) and polyvinylpyrrolidone are dissolved in water, principal cartridge is rolled on the celphere through liquid medicine-feeding mode; Then acrylic resin, triethyl citrate, Pulvis Talci are made into the suspension coating, add carbomer with powder type during coating, contain the coatings of carbomer, promptly get the Arechin (Polfa) micropill with formation.
Embodiment 5: the taste masking contrast test
The taste evaluation is the important step of taste masking technology, and the mouthfeel evaluation of food and medicine is main with people's trial test still at present.
The applicant has carried out double blinding, random searching development test to the bitterness of two kinds of Biaxins (dry suspension and tablet).
One, the contrast of clarithromycin dry suspension
Trial drug: clarithromycin A (pressing the medicine of embodiment 1 preparation)
Clarithromycin B (commercially available clarithromycin dry suspension, product batch number: 091202, manufacturing enterprise: Zhongmei Huadong Pharmaceutical Co., Ltd. Hangzhou)
Study population: 18-40 one full year of life, healthy male
Research number: 200 examples
EXPERIMENTAL DESIGN: medicine is poured in the cup in advance, adds in 30-50 ℃ the eliminating cold for resuscitation water to stir, and is subsequent use.
Test is divided into 2 groups, every group 100 example.The experimenter contains in the inlet compiling blind medicine in advance after going into group at random, does not swallow, and when feeling bitterness, the report researcher is by researcher record bitterness time of origin.
Statistics: adopt SAS 9.10 software analysis.The result is as shown in table 1.
The taste masking contrast of table 1 clarithromycin A, B
| Clarithromycin A | Clarithromycin B | The P value | |
| Bitterness time of origin average | 25.2 minute | 3.1 second | ＜0.01 |
Common dry suspension will be felt bitterness in 3.1 seconds; And carbomer taste masking dry suspension is put into mouth and was just felt bitterness in back 25.2 minutes; Being clarithromycin A has very clear superiority than clarithromycin B aspect the bitterness covering; Both time phase differences nearly 500 times, its effect has exceeded inventor's expectation widely.
Two, the contrast of clarithromycin tablet
Trial drug: clarithromycin C (pressing the medicine of embodiment 2 preparations)
Clarithromycin D (commercially available clarithromycin tablet, product batch number: 100101, manufacturing enterprise: Zhongmei Huadong Pharmaceutical Co., Ltd. Hangzhou)
Study population: 18-40 one full year of life, healthy male
Research number: 200 examples
EXPERIMENTAL DESIGN: test is divided into 2 groups, every group 100 example.The experimenter contains in the inlet compiling blind medicine in advance after going into group at random, does not swallow, and when feeling bitterness, the report researcher is by researcher record bitterness time of origin.
Statistics: adopt SAS 9.10 software analysis.The result is as expressing shown in 2.
The taste masking contrast of table 2 clarithromycin C, D
| Clarithromycin C | Clarithromycin D | The P value | |
| Bitterness time of origin average | Plant 28.3 divide | 5.8 second | ＜0.01 |
The normal packet garment piece will be felt bitterness about 5.8 seconds, and carbomer taste masking sheet puts into mouth and just feel bitterness after back 28.3 minutes, and promptly clarithromycin C has advantage than clarithromycin D aspect the bitterness covering.Both time phase differences nearly 300 times, its effect has exceeded inventor's expectation widely.
Claims (4)
1. the clarithromycin taste masking preparation with taste masking effect is characterized in that containing the water-swellable adjuvant, and wherein said water-swellable adjuvant is a carbomer; The quality of the water-swellable adjuvant that it contained is 0.005-4 a times of clarithromycin; When coating, the water-swellable adjuvant is wrapped in the preparation skin with powder type.
2. clarithromycin taste masking preparation as claimed in claim 1, the quality of the water-swellable adjuvant that it is characterized in that being contained be principal agent 0.03-2 doubly.
3. clarithromycin taste masking preparation as claimed in claim 1 is characterized in that described preparation is any in granule, tablet, capsule, micropill, the dry suspension.
4. prepare taste masking preparation as claimed in claim 1, it is characterized in that when coating, the water-swellable adjuvant being wrapped in the preparation skin with powder type, wherein said water-swellable adjuvant is a carbomer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102352276A CN101912613B (en) | 2010-07-22 | 2010-07-22 | Taste masking preparation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102352276A CN101912613B (en) | 2010-07-22 | 2010-07-22 | Taste masking preparation |
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| Publication Number | Publication Date |
|---|---|
| CN101912613A CN101912613A (en) | 2010-12-15 |
| CN101912613B true CN101912613B (en) | 2012-01-04 |
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| CN2010102352276A Active CN101912613B (en) | 2010-07-22 | 2010-07-22 | Taste masking preparation |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104274409B (en) * | 2013-07-10 | 2017-11-03 | 北京科信必成医药科技发展有限公司 | A kind of medicine microspheres for being easy to swallow and preparation method thereof |
| CN104382869B (en) * | 2014-10-23 | 2016-10-12 | 温州芳植生物科技有限公司 | A kind of oral cavity disintegration tablet benumbing oral cavity taste masking and preparation method thereof |
| CN107625740A (en) * | 2016-07-18 | 2018-01-26 | 北京科信必成医药科技发展有限公司 | A kind of Ondansetron is anhydrous to swallow particle |
| CN107625742A (en) * | 2016-07-19 | 2018-01-26 | 北京科信必成医药科技发展有限公司 | One kind is anhydrous to swallow taste masking preparation and preparation method thereof |
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| WO2008129730A1 (en) * | 2007-03-30 | 2008-10-30 | Lintec Corporation | Process for producing preparation for oral administration |
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