CN105106968A - Gastric-soluble film coating premix and method for preparing same - Google Patents
Gastric-soluble film coating premix and method for preparing same Download PDFInfo
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- CN105106968A CN105106968A CN201510630022.0A CN201510630022A CN105106968A CN 105106968 A CN105106968 A CN 105106968A CN 201510630022 A CN201510630022 A CN 201510630022A CN 105106968 A CN105106968 A CN 105106968A
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Abstract
The invention discloses gastric-soluble film coating premix and a method for preparing the same. The gastric-soluble film coating premix comprises, by weight, 30-50 parts of film forming materials, 10-20 parts of anti-sticking agents, 0.5-5 parts of colorants, 20-30 parts of covering agents, 5-15 parts of plasticizers and 1-3 parts of colloid MCC (microcrystalline cellulose and carboxymethylcellulose sodium). The method includes (1), uniformly mixing the film forming materials, the anti-sticking agents, the plasticizers and the colloid MCC with purified water or ethyl alcohol for 0.8-1h to obtain mixtures and drying the mixtures at the temperature of 35-45 DEG C for 5h; (2), mixing the colorants and the covering agents with the dried mixtures for 0.5-1h to obtain second mixtures, grinding the second mixtures by the aid of a grinder for 4-5h, and sieving the second mixtures by the aid of a 50-mesh sieve to obtain the premix. The gastric-soluble film coating premix and the method have the advantages that the stability of coating liquid can be improved by the colloid MCC in the premix, good effects of reducing the precipitation speeds of the coating liquid can be realized, the sedimentation speeds of the coating liquid can be reduced by means of adding thickeners into the premix, accordingly, coating procedures can be smoothly carried out, the gastric-soluble film coating premix is high in coating speed, and exquisite coated tablet surface effects can be realized; the colloid MCC mainly comprises microcrystalline cellulose, and effects of dispersing agents and colloid protecting effects can be realized by sodium carboxymethyl cellulose.
Description
Technical field
The invention belongs to drug coating and make formula and Technology field, be specifically related to a kind of stomach dissolved film coating pre-mix dose and preparation method thereof.
Background technology
Be in the process of accelerated development in the application of China's film-coated technique, film-coated market prospect is very wide, and the perfect raising innovation of coating material and packaging technique is also imperative.Have increasing pharmaceutical preparation be by film coating to hide its exception taste, hide various by the popular color liked.Both direction is mainly contained when adopting film-coated technique to want to reach and hide label this order of color completely.One is increase coating weight gain; Two is the coated product adopting high covering power.The coated product that pharmacy corporation then more favors high covering power reaches the object hiding label.Because relative to increase coating weight gain, employing high covering power coated product is shorter on Coating times, coated product use amount less, and cost of drugs is lower.As film-coating product research and development side, its main technological means is exactly reach this purpose by the ratio of covering effect in increase product, and these compositions major parts are made up of the insoluble raw material such as titanium dioxide, Pulvis Talci.More particulate matter can cause and be mixed with the quickening of coating solution postprecipitation speed, brings very large impact in coating process and on coating effect.
According to square being directly proportional of the speed of sedimentation theory (Stokes theory) sedimentation and particle diameter, be inversely proportional to the viscosity of continuous phase medium.Because when development film coating pre-mix dose, titanium dioxide insoluble in composition, Pulvis Talci be all supplier in process of production Task-size Controlling to very small material, also will through the operation such as grinding in interpolation use procedure, so the method adopted in research coating solution free settling problem adds thickening agent to improve dielectric viscosity in the past.But what too high coating solution viscosity was brought is thorough, the stifled rifle of coating process atomization thereupon; Unilateral coarse series of problems such as grade after coating.
Summary of the invention
In order to solve, by increasing liquid viscosity, above-mentioned high cover film coating only reduces that the rate of settling easily causes that coating is smooth, the unilateral technical problem such as coarse after coating, the invention provides a kind ofly to comprise stomach dissolved film coating pre-mix dose of colloid MCC stabilizing agent and preparation method thereof.
The invention provides a kind of stomach dissolved film coating pre-mix dose, this pre-mixing agent comprises the component of following mass parts: filmogen 30-50 part, antiplastering aid 10-20 part, coloring agent 0.5-5 part, covering agent 20-30 part, plasticizer 5-15 part, colloid MCC1-3 part;
Wherein, colloid MCC comprises microcrystalline Cellulose and sodium carboxymethyl cellulose, and the mass ratio of microcrystalline Cellulose and sodium carboxymethyl cellulose is 1-1.5:8.5-9.
Preferably, filmogen comprises the component of following mass parts: hydroxypropyl methylcellulose 1-5 part, polyvinyl alcohol 1-3 part, copolyvidone 1-2 part.
Preferably, antiplastering aid is any one in Pulvis Talci, magnesium stearate, stearic acid.
Preferably, covering agent is titanium dioxide.
Preferably, plasticizer is any one in polyethylene glycol 6000, Liquid Macrogol, PEG400, propanol, glycerol, glyceryl triacetate, dicarboxylic acid dimethyl ester, triacetyl glycerine.
A kind of method preparing stomach dissolved film coating pre-mix dose of the present invention, the method comprises the following steps:
(1) filmogen 30-50 part, antiplastering aid 10-20 part, plasticizer 5-15 part, colloid MCC1-3 part is got, with purified water 6-12 part, ethanol 2-4 part Homogeneous phase mixing 0.8-1h, 35-45 DEG C of dry 4-5h;
(2) in the dried mixture of upper step, add coloring agent 0.5-5 part, opacifier 20-30 part, after mixing 0.5-1h, be transferred on grinder and grind 4-5h, cross 50 mesh sieves, can pre-mixing agent be obtained.
Beneficial effect of the present invention: the colloid MCC in pre-mixing agent of the present invention improves the stability of coating solution, reduce coating solution settling rate effect and be better than dependence interpolation thickening agent to alleviate the coating solution rate of settling, and coating process is more smooth and easy, coating speed is faster, and after coating, unilateral effect is finer and smoother.Colloid MCC comprises microcrystalline Cellulose and sodium carboxymethyl cellulose, and colloid MCC is with microcrystalline Cellulose with main body, and sodium carboxymethyl cellulose plays the effect of dispersant and protecting colloid.
Detailed description of the invention
Below in conjunction with embodiment, in detail explanation is explained to the present invention.
Introduce a kind of new adjuvant colloid MCC in pre-mixing agent formula of the present invention to increase the stability of liquid, the unilateral effect after coating solution viscosity in use and coating can not have been affected again simultaneously.Colloid MCC is scattered in liquid phase, can not produce larger viscosity B coefficent, but have the effect of hydrogen bond when solution stand in continuous phase, can form the space three-dimensional network structure of Weak Gels in continuous phase solution.This network structure makes continuous print solution increase its yield value, thus makes molecule be evenly dispersed in continuous phase, unlikely sinking.This structure can be disappeared or be damaged again when shaking or shake, and viscosity reduces rapidly, and recovers the good mobility of its liquid.Colloid MCC is incorporated in the middle of film-coated technique of the present invention, can be uniformly dispersed under high shear force (whipping process) effect, utilize its above-mentioned characteristic, the colloid solution of final formation uniformity, strengthen the yield value of liquid phase, prevent the sedimentation of insoluble microgranule, this stable mechanism is different from originally single increase viscosity, its stabiliser is network struture system, instead of high viscosity systems.
The deterministic process of formula:
1, the present invention carries out based on original high soverlay technique, so first directly replace thickening agent of the prior art with colloid MCC stabilizing agent.In the middle of whole ratio examination process, do not find have incompatibility phenomenon to occur with other components in formula.
2, optimum proportioning examination
In formula based on different covering agent ratio, add not commensurability colloid MCC stabilizing agent from the rate of settling, bag make process and coating after unilateral effect observe, try coating, gather analysis of experimental data table, determine optimum proportioning.
Table 1 adds not commensurability colloid MCC to the impact of coating process
Analysis and summary: along with the ratio of covering agent microgranule insoluble in film coating pre-mix dose increases, need colloid MCC stabilizing agent adding proportion also different, for tested recipe, adding covering agent maximum ratio is wherein 50%, and when colloid MCC stabilizing agent adds 3% to, effect is the most desirable.Excessive interpolation colloid MCC stabilizing agent can cause liquid to be tending towards gel, needs larger shearing force to destroy hydrogen bond structure, is unfavorable for that bag is made.So the colloid MCC stabilizing agent optimal proportion be used in film coating pre-mix dose formula of the present invention is 1-3%.
Embodiment 1
Red colour system stomach dissolution type pre-mixing agent of the present invention comprises the component of following mass parts:
The preparation method of red colour system stomach dissolved film coating pre-mix dose of the present invention comprises the following steps:
By the Pulvis Talci of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, polyethylene glycol 6000, colloid MCC, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 0.8h, 35 DEG C of dry 5h, wherein in colloid MCC, the weight ratio of microcrystalline Cellulose and sodium carboxymethyl cellulose is 1:9, get intermediate to detect, being of moisture≤5% is qualified; After qualified, add the carmine lake of above-mentioned mass parts, titanium dioxide, after mixing 0.5h, be transferred to grinder grinding 5h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.
Comparative example:
Comprise the component proportioning of the red colour system film coating pre-mix dose of thickening agent:
Prepare the method for this red colour system film coating pre-mix dose:
By the Pulvis Talci of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, polyethylene glycol 6000, hydroxypropyl methylcellulose E200, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 0.8h, 35 DEG C of dry 5h, get intermediate to detect, being of content≤5% of moisture is qualified; After qualified, add the carmine lake of above-mentioned mass parts, titanium dioxide, after mixing 0.5h, be transferred to grinder grinding 5h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.Comparing with pre-mixing agent of the present invention of obtained film coating pre-mix dose, comparative result is in table 2.
The comparative result of the pre-mixing agent performance of table 2 pre-mixing agent of the present invention and comparative example
Embodiment 2
Green of the present invention is the component that stomach dissolution type pre-mixing agent comprises following mass parts:
Green of the present invention is that the preparation method of stomach dissolved film coating pre-mix dose comprises the following steps:
By the magnesium stearate of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, Liquid Macrogol, colloid MCC, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 1h, 40 DEG C of dry 5h, wherein in colloid MCC, the weight ratio of microcrystalline Cellulose and sodium carboxymethyl cellulose is 1.2:8.8, get intermediate to detect, being of content≤5% of moisture is qualified; After qualified, add the light green color lake of above-mentioned mass parts, titanium dioxide, after mixing 0.8h, be transferred to grinder grinding 4h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.
Comparative example:
The green comprising thickening agent is the component of film coating pre-mix dose:
Preparing this green is that the method for film coating pre-mix dose comprises the following steps:
By the magnesium stearate of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, Liquid Macrogol, hydroxypropyl methylcellulose E200, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 1h, 40 DEG C of dry 5h, get intermediate to detect, being of content≤5% of moisture is qualified; After qualified, add the light green color lake of above-mentioned mass parts, titanium dioxide, after mixing 0.8h, be transferred to grinder grinding 4h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.Comparing with pre-mixing agent of the present invention of obtained film coating pre-mix dose, comparative result is in table 3.
The comparative result of the pre-mixing agent performance of table 3 pre-mixing agent of the present invention and comparative example
Embodiment 3
Yellow of the present invention is the component that stomach dissolution type pre-mixing agent comprises following mass parts:
Green of the present invention is that the preparation method of stomach dissolved film coating pre-mix dose comprises the following steps:
By the stearic acid of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, glyceryl triacetate, colloid MCC, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 1h, 45 DEG C of dry 5h, wherein in colloid MCC, the weight ratio of microcrystalline Cellulose and sodium carboxymethyl cellulose is 1.5:8.5, get intermediate to detect, being of content≤5% of moisture is qualified; After qualified, add the lemon yellow color lake of above-mentioned mass parts, titanium dioxide, after mixing 1h, be transferred to grinder grinding 5h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.
Comparative example:
The yellow comprising thickening agent is the component of film coating pre-mix dose:
Preparing this green is that the method for film coating pre-mix dose comprises the following steps:
By the stearic acid of above-mentioned mass parts, hydroxypropyl methylcellulose, copolyvidone, polyvinyl alcohol, glyceryl triacetate, hydroxypropyl methylcellulose E200, purified water and ethanol (mass concentration is 99%) Homogeneous phase mixing 1h, 45 DEG C of dry 5h, get intermediate to detect, being of moisture≤5% is qualified; After qualified, add the lemon yellow color lake of above-mentioned mass parts, titanium dioxide, after mixing 1h, be transferred to grinder grinding 5h, cross 50 mesh sieves, detect, it is qualified that △ E≤2 are, and needs to finely tune until △ E≤2 color, obtain pre-mixing agent during △ E > 2.Comparing with pre-mixing agent of the present invention of obtained film coating pre-mix dose, comparative result is in table 4.
The comparative result of the pre-mixing agent performance of table 4 pre-mixing agent of the present invention and comparative example
To sum up, thickening agent of the prior art is substituted with colloid MCC stabilizing agent, after film coating pre-mix dose dry powder and coating, tablet is through accelerated test stability test, result finds no the phenomenon affecting film coating pre-mix dose serviceability, confirms that colloid MCC stabilizing agent can solve the technical problem that in prior art, high covering type film coating pre-mix dose easily precipitates.
Preferred embodiment of the present invention, not in order to limit the present invention, all do in flesh and blood of the present invention any amendment, equivalent to replace and simple modifications etc., all should be included within protection scope of the present invention.
Claims (6)
1. a stomach dissolved film coating pre-mix dose, is characterized in that, this pre-mixing agent comprises the component of following mass parts: filmogen 30-50 part, antiplastering aid 10-20 part, coloring agent 0.5-5 part, covering agent 20-30 part, plasticizer 5-15 part, colloid MCC1-3 part;
Wherein, colloid MCC comprises microcrystalline Cellulose and sodium carboxymethyl cellulose, and the mass ratio of microcrystalline Cellulose and sodium carboxymethyl cellulose is 1-1.5:8.5-9.
2. stomach dissolved film coating pre-mix dose according to claim 1, is characterized in that, filmogen comprises the component of following mass parts: hydroxypropyl methylcellulose 1-5 part, polyvinyl alcohol 1-3 part, copolyvidone 1-2 part.
3. stomach dissolved film coating pre-mix dose according to claim 1, is characterized in that, antiplastering aid is any one in Pulvis Talci, magnesium stearate, stearic acid.
4. stomach dissolved film coating pre-mix dose according to claim 1, is characterized in that, covering agent is titanium dioxide.
5. stomach dissolved film coating pre-mix dose according to claim 1, it is characterized in that, plasticizer is any one in polyethylene glycol 6000, Liquid Macrogol, PEG400, propanol, glycerol, glyceryl triacetate, dicarboxylic acid dimethyl ester, triacetyl glycerine.
6. prepare a method for the stomach dissolved film coating pre-mix dose described in any one of claim 1-5, it is characterized in that, the method comprises the following steps:
(1) filmogen 30-50 part, antiplastering aid 10-20 part, plasticizer 5-15 part, colloid MCC1-3 part is got, with purified water 6-12 part, ethanol 2-4 part Homogeneous phase mixing 0.8-1h, 35-45 DEG C of dry 4-5h;
(2) in the dried mixture of upper step, add coloring agent 0.5-5 part, opacifier 20-30 part, after mixing 0.5-1h, be transferred on grinder and grind 4-5h, cross 50 mesh sieves, can pre-mixing agent be obtained.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN106075461A (en) * | 2016-07-11 | 2016-11-09 | 成都中牧生物药业有限公司 | A kind of film coating pre-mix dose hiding abnormal flavour and preparation method |
| CN106214658A (en) * | 2016-08-29 | 2016-12-14 | 北京英茂药业有限公司 | A kind of compound coating pre-mixing agent and preparation method thereof |
| CN108785267A (en) * | 2018-08-14 | 2018-11-13 | 北京百奥药业有限责任公司 | A kind of valsartan amlodipine piece and preparation method thereof |
| CN110101678A (en) * | 2019-04-26 | 2019-08-09 | 安阳天助药业有限责任公司 | The coating pre-mixing agent and production method containing magnesium stearate of improvement |
| CN110559270A (en) * | 2019-09-17 | 2019-12-13 | 扬子江药业集团广州海瑞药业有限公司 | Sitagliptin phosphate pharmaceutical composition and preparation method thereof |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106075461A (en) * | 2016-07-11 | 2016-11-09 | 成都中牧生物药业有限公司 | A kind of film coating pre-mix dose hiding abnormal flavour and preparation method |
| CN106214658A (en) * | 2016-08-29 | 2016-12-14 | 北京英茂药业有限公司 | A kind of compound coating pre-mixing agent and preparation method thereof |
| CN106214658B (en) * | 2016-08-29 | 2019-05-03 | 北京英茂药业有限公司 | A kind of compound coating pre-mixing agent and preparation method thereof |
| CN108785267A (en) * | 2018-08-14 | 2018-11-13 | 北京百奥药业有限责任公司 | A kind of valsartan amlodipine piece and preparation method thereof |
| CN108785267B (en) * | 2018-08-14 | 2020-05-19 | 北京百奥药业有限责任公司 | Valsartan amlodipine tablet and preparation method thereof |
| CN110101678A (en) * | 2019-04-26 | 2019-08-09 | 安阳天助药业有限责任公司 | The coating pre-mixing agent and production method containing magnesium stearate of improvement |
| CN110101678B (en) * | 2019-04-26 | 2021-04-30 | 安阳天助药业有限责任公司 | Improved coating premix containing magnesium stearate and preparation method |
| CN110559270A (en) * | 2019-09-17 | 2019-12-13 | 扬子江药业集团广州海瑞药业有限公司 | Sitagliptin phosphate pharmaceutical composition and preparation method thereof |
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