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CN107536822A - A kind of erythromycin enteric preparation - Google Patents

A kind of erythromycin enteric preparation Download PDF

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Publication number
CN107536822A
CN107536822A CN201610492112.2A CN201610492112A CN107536822A CN 107536822 A CN107536822 A CN 107536822A CN 201610492112 A CN201610492112 A CN 201610492112A CN 107536822 A CN107536822 A CN 107536822A
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China
Prior art keywords
erythromycin
enteric
substrate
tween
parts
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Pending
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CN201610492112.2A
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Chinese (zh)
Inventor
曾培安
余小娟
吴健民
贺莲
吴成龙
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Kamp Pharmaceuticals Co Ltd
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Kamp Pharmaceuticals Co Ltd
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Priority to CN201610492112.2A priority Critical patent/CN107536822A/en
Publication of CN107536822A publication Critical patent/CN107536822A/en
Pending legal-status Critical Current

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Abstract

A kind of erythromycin enteric preparation, belongs to antibiotics, is made up of substrate and enteric coating two parts, substrate composition weight number meter:Erythromycin:12.5 parts, starch:2.5~3.0 parts, Tween 80:0.21~0.25 part, hydroxypropyl cellulose:1~1.5 part, magnesium stearate:0.3~0.5 part, talcum powder:0.8~1.5 part;Enteric coating composition weight number meter:Polyacrylic resin (II):0.81~0.84 part, ethanol:15~16 parts, Tween 80:0.16~0.2 part, diethyl phthalate:0.16~0.2 part, castor oil:0.48~0.6 part, talcum powder:0.59~0.7 part.Using the substrate of the present invention, enteric coating formula made from erythromycin enteric-coated tabletses average release >=90% in drug effect, far above NF standard, and discharge steady, drug effect is higher than NF standard before the deadline;Outward appearance upper surface exquisiteness is glossy, long time stored not influence effectiveness.

Description

A kind of erythromycin enteric preparation
Technical field
The invention belongs to antibiotics formulation art, and in particular to a kind of erythromycin enteric-coated tabletses and preparation method thereof.
Background technology
Dissolution rate refers to medicine from the speed and degree of the dissolution in regulation solvent of the solid pharmaceutical preparations such as tablet.Dissolution rate is piece One important indicator of agent quality control, the inspection of dissolution rate typically should all be made to the medicine of slightly solubility.Erythromycin is conventional anti- Raw plain medicine, anti-microbial property is similar with penicillin, and the bacterial strain of drug resistance is produced to penicillin typically to erythromycin-sensitive.In order to tie up Protect erythromycin drug effect and in order to avoid the stimulation to stomach, be prepared into erythromycin enteric-coated tabletses so that patient takes.2015 editions pharmacopeia rule Determine erythromycin enteric-coated tabletses dissolution rate limit >=80%.For a long time, the dissolution rates of erythromycin enteric-coated tabletses how is controlled to reach state Family's standards of pharmacopoeia, so as to produce the product for meeting patient requests, perplexs numerous similar drug manufacturers always.So seek Asking a kind of stimulates erythromycin enteric-coated tabletses small, that release is high, stability is good to show important especially stomach.
The content of the invention
The technical problem to be solved in the present invention is:The problem of overcoming prior art to exist, there is provided a kind of erythromycin release is flat Surely, dissolution rate is all higher than 90%, and the change of its dissolution rate is little after long-term storage, the erythromycin enteric-coated tabletses of efficacy stability;It is and raw Production. art step is few, flow is simple, the preparation method of easily operated erythromycin enteric-coated tabletses.
The technical solution adopted for the present invention to solve the technical problems is:This kind of erythromycin enteric preparation, by substrate and intestines Molten clothing two parts composition, it is characterised in that:
Substrate composition weight number meter:Erythromycin:12.5 parts, starch:2.5~3.0 parts, Tween-80:0.21~0.25 part, hydroxyl Propyl cellulose:1~1.5 part, magnesium stearate:0.3~0.5 part, talcum powder:0.8~1.5 part;Enteric coating composition weight number Meter:Polyacrylic resin (II):0.81~0.84 part, ethanol:15~16 parts, Tween-80:0.16~0.2 part, phthalic acid Diethylester:0.16~0.2 part, castor oil:0.48~0.6 part, talcum powder:0.59~0.7 part.
The specific enteric coated preparations prescription each component parts by weight are calculated as:Substrate component includes:Erythromycin:12.5 parts, form sediment Powder:2.7 parts, Tween-80:0.23 part, hydroxypropyl cellulose:1.2 part, magnesium stearate:0.4 part, talcum powder:1.1 part;Enteric coating Composition weight number meter:Polyacrylic resin (II):0.82 part, the ethanol of concentration more than 90%:15 parts, Tween-80:0.17 Part, diethyl phthalate:0.18 part, castor oil:0.54 part, talcum powder:0.62 part.
A kind of preparation method of erythromycin enteric preparation, making step are as follows:
The making of described enteric coating comprises the following steps:
Will according to the desired amount of polyacrylic resin of aforementioned formula (II), Tween-80, diethyl phthalate, castor oil and Talcum powder mixes, and adds the ethanol dissolving of concentration more than 90%, is put into mixed grinding one time in colloid mill after dissolving, cross 100~ 300 mesh sieves, the blending ingredients of excessively complete sieve are transferred to agitator tank, stirred by peristaltic pump, it is standby after stirring.
The making of described substrate comprises the following steps:
After a crushes three kinds of erythromycin powder, starch and hydroxypropyl cellulose raw materials, sieved respectively now 80~100, three Uniformly after mixing, add adhesive and disintegrant is well mixed, be then transferred to 10~15min of granulation in granulator, obtain wet Grain;
Wet granular is dried b in ebullated dryer, 50~60 DEG C of temperature control, make its water content be maintained at 5%~ 6%, particle then is arranged with wire netting, arranges to finish and adds lubricant and further mix, afterwards with tabletting machine, obtains base Piece;
Above-mentioned gained erythromycin substrate is placed in seed-coating machine, starts seed-coating machine, deployed intestines will be formulated by foregoing enteric coating Molten clothing liquid is equably sprayed on substrate surface by spray gun and obtains finished product erythromycin enteric-coated tabletses.
Described adhesive is 13~13.5% starch slurry, and its addition is 10~13kg.
Described disintegrant refers to Tween-80, and addition is every 100,000 0.21~0.25kg.
Described lubricant refers to magnesium stearate and talcum powder.
Compared with existing erythromycin enteric-coated tabletses and preparation method thereof, the invention has the advantages that:
1st, erythromycin enteric-coated tabletses appearance according to gained of the invention is fine and smooth, smooth, smooth, flexible.Pass through dissolution rate instrument for several times Detect its release, release is all higher than 90%, and higher than NF standard, and erythromycin release is steady, after long-term storage its Release change is little, efficacy stability.
2nd, production craft step of the present invention is few, flow is simple, easily operated.
Embodiment
Embodiment 1
Make a kind of erythromycin enteric-coated tabletses, substrate component is (with the gauge of erythromycin enteric-coated tabletses finished product 100,000):Erythromycin: 12.5 (BOUs), starch:2.5kg, hydroxypropyl cellulose:1kg, Tween-80:0.21kg, magnesium stearate:0.3kg, talcum Powder:0.8kg;
Enteric coating component is (with the gauge of erythromycin enteric-coated tabletses finished product 100,000):Polyacrylic resin (II):0.81kg, tell Temperature -80:0.16kg, diethyl phthalate:0.16kg, castor oil:0.48kg, talcum powder:0.59kg, concentration more than 90% Ethanol:15kg.
Preparation method step is as follows:
1st, enteric coating is made:By polyacrylic acid resin (II) 0.81kg, Tween-80 0.16kg, diethyl phthalate 0.16kg, castor oil 0.48kg, talcum powder 0.59kg mixing, after adding the ethanol 15kg dissolvings of concentration 90%, it is put into colloid mill Middle grinding several times, is inserted in agitator tank after crossing 300 mesh sieves, is stirred until homogeneous by peristaltic pump bright, obtain erythromycin enteric clothing liquid It is standby.
2nd, substrate is made:By tri- kinds of erythromycin powder 12.5 (BOU), starch 2.5kg and hydroxypropyl cellulose 1kg Raw material crushes respectively, is uniformly mixed after crossing 100 mesh sieves, obtains mixture;13% starch slurry 10kg is added in this mixture again And Tween-80 0.21kg, it is put into after well mixed in granulator and is granulated 10min, obtains wet granular.Gained wet granular is dry in boiling It is dried in dry device, keeping temperature is 50 DEG C, and water content is about 6% after drying, and after arranging particle with wire netting, adds cunning Stone flour 0.8kg, magnesium stearate 0.3kg are further well mixed, and insert tabletting machine, obtain erythromycin enteric-coated tabletses substrate.
3rd, it is enteric coated:Above-mentioned gained erythromycin substrate is turned, in seed-coating machine, to start seed-coating machine, by gained enteric coating liquid Substrate surface is equably sprayed on by spray gun and obtains finished product erythromycin enteric-coated tabletses.
Embodiment 2
A kind of erythromycin enteric-coated tabletses are made, substrate component is:Erythromycin:12.5 (BOUs), starch:2.8kg, hydroxypropyl are fine Dimension element:1.2kg, Tween-80:0.22kg, magnesium stearate:0.35kg, talcum powder:1.2kg;
Enteric coating component is:Polyacrylic resin (II):0.82kg, Tween-80:0.16kg, diethyl phthalate: 0.18kg, castor oil:0.51kg, talcum powder:0.61kg, the ethanol of concentration more than 90%:15.2kg.
Preparation method step is as follows:
1st, enteric coating solution is prepared:By polyacrylic acid resin (II) 0.82kg, Tween-80 0.16kg, diethyl phthalate 0.18kg, castor oil 0.51kg, talcum powder 0.61kg mixing, after adding the ethanol 15.2kg dissolvings of concentration 90%, it is put into colloid Ground in mill several times, inserted after crossing 200 mesh sieves in agitator tank, be stirred until homogeneous by peristaltic pump bright, obtain erythromycin enteric clothing Liquid is standby.
2nd, substrate is made:By erythromycin powder 12.5 (BOU), starch 2.8kg and hydroxypropyl cellulose 1.2kg tri- Kind raw material crushes respectively, is uniformly mixed after crossing 80 mesh sieves, obtains mixture;13% starch slurry 10kg is added in this mixture again And Tween-80 0.22kg, it is put into after well mixed in granulator and is granulated 12min, obtains wet granular.Gained wet granular is dry in boiling It is dried in dry device, keeping temperature is 55 DEG C, and water content is about 5% after drying, and after arranging particle with wire netting, adds cunning Stone flour 1.2kg, magnesium stearate 0.35kg are further well mixed, and insert tabletting machine, obtain erythromycin enteric-coated tabletses substrate.
3rd, it is enteric coated:Above-mentioned gained erythromycin substrate is turned, in seed-coating machine, to start seed-coating machine, by gained enteric coating liquid Substrate surface is equably sprayed on by spray gun and obtains finished product erythromycin enteric-coated tabletses.
Embodiment 3
A kind of erythromycin enteric-coated tabletses are made, substrate component is:Erythromycin:12.5 (BOUs), starch:2.6kg, hydroxypropyl are fine Dimension element:1.3kg, Tween-80:0.22kg, magnesium stearate:0.35kg, talcum powder:1.2kg;
Enteric coating component is:Polyacrylic resin (II):0.83kg, Tween-80:0.18kg, diethyl phthalate: 0.18kg, castor oil:0.55kg, talcum powder:0.65kg, the ethanol of concentration more than 90%:15.5kg.
Preparation method step is as follows:
1st, enteric coating solution is prepared:By polyacrylic acid resin (II) 0.83kg, Tween-80 0.18kg, diethyl phthalate 0.18kg, castor oil 0.55kg, talcum powder 0.65kg mixing, after adding the ethanol 15.5kg dissolvings of concentration 90%, it is put into colloid Ground in mill several times, inserted after crossing 100 mesh sieves in agitator tank, be stirred until homogeneous by peristaltic pump bright, obtain erythromycin enteric clothing Liquid is standby.
2nd, substrate is made:By erythromycin powder 12.5 (BOU), starch 2.6kg and hydroxypropyl cellulose 1.3kg tri- Kind raw material crushes respectively, is uniformly mixed after crossing 80 mesh sieves, obtains mixture;13.5% starch slurry is added in this mixture again 12kg and Tween-80 0.22kg, it is put into after well mixed in granulator and is granulated 12min, obtain wet granular.Gained wet granular is being boiled Rise in drier and be dried, keeping temperature is 55 DEG C, and water content is about 5% after drying, and after arranging particle with wire netting, then is added Enter talcum powder 1.2kg, magnesium stearate 0.35kg is further well mixed, and inserts tabletting machine, obtain erythromycin enteric-coated tabletses substrate.
3rd, it is enteric coated:Above-mentioned gained erythromycin substrate is turned, in seed-coating machine, to start seed-coating machine, by gained enteric coating liquid Substrate surface is equably sprayed on by spray gun and obtains finished product erythromycin enteric-coated tabletses.
Embodiment 4
A kind of erythromycin enteric-coated tabletses are made, substrate component is:Erythromycin:12.5 (BOUs), starch:3.0kg, hydroxypropyl are fine Dimension element:1.5kg, Tween-80:0.25kg, magnesium stearate:0.50kg, talcum powder:1.5kg;
Enteric coating component is (with the gauge of erythromycin enteric-coated tabletses finished product 100,000):Polyacrylic resin (II):0.84kg, tell Temperature -80:0.20kg, diethyl phthalate:0.20kg, castor oil:0.60kg, talcum powder:0.70kg, concentration more than 90% Ethanol:16kg.
Preparation method step is as follows:
1st, enteric coating solution is prepared:By polyacrylic acid resin (II) 0.84kg, Tween-80 0.20kg, diethyl phthalate 0.20kg, castor oil 0.60kg, talcum powder 0.70kg mixing, after adding the ethanol 16kg dissolvings of concentration 90%, it is put into colloid mill Middle grinding several times, is inserted in agitator tank after crossing 100 mesh sieves, is stirred until homogeneous by peristaltic pump bright, obtain erythromycin enteric clothing liquid It is standby.
2nd, substrate is made:By erythromycin powder 12.5 (BOU), starch 3.0kg and hydroxypropyl cellulose 1.5kg tri- Kind raw material crushes respectively, is uniformly mixed after crossing 100 mesh sieves, obtains mixture;13.5% starch slurry is added in this mixture again 13kg and Tween-80 0.25kg, it is put into after well mixed in granulator and is granulated 15min, obtain wet granular.Gained wet granular is being boiled Rise in drier and be dried, keeping temperature is 60 DEG C, and water content is about 5% after drying, and after arranging particle with wire netting, then is added Enter talcum powder 1.5kg, magnesium stearate 0.50kg is further well mixed, and inserts tabletting machine, obtain erythromycin enteric-coated tabletses substrate.
3rd, it is enteric coated:Above-mentioned gained erythromycin substrate is turned, in seed-coating machine, to start seed-coating machine, by gained enteric coating liquid Substrate surface is equably sprayed on by spray gun and obtains finished product erythromycin enteric-coated tabletses.
The above described is only a preferred embodiment of the present invention, being not the limitation for making other forms to the present invention, appoint What those skilled in the art changed or be modified as possibly also with the technology contents of the disclosure above equivalent variations etc. Imitate embodiment.But it is every without departing from technical solution of the present invention content, the technical spirit according to the present invention is to above example institute Any simple modification, equivalent variations and the remodeling made, still fall within the protection domain of technical solution of the present invention.

Claims (6)

1. a kind of erythromycin enteric preparation, is made up of substrate and enteric coating two parts, it is characterised in that:Substrate composition weight number Meter:Erythromycin:12.5 parts, starch:2.5~3.0 parts, Tween-80:0.21~0.25 part, hydroxypropyl cellulose:1~1.5 part, Magnesium stearate:0.3~0.5 part, talcum powder:0.8~1.5 part;Enteric coating composition weight number meter:Polyacrylic resin (II): 0.81~0.84 part, ethanol:15~16 parts, Tween-80:0.16~0.2 part, diethyl phthalate:0.16~0.2 part, Castor oil:0.48~0.6 part, talcum powder:0.59~0.7 part.
A kind of 2. erythromycin enteric preparation according to claim 1, it is characterised in that:Substrate component includes:Erythromycin:12.5 Part, starch:2.7 part, Tween-80:0.23 part, hydroxypropyl cellulose:1.2 parts, magnesium stearate:0.4 part, talcum powder:1.1 part; Enteric coating composition weight number meter:Polyacrylic resin (II):0.82 part, the ethanol of concentration more than 90%:15 parts, Tween-80: 0.17 part, diethyl phthalate:0.18 part, castor oil:0.54 part, talcum powder:0.62 part.
A kind of 3. preparation method of erythromycin enteric preparation according to claim 2, it is characterised in that:Making step is as follows:
1)Prepare enteric coating solution:By polyacrylic resin (II), Tween-80, diethyl phthalate, castor oil and talcum Powder is mixed according to recipe ingredient aequum, adds the ethanol dissolving of concentration more than 90%, and mixing in colloid mill is put into after dissolving and is ground Mill several times, crosses 100~300 mesh sieves, the mixture after sieving is transferred into agitator tank, stirred by peristaltic pump, after stirring Enteric coating liquid is standby;
2)Make substrate:
After a crushes three kinds of erythromycin powder, starch and hydroxypropyl cellulose raw materials, sieved respectively now 80~100, three Uniformly mixing, adds adhesive and disintegrant is well mixed, and is then transferred to 10~15min of granulation in granulator, obtains wet granular;
Wet granular is dried b in ebullated dryer, controls 50~60 DEG C of temperature, make its water content be maintained at 5%~ 6%, particle then is arranged with wire netting, arranges to finish to add after lubricant further mixes and uses tabletting machine, obtain substrate;
3)It is enteric coated:Step 2.2 gained erythromycin substrate is placed in seed-coating machine, starts seed-coating machine, by step 1)Gained intestines Molten clothing liquid is equably sprayed on substrate surface finished product by spray gun.
A kind of 4. preparation method of erythromycin enteric preparation according to claim 3, it is characterised in that:Step 2)Institute in a The adhesive stated is 13~13.5% starch slurry, addition (with the gauge of erythromycin enteric-coated tabletses finished product 100,000) for 10~ 13kg。
A kind of 5. preparation method of erythromycin enteric preparation according to claim 3, it is characterised in that:Step 2)Institute in a The disintegrant stated refers to Tween-80.
A kind of 6. preparation method of erythromycin enteric preparation according to claim 3, it is characterised in that:Step 2)Institute in b The lubricant stated refers to magnesium stearate and talcum powder.
CN201610492112.2A 2016-06-29 2016-06-29 A kind of erythromycin enteric preparation Pending CN107536822A (en)

Priority Applications (1)

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CN201610492112.2A CN107536822A (en) 2016-06-29 2016-06-29 A kind of erythromycin enteric preparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610492112.2A CN107536822A (en) 2016-06-29 2016-06-29 A kind of erythromycin enteric preparation

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110123772A (en) * 2019-05-07 2019-08-16 安徽金太阳生化药业有限公司 A kind of erythromycin enteric-coated tablets and preparation method thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110123772A (en) * 2019-05-07 2019-08-16 安徽金太阳生化药业有限公司 A kind of erythromycin enteric-coated tablets and preparation method thereof

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Application publication date: 20180105