CN102920679A - Preparation method of hot-melt plasticizing ethyecellulose water dispersion sustained and controlled release coating material - Google Patents
Preparation method of hot-melt plasticizing ethyecellulose water dispersion sustained and controlled release coating material Download PDFInfo
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- CN102920679A CN102920679A CN2012104945561A CN201210494556A CN102920679A CN 102920679 A CN102920679 A CN 102920679A CN 2012104945561 A CN2012104945561 A CN 2012104945561A CN 201210494556 A CN201210494556 A CN 201210494556A CN 102920679 A CN102920679 A CN 102920679A
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Abstract
The invention discloses a preparation method of a hot-melt plasticizing ethyecellulose water dispersion sustained and controlled release coating material, comprising the following steps of: (1) hot-melt plasticizing: putting ethyecellulose, ethanol and dibutyl sebacate in a reaction tank, stirring for 20-300 minutes under the conditions that a temperature is 80-145 DEG C and a rotation speed is 25-60rpm, and stopping stirring; and (2) converting phases: insulating the product of the step (1) for 3-8hours at a temperature of 80-145 DEG C, sequentially adding oleic acid, ammonia water, distilled water and silicon dioxide, emulsifying the mixture for 10-15hours under the conditions that a temperature is 80-145 DEG C and a rotation speed is 25-60rpm, cooling to the room temperature, so as to obtain the finished product. The coating material prepared by the method disclosed by the invention has the characteristics of high solid content, low viscosity, good film-forming property and obvious sustained and controlled release effect. Meanwhile, the processing technique is more simplified, the requirement for the processing apparatus is low and the price of the product is low.
Description
Technical field
The present invention relates to the preparation method of the slow release controlling coating material of a kind of aqueous dispersion, belong to biological field of pharmaceutical excipients.
Background technology
Ethyl cellulose is a kind of non-water-soluble slow release controlling coating material, stable in properties, have chemical-resistant resistance, acidproof, alkaline-resisting and heat-resisting characteristic, simultaneously easily compatible with wax, resin, plasticizer etc., therefore be widely used in field of pharmaceutical preparations, especially the release film coating field is used morely, but needs a large amount of organic solvent dissolutions when using, contaminated environment, cost is high.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, provide a kind of thermosol plasticising Aquacoat to delay the release controlling coating material preparation method.
Technical scheme of the present invention is summarized as follows:
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: be the ratio of 100:60-100:10-50 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, be that 80 ℃-145 ℃, rotating speed are under 25-60 rev/min the condition in temperature, stir 20-300min, stop to stir;
(2) change mutually: the product insulation 3-8h under 80 ℃-145 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 80 ℃-145 ℃, be to carry out emulsifying under 25-60 rev/min the condition at rotating speed, emulsification times is 10-15h, is cooled to room temperature, obtain finished product, the mass ratio of described oleic acid, ammonia, distilled water, silicon dioxide and ethyl cellulose is 2-100:50-500:50-700:1-75:100.
Step (1) thermosol plasticising is preferably: be in mass ratio the ratio of 100:80:30, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, be that 100 ℃, rotating speed are under 40 rev/mins the condition in temperature, stir 100-200min, stop to stir.
Step (2) changes mutually and is preferably: the product of step (1) at 100 ℃ of lower insulation 4-6h, is added oleic acid, ammonia, distilled water and silicon dioxide successively; At 100 ℃, be to carry out emulsifying under 40 rev/mins the condition at rotating speed, emulsification times is 13h, is cooled to room temperature, obtains finished product. the mass ratio of described oleic acid, ammonia, distilled water, silicon dioxide and ethyl cellulose is 4-50:100-300:100-500:2-37:100.
Advantage of the present invention: the present invention utilizes the thermosol plasticization process in advance ethyl cellulose to be mixed with Dibutyl Sebacate, ethanol.Then adopt and change mutually the slow release controlling coating material of preparation aqueous dispersion, the coating material of method of the present invention preparation has solids content high (25-33%), low viscosity (room temperature 25 ℃ time detect less than 100mPa*s), good film-forming property, the slow obvious characteristics of controlled-release effect, processing technique is simplified more simultaneously, less demanding to process equipment, product price is lower.
Description of drawings
Fig. 1 is that the slow release controlling coating material of the thermosol plasticising Aquacoat of method preparation of the present invention is to the mensuration of drug release rate.
The specific embodiment
The present invention is further illustrated below in conjunction with specific embodiment.
Embodiment 1
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: being the ratio of 100:80:30 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, is that 100 ℃, rotating speed are under 40 rev/mins the condition in temperature, stirs 150min, stops to stir;
(2) change mutually: the product insulation 5h under 100 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 100 ℃, be to carry out emulsifying under 40 rev/mins the condition at rotating speed, emulsification times is 13h, be cooled to room temperature, obtain finished product, detecting its viscosity number during 25 ℃ of gained finished product room temperatures is 99mPa*s, and the mass ratio of described oleic acid, ammonia, distilled water, silicon dioxide and ethyl cellulose is 40:200:300:25:100.
Embodiment 2
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: being the ratio of 100:70:20 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, is that 110 ℃, rotating speed are under 30 rev/mins the condition in temperature, stirs 100min, stops to stir;
(2) change mutually: the product insulation 6h under 110 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 110 ℃, be to carry out emulsifying under 30 rev/mins the condition at rotating speed, emulsification times is 12h, be cooled to room temperature, obtain finished product, the mass ratio that detects its viscosity number during 25 ℃ of gained finished product room temperatures and be the described oleic acid of 97mPa*s, ammonia, distilled water, silicon dioxide and ethyl cellulose is 50:100:500:2:100.
Embodiment 3
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: being the ratio of 100:90:40 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, is that 135 ℃, rotating speed are under 50 rev/mins the condition in temperature, stirs 200min, stops to stir;
(2) change mutually: the product insulation 7h under 135 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 135 ℃, be to carry out emulsifying under 50 rev/mins the condition at rotating speed, emulsification times is 13h, be cooled to room temperature, obtain finished product, the mass ratio that detects its viscosity number during 25 ℃ of gained finished product room temperatures and be the described oleic acid of 95mPa*s, ammonia, distilled water, silicon dioxide and ethyl cellulose is 4:300:100:37:100.
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: being the ratio of 100:60:10 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, is that 80 ℃, rotating speed are under 25 rev/mins the condition in temperature, stirs 300min, stops to stir;
(2) change mutually: the product insulation 8h under 80 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 80 ℃ ℃, be to carry out emulsifying under 25 rev/mins the condition at rotating speed, emulsification times is 15h, be cooled to room temperature, obtain finished product, the mass ratio that detects its viscosity number during 25 ℃ of gained finished product room temperatures and be the described oleic acid of 99mPa*s, ammonia, distilled water, silicon dioxide and ethyl cellulose is 100:500:50:75:100.
Embodiment 5
Thermosol plasticising Aquacoat delays the release controlling coating material preparation method, comprises the steps:
(1) thermosol plasticising: being the ratio of 100:100:50 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, is that 145 ℃, rotating speed are under 60 rev/mins the condition in temperature, stirs 20min, stops to stir;
(2) change mutually: the product insulation 3h under 145 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 145 ℃, be to carry out emulsifying under 60 rev/mins the condition at rotating speed, emulsification times is 10h, be cooled to room temperature, obtain finished product, the mass ratio that detects its viscosity number during 25 ℃ of gained finished product room temperatures and be the described oleic acid of 89mPa*s, ammonia, distilled water, silicon dioxide and ethyl cellulose is 2:50:700:1:100.
Embodiment 6
Test with the diclofenac sodium coated tablet drug release determination that the slow release controlling coating material of the thermosol plasticising Aquacoat of preparation method preparation of the present invention makes:
Materials and methods
1, medicine and instrument
The slow release controlling coating material of the thermosol plasticising Aquacoat of the embodiment of the invention 1 preparation; Diclofenac sodium (Qilu Pharmaceutical Co., Ltd.'s production); Single punch tablet machine (Shanghai Tianfan Pharmaceutical Machinery Factory); Use for laboratory seed-coating machine (Xi'an profit day pharmaceutical machine company limited); ZRS-4 digestion instrument (Tianda Tianfa Technology Co., Ltd.).
2, experimental technique
2.1 the preparation of the sheet heart: with diclofenac sodium 100g, lactose 240g crosses respectively 100 mesh sieves, mixing, and take the 10%PVP ethanol as binding agent, soft material processed is crossed 30 mesh sieves granule processed, and 60 ℃ of oven dry add magnesium stearate 2.4g, tabletting.
2.2 the preparation of coated tablet: get a certain amount of heart, after weighing, put in the use for laboratory coating pan of middling speed rotation, with spray gun the slow controlled release coat liquid of the thermosol plasticising Aquacoat of the present invention's preparation is carried out coating, hot air drying, coating take out freeze-day with constant temperature (60 ℃ of dry 12h) during to 1.15 times of label weight, namely get diclofenac sodium Aquacoat coated tablet, coated tablet is for subsequent use.
2.4 the mensuration of release ［ 4 ］: adopt " 95 editions the second methods of Chinese pharmacopoeia, dissolution medium is the phosphate buffer 900ml of pH6.8, rotating speed is 100r/min, temperature is (37 ± 0.1) ℃, respectively at certain hour interval sample thief 5ml, mend dissolution medium 5ml, sample filters through the microporous filter membrane of 0.8 μ m, get subsequent filtrate and measure, measuring wavelength is (276 ± 2) nm.
2.5 influence factor's observation
2.5.1 blank group (diclofenac sodium sheet) and the impact contrast of coating group (diclofenac sodium coated tablet) on drug release:
Make the diclofenac sodium coated tablet that diclofenac sodium sheet and 2.2 makes with 2.1 and carry out the drug release determination experiment, investigate the diclofenac sodium coated tablet to the impact of drug release.
3, result: see Fig. 1.
4, conclusion: prove absolutely with the diclofenac sodium coated tablet drug releasing rate that makes behind the slow controlled release coat liquid coating of the thermosol plasticising Aquacoat of method of the present invention preparation obviously slow than the diclofenac sodium sheet drug release rate of coating not and the persistent period is longer by Fig. 1 experimental data, can reach 8h, confirm that effectively the slow release controlling coating material of thermosol plasticising Aquacoat has preferably slow controlled-release effect.
Experimental results show that: the slow release controlling coating material of the thermosol plasticising Aquacoat of the method for embodiment 2-embodiment 5 preparation is carried out coating to the diclofenac sodium sheet, also has the effect similar to embodiment 1.
Claims (3)
1. the slow release controlling coating material preparation method of thermosol plasticising Aquacoat is characterized in that comprising the steps:
(1) thermosol plasticising: be the ratio of 100:60-100:10-50 in mass ratio, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, be that 80 ℃-145 ℃, rotating speed are under 25-60 rev/min the condition in temperature, stir 20-300min, stop to stir;
(2) change mutually: the product insulation 3-8h under 80 ℃-145 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 80 ℃-145 ℃, be to carry out emulsifying under 25-60 rev/min the condition at rotating speed, emulsification times is 10-15h, is cooled to room temperature, obtain finished product, the mass ratio of described oleic acid, ammonia, distilled water, silicon dioxide and ethyl cellulose is 2-100:50-500:50-700:1-75:100.
2. thermosol plasticising Aquacoat according to claim 1 delays the release controlling coating material preparation method, it is characterized in that step (1) thermosol plasticising is: be in mass ratio the ratio of 100:80:30, ethyl cellulose, ethanol and dibutyl sebacate are put into retort, be that 100 ℃, rotating speed are under 40 rev/mins the condition in temperature, stir 100-200min, stop to stir.
3. thermosol plasticising Aquacoat according to claim 1 delays the release controlling coating material preparation method, it is characterized in that step (2) changes into mutually: the product insulation 4-6h under 100 ℃ with step (1) add oleic acid, ammonia, distilled water and silicon dioxide successively; At 100 ℃, be to carry out emulsifying under 40 rev/mins the condition at rotating speed, emulsification times is 13h, is cooled to room temperature, obtains finished product. the mass ratio of described oleic acid, ammonia, distilled water, silicon dioxide and ethyl cellulose is 4-50:100-300:100-500:2-37:100.
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| CN2012104945561A CN102920679A (en) | 2012-11-27 | 2012-11-27 | Preparation method of hot-melt plasticizing ethyecellulose water dispersion sustained and controlled release coating material |
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| CN2012104945561A CN102920679A (en) | 2012-11-27 | 2012-11-27 | Preparation method of hot-melt plasticizing ethyecellulose water dispersion sustained and controlled release coating material |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111248043A (en) * | 2020-03-25 | 2020-06-09 | 宋万鹏 | High-quality astragalus membranaceus planting method combining deep ploughing regulation and water-retention fertilizer application |
Citations (3)
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|---|---|---|---|---|
| CN1111126A (en) * | 1993-11-23 | 1995-11-08 | 欧罗赛铁克有限公司 | Immediate release tablet cores of insoluble drugs having sustained release coating |
| CN1270026A (en) * | 1999-01-18 | 2000-10-18 | 格吕伦塔尔有限公司 | Controlled releasing Qumaduo preparation having stably releasing mode and preparing method thereof |
| CN101342154A (en) * | 2007-07-10 | 2009-01-14 | 天津科技大学 | Preparation of internal plasticization type cellulose ethyl ether (EC) medicament sustained and controlled release aqueous clothing sheet agent |
-
2012
- 2012-11-27 CN CN2012104945561A patent/CN102920679A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1111126A (en) * | 1993-11-23 | 1995-11-08 | 欧罗赛铁克有限公司 | Immediate release tablet cores of insoluble drugs having sustained release coating |
| CN1270026A (en) * | 1999-01-18 | 2000-10-18 | 格吕伦塔尔有限公司 | Controlled releasing Qumaduo preparation having stably releasing mode and preparing method thereof |
| CN101342154A (en) * | 2007-07-10 | 2009-01-14 | 天津科技大学 | Preparation of internal plasticization type cellulose ethyl ether (EC) medicament sustained and controlled release aqueous clothing sheet agent |
Non-Patent Citations (1)
| Title |
|---|
| 黄雁等: "乙基纤维素水分散体在缓控释薄膜包衣领域中的应用", 《塑料》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111248043A (en) * | 2020-03-25 | 2020-06-09 | 宋万鹏 | High-quality astragalus membranaceus planting method combining deep ploughing regulation and water-retention fertilizer application |
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Application publication date: 20130213 |