CN109432033B - Amlodipine besylate dripping pill and its prepn - Google Patents
Amlodipine besylate dripping pill and its prepn Download PDFInfo
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- CN109432033B CN109432033B CN201811598691.4A CN201811598691A CN109432033B CN 109432033 B CN109432033 B CN 109432033B CN 201811598691 A CN201811598691 A CN 201811598691A CN 109432033 B CN109432033 B CN 109432033B
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- polyethylene glycol
- dripping
- amlodipine besylate
- drip irrigation
- cooling
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- General Chemical & Material Sciences (AREA)
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- Urology & Nephrology (AREA)
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Abstract
The preparation method of the amlodipine besylate dropping pill comprises the following steps: s1, stirring and mixing polyethylene glycol 4000 and polyethylene glycol 6000, and slowly heating to 55 ℃ to be molten; s2, adding the melt obtained in the step S1 into a drip irrigation device, keeping the temperature in the drip irrigation device at 75 ℃, adding amlodipine besylate after the polyethylene glycol 4000 and the polyethylene glycol 6000 are liquefied, and fully mixing for 1 h; s3, dripping, namely adjusting the dripping speed by controlling the pressure in the drip irrigation equipment, primarily cooling the liquid medicine dripped from the drip irrigation equipment by cooling gas, then dripping into the simethicone cooling liquid for secondary cooling, draining the simethicone, cleaning by using petroleum ether, and volatilizing to form primary dripping pills; s4, coating the preliminary dripping pills in the step S3 to form finished dripping pills. The scheme also discloses components of the amlodipine besylate dropping pill. The invention achieves the following beneficial effects: long storage time and easy disintegration.
Description
Technical Field
The invention relates to the field of biomedicine, in particular to amlodipine besylate dropping pills.
Background
Amlodipine besylate tablets are indicated for hypertension and are suitable for treating hypertension. Can be used alone or in combination with other antihypertensive drugs. Can also be used for treating chronic stable angina pectoris of coronary heart disease (CAD). Can be used alone or in combination with other anti-angina pectoris drugs. Vasospastic angina (Prinzmetal's or variant angina) the product is suitable for the treatment of diagnosed or suspected vasospastic angina. Can be used alone or in combination with other anti-angina pectoris drugs. The coronary heart disease proved by angiography is proved to be coronary heart disease, but the ejection fraction is more than or equal to 40 percent and patients without heart failure can reduce the hospitalization risk caused by angina pectoris and reduce the risk of coronary artery reconstruction.
However, the tablets are available in the market, and the surface area of the tablets is lower than that of the dripping pills under the same weight, which is not beneficial to absorption.
Disclosure of Invention
The invention aims to overcome the defects of the prior art and provide an amlodipine besylate dropping pill which is easy to absorb and has high yield.
The purpose of the invention is realized by the following technical scheme: amlodipine besylate dripping pills, an active agent, a disintegrating agent and a pill forming matrix;
the active agent is amlodipine besylate, the disintegrating agent is polacrilin potassium, and the pelleting matrix comprises polyethylene glycol 4000 and polyethylene glycol 6000;
in each dripping pill, 2.5-10 mg of amlodipine besylate, 1-4 mg of polacrilin potassium, 10-17.5 mg of polyethylene glycol 4000 and 2-6 mg of polyethylene glycol 6000 are adopted.
The coating powder is characterized by also comprising the following components in percentage by weight: the content of amlodipine besylate is 0.13-0.53: 5.
the preparation method of the amlodipine besylate dropping pill comprises the following steps:
s1, stirring and mixing polyethylene glycol 4000 and polyethylene glycol 6000, and slowly heating to 55 ℃ to be molten;
s2, adding the melt obtained in the step S1 into a drip irrigation device, keeping the temperature in the drip irrigation device at 75 ℃, adding amlodipine besylate after the polyethylene glycol 4000 and the polyethylene glycol 6000 are liquefied, and fully mixing for 1 h;
s3, dripping, namely adjusting the dripping speed by controlling the pressure in the drip irrigation equipment, primarily cooling the liquid medicine dripped from the drip irrigation equipment by cooling gas, then dripping into the simethicone cooling liquid for secondary cooling, draining the simethicone, cleaning by using petroleum ether, and volatilizing to form primary dripping pills;
s4, coating the preliminary dripping pills in the step S3 to form finished dripping pills.
The drip irrigation equipment is an DWJ-AS type test pill dropping machine, the pipe diameter is 1.3 mm-1.1 mm, and the dropping speed is 50 drops/min-60 drops/min.
The cooling gas is made of a refrigerating machine, the cooling gas of the refrigerating machine is led out through an output pipe, the end of the output pipe is in a spray head shape, and the spray head is positioned between the outlet of the drip irrigation equipment and the liquid level of the dimethyl silicon oil.
The invention has the following advantages: the drop pill type is adopted, so that the absorption is facilitated; the cooling gas is used for primary cooling before the dimethyl silicon cooling liquid enters, so that the condition that some dropping liquid enters the dimethyl silicon cooling liquid and is broken into a plurality of small dropping pills is avoided, and the product percent of pass is improved.
Detailed Description
The present invention is further described below, but the scope of the present invention is not limited to the following.
The amlodipine besylate dropping pill comprises the following preparation steps:
s1, stirring and mixing polyethylene glycol 4000 and polyethylene glycol 6000, and slowly heating to 55 ℃ to be molten;
s2, adding the melt obtained in the step S1 into a drip irrigation device, keeping the temperature in the drip irrigation device at 75 ℃, adding amlodipine besylate and polacrilin potassium after polyethylene glycol 4000 and polyethylene glycol 6000 are liquefied, and fully mixing for 1 hour;
s3, dripping, namely adjusting the dripping speed by controlling the pressure in the drip irrigation equipment, primarily cooling the liquid medicine dripped from the drip irrigation equipment by cooling gas, then dripping into the simethicone cooling liquid for secondary cooling, draining the simethicone, cleaning by using petroleum ether, and volatilizing to form primary dripping pills;
s4, coating the preliminary dripping pills in the step S3 to form finished dripping pills.
Also discloses components of the amlodipine besylate dripping pill, and specific examples are as follows.
[ EXAMPLE one ] amlodipine besylate dripping pill
The composition comprises an active agent, a disintegrating agent and a pelleting matrix, wherein the active agent is amlodipine besylate, the disintegrating agent is polacrilin potassium, and the pelleting matrix comprises polyethylene glycol 4000 and polyethylene glycol 6000.
Specifically, in each dripping pill, amlodipine besylate is 2.5mg, polacrilin potassium is 1mg, polyethylene glycol 4000 is 10mg, and polyethylene glycol 6000 is 2 mg.
The coating powder is characterized by also comprising the following components in percentage by weight: amlodipine besylate is 0.13: 5.
[ EXAMPLE II ] A method for preparing amlodipine besylate dripping pills
The composition comprises an active agent, a disintegrating agent and a pelleting matrix, wherein the active agent is amlodipine besylate, the disintegrating agent is polacrilin potassium, and the pelleting matrix comprises polyethylene glycol 4000 and polyethylene glycol 6000.
Specifically, in each dripping pill, 6.25mg of amlodipine besylate, 2.5mg of polacrilin potassium, 13.75mg of polyethylene glycol 4000 and 4mg of polyethylene glycol 6000 are adopted.
The coating powder is characterized by also comprising the following components in percentage by weight: amlodipine besylate is 0.33: 5.
[ EXAMPLE III ] A method for preparing amlodipine besylate dripping pills
The composition comprises an active agent, a disintegrating agent and a pelleting matrix, wherein the active agent is amlodipine besylate, the disintegrating agent is polacrilin potassium, and the pelleting matrix comprises polyethylene glycol 4000 and polyethylene glycol 6000.
Specifically, in each dripping pill, 10mg of amlodipine besylate, 4mg of polacrilin potassium, 17.5mg of polyethylene glycol 4000 and 6mg of polyethylene glycol 6000 are adopted.
The coating powder is characterized by also comprising the following components in percentage by weight: amlodipine besylate is 0.53: 5.
dissolution test tests were performed on the dropping pills prepared in example one, example two, and example three as test samples. When the experimental samples are selected, the samples which are rolled but coated are selected for experiment and observed. A, B, C three sets of experiments are selected, which respectively correspond to the first embodiment, the second embodiment and the third embodiment, and the number of the experimental cups in each set is 3.
Before the dissolution experiment, the pills were weighed, and in order to show the weight gradient, the average of the selected pills satisfied the equal difference, which is shown in table one.
Experiments show that the dissolution rates of A, B, C three groups all meet the regulation of pharmacopoeia 2015 edition. And the group A is better than the group C, and the group C is better than the group B, so that the weight difference between the group A and the group B and the group C is not large, but the dissolving time is much shorter, so that the parameters in the group A (namely the first embodiment) are preferred during preparation.
Table one:
| A | B | C | pharmacopeia 2015 edition | |
| Average pill weight | 19.6mg | 19.9mg | 20.2mg | <30mg |
| Difference in pill weight | -3.5%~+7.2% | -6.7%~+2.8% | -6.3%~+3.8% | ±15% |
| Time limit of dissolution | 12min | 16min | 14min | <60min |
Claims (3)
1. The amlodipine besylate dropping pill is characterized in that: comprises an active agent, a disintegrating agent and a pelleting matrix;
the active agent is amlodipine besylate, the disintegrating agent is polacrilin potassium, and the pelleting matrix comprises polyethylene glycol 4000 and polyethylene glycol 6000;
in each dripping pill, 2.5-10 mg of amlodipine besylate, 1-4 mg of polacrilin potassium, 10-17.5 mg of polyethylene glycol 4000 and 2-6 mg of polyethylene glycol 6000 are contained;
the coating powder is characterized by also comprising the following components in percentage by weight: the content of amlodipine besylate is 0.13-0.53: 5;
the preparation method of the amlodipine besylate dropping pill comprises the following steps:
s1, stirring and mixing polyethylene glycol 4000 and polyethylene glycol 6000, and slowly heating to 55 ℃ to be molten;
s2, adding the melt obtained in the step S1 into a drip irrigation device, keeping the temperature in the drip irrigation device at 75 ℃, adding amlodipine besylate after the polyethylene glycol 4000 and the polyethylene glycol 6000 are liquefied, and fully mixing for 1 h;
s3, dripping, namely adjusting the dripping speed by controlling the pressure in the drip irrigation equipment, primarily cooling the liquid medicine dripped from the drip irrigation equipment by cooling gas, then dripping into the simethicone cooling liquid for secondary cooling, draining the simethicone, cleaning by using petroleum ether, and volatilizing to form primary dripping pills;
s4, coating the preliminary dripping pills in the step S3 to form finished dripping pills.
2. The amlodipine besylate dripping pill according to claim 1, wherein: the drip irrigation equipment is an DWJ-AS type test pill dropping machine, the pipe diameter is 1.3 mm-1.1 mm, and the dropping speed is 50 drops/min-60 drops/min.
3. Amlodipine besylate dropping pill according to claim 2, characterized in that: the cooling gas is made of a refrigerating machine, the cooling gas of the refrigerating machine is led out through an output pipe, the end of the output pipe is in a spray head shape, and the spray head is positioned between the outlet of the drip irrigation equipment and the liquid level of the dimethyl silicon oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811598691.4A CN109432033B (en) | 2018-12-26 | 2018-12-26 | Amlodipine besylate dripping pill and its prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811598691.4A CN109432033B (en) | 2018-12-26 | 2018-12-26 | Amlodipine besylate dripping pill and its prepn |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109432033A CN109432033A (en) | 2019-03-08 |
| CN109432033B true CN109432033B (en) | 2021-03-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811598691.4A Active CN109432033B (en) | 2018-12-26 | 2018-12-26 | Amlodipine besylate dripping pill and its prepn |
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| Country | Link |
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| CN (1) | CN109432033B (en) |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004219195A (en) * | 2003-01-14 | 2004-08-05 | Japan Nuclear Cycle Development Inst States Of Projects | External gelation method for manufacturing spherical nuclear fuel particle |
| CN1552313A (en) * | 2003-12-19 | 2004-12-08 | 北京正大绿洲医药科技有限公司 | Process for preparing drops or other drop agents |
| CN1879621A (en) * | 2006-05-18 | 2006-12-20 | 赵伟庆 | Drop pills of amlodipine maleate and preparation method thereof |
| CN1899268A (en) * | 2006-07-13 | 2007-01-24 | 北京国仁堂医药科技发展有限公司 | L-amlodipine besilate dripping pill and its preparing method |
| CN1915225A (en) * | 2005-06-07 | 2007-02-21 | 北京振东光明药物研究院 | Drop pills of Amlodipine, and preparation method |
| CN1939282A (en) * | 2005-07-11 | 2007-04-04 | 刘凤鸣 | Amlodipine benesanli dropping balls and production thereof |
| CN1981759A (en) * | 2005-12-14 | 2007-06-20 | 陈茜 | Levamlodipine besylate dropping balls and their making method |
| CN101406461A (en) * | 2008-10-24 | 2009-04-15 | 北京九龙制药有限公司 | Amlodipine besylate dropping pills and preparation method thereof |
| CN104274519A (en) * | 2013-07-11 | 2015-01-14 | 天士力制药集团股份有限公司 | Compound salvia miltiorrhiza drop pill prepared by vibration method |
-
2018
- 2018-12-26 CN CN201811598691.4A patent/CN109432033B/en active Active
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004219195A (en) * | 2003-01-14 | 2004-08-05 | Japan Nuclear Cycle Development Inst States Of Projects | External gelation method for manufacturing spherical nuclear fuel particle |
| CN1552313A (en) * | 2003-12-19 | 2004-12-08 | 北京正大绿洲医药科技有限公司 | Process for preparing drops or other drop agents |
| CN1915225A (en) * | 2005-06-07 | 2007-02-21 | 北京振东光明药物研究院 | Drop pills of Amlodipine, and preparation method |
| CN1939282A (en) * | 2005-07-11 | 2007-04-04 | 刘凤鸣 | Amlodipine benesanli dropping balls and production thereof |
| CN1981759A (en) * | 2005-12-14 | 2007-06-20 | 陈茜 | Levamlodipine besylate dropping balls and their making method |
| CN1879621A (en) * | 2006-05-18 | 2006-12-20 | 赵伟庆 | Drop pills of amlodipine maleate and preparation method thereof |
| CN1899268A (en) * | 2006-07-13 | 2007-01-24 | 北京国仁堂医药科技发展有限公司 | L-amlodipine besilate dripping pill and its preparing method |
| CN101406461A (en) * | 2008-10-24 | 2009-04-15 | 北京九龙制药有限公司 | Amlodipine besylate dropping pills and preparation method thereof |
| CN104274519A (en) * | 2013-07-11 | 2015-01-14 | 天士力制药集团股份有限公司 | Compound salvia miltiorrhiza drop pill prepared by vibration method |
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| Publication number | Publication date |
|---|---|
| CN109432033A (en) | 2019-03-08 |
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