CN104523622A - Fimasartan dropping pill and preparation method thereof - Google Patents
Fimasartan dropping pill and preparation method thereof Download PDFInfo
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- CN104523622A CN104523622A CN201410771729.9A CN201410771729A CN104523622A CN 104523622 A CN104523622 A CN 104523622A CN 201410771729 A CN201410771729 A CN 201410771729A CN 104523622 A CN104523622 A CN 104523622A
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- fimasartan
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- drop pill
- pill
- acid
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Abstract
The invention discloses a fimasartan dropping pill for treating hypertension and a preparation method of the fimasartan dropping pill. The preparation method comprises the steps of with fimasartan as a raw material, adding a matrix according to a prescription, and uniformly mixing to obtain a mixed material; heating the mixed material to be molten, and uniformly stirring to obtain a mixture; placing the mixture into a special pill dropping machine; and dropping pills into a condensing agent at a proper speed to condense to form the fimasartan dropping pill. The fimasartan dropping pill is high in bioavailability, capable of rapidly releasing drugs, high in effect taking speed and drug stability and convenient to take; in addition, the consumption of auxiliary materials is reduced, the production process is simple, the preparation method is easy to operate, the weight difference is small, and the production cost is reduced; and no dust is generated, and labor protection can be favorably realized.
Description
Technical field
The invention relates to medicament preparation and preparation method thereof, is specially a kind of Fimasartan drop pill and preparation method thereof.
Background technology
Fimasartan is developed by Boryung Pharmaceutical Co., Ltd. of Korea S, in Korea S's listing in 2011, is a kind of novel angiotensin II receptor antagonist, has the effect of selectivity retardance AT1 receptor.Preclinical study shows, Fimasartan toleration is fine, and blood pressure lowering onset is faster compared with losartan, and antihypertensive effect is better.Compared with reducing siDBP or 24ABP result with other current research ARB class medicine, Fimasartan group siDBP fall is larger than other drug, and the Olmesartan that its 24ABP fall also reduces 24ABP the strongest with ARB class medicine has comparability.Fimasartan can improve the activity of feritin and Angiotensin II.Fimasartan absorbs rapidly, and successive administration does not find drug accumulation in 7 days.Preclinical study and clinical experiment show, Fimasartan may be higher than other ARB class drug safeties, and more effective in reduction diastole pressure, Fimasartan is very potential becomes ARB medicine the most excellent in next two decades.
The medicine of existing Fimasartan class is mostly tablet, have that dose is large, the heavy shortcomings such as difficulty is swallowed, onset is slow of taste, the new formulation type of therefore seeking such medicine is the needs of current clinical treatment, meanwhile, the technique finding out applicable new medicine medicine type also becomes the major issue of research at present.
Summary of the invention
The problem that the invention will solve is to provide drops of a kind of Fimasartan and preparation method thereof.
For solving the problems of the technologies described above, the technical scheme that the invention adopts is: a kind of Fimasartan drop pill, described drop pill be by Fimasartan fine powder and substrate with 1: the weight ratio of (1-60) combines; Described Fimasartan fine powder is the mixture of one or more in Fimasartan and acid group derivant thereof, and wherein said Fimasartan acid group derivant comprises at least one in phosphoric acid, sulphuric acid, hydrochloric acid, nitric acid, hydroiodic acid, maleate derivant; Described substrate is one or more mixture mixed according to any weight ratio in Polyethylene Glycol 500-6000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, the acid of monostearate drier oil, insect wax, tween, class of department.
Described drop pill can be made into common drop pill, may also be slow-release pill preparation, controlled release dropping pill formulation, enteric coated drop pill preparation, coated drop pill preparation.
The preparation method step of described Fimasartan drop pill is as follows:
(1) proportionally take Fimasartan fine powder and substrate respectively, and described substrate is heated to molten condition;
(2) added by the Fimasartan fine powder taken in the substrate of the molten condition prepared in described step (1), fully stirring makes described Fimasartan fine powder be dispersed in the substrate of melting and forms fused solution;
(3) described fused solution is inserted in pill dripping machine funnel, insulation, and adjust water dropper temperature;
(4) sizeable drip nozzle is selected, with suitable speed by described fused solution instillation coolant;
(5) treat that described fused solution shrinks molding in described coolant, take out, throw away the refrigerant, the described Fimasartan drop pill be drying to obtain.
Described coolant comprises the mixture of one or more in dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution.
Step (3) described holding temperature is 80 DEG C, and the temperature of the described instillation coolant of step (4) is-5 DEG C.
The advantage that the invention has and good effect are: the present invention studies by experiment and transforms Fimasartan dosage form; drop pill is changed into from tablet; ingredient, colloid or microcrystalline state is made to be scattered in substrate; the total surface area of medicine increases, and substrate is hydrophilic, has wetting action to medicine; medicine can be made to leach into rapidly microgranule or solution; thus make the dissolving of medicine and absorb to accelerate, thus improve bioavailability and medicine stability, produce and efficiently, easily act on.And production technology of the present invention is technically optimized original and improve, produce the dispersion of drop pill Chinese medicine comparatively even, more easily absorb after medicine stability is high, oral, be applicable to large-scale production.
Detailed description of the invention
The invention provides a kind of Fimasartan drop pill and preparation method thereof, be primary raw material with Fimasartan in the method, according to certain ratio, add the substrate such as Polyethylene Glycol, be prepared from through specific technique, apparatus processing.Specific as follows:
(1) prescription: Fimasartan+substrate
Substrate: one or more the composition including Polyethylene Glycol (1500,2000,4000,6000,8000,10000,20000), s6, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers.
The weight ratio of Fimasartan and substrate is 1:(1-60).
Preparation technology: concrete implementation step is as follows:
Pramipexole mixes with substrate according to certain ratio by the first step.
Second step adopts water-bath, oil bath or other mode of heating, mixed material is heated to molten condition, stirs.
Above molten mixture is inserted in pill dripping machine funnel by the 3rd step, insulation, and to adjust water dropper temperature be 80 DEG C.
4th step selects sizeable drip nozzle, with suitable speed, instills in the condensing agent of-5 DEG C.Condensing agent can be any one or a few in liquid paraffin, methyl-silicone oil, vegetable oil.
5th step type to be shrunk to, takes out, removing surface condensation agent, dry, pack and get final product.
Wherein, the Fimasartan selected in the present invention is compound and acid group (including but not limited to phosphoric acid, sulphuric acid, hydrochloric acid, nitric acid, hydroiodic acid, the maleate etc.) derivant thereof with following features:
Chinese: Fimasartan and acid group analog derivative thereof
English name: Fimasartan
Chemical name: 2-butyl-5-dimethylamino sulfo-formyl methyl-6-methyl-3-[[2'-(1H-TETRAZOLE-5-base) biphenyl-4-base] methyl] pyrimidine-4 (3H)-one
Molecular formula: C
27h
31n
7oS
Structural formula:
Substrate wherein can be that any one or a few in Polyethylene Glycol (1500,2000,4000,6000,8000,10000,20000), s6, betacyclodextrin, poloxamer, carboxymethyl starch sodium, stearic acid, sodium stearate, glycerin gelatine, glyceryl monostearate, Lac, polyoxyethylene monostearate, polyethers etc. mixes mutually;
Wherein this drop pill can be made into common drop pill, also can support slow-release pill preparation, controlled release dropping pill formulation, enteric coated drop pill preparation, coated drop pill preparation.
Below in conjunction with concrete embodiment, the present invention can be understood further, but following instance not limitation of the invention.
Embodiment 1:
Prescription: Fimasartan 0.5g; PEG4000 5g;
PEG8000 25g; Make 1000 altogether.
Preparation method: after Fimasartan, PEG4000, PEG8000 mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Embodiment 2:
Prescription: Fimasartan 1g; PEG1500 5g;
PEG6000 25g; Make 1000 altogether.
Preparation method: after getting Fimasartan, PEG1500, PEG6000 mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Embodiment 3:
Prescription: Fimasartan 2.5g; PEG1500 5g;
Poloxamer 5g; PEG4000 25g; Make 1000 altogether.
Preparation method: after getting Fimasartan, PEG1500, PEG4000, poloxamer mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Embodiment 4:
Prescription: Fimasartan 5g; PEG4000 5g;
Stearic acid 5g; PEG8000 25g; Make 1000 altogether.
Preparation method: after getting Fimasartan, PEG4000, PEG8000, stearic acid mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Embodiment 5:
Prescription: Fimasartan 7.5g; PEG4000 5g;
Carboxymethyl starch sodium 5g; PEG8000 25g; Make 1000 altogether.
Preparation method: after getting Fimasartan, PEG4000, PEG8000, carboxymethyl starch sodium mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Embodiment 6:
Prescription: Fimasartan 10g; Carboxymethyl starch sodium 5g;
Stearic acid 5g; PEG8000 25g; Make 1000 altogether.
Preparation method: after getting Fimasartan, carboxymethyl starch sodium, PEG8000, stearic acid mix homogeneously, heating in water bath, makes its complete melting, is poured into by this fused solution in drop pill dripping machine Materials hopper, 80 DEG C of insulations, select drip nozzle, instill in the dimethicone of-5 DEG C, after to be formed, filter, be separated, wiped clean, to obtain final product.
Above specific embodiments of the invention have been described in detail, but described content being only this preferred embodiment, the practical range for limiting this can not being considered to.All equalizations done according to the application's scope change and improve, and all should still belong within patent covering scope originally.
Claims (5)
1. a Fimasartan drop pill, is characterized in that: described drop pill be by Fimasartan fine powder and substrate with 1: the weight ratio of (1-60) combines; Described Fimasartan fine powder is the mixture of one or more in Fimasartan and acid group derivant thereof, and wherein said Fimasartan acid group derivant comprises at least one in phosphoric acid, sulphuric acid, hydrochloric acid, nitric acid, hydroiodic acid, maleate derivant; Described substrate is one or more mixture mixed according to any weight ratio in Polyethylene Glycol 500-6000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, the acid of monostearate drier oil, insect wax, tween, class of department.
2. Fimasartan drop pill according to claim 1, is characterized in that: described drop pill can be made into common drop pill, may also be slow-release pill preparation, controlled release dropping pill formulation, enteric coated drop pill preparation, coated drop pill preparation.
3. a preparation method for Fimasartan drop pill according to claim 1, is characterized in that: the preparation method step of described Fimasartan drop pill is as follows:
(1) proportionally take Fimasartan fine powder and substrate respectively, and described substrate is heated to molten condition;
(2) added by the Fimasartan fine powder taken in the substrate of the molten condition prepared in described step (1), fully stirring makes described Fimasartan fine powder be dispersed in the substrate of melting and forms fused solution;
(3) described fused solution is inserted in pill dripping machine funnel, insulation, and adjust water dropper temperature;
(4) sizeable drip nozzle is selected, with suitable speed by described fused solution instillation coolant;
(5) treat that described fused solution shrinks molding in described coolant, take out, throw away the refrigerant, the described Fimasartan drop pill be drying to obtain.
4. the preparation method of Fimasartan drop pill according to claim 3, is characterized in that: described coolant comprises the mixture of one or more in dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution.
5. the preparation method of Fimasartan drop pill according to claim 3, is characterized in that: step (3) described holding temperature is 80 DEG C, and the temperature of the described instillation coolant of step (4) is-5 DEG C.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410771729.9A CN104523622A (en) | 2014-12-14 | 2014-12-14 | Fimasartan dropping pill and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410771729.9A CN104523622A (en) | 2014-12-14 | 2014-12-14 | Fimasartan dropping pill and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN104523622A true CN104523622A (en) | 2015-04-22 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410771729.9A Pending CN104523622A (en) | 2014-12-14 | 2014-12-14 | Fimasartan dropping pill and preparation method thereof |
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| CN (1) | CN104523622A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105784867A (en) * | 2016-03-28 | 2016-07-20 | 北京睿创康泰医药研究院有限公司 | HPLC (High Performance Liquid Chromatography) method for analyzing fimasartan associated substances and use of impurities as reference standard |
-
2014
- 2014-12-14 CN CN201410771729.9A patent/CN104523622A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105784867A (en) * | 2016-03-28 | 2016-07-20 | 北京睿创康泰医药研究院有限公司 | HPLC (High Performance Liquid Chromatography) method for analyzing fimasartan associated substances and use of impurities as reference standard |
| CN105784867B (en) * | 2016-03-28 | 2019-01-01 | 北京睿创康泰医药研究院有限公司 | Make the purposes of reference standard for analyzing HPLC method and these impurity of the Fimasartan in relation to substance |
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150422 |