CN105395552A - Solid preparation containing fimasartan and salt thereof - Google Patents
Solid preparation containing fimasartan and salt thereof Download PDFInfo
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- CN105395552A CN105395552A CN201410460604.4A CN201410460604A CN105395552A CN 105395552 A CN105395552 A CN 105395552A CN 201410460604 A CN201410460604 A CN 201410460604A CN 105395552 A CN105395552 A CN 105395552A
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- fimasartan
- salt
- solid preparation
- potassium
- tablet
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Abstract
The invention relates to a solid preparation containing fimasartan and a salt thereof, wherein the solid preparation further contains hydroxypropyl cellulose. According to the present invention, hydroxypropyl cellulose is added to the fimasartan and the salt thereof, such that the solubility of the fimasartan is improved so as to further improve the bioavailability.
Description
Technical field
The invention belongs to pharmaceutical technology sectors, be specifically related to the pharmaceutical preparation as active component of a kind of Fimasartan and salt thereof.In addition, the invention still further relates to Fimasartan and salt thereof the preparation method as the pharmaceutical preparation of active component.
Background technology
Fimasartan, Chinese name: 2-butyl-5-dimethylamino sulfo-formyl methyl-6-methyl-3-[[2 '-(1H-TETRAZOLE-5-base) biphenyl-4-base] methyl] pyrimidine-4 (3H)-one, English name: fimasartan, structural formula is as follows:
Fimasartan, be a kind of novel angiotensin II receptor antagonist (ARBs) class antihypertensive, there is the effect of selectivity retardance AT1 receptor, researched and developed by Boryung Pharmaceutical Co., Ltd. of Korea S, in 2011 in Korean market, within 2013, sell more than 100,000,000.At present, the intermediate of Fimasartan raw material has had a small amount of outlet.
Preclinical study shows, Fimasartan shows quick and effective resisting hypertension effect in multiple Type of Hypertension, very safety and have good toleration, be better than other medicines of the same type, it is very potential becomes ARBs medicine the most excellent in next two decades.
After we find that Fimasartan potassium mixes with hyprolose (HPC) in the process of the potassium salt Fimasartan potassium sheet of research Fimasartan, significantly improve the dissolubility that its pH is the buffer salt of 3.0 ~ 6.0, improve the bioavailability that dissolubility can further improve medicine.
Summary of the invention
The invention provides a kind of solid preparation containing Fimasartan, said preparation is have good dissolubility in the buffer salt of 3.0 ~ 6.0 at its pH relative to Fimasartan potassium tablets, the object of the present invention is to provide a kind of Fimasartan solid preparation with higher bioavailability further.In addition, present invention also offers the method for this solid preparation of preparation.
Object of the present invention can be realized by following measures:
Contain a solid preparation for Fimasartan and salt thereof, said preparation is also containing hyprolose.Wherein, described Fimasartan and salt thereof comprise potassium salt, sodium salt, magnesium salt, strontium salt or other can for salt.Further, the mass content of described Fimasartan is 5.0% ~ 90.0%, and the mass content of described hyprolose is 0.5% ~ 50%.
Granule, tablet, chewable tablet or capsule is can be made into, preferred tablet and capsule in specific embodiments of the present invention.Pharmaceutical preparation of the present invention can be produced by the method for known for those skilled in the art production granule, tablet or capsule, comprises the following steps:
(1) Fimasartan or its salt of appropriate particle size size is prepared;
(2) Fimasartan or its salt are mixed homogeneously with hyprolose and adjuvant;
(3) appropriate lubricant is added;
(4) mould be applicable to is adopted to carry out tabletting;
(5) film coating.
We can improve it significantly after finding Fimasartan potassium to mix with hyprolose be under study for action dissolubility in the buffer salt of 3.0 ~ 6.0 at pH, and improve dissolubility at drug world drug bioavailability can be caused to significantly improve.
It is better that the present invention obtains dissolubility simultaneously, the dosage form containing Fimasartan and salt thereof that drug bioavailability is high.
In different medium, carried out solubility study to Fimasartan crude drug, result is as follows:
Assay method: take Fimasartan potassium raw material 100mg respectively and be placed in 5mL measuring bottle, add 0.1mol/L hydrochloric acid, acetate buffer that water, pH are respectively 3.5,4.5,5.5 is settled to corresponding scale, centrifuging and taking supernatant after 37 DEG C of ultrasonic 1h, measures absorbance with after respective solvent dilution to debita spissitudo respectively.Configure corresponding reference substance solution, measure absorbance, calculate dissolubility, separately get Fimasartan potassium (API) 100mg and hyprolose (HPC) 5mg, operate with method.Solubility test the results are shown in following table 1.
Table 1: Fimasartan crude drug dissolubility in media as well
| Medium | Principal agent concentration (mg/ml) |
| PH3.5 acetate buffer solution (API) | 0.011 |
| PH3.5 acetate buffer solution (API+HPC) | 0.2065 |
| PH4.5 acetate buffer solution (API) | 0.018 |
| PH4.5 acetate buffer solution (API+HPC) | 0.195 |
| PH5.5 acetate buffer solution (API) | 0.020 |
| PH5.5 acetate buffer solution (API+HPC) | 0.162 |
Result of the test shows, after Fimasartan potassium raw material adds the hyprolose of recipe quantity, is that in the acetate buffer of 3.5 ~ 5.5, dissolubility significantly improves at pH.
Detailed description of the invention
The production of invention formulation is described by exemplifying embodiment below, and exemplifying embodiment below explains the present invention in more detail and is not construed as limiting the invention.
Embodiment 1: containing the tablet of Fimasartan potassium
| Supplementary material title | Consumption (mg/ sheet) |
| Fimasartan potassium trihydrate | 66.01 |
| Lactose | 60.0 |
| Starch | 20.5 |
| Microcrystalline Cellulose | 20.0 |
| Cross-linking sodium carboxymethyl cellulose | 4.5 |
| Hydroxypropyl cellulose | 10.0 |
| Magnesium stearate | 1.5 |
Produce: add magnesium stearate mixing again by after Fimasartan potassium and the first mix homogeneously of adjuvant except for magnesium stearate, select suitable mould tabletting, obtain the tablet containing Fimasartan potassium.
Embodiment 2: containing the tablet of Fimasartan potassium
| Supplementary material title | Consumption (mg/ sheet) |
| Fimasartan potassium trihydrate | 133.02 |
| Lactose | 100.0 |
| Starch | 20.5 |
| Microcrystalline Cellulose | 20.0 |
| Cross-linking sodium carboxymethyl cellulose | 20.0 |
| Hydroxypropyl cellulose | 10.0 |
| Magnesium stearate | 3.0 |
Produce: add magnesium stearate mixing again by after Fimasartan potassium and the first mix homogeneously of adjuvant except for magnesium stearate, select suitable mould tabletting, obtain the tablet containing Fimasartan potassium.
Embodiment 3: containing the capsule of Fimasartan potassium
| Supplementary material title | Consumption (mg/ sheet) |
| Fimasartan potassium trihydrate | 133.02 |
| Mannitol | 80.0 |
| Starch | 20.5 |
| Microcrystalline Cellulose | 40.0 |
| Cross-linking sodium carboxymethyl cellulose | 20.0 |
| Hydroxypropyl cellulose | 10.0 |
| Magnesium stearate | 3.0 |
Produce: add magnesium stearate mixing again by after Fimasartan potassium and the first mix homogeneously of adjuvant except for magnesium stearate, namely fill capsule obtains the capsule containing Fimasartan.
Claims (5)
1. contain a solid preparation for Fimasartan and salt thereof, it is characterized in that: described solid preparation is also containing hyprolose.
2. solid preparation according to claim 1, is characterized in that: described Fimasartan and salt thereof comprise potassium salt, sodium salt, magnesium salt, strontium salt or other can for salt.
3. solid preparation according to claim 1 and 2, is characterized in that: the mass content of described Fimasartan is 5.0% ~ 90.0%, and the mass content of described hyprolose is 0.5% ~ 50%.
4. solid preparation according to claim 1, is characterized in that: described solid preparation is granule, tablet, chewable tablet or capsule.
5. solid preparation according to claim 4, is characterized in that: described solid preparation is tablet or capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410460604.4A CN105395552A (en) | 2014-09-05 | 2014-09-05 | Solid preparation containing fimasartan and salt thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410460604.4A CN105395552A (en) | 2014-09-05 | 2014-09-05 | Solid preparation containing fimasartan and salt thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105395552A true CN105395552A (en) | 2016-03-16 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410460604.4A Pending CN105395552A (en) | 2014-09-05 | 2014-09-05 | Solid preparation containing fimasartan and salt thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105395552A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111405893A (en) * | 2017-11-30 | 2020-07-10 | 保宁制药株式会社 | Pharmaceutical composition containing fimasartan |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102485227A (en) * | 2010-12-02 | 2012-06-06 | 鲁南制药集团股份有限公司 | Medicine composition and applications thereof |
| WO2012141385A1 (en) * | 2011-04-12 | 2012-10-18 | Boryung Pharmaceutical Co., Ltd. | Antihypertensive pharmaceutical composition |
| WO2014003305A1 (en) * | 2012-06-28 | 2014-01-03 | 보령제약 주식회사 | Pharmaceutical composition containing fimasartan and hydrochlorothiazide |
-
2014
- 2014-09-05 CN CN201410460604.4A patent/CN105395552A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102485227A (en) * | 2010-12-02 | 2012-06-06 | 鲁南制药集团股份有限公司 | Medicine composition and applications thereof |
| WO2012141385A1 (en) * | 2011-04-12 | 2012-10-18 | Boryung Pharmaceutical Co., Ltd. | Antihypertensive pharmaceutical composition |
| WO2014003305A1 (en) * | 2012-06-28 | 2014-01-03 | 보령제약 주식회사 | Pharmaceutical composition containing fimasartan and hydrochlorothiazide |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111405893A (en) * | 2017-11-30 | 2020-07-10 | 保宁制药株式会社 | Pharmaceutical composition containing fimasartan |
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Application publication date: 20160316 |
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