CN103070848A - Losartan potassium gastric floating capsule and preparation method thereof - Google Patents
Losartan potassium gastric floating capsule and preparation method thereof Download PDFInfo
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- CN103070848A CN103070848A CN2013100438721A CN201310043872A CN103070848A CN 103070848 A CN103070848 A CN 103070848A CN 2013100438721 A CN2013100438721 A CN 2013100438721A CN 201310043872 A CN201310043872 A CN 201310043872A CN 103070848 A CN103070848 A CN 103070848A
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Abstract
The invention relates to a losartan potassium gastric floating capsule, which comprises losartan potassium, PEG6000 (polyethyleneglycol), stearic acid, octodecyl alcohol, pre-gelatinized starch and mannite, wherein the losartan potassium is a powdery substance which is sieved with a 100-mesh sieve. A preparation method of the capsule comprises the following steps of: S1, mixing the PEG6000, the stearic acid and the octodecyl alcohol according to a certain proportion, heating to 64-66 DEG C, and smelting into a liquid; S2, heating the liquid mixture to 69-72 DEG C, and preserving heat for 9-11 minutes; S3, adding a proportional amount of losartan potassium into the mixture obtained in the step S2, keeping the temperature at 69-72 DEG C, and stirring uniformly; S4, adding a proportional amount of the pre-gelatinized starch and the mannite, and stirring uniformly; and S5, after the uniformity is qualified, filling in a hot state, covering a capsule cap, and cooling to the room temperature. The losartan potassium gastric floating capsule has the advantages that the medicament releasing time is long, the medicine taking times of a patient are reduced, the treatment compliance of the patient is enhanced, and the quality in a storage life is stable.
Description
Technical field
The present invention relates to the biological medicine technology field, particularly a kind of Losartan Potassium gastric floating capsule and preparation method thereof.
Background technology
Losartan Potassium (molecular formula: C
22H
22ClKN
6O, molecular weight: 461.001) for synthetic, potent Orally active medicine, be used to treat essential hypertension, be applicable to the patient of drug combination treatment.Prove in conjunction with test and pharmacology's biological detection, it can with AT1 receptor (such as vascular smooth muscle, adrenal gland, kidney and heart) selective binding, produce and to comprise that vasoconstriction and aldosterone are released in interior multiple important biological effect.Studies show that in the body: Losartan Potassium and the carboxylic acid metabolite (E-3174) with pharmacologically active thereof can be blocked the corresponding physiological action that any source or the synthetic angiotensinⅡ of any approach produce.Compare with the angiotensinⅡantagonist of other peptide classes, Losartan Potassium is without agonism.
Losartan Potassium optionally acts on the AT1 receptor, does not affect the function of ion channel important in other hormone receptors or the cardiovascular, the angiotensin converting enzyme (kininase II) of the Kallidin I that also do not suppress to degrade.
Sufferer take adopt the Losartan Potassium that traditional handicraft makes after, the Losartan Potassium hygroscopicity is strong, responsive especially to water, cause pharmaceutical release time short, namely medicine is absorbed fully by sufferer at short notice, causes the fluctuation of blood drug level peak valley larger, easily produces some untoward reaction, such as fatigue, puffiness of face, fever, even confused fault.And in order to reach therapeutic effect, patient's medicining times increases, and indirectly causes so that the treatment compliance of sufferer reduces.Because the Losartan Potassium hygroscopicity that traditional handicraft makes is strong, the ordinary preparation technology can not guarantee its steady quality within storage life.
Summary of the invention
The object of the invention is to overcome the shortcoming of prior art, a kind of pharmaceutical release time length is provided, reduces patient's medicining times, strengthens stay-in-grade Losartan Potassium gastric floating capsule and preparation method thereof in Treatment Compliance and storage life.
Purpose of the present invention is achieved through the following technical solutions: a kind of Losartan Potassium gastric floating capsule, and it comprises following component, and the parts by weight of each component are:
The preparation method of described Losartan Potassium gastric floating capsule, it may further comprise the steps:
S1, PEG6000, stearic acid, octadecanol are mixed in proportion, and are heated to 64～66 ℃, it is aqueous to treat that it is fused into;
S2, above-mentioned aqueous mixture is warmed up to 69～72 ℃, keeps 9～11min;
S3, in the aqueous mixture of step S2 gained the Losartan Potassium of additional proportion amount, keeping temperature is 69～72 ℃, and stirs;
Pre-paying starch and the mannitol of S4, additional proportion amount, and stir;
After S5, the uniformity were qualified, while hot fill covered the capsule medicated cap, is cooled to room temperature.
Described Losartan Potassium was the Losartan Potassium granule of 100 mesh sieve gained.
The present invention has the following advantages:
1, the hydrophobic auxiliary that adds significant proportion has strengthened the stability of Losartan Potassium, can effectively guarantee capsule steady quality within storage life.
2, increased the release time of medicine, the fluctuation of blood drug level peak valley is little, and has reduced patient's medicining times, has improved the compliance of sufferer treatment.
The specific embodiment
The present invention will be further described below in conjunction with embodiment, but protection scope of the present invention is not limited to the following stated.
Embodiment 1:
A kind of Losartan Potassium gastric floating capsule, it comprises following component, and each component by the parts by weight of 1000 institute's consumptions is:
Described Losartan Potassium was the Losartan Potassium granule of 100 mesh sieve gained.
The preparation of Losartan Potassium gastric floating capsule prepares by the following method:
S1, PEG6000, stearic acid, octadecanol are mixed in proportion, and are heated to 64 ℃, it is aqueous to treat that it is fused into;
S2, above-mentioned aqueous mixture is warmed up to 72 ℃, keeps 9min;
S3, in the aqueous mixture of step S2 gained the Losartan Potassium of additional proportion amount, keeping temperature is 72 ℃, and stirs;
Pre-paying starch and the mannitol of S4, additional proportion amount, and stir;
After S5, the uniformity were qualified, while hot fill covered the capsule medicated cap, is cooled to room temperature.
Embodiment 2:
A kind of Losartan Potassium gastric floating capsule, it comprises following component, and each component by the parts by weight of 1000 institute's consumptions is:
Described Losartan Potassium was the Losartan Potassium granule of 100 mesh sieve gained.
The Losartan Potassium gastric floating capsule prepares by the following method:
S1, PEG6000, stearic acid, octadecanol are mixed in proportion, and are heated to 65 ℃, it is aqueous to treat that it is fused into;
S2, above-mentioned aqueous mixture is warmed up to 70 ℃, keeps 10min;
S3, in the aqueous mixture of step S2 gained the Losartan Potassium of additional proportion amount, keeping temperature is 70 ℃, and stirs;
Pre-paying starch and the mannitol of S4, additional proportion amount, and stir;
After S5, the uniformity were qualified, while hot fill covered the capsule medicated cap, is cooled to room temperature.
Present embodiment is most preferred embodiment.
Embodiment 3:
A kind of Losartan Potassium gastric floating capsule, it comprises following component, and each component by the parts by weight of 1000 institute's consumptions is:
Described Losartan Potassium was the Losartan Potassium granule of 100 mesh sieve gained.
The Losartan Potassium gastric floating capsule prepares by the following method:
S1, PEG6000, stearic acid, octadecanol are mixed in proportion, and are heated to 66 ℃, it is aqueous to treat that it is fused into;
S2, above-mentioned aqueous mixture is warmed up to 69 ℃, keeps 11min;
S3, in the aqueous mixture of step S2 gained the Losartan Potassium of additional proportion amount, keeping temperature is 69 ℃, and stirs;
Pre-paying starch and the mannitol of S4, additional proportion amount, and stir;
After S5, the uniformity were qualified, while hot fill covered the capsule medicated cap, is cooled to room temperature.
Further specify effect of the present invention below by experiment:
A kind of Losartan Potassium gastric floating capsule that embodiments of the invention 1～3 are made is according to two X D of Chinese Pharmacopoeia version in 2010 drug release determination first method, take purified water 1000ml as solvent, rotating speed is 50rpm, respectively at 1,3,6,10 and 12 hour sampling and measuring, and the while compares with the sample that common wet method and dry granulation prepare, common hard capsule sample is with mixing such as Losartan Potassium, lactose, hyprolose, and dehydrated alcohol is granulated, and fills and gets.Under equal conditions respectively test 6 capsules,
Get the result of the test meansigma methods, its result of the test is as shown in the table:
Can find out by contrast and experiment, the flotation time of the Losartan Potassium gastric floating capsule that the present invention makes is all more than 10h, the release time of medicine is long, can effectively reduce the medicining times of sufferer, and common hard capsule can not rise at all and floats, medicine enters in the body and is just almost discharged fully, and the fluctuation of blood drug level peak valley is larger, can not obtain well therapeutic effect.
Claims (2)
1. Losartan Potassium gastric floating capsule, it is characterized in that: it comprises following component, and the parts by weight of each component are:
Losartan Potassium 25～100
PEG6000 60～120
Stearic acid 40～60
Octadecanol 40～60
Pre-paying starch 20～25
Mannitol 20～40;
The preparation method of described Losartan Potassium gastric floating capsule, its preparation method may further comprise the steps:
S1, PEG6000, stearic acid, octadecanol are mixed in proportion, and are heated to 64～66 ℃, it is aqueous to treat that it is fused into;
S2, above-mentioned aqueous mixture is warmed up to 69～72 ℃, keeps 9～11min;
S3, in the aqueous mixture of step S2 gained the Losartan Potassium of additional proportion amount, keeping temperature is 69～72 ℃, and stirs;
Pre-paying starch and the mannitol of S4, additional proportion amount, and stir;
After S5, the uniformity were qualified, while hot fill covered the capsule medicated cap, is cooled to room temperature.
2. a kind of Losartan Potassium gastric floating capsule according to claim 1, it is characterized in that: described Losartan Potassium was the Losartan Potassium granule of 100 mesh sieve gained.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310043872.1A CN103070848B (en) | 2013-02-04 | 2013-02-04 | Losartan potassium gastric floating capsule and preparation method thereof |
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| CN201310043872.1A CN103070848B (en) | 2013-02-04 | 2013-02-04 | Losartan potassium gastric floating capsule and preparation method thereof |
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| CN103070848B CN103070848B (en) | 2014-05-28 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644588A (en) * | 2015-02-13 | 2015-05-27 | 山东鲁抗立科药业有限公司 | Azilsartan intragastric-floating sustained release tablet and preparation method thereof |
| CN105147641A (en) * | 2015-09-21 | 2015-12-16 | 四川维尔康动物药业有限公司 | Abamectin gastric floating capsules and preparation method thereof |
| US20210205253A1 (en) * | 2018-05-31 | 2021-07-08 | The Asan Foundation | Use Of Stearic Acid For Preventing Or Treating Pulmonary Fibrosis |
Citations (2)
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|---|---|---|---|---|
| CN1951443A (en) * | 2006-11-14 | 2007-04-25 | 南京中医药大学 | Gastric floating capsule of 'Zuo Jin Wan' and preparation method thereof |
| CN101288659A (en) * | 2007-04-18 | 2008-10-22 | 王雷波 | Floating type pellets in stomach and preparation method thereof |
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2013
- 2013-02-04 CN CN201310043872.1A patent/CN103070848B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1951443A (en) * | 2006-11-14 | 2007-04-25 | 南京中医药大学 | Gastric floating capsule of 'Zuo Jin Wan' and preparation method thereof |
| CN101288659A (en) * | 2007-04-18 | 2008-10-22 | 王雷波 | Floating type pellets in stomach and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 夏运岳等: "双氯芬酸钠胃漂浮型缓释胶囊的制备", 《中国医院药学杂志》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644588A (en) * | 2015-02-13 | 2015-05-27 | 山东鲁抗立科药业有限公司 | Azilsartan intragastric-floating sustained release tablet and preparation method thereof |
| CN105147641A (en) * | 2015-09-21 | 2015-12-16 | 四川维尔康动物药业有限公司 | Abamectin gastric floating capsules and preparation method thereof |
| CN105147641B (en) * | 2015-09-21 | 2018-02-13 | 四川维尔康动物药业有限公司 | A kind of AVM gastric floating capsule and preparation method thereof |
| US20210205253A1 (en) * | 2018-05-31 | 2021-07-08 | The Asan Foundation | Use Of Stearic Acid For Preventing Or Treating Pulmonary Fibrosis |
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| Publication number | Publication date |
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| CN103070848B (en) | 2014-05-28 |
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