CN105030726A - Method for preparing isradipine capsule - Google Patents
Method for preparing isradipine capsule Download PDFInfo
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- CN105030726A CN105030726A CN201510539483.7A CN201510539483A CN105030726A CN 105030726 A CN105030726 A CN 105030726A CN 201510539483 A CN201510539483 A CN 201510539483A CN 105030726 A CN105030726 A CN 105030726A
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- isradipine
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Abstract
The invention discloses a method for preparing an isradipine capsule. The method comprises the following steps: dissolving an isradipine raw material according to the amount of a prescription in prescribed ethanol, and adding povidone K3 to stir and dissolve; putting prescribed pregelatinized starch and microcrystalline cellulose in a fluidized bed, starting a fan, regulating the air volume to excellent fluidizing, setting the air inlet temperature to be 35-40 DEG C, spraying the solution prepared in the step A when the material temperature rises to 25 DEG C to granulate; and finishing the prepared particles through a 30-mesh screen, adding magnesium stearate, uniformly mixing, and filling capsules with the particles. According to the method, the raw materials and the auxiliaries are used for preparing solid dispersion by adopting a spray drying mode, are prepared to form fine particles by one step, and are used for filling capsules, so that the dissolution in vitro of the capsule can be effectively increased, the production cost can be reduced, the bioavailability of the capsule can be improved, and a better clinical curative effect can be achieved.
Description
Technical field
The invention belongs to technical field of pharmaceutical chemistry, relate to a kind of preparation method of isradipine capsule.
Background technology
Isradipine is dihydropyridine calcium channel blocker, by retardance cross-film flow of calcium ions, and the contraction that causes of Selective depression depolarization effectively, and play a role on cardiac muscle and vascular smooth muscle.This product has stronger vasorelaxation action, and acardia inhibitory action, cause reflex tachycardia hardly.Clinical and zoopery proves; this medical instrument has obvious hypotensive effect and study of anti-atherogenic effect; by maintaining or recovering the SE blood flow of left ventricle; prevent ischemic injuries; improve the quantity of motion of angina pectoris and congestive heart failure patients; treating hypertensive while, there is protective effect to heart.Isradipine can increase the excretion of sodium ion and water, has diuresis, and energy nephrectasia efferent artery, reduces capillary of kidney pressure, have protective effect to kidney.
Isradipine is a kind of effective calcium channel blocker, there is the effect of blood vessel dilating, minimizing peripheral vascular resistance, increase arteria coronaria and brain vessel blood significantly, very little to Cardiac depression effect especially, prolonged application well-tolerated, one of critical treatment medicine becoming the diseases such as hypertension.
Raw material isradipine is not soluble drug in water, existing capsule preparation method thereof be by after isradipine raw material micronization processes again with adjuvant mixing granulation, filled capsules after dry.Capsule dissolubility prepared by existing preparation method is low, and the production cycle is long, and cost is higher.
Summary of the invention
The object of the invention is to for the deficiencies in the prior art, a kind of preparation method of isradipine capsule is provided.
For achieving the above object, the technical solution adopted for the present invention to solve the technical problems is:
A preparation method for isradipine capsule, comprises the steps:
A, get recipe quantity isradipine raw material and be dissolved in recipe quantity ethanol, then add PVP K30 stirring and dissolving;
B, get recipe quantity pregelatinized Starch and microcrystalline Cellulose is put in fluid bed, start blower fan, regulating air volume is good to fluidisation, and arranging inlet temperature is 35 ~ 40 DEG C, when temperature of charge rises to 25 DEG C, sprays into solution prepared by steps A and granulates;
C, obtained granule is crossed 30 mesh sieve granulate, add magnesium stearate, mix homogeneously, particles filled capsule after mixing.
As preferably, described isradipine capsule comprises the component of following parts by weight:
Isradipine 2.5-5.0 part
Pregelatinized Starch 35-65 part
Microcrystalline Cellulose 15-25 part
PVP K30 8-12 part
Magnesium stearate 0.5-1.5 part
Ethanol 60-70 part
Make: 1000 capsules.
As optimal way, in described step B, in pelletization, control atomizing pressure 0.2 ~ 0.5mpa and peristaltic pump rotating speed 10 ~ 15r/min.
As optimal way, in described step B, continue after having granulated to be dried to moisture≤2%.
The present invention adopts spray-dired mode to be prepared into solid dispersion by raw materials used together with adjuvant, a step makes fine grained simultaneously, and then filled capsules, effectively can increase the dissolution in vitro of this product and reduce production cost, improve the bioavailability of this medicine simultaneously, reach better clinical efficacy.
Detailed description of the invention
All features disclosed in this description, or the step in disclosed all methods or process, except mutually exclusive feature and/or step, all can combine by any way.
Comparative example 1: isradipine raw material different-grain diameter is on the impact of stripping
Get isradipine raw material, adopt different processing modes (to cross 100 mesh sieves; Pulverized 200 mesh sieves, super micron mill micropowder) prepare different particle diameters, add pregelatinized Starch and mix homogeneously with microcrystalline Cellulose, add 3% povidone solution and granulate, difference filled capsules after dry granulate, with intelligent dissolution determination dissolution.Result is as follows:
Table 1 isradipine different-grain diameter stripping curve measurement result
| Processing mode | Particle diameter (μm) | 15min | 30min | 45min | 60min |
| Cross 100 orders | D50＝90.5，D90＝157.3 | 32.8 | 47.3 | 53.4 | 58.7 |
| Pulverized 200 orders | D50＝38.7，D90＝70.5 | 37.9 | 48.8 | 55.2 | 60.8 |
| Micronizing | D50＝14.5，D90＝30.7 | 45.2 | 52.4 | 60.3 | 65.7 |
Comparative example 2: the different prescription of isradipine capsule is on the impact of dissolution
Get isradipine raw material, after adopting super micron mill to pulverize (raw material particle size D50=14.5, D90=30.7), with different prescriptions, granulate.Prescription is as follows:
| Supplementary material title | Prescription one | Prescription two | Prescription three |
| Isradipine | 5.0 g | 5.0g | 5.0g |
| Pregelatinized Starch | 50g | 50g | 50g |
| Microcrystalline Cellulose | 20 g | 20 g | 20 g |
| Carboxymethylstach sodium | 5 g | 10g | 10g |
| Sodium lauryl sulphate | —— | 5 g |
Get after above-mentioned different prescription takes supplementary material mix homogeneously, add 3% povidone solution and granulate, filled capsules respectively after dry granulate after dry granulate, with intelligent dissolution determination dissolution.Result is as follows:
Table 2 isradipine different prescription stripping curve measurement result
| Prescription | 15min | 30min | 45min | 60min |
| One | 46.7 | 54.3 | 60.3 | 64.7 |
| Two | 45.8 | 56.2 | 61.8 | 66.4 |
| Three | 50.8 | 60.3 | 65.7 | 70.5 |
These results suggest that employing prior art, change isradipine raw material particle size and prescription, the result of extraction of this product is not improved.
Embodiment 1: a kind of isradipine capsule, prescription is as follows:
Isradipine 5.0g
Pregelatinized Starch 50.0g
Microcrystalline Cellulose 20.0g
PVP K30 10.0g
Magnesium stearate 1.0g
Ethanol 65g
Make: 1000 capsules;
Preparation method is as follows:
A, get recipe quantity isradipine raw material and be dissolved in recipe quantity ethanol, then add PVP K30 stirring and dissolving;
B, get recipe quantity pregelatinized Starch and microcrystalline Cellulose is put in fluid bed, start blower fan, regulating air volume is good to fluidisation, and arranging inlet temperature is 35 ~ 40 DEG C, when temperature of charge rises to 25 DEG C, sprays into solution prepared by steps A and granulates;
C, obtained granule is crossed 30 mesh sieve granulate, add magnesium stearate, mix homogeneously, particles filled capsule after mixing.
Embodiment 2: a kind of isradipine capsule, prescription is as follows:
Isradipine 2.5g
Pregelatinized Starch 50.0g
Microcrystalline Cellulose 20.0g
PVP K30 5.0g
Magnesium stearate 1.0g
Ethanol 32.5g
Make: 1000 capsules;
Preparation method is as follows:
A, get recipe quantity isradipine raw material and be dissolved in recipe quantity ethanol, then add PVP K30 stirring and dissolving;
B, get recipe quantity pregelatinized Starch and microcrystalline Cellulose is put in fluid bed, start blower fan, regulating air volume is good to fluidisation, arranging inlet temperature is 35 ~ 40 DEG C, when temperature of charge rises to 25 DEG C, spray into solution granulation prepared by steps A, control atomizing pressure and peristaltic pump rotating speed, continue after having granulated to be dried to moisture≤2%;
C, obtained granule is crossed 30 mesh sieve granulate, add magnesium stearate, mix homogeneously, particles filled capsule after mixing.
Embodiment 1, embodiment 2 isradipine capsule stripping curve measurement result are as follows:
Table 3 isradipine stripping curve measurement result
| Embodiment | 15min | 30min | 45min | 60min |
| 1 | 75.8 | 95.4 | 96.7 | 98.8 |
| 2 | 76.2 | 93.5 | 98.6 | 100.4 |
The isradipine capsule accelerated stability that table 4 is prepared by the application's method investigates result
Can obviously be found out by the experimental data of above-described embodiment, the isradipine capsule prepared of prior art is about 60% at the dissolution of 60 minutes, isradipine capsule prepared by the application's method is about 99% at 60 minutes dissolutions, dissolution is significantly better than prior art, and in acceleration stability study in June, steady quality, this technology on the quality of product without impact.Achieve unforeseeable technique effect.
The present invention is not limited to aforesaid detailed description of the invention.The present invention expands to any new feature of disclosing in this manual or any combination newly, and the step of the arbitrary new method disclosed or process or any combination newly.
Claims (4)
1. a preparation method for isradipine capsule, is characterized in that, comprises the steps:
A, get recipe quantity isradipine raw material and be dissolved in recipe quantity ethanol, then add PVP K30 stirring and dissolving;
B, get recipe quantity pregelatinized Starch and microcrystalline Cellulose is put in fluid bed, start blower fan, regulating air volume is good to fluidisation, and arranging inlet temperature is 35 ~ 40 DEG C, when temperature of charge rises to 25 DEG C, sprays into solution prepared by steps A and granulates;
C, obtained granule is crossed 30 mesh sieve granulate, add magnesium stearate, mix homogeneously, particles filled capsule after mixing.
2. the preparation method of a kind of isradipine capsule as claimed in claim 1, is characterized in that: described isradipine capsule comprises the component of following parts by weight:
Isradipine 2.5-5.0 part;
Pregelatinized Starch 35-65 part;
Microcrystalline Cellulose 15-25 part;
PVP K30 8-12 part;
Magnesium stearate 0.5-1.5 part;
Ethanol 60-70 part;
Make: 1000 capsules.
3. the preparation method of a kind of isradipine capsule as claimed in claim 1 or 2, is characterized in that: in described step B, in pelletization, controls atomizing pressure 0.2 ~ 0.5mpa and peristaltic pump rotating speed 10 ~ 15r/min.
4. the preparation method of a kind of isradipine capsule as claimed in claim 1 or 2, is characterized in that: in described step B, continues to be dried to moisture≤2% after having granulated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510539483.7A CN105030726A (en) | 2015-08-30 | 2015-08-30 | Method for preparing isradipine capsule |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510539483.7A CN105030726A (en) | 2015-08-30 | 2015-08-30 | Method for preparing isradipine capsule |
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| CN105030726A true CN105030726A (en) | 2015-11-11 |
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| CN201510539483.7A Pending CN105030726A (en) | 2015-08-30 | 2015-08-30 | Method for preparing isradipine capsule |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4816263A (en) * | 1987-10-02 | 1989-03-28 | Alza Corporation | Dosage form for treating cardiovascular diseases comprising isradipine |
| CN104739770A (en) * | 2013-12-27 | 2015-07-01 | 上海睿智化学研究有限公司 | Nimodipine solid dispersant and tablet and their preparation methods |
| CN104784181A (en) * | 2015-03-26 | 2015-07-22 | 合肥华方医药科技有限公司 | Preparation method of pharmaceutical composition capable of increasing dissolution rate of indissolvable drug isradipine |
-
2015
- 2015-08-30 CN CN201510539483.7A patent/CN105030726A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4816263A (en) * | 1987-10-02 | 1989-03-28 | Alza Corporation | Dosage form for treating cardiovascular diseases comprising isradipine |
| CN104739770A (en) * | 2013-12-27 | 2015-07-01 | 上海睿智化学研究有限公司 | Nimodipine solid dispersant and tablet and their preparation methods |
| CN104784181A (en) * | 2015-03-26 | 2015-07-22 | 合肥华方医药科技有限公司 | Preparation method of pharmaceutical composition capable of increasing dissolution rate of indissolvable drug isradipine |
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Application publication date: 20151111 |