CN105596316A - Azilsartan sustained-release pellets and preparation method thereof - Google Patents
Azilsartan sustained-release pellets and preparation method thereof Download PDFInfo
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- CN105596316A CN105596316A CN201410671323.3A CN201410671323A CN105596316A CN 105596316 A CN105596316 A CN 105596316A CN 201410671323 A CN201410671323 A CN 201410671323A CN 105596316 A CN105596316 A CN 105596316A
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Abstract
The invention discloses azilsartan sustained-release pellets. The azilsartan sustained-release pellets comprise a coating layer, drug-containing pellets; the coating layer is used for coating the drug-containing pellets, the drug-containing pellets comprise 40mg of azilsartan, 80mg of blank-pellets, 160-215mg of a filler, 10-50mg of a lubricant, and 5-25mg of an adhesive. The coating layer comprises 35-175mg of Eudragit NE 30D and 5-53mg of powdered steatile. A preparation method comprises the following steps: 1) material preparation; 2) mixing; 3) preparation of the adhesive; 4) pelleting; 5) preparation of a coating agent; 6) coating; 7) loading; and 8) moulding by aluminum and product obtaining. The azilsartan sustained-release pellets have the advantages of stable drug effect, high biological availability, and side-effect, and effectively treat hypertension. Two advanced technologies of a sustained release preparation and a pellets preparation are employed, the azilsartan sustained-release pellets have the advantages of stable treatment effect, high biological availability, good drug stability, convenient package, transport and storage, the preparation method is simple and easy to operate, and is suitable for industrial production.
Description
Technical field
The invention belongs to chemical drug sustained release preparation field, be specifically related to husky smooth sustained release pellet of a kind of Archie and preparation method thereof.
Background technology
Hypertension refers to that under quiescent condition SAP and/or diastolic pressure increase. Hypertension is a kind of taking angiosthenia rising as feature, can be functional with heart, blood vessel, brain and kidney and other organs or the systemic disease of organic change, it have essential hypertension and secondary hypertension point. The reason of hypertension incidence is a lot, can be divided into two aspects of h and E.
Normocyte, colloid particle etc. are electronegative, between them, mutually repel, and maintain a certain distance, and the aging red blood cell of pathology are because electronics is fought for, positively charged, due to positive negative inhale, that red blood cell condensation is agglomerating. Anion can effectively be repaired aging cell membrane potential, impels it to become normal electronegative cell, thus negative scold and effectively reduce blood viscosity, erythrocyte sedimentation rate is slowed down. Anion can be strengthened the own negative polarity trend of colloid particle in blood simultaneously, and the colloidal stability of plasma protein is increased, and keeps the normal health state of blood. Therefore, if the anion concentration deficiency in blood will cause the erythrocytic cell membrane potential that pathology is aging not to be repaired, thereby cause hypertensive generation.
The blood pressure standard using according to the World Health Organization (Who) suggestion is: all normal adult systolic pressures should be less than or equal to 140mmHg (18.6kPa), and diastolic pressure is less than or equal to 90mmHg (12kPa). That is systolic pressure is between 141-159mmHg (18.9-21.2kPa), diastolic pressure, between 91-94mmHg (12.1-12.5kPa), is BH. When office hypertension, repeatedly Measure blood pressure, the mean value that has double diastolic pressure at least is at 90mmHg (12.0kPa) or just can be diagnosed as above hypertension. Only a blood pressure rising person still can not make a definite diagnosis, but needs follow-up observation. Hypertension is modal cardiovascular disease, is the great public health problem in global range. The Chinese residents nutrition of 2004 and the demonstration of Health Situation investigation result, China 18 years old and above prevalence of hypertension rate are 18.8%, estimate that national number of patients exceedes 1.6 hundred million. Compared with 1991, illness rate rises 31%, and number of patients increases by approximately more than 7,000 ten thousand people.
1998, China's cerebrovascular disease occupied the second of city dweller's cause of death, ranks first in rural area. The annual death in the whole nation exceedes 1,000,000, and the patient of survival approximately 5,000,000～6,000,000, wherein more than 75% leave deformity in various degree, has caused white elephant to individual, family and society. And Major Risk Factors in brain death is hypertension. Meanwhile, blood pressure raises or the fuse cord of various diseases, can make the onset risk of the diseases such as coronary heart disease, heart failure and kidney disease increase. Because part hyperpietic there is no obvious clinical symptoms, hypertension be otherwise known as " the invisible killer " of human health.
By onset emergency and course advancement, can be divided into and delaying into type and radical type, common to delay into type.
One, benign hypertension.
(1) Early manifestation: in early days how asymptomatic, find that blood pressure increases when health check-up once in a while, or in stress, excited or tired rear sense dizziness, headache, dim eyesight, tinnitus, insomnia, the symptom such as weak, absent minded, may be due to senior moral function imbalance. Early stage blood pressure only temporarily raises, and continues to raise with course advancement blood pressure, and internal organs are got involved.
(2) brain performance: headache, dizzy common. How due to excited, overtired, climate change or inactive depressor and bring out. The hurried rising of blood pressure. Severe headache, vision disorder, feel sick, vomiting, twitch, stupor, crosses property hemiplegia, aphasia etc.
(3) Cardiac Manifestation: early stage, cardiac functional compensation, symptom is not obvious, and in the later stage, heart function loses compensatory, occurs in heart failure.
(4) kidney performance: long-term hypertension causes renal arteriolosclerosis. When renal hypofunction, enuresis nocturna be can cause, in diuresis, urine, albumen, cast and red blood cell contained. Urine concentrating power is low, and phenol red excretion and urea are cleaned up obstacle. There is azotemia and uremia.
(5) artery changes.
(6) eyeground changes.
Two, accelerated hypertension: also claim accelerated hypertension, account for 1% of high blood pressure, can be by delaying into type sudden transition, also can onset. Accelerated hypertension can occur in any age, but with 30-40 year for the most common. Blood pressure obviously raises, and diastolic pressure is many more than 17.3Kpa (130mmHg), has the symptoms such as weak, thirsty, diuresis. Eyesight goes down rapidly, and there is retinal hemorrhage on eyeground and oozes out, and often has bilateral papilledema. There is rapidly albuminuria, blood urine and renal insufficiency. Also can there is heart failure, hypertensive encephalopathy and hypertensive crisis, course advancement is died from rapidly uremia more.
Treating in the market hypertensive medicine has a lot, but the effect of most drug is not fine, cannot thoroughly reduce, stabilizing blood pressure, along with people's fatigue or emotional change or other reasons, often cause blood pressure to raise, and the side effect of depressor is more in the market, as diseases such as headache, flushing, tachycardia, edema, mental depressions.
Summary of the invention
The object of this invention is to provide husky smooth sustained release pellet of Archie of a kind of efficacy stability, bioavilability is high, side effect is low effective step-down and preparation method thereof.
Object of the present invention is achieved through the following technical solutions: the husky smooth sustained release pellet of a kind of Archie, comprise pastille micropill, coatings, described coatings is wrapped up pastille micropill, described pastille micropill comprises: 40mg Archie sand is smooth, 80mg blank pill core, 160-215mg filler, 10-50mg lubricant, 5-25mg adhesive, and described coatings comprises: 35-175mg is strange NE30D, 5-53mg talcum powder especially.
The best in quality proportioning of described pastille micropill Raw is: 40mg Archie sand is smooth, 80mg blank pill core, 200mg filler, 20mg lubricant, 10mg adhesive.
The best in quality proportioning of described coatings Raw is: 32mg is strange NE30D, 7mg talcum powder especially.
Described filler is microcrystalline cellulose.
Described lubricant is talcum powder.
Described adhesive is Hydroxypropyl methylcellulose.
In described coatings, also comprise lauryl sodium sulfate or polyethylene glycol trace.
The preparation method of the described husky smooth sustained release pellet of a kind of Archie, comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, husky Archie smooth use pulverizer is pulverized, crossed 100 mesh sieves;
Step 2: mix: take according to above-mentioned quality proportioning that Archie sand is smooth, microcrystalline cellulose is put into three-dimensional mixer and mixed 30 minutes, make fine drug powder, take out for subsequent use;
Step 3: the preparation of adhesive: take appropriate Hydroxypropyl methylcellulose by above-mentioned quality proportioning, adding appropriate hot water, to be mixed with concentration be 2% adhesive, for subsequent use;
Step 4: pill: the charging spout of mixed fine drug powder being put into centrifugal pellet processing machine, adhesive is put into feed tank, and blank pill core is put in pot, opens machine, adjust parameter, start hydrojet, in the time that ball core has damp, start for powder, after fine drug powder has all spread, in charging spout, add talcum powder, continue for powder, after talcum powder has all spread, discharging; Then use vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses 14,24 mesh sieves to sieve after drying, and the pastille micropill of getting 14-24 order size is for subsequent use;
Step 5: the preparation of coating agent: take especially strange NE30D, talcum powder, lauryl sodium sulfate, purified water by above-mentioned quality proportioning, first lauryl sodium sulfate is joined and in purified water, stir evenly dissolving, after adding again especially strange NE30D to stir evenly, limit is stirred and is just added talcum powder, stirs for subsequent use after 10 minutes;
Step 6: dressing: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating agent is put into feed tank, stir constantly, open machine, adjust parameter, start dressing, after coating agent is finished, starting to heat up keeps temperature of charge more than 40 degree, dries cooling 30 minutes, discharging, closing machine;
Step 7: filling: the pastille micropill after above-mentioned dressing is used to capsule filling machine, pastille micropill is packed in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
Beneficial effect of the present invention: a kind of efficacy stability of the present invention, the husky smooth sustained release pellet of the Archie that bioavilability is high, side effect is low, adopt two kinds of advanced technology of novel sustained release preparation and pellet preparations, slowly-releasing refers to by delaying the rate of releasing drug of medicine from this formulation, reduce medicine and enter the absorption rate of body, thereby play more stable result for the treatment of; Micropill has medicine and increases at intestines and stomach surface distributed area, can reduce excitant, improves bioavilability, not affected by gastric emptying factor simultaneously, uniform absorption in medicine body, and individual difference is little; Two kinds of advanced technology are applied the technical advantage that has more strengthened this medicine simultaneously, compared with oral liquid, have medicine stability good, packaging, and transport, preserves the advantages such as convenient, and its preparation method is simple, is applicable to industrial production.
The present invention is through two groups of clinical verifications, wherein one group is that treatment group is taken the present invention, within 7 days, is a course for the treatment of, and another group control group is taken Zhenju Jiangya Tablet, every group selection outpatient 110 examples, wherein male 25 examples, female's 70 examples, maximum 75 years old age, minimal ages 35 years old, within 7 days, be a course for the treatment of, clinical manifestation is dizziness, dim eyesight, tinnitus, severe headache, insomnia, weak, stupor, and table one is for taking a contrasting data after the course for the treatment of:
Table 1 is taken two groups of comparisons course for the treatment of in front and back (unit: people)
There were significant differences for treatment group and control group, thereby can find out that the present invention's application clinically has significant curative effect.
Detailed description of the invention
Embodiment 1
The husky smooth sustained release pellet of a kind of Archie, comprise pastille micropill, coatings, described coatings is wrapped up pastille micropill, described pastille micropill comprises: 40mg Archie sand is smooth, 80mg blank pill core, 160-215mg filler, 10-50mg lubricant, 5-25mg adhesive, and described coatings comprises: 35-175mg is strange NE30D, 5-53mg talcum powder especially.
The best in quality proportioning of described pastille micropill Raw is: 40mg Archie sand is smooth, 80mg blank pill core, 200mg filler, 20mg lubricant, 10mg adhesive.
The best in quality proportioning of described coatings Raw is: 32mg is strange NE30D, 7mg talcum powder especially.
Described filler is microcrystalline cellulose.
Described lubricant is talcum powder.
Described adhesive is Hydroxypropyl methylcellulose.
In described coatings, also comprise lauryl sodium sulfate or polyethylene glycol trace.
Embodiment 2
A preparation method for the husky smooth sustained release pellet of Archie, comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, husky Archie smooth use pulverizer is pulverized, crossed 100 mesh sieves;
Step 2: mix: take according to above-mentioned quality proportioning that Archie sand is smooth, microcrystalline cellulose is put into three-dimensional mixer and mixed 30 minutes, make fine drug powder, take out for subsequent use;
Step 3: the preparation of adhesive: take appropriate Hydroxypropyl methylcellulose by above-mentioned quality proportioning, adding appropriate hot water, to be mixed with concentration be 2% adhesive, for subsequent use;
Step 4: pill: the charging spout of mixed fine drug powder being put into centrifugal pellet processing machine, adhesive is put into feed tank, and blank pill core is put in pot, opens machine, adjust parameter, start hydrojet, in the time that ball core has damp, start for powder, after fine drug powder has all spread, in charging spout, add talcum powder, continue for powder, after talcum powder has all spread, discharging; Then use vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses 14,24 mesh sieves to sieve after drying, and the pastille micropill of getting 14-24 order size is for subsequent use;
Step 5: the preparation of coating agent: take especially strange NE30D, talcum powder, lauryl sodium sulfate, purified water by above-mentioned quality proportioning, first lauryl sodium sulfate is joined and in purified water, stir evenly dissolving, after adding again especially strange NE30D to stir evenly, limit is stirred and is just added talcum powder, stirs for subsequent use after 10 minutes;
Step 6: dressing: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating agent is put into feed tank, stir constantly, open machine, adjust parameter, start dressing, after coating agent is finished, starting to heat up keeps temperature of charge more than 40 degree, dries cooling 30 minutes, discharging, closing machine;
Step 7: filling: the pastille micropill after above-mentioned dressing is used to capsule filling machine, pastille micropill is packed in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
Claims (8)
1. the husky smooth sustained release pellet of Archie, comprise pastille micropill, coatings, it is characterized in that: described coatings is wrapped up pastille micropill, described pastille micropill comprises: 40mg Archie sand is smooth, 80mg blank pill core, 160-215mg filler, 10-50mg lubricant, 5-25mg adhesive, and described coatings comprises: 35-175mg is strange NE30D, 5-53mg talcum powder especially.
2. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: the best in quality proportioning of described pastille micropill Raw is: 40mg Archie sand is smooth, 80mg blank pill core, 200mg filler, 20mg lubricant, 10mg adhesive.
3. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: the best in quality proportioning of described coatings Raw is: 32mg is strange NE30D, 7mg talcum powder especially.
4. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: described filler is microcrystalline cellulose.
5. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: described lubricant is talcum powder.
6. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: described adhesive is Hydroxypropyl methylcellulose.
7. the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: in described coatings, also comprise lauryl sodium sulfate or polyethylene glycol trace.
8. the preparation method of the husky smooth sustained release pellet of a kind of Archie according to claim 1, is characterized in that: comprise following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, husky Archie smooth use pulverizer is pulverized, crossed 100 mesh sieves;
Step 2: mix: take according to above-mentioned quality proportioning that Archie sand is smooth, microcrystalline cellulose is put into three-dimensional mixer and mixed 30 minutes, make fine drug powder, take out for subsequent use;
Step 3: the preparation of adhesive: take appropriate Hydroxypropyl methylcellulose by above-mentioned quality proportioning, adding appropriate hot water, to be mixed with concentration be 2% adhesive, for subsequent use;
Step 4: pill: the charging spout of mixed fine drug powder being put into centrifugal pellet processing machine, adhesive is put into feed tank, and blank pill core is put in pot, opens machine, adjust parameter, start hydrojet, in the time that ball core has damp, start for powder, after fine drug powder has all spread, in charging spout, add talcum powder, continue for powder, after talcum powder has all spread, discharging; Then use vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses 14,24 mesh sieves to sieve after drying, and the pastille micropill of getting 14-24 order size is for subsequent use;
Step 5: the preparation of coating agent: take especially strange NE30D, talcum powder, lauryl sodium sulfate, purified water by above-mentioned quality proportioning, first lauryl sodium sulfate is joined and in purified water, stir evenly dissolving, after adding again especially strange NE30D to stir evenly, limit is stirred and is just added talcum powder, stirs for subsequent use after 10 minutes;
Step 6: dressing: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating agent is put into feed tank, stir constantly, open machine, adjust parameter, start dressing, after coating agent is finished, starting to heat up keeps temperature of charge more than 40 degree, dries cooling 30 minutes, discharging, closing machine;
Step 7: filling: the pastille micropill after above-mentioned dressing is used to capsule filling machine, pastille micropill is packed in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
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| CN201410671323.3A CN105596316A (en) | 2014-11-21 | 2014-11-21 | Azilsartan sustained-release pellets and preparation method thereof |
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| CN201410671323.3A CN105596316A (en) | 2014-11-21 | 2014-11-21 | Azilsartan sustained-release pellets and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108434113A (en) * | 2018-04-11 | 2018-08-24 | 安徽中医药大学 | Azilsartan osmotic pump type controlled release tablets and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108434113A (en) * | 2018-04-11 | 2018-08-24 | 安徽中医药大学 | Azilsartan osmotic pump type controlled release tablets and preparation method thereof |
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Application publication date: 20160525 |