CN107519137A - A kind of captopril microplate and preparation method thereof - Google Patents
A kind of captopril microplate and preparation method thereof Download PDFInfo
- Publication number
- CN107519137A CN107519137A CN201610443201.8A CN201610443201A CN107519137A CN 107519137 A CN107519137 A CN 107519137A CN 201610443201 A CN201610443201 A CN 201610443201A CN 107519137 A CN107519137 A CN 107519137A
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- Prior art keywords
- microplate
- captopril
- preparation
- granulation
- stearic acid
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of captopril microplate preparation for treating hypertension class disease, a kind of and method for preparing captopril microplate, pass through the preparation methods such as top spray fluidized bed granulation, the good captopril microplate of compressibility has been prepared, the captopril microplate of the present invention can be with low dose of multiple dosing, especially for the big crowd of individual Difference of Metabolism, such as the elderly and child, it can count and take, accomplish precisely to be administered, and the crowd being had any problem for taking conventional formulation, the compliance of medication can be improved.
Description
Technical field
The invention belongs to technical field of medicine, and in particular to a kind of captopril microplate, and one kind is provided and is used for
The method for preparing captopril microplate.
Background technology
Hypertension (hypertension) refers to increase to be main with systemic arterial blood pressure (systolic pressure and/or diastolic pressure)
Feature (millimetres of mercury of systolic pressure >=140, the millimetres of mercury of diastolic pressure >=90), can be with the function or device matter of the organs such as the heart, brain, kidney
Property infringement clinical syndrome.Hypertension is most common chronic disease, and the most important hazards of cardiovascular and cerebrovascular diseases.Normally
The blood pressure of people fluctuates within the specific limits with internal and external environment change.In overall crowd, blood pressure level gradually rises with the age, to receive
Contractive pressure becomes apparent, but downward trend is presented in diastolic pressure after 50 years old, and pulse pressure also increases therewith.Pressure value and hazard factor assessment are
Diagnosis and the Main Basiss for formulating hypertension therapeutic scheme, the target of different patient's hypertension management is different, and doctor faces patient
When on the basis of normative reference, the most suitable blood pressure range of the patient is judged according to its concrete condition, using targetedly controlling
Treatment measure.
A series of medicine is developed for hypertension both at home and abroad at present, (lyso-propanic acid, first dredge third to captopril
Dried meat acid, Captopril), it is the orally active angiotensin converting enzyme inhibitors of the first generation (ACEI), since 1997 come out,
The effect of its anti-hypertension and treatment congested rhythm of the heart failure, has been recognized.Captopril has to polytype hypertension
Obvious antihypertensive effect, and the cardiac function of congested rhythm of the heart failure patient can be improved.Clinical practice in all kinds hypertension,
Especially severe hypertension invalid to routine treatment is effective.Also it can be used for intractable chronic heart failure.
Microplate refers to that the micro tablet between 1~3mm, microplate belong to through the diameter that special tablet press machine stamping compacting forms
Dosage dispersiveness preparation, it is dispersed in intestines and stomach after the oral microplate of patient, reduce the excitant to intestines and stomach, the intestines of medicine
Stomach transports and absorbed that to be influenceed smaller thus individual difference by gastric emptying rate small；The drug release behavior of microplate is one agent of composition
The summation of multiple junior unit drug release behaviors of amount, the defects of indivedual junior unit preparation technologies will not be to overall preparation after oral
Drug release behavior produces serious influence.For the big crowd of drug metabolism individual difference, such as the elderly and child, or for
For the medicine that dosage need to adjust at any time, microplate is a kind of more satisfactory form of administration, and patient can be according to personalized medicine side
Case, counting is carried out to microplate and taken, metering is more accurate.Compared with other multiple-unit formulations, microplate shape is more regular, size
It is more uniform.Because microplate is formed through fixed mould compacting, thus possesses the feature of conventional tablet, its piece weight and size are all
Controllable precise, the favorable reproducibility of production, each the equal sized of microplate unit, weight is identical, medicament contg is identical.
The captopril preparation clinically used both at home and abroad at present only has two kinds of general formulations of tablet and dripping pill, and all
The dosage specification for adult, must low dose of administration occasion, such as when be administered for children, or dosage needs with
When the occasion that adjusts, such as when being administered for old man, existing captopril formulation can not meet personalized medicine requirement, accomplish essence
Quasi- administration.In addition, when existing pharmaceutical dosage form is taken, because formulation volume is excessive, for special population especially children, clothes
The compliance of medicine is poor.
The content of the invention
To overcome prior art defect, the present invention provides a kind of captopril microplate preparation.Pass through special granulation formula
And preparation technology, captopril microplate of the invention can be with low dose of multiple dosings, especially for individual Difference of Metabolism
It big crowd, such as the elderly and child, can accurately take, while accomplishing precisely to be administered, medication inaccuracy band can be reduced
The various side effects come, and the crowd being had any problem for taking conventional formulation, the compliance of medication can be improved.
For achieving the above object, the invention provides a kind of captopril microplate preparation, its prescription raw material and its use
It is as follows to measure ratio：
Captopril microplate preparation of the present invention, wherein raw material and its amount ratio are preferably as follows in the microplate：
The one kind or more of wherein described diluent in starch, pregelatinized starch, dextrin, microcrystalline cellulose, lactose
Kind.Described adhesive is selected from：One in HPMC, PVP, gelatin, poloxamer, microcrystalline cellulose, polyvinylpyrrolidone
Kind is a variety of.The lubricant is selected from：Magnesium stearate, talcum powder, cornstarch, stearic acid, calcium stearate, talcum, behenic acid
One or more in calcium.
The auxiliary material that microplate preparation of the present invention includes is not limited to the species enumerated in the content of the invention and embodiment, also
Other medicines auxiliary material can be included, on condition that not influenceing the compressing of microplate.Such as surfactant can also be included, it is described
Surfactant is chosen as：D-sorbite, mannitol, lauryl sodium sulfate, AEO, alkyl phenol polyoxy
Vinethene etc..
The spatial form of microplate can select as needed in principle.Microplate in the present invention is preferably in cylinder, ellipse
Shape or spherical spatial form.Preferably height and diameter can be 1~4mm cylinder, highly can basis with diameter
Any selection is needed, such as height and diameter can be respectively 1.5mm, 2mm, 2.5mm, 3mm, 3.5mm, 4mm.
In the microplate preparation of the present invention, the surface of microplate can also carry out coating cladding with known method.Such as can be with
Make active material captopril that release is controlled and (generally delayed) in aqueous medium by coating at least one layer of coating.Suitable can
Control release coating contains wax or polymer not soluble in water, preferred, ethyl.
The coating that the microplate preparation of the present invention can also contain can for example dissolve in a manner of a kind of pH is relied on, it is ensured that micro-
Tablet preparation does not dissolve by stomach, is just discharged until reaching enteron aisle.
Described captopril microplate preparation can also be loaded capsule by the present invention, be prepared as the oral formulations of capsule form,
The micro-tablet of controllable release medicine containing certain amount in capsule, the number of micro-tablet is according to single release time and will
The medication amount for completing release determines.The number of micro-tablet is preferably enough to dosage by daily single or twice in capsule.
It is with the advantages of this dosage form：The dosage of active component segments between many directly countable micro-tablets, but due to agent
Measure in capsule it has been determined that therefore patient need not cumbersome counting again.
Microplate preparation of the present invention can be used alone, and can also be filled with such as medicine distribution of special doser
Put and be used cooperatively together, to provide more convenient accurately administration.
It is a further object to provide a kind of preparation method of captopril microplate, the microplate can use fluidisation
The granulation of bed top spray, wet granulation, dry granulation or fluid bed bottom spray method of granulating are prepared.
Such as when using top spray granulating process, preparation method is as follows：Captopril, adhesive are added to purified water
In, stirring to formation clear transparent solutions is as granulation binders solution for standby；By diluent after premix, fluid bed is put into
In top spray pot；Fluid bed air blast is opened, adjusts atomizing pressure and air quantity EAT, while sprays into binder solution progress
Top spray is pelletized；After agent solution to be bonded sprays into, particle is taken out, carries out dry whole grain；By the dry particl and recipe quantity of gained
Lubricant uniformly mixing after, mixed material is transferred on high speed rotary tablet press and carries out tabletting, gets product tablet.
Or during using wet granulation technology, preparation method is：Captopril, diluent and adhesive are put in wet method system
In grain machine pot, after mixing, spray into purified water and carry out wet granulation, wet whole grain, be subsequently dried, particle is through overdrying after drying
Whole grain；After dry particl is uniformly mixed with recipe quantity lubricant, mixed material is transferred on high speed rotary tablet press and pressed
Piece, both obtain finished tablet.
Embodiment
Embodiment 1：
| Title | Dosage |
| Captopril | 0.6mg |
| Microcrystalline cellulose 102 | 2.4mg |
| Lactose Flowlac100 | 5.2mg |
| HPMC E3 | 0.4mg |
| Stearic acid | 0.08mg |
Preparation technology is as follows：Captopril, HPMC E3 are added in purified water, stirring to formation clear transparent solutions
As granulation binders solution for standby；By microcrystalline cellulose 102, lactose Flowlac100 is put into fluid bed top after premix
Spray in pot；Fluid bed air blast is opened, adjusts atomizing pressure and air quantity EAT, while spray into binder solution and pushed up
Spray grain；After agent solution to be bonded sprays into, particle is taken out, carries out dry whole grain；By the dry particl of gained and recipe quantity
Stearic acid uniformly after mixing, mixed material is transferred on high speed rotary tablet press and carries out tabletting, and it is micro- both to have obtained finished product captopril
Tablet.
Embodiment 2：
Preparation technology is as follows：Captopril, lactose Flowlac100 and HPMC E3 are put in wet granulator pot
It is interior, open blade and mixed at the beginning of 10min, after mixing, unlatching blade sprays into purified water and carries out wet granulation simultaneously；Purified water
Continue to be granulated 5min after penetrating；Then obtained wet granular is subjected to wet whole grain, is subsequently placed into fluid bed and is dried,
Particle is through overdrying whole grain after drying；After dry particl is uniformly mixed with recipe quantity stearic acid, mixed material is transferred to and revolved at a high speed
Turn to carry out tabletting on tablet press machine, both obtain finished product captopril micro-tablet.
Embodiment 3：
Preparation technology：After captopril, microcrystalline cellulose 102 and HPMC E3 are well mixed, mixed material is added
In dry granulating machine, suitable dry method pelleting is obtained；After particle uniformly mixes with stearic acid, mixed material is transferred at a high speed
Tabletting is carried out on rotary pelleting machine, both obtains finished tablet.
Embodiment 4
| Title | Dosage |
| Captopril | 0.7mg |
| Microcrystalline cellulose 102 | 3.0mg |
| Pregelatinized starch | 4.8mg |
| PVP K30 | 0.4mg |
| Stearic acid | 0.05mg |
Preparation technology：Captopril, PVP K30 are added in purified water, stirring is made to clear transparent solutions are formed
For granulation binders solution for standby；By microcrystalline cellulose 102, pregelatinized starch is put into fluid bed top spray pot after premix
It is interior；Fluid bed air blast is opened, adjusts atomizing pressure and air quantity EAT, while sprays into binder solution and carries out top spray system
Grain；After agent solution to be bonded sprays into, particle is taken out, carries out dry whole grain；By the dry particl of gained and the tristearin of recipe quantity
After sour uniformly mixing, mixed material is transferred on high speed rotary tablet press and carries out tabletting, both obtains finished product microplate preparation.
Claims (9)
1. a kind of captopril microplate, it is characterised in that in the microplate under raw material and its amount ratio：
2. microplate according to claim 1, it is characterised in that in the microplate under raw material and its amount ratio：
3. microplate according to claim 1 or 2, wherein described diluent is selected from starch, pregelatinized starch, dextrin, micro-
One or more in crystalline cellulose, lactose.
4. according to the microplate described in any one of claims 1 to 3, wherein described adhesive is selected from：HPMC, PVP, gelatin,
One or more in poloxamer, microcrystalline cellulose, polyvinylpyrrolidone, preferably HPMC E5.
5. according to the microplate described in any one of Claims 1 to 4, wherein the lubricant is selected from：Magnesium stearate, talcum powder, jade
One or more in rice starch, stearic acid, calcium stearate, talcum, behenic acid calcium, lubricant are preferably stearic acid.
6. according to the microplate described in any one of Claims 1 to 5, wherein the microplate is in cylindrical, oval or spherical sky
Between shape.
7. according to the microplate described in any one of claim 1~6, wherein the microplate is in 1~3mm of height, a diameter of 1~3mm
Cylinder.
8. according to the microplate described in any one of claim 1~7, wherein the microplate can be coated with one or more layers bag again
Clothing.
9. the preparation method of any one of the claim 1~8 captopril microplate, it is characterised in that the microplate is using fluidisation
The granulation of bed top spray, wet granulation, dry granulation, direct powder compression or fluid bed bottom spray method of granulating are prepared.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610443201.8A CN107519137A (en) | 2016-06-20 | 2016-06-20 | A kind of captopril microplate and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610443201.8A CN107519137A (en) | 2016-06-20 | 2016-06-20 | A kind of captopril microplate and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN107519137A true CN107519137A (en) | 2017-12-29 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610443201.8A Pending CN107519137A (en) | 2016-06-20 | 2016-06-20 | A kind of captopril microplate and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4666705A (en) * | 1985-06-03 | 1987-05-19 | E. R. Squibb & Sons, Inc. | Controlled release formulation |
| US5298497A (en) * | 1990-05-15 | 1994-03-29 | E. R. Squibb & Sons, Inc. | Method for preventing onset of hypertension employing a cholesterol lowering drug |
| CN1546018A (en) * | 2003-12-10 | 2004-11-17 | 杭州民生药业集团有限公司 | Controlled release preparation of captopril and its preparation process |
| CN104490754A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Lyophilized tablet prepared from captopril composition and preparation method thereof |
-
2016
- 2016-06-20 CN CN201610443201.8A patent/CN107519137A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4666705A (en) * | 1985-06-03 | 1987-05-19 | E. R. Squibb & Sons, Inc. | Controlled release formulation |
| US5298497A (en) * | 1990-05-15 | 1994-03-29 | E. R. Squibb & Sons, Inc. | Method for preventing onset of hypertension employing a cholesterol lowering drug |
| CN1546018A (en) * | 2003-12-10 | 2004-11-17 | 杭州民生药业集团有限公司 | Controlled release preparation of captopril and its preparation process |
| CN104490754A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Lyophilized tablet prepared from captopril composition and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 梅兴国主编: "《微载体药物递送系统》", 30 November 2009, 华中科技大学出版社 * |
| 沢井製薬株式会社: "カプトプリル錠", 《カプトプリル錠》 * |
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Effective date of registration: 20230327 Address after: 8639, Floor 6, Building 3, No. 3, Yongchang North Road, Daxing District, Beijing, 100176 Applicant after: Beijing Kexin Jurun Pharmaceutical Technology Co.,Ltd. Address before: 100083 room 15, 15 / F, block a, Tiangong building, 30 Xueyuan Road, Haidian District, Beijing Applicant before: COSCI MED-TECH Co.,Ltd. |
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