CN1864692A - A drug action released evenly sustained release capsule of benproperine phosphate - Google Patents
A drug action released evenly sustained release capsule of benproperine phosphate Download PDFInfo
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- CN1864692A CN1864692A CN 200510034600 CN200510034600A CN1864692A CN 1864692 A CN1864692 A CN 1864692A CN 200510034600 CN200510034600 CN 200510034600 CN 200510034600 A CN200510034600 A CN 200510034600A CN 1864692 A CN1864692 A CN 1864692A
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- benproperine phosphate
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- benproperine
- phosphate
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Abstract
The slow released benproperine phosphate preparation with homogeneous release is one kind slow released capsule with slow released micro pill as main component. The slow released micro pill includes benproperine phosphate micro pill as the active component and slow releasing coating outside the benproperine phosphate micro pill. The slow released micro pill consists of benproperine phosphate, supplementary material forming the micro pill together with the benproperine phosphate, and slow releasing material in the weight ratio of 1 to 1.5-4 to 0.5-1.5. The slow released micro pill is prepared through a coating and pill forming process. The slow released benproperine phosphate preparation has prolonged intracorporeal medicine detention time, controlled medicine release, reduced medicine taking times, lowered toxic side effect of the medicine and raised curative effect.
Description
Technical field:
The present invention relates to a kind of medicine that is mainly used in the treatment cough, mainly being meant a kind of is the capsule of main therapeutic component with benproperine phosphate, refers to that specifically a kind of drug effect discharges uniform benproperine phosphate slow releasing capsule.
Background technology:
Cough is human common a kind of respiratory tract diseases because this sick paathogenic factor is very many, thereby people to suffer from the probability of this disease very high, almost nobody can escape by luck.People also are being devoted to the medicine of inhibition cough and the research of method when making great efforts to study the medicine and Therapeutic Method for the treatment of the various diseases that causes cough for this reason.Chemicals as present normally used various Chinese patent medicines of medical profession and various dosage forms.In numerous chemicalses, by research and clinical proof, benproperine phosphate is a kind of comparatively effective powerful antitussive medicine, belongs to non-narcotic and obeys no addicted maincenter cough suppressing medicine for a long time.At present, the benproperine phosphate antitussive medicine that medical profession adopts usually mainly contains tablet, dosage form such as capsule and slow releasing tablet, wherein slow releasing tablet has the length of holding time, advantage such as easy to use, but in actual clinical, find, though the slow releasing tablet antitussive effect of prior art is remarkable, for acute, sudden emergency case, because the drug release rate of its slow releasing tablet is slow, it is slow to play a role, it is slow to prove effective, be unfavorable for removing rapidly slight illness, its range of application is restricted, and slow releasing tablet be big at the gastrointestinal tract local concentration, also big to GI irritation, therefore be difficult to satisfy the demand of medical profession to this medicine.Thereby, on the prior art basis, provide new benproperine phosphate slow-releasing agent type, improve its prescription and preparation method simultaneously, make it overcome the deficiencies in the prior art effectively, seem very important and urgent.
Goal of the invention:
Purpose of the present invention just is to provide a kind of drug effect to discharge uniform benproperine phosphate slow releasing capsule, by adjusting as the benproperine phosphate consumption of active component and to the optimization of its adjuvant, in preparation process, benproperine phosphate is evenly distributed in each micropill in the capsule, thereby this medicine can extensively be evenly distributed in the patient's gastrointestinal tract after taking, and since dosage incline and dispersion, medicine increases at gastrointestinal surface distributed area, drug bioavailability is effectively improved, make the sustained-release micro-pill capsules drug release even and reach, blood drug level is steady, avoid the blood medicine peak value of ordinary preparation, thereby reduced the purpose of the generation of poisonous side effect of medicine to greatest extent.Simultaneously by prior art is improved effectively, make the easier control of free list speed of its pharmaceutical compositions, technology is simpler, and the operation simple and feasible guarantees to reduce production costs the quality of product easily, shortens the cycle of producing, and remarkable in economical benefits improves.
Summary of the invention:
The present invention is in order to solve the existing in prior technology problem, adopt following scheme to solve: a certain amount of benproperine phosphate is evenly distributed on each ball core skin to form the pastille micropill, wrap slow release layer on the micropill surface of phosphoric acid benproperine then, make slow-release micro-pill.
The technical problem to be solved in the present invention is the prescription of the sustained-release pellet preparation of research preparation benproperine phosphate, and the preparation technology who carries out large-scale production.This technology is not only simpler, the operation simple and feasible, and the cycle of production is short, and guarantees the quality of product easily, and production cost is also less simultaneously.
A kind of drug effect of the present invention discharges uniform benproperine phosphate slow-releasing agent, consist predominantly of benproperine phosphate and corresponding auxiliary material, it is characterized in that above-mentioned medicament is a kind of slow releasing capsule based on slow-release micro-pill, its slow-release micro-pill comprises and contains as the pastille micropill of the benproperine phosphate of active component and be coated on the sustained release coating layer that pastille micropill skin has slow releasing function, and above-mentioned adjuvant comprises and mixes the auxiliary material of back composition pastille micropill with benproperine phosphate and have the slow-release material of slow releasing function.The optimum content of the benproperine phosphate in its simple grain capsule is 52.7mg or this numerical value 0.5～2 times.Benproperine phosphate in the above-mentioned slow-release micro-pill: auxiliary material: slow-release material (weight ratio) is 1: 1.5～4: 0.5～1.5.
Above-mentioned slow-release micro-pill mainly is made up of the pastille micropill sustained release coating layer outer with being coated on the pastille micropill, and wherein the pastille micropill also can directly be made by the pastille mixture by forming as the celphere of parent nucleus and the medicated layer that is coated on outside the ball core.Wherein, described celphere is to comprise self-control or commercially available blank basic ball, and its material adopts lactose, starch, dextrin, sugar etc.; Described medicated layer or pastille micropill are made up of benproperine phosphate and auxiliary material, and these auxiliary material are meant one or more in Carboxymethyl cellulose sodium, hydroxypropyl emthylcellulose, sodium alginate, arabic gum, starch, sugar and the dextrin; Outer surface is surrounded by one deck sustained release coating layer, the slow-release material of this sustained release coating layer be in acrylic resin, hydroxypropyl emthylcellulose, ethyl cellulose and the polyvinylpyrrolidone any one to multiple, also comprise a kind of in triethyl citrate, Pulvis Talci, magnesium stearate, Polyethylene Glycol, diethyl phthalate and the dibutyl sebacate in this sustained release coating layer to other multiple adjuvants.
A kind of drug effect discharges uniform benproperine phosphate slow releasing capsule, mainly by benproperine phosphate, acrylic resin or cellulose and derivant thereof, dextrin, sugar, starch or carboxymethyl starch, polyvidone (promptly poly-acetyl pyrrole alkane ketone is called for short PVP) is formed, the proportioning of its composition is: 1 part of benproperine phosphate, 0.5～1.5 part of acrylic resin or cellulose and derivant thereof, 2～4 parts of dextrin, sugar, starch or carboxymethyl starch, polyvidones can add the moderate lubrication agent.
Cellulose recited above and derivant thereof are microcrystalline Cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose or/and sodium carboxymethyl cellulose, and lubricant is Pulvis Talci, stearic acid, silica sol and magnesium stearate.
Benproperine phosphate slow releasing capsule of the present invention, its Main Ingredients and Appearance proportioning is: 1 part of benproperine phosphate, 0.5～0.8 part of acrylic resin or cellulose and derivant thereof, 2.2～3.5 parts of dextrin, sugar, starch or carboxymethyl starch, polyvidones.
Carry out the test of release in vitro degree after the benproperine phosphate slow releasing capsule of above-mentioned treatment cough made micropill, the release scope of its release is that the release dose is 20～45% of a labelled amount in 2 hours, discharge dose in 4 hours and be in 50～70%, 8 hours of labelled amount and discharge dose greater than 75% of labelled amount.
The slow releasing preparation prescription screening drug release determination method of benproperine phosphate is dissolution medium according to drug release determination method (two appendix XD second methods of Chinese Pharmacopoeia version in 2000) with aquae destillata 500ml, adopts and changes blue laws, and rotating speed is that per minute 100 changes, operation in accordance with the law.The had good sustained release effect of the slow releasing preparation of test result proof benproperine phosphate of the present invention, easier granulation, outward appearance, repeatability are all good.
The preparation method of slow-release micro-pill adopts coating to become the ball method in the benproperine phosphate slow releasing capsule of the present invention, comprising:
1.: at first ready-made celphere or commercially available celphere are placed the coating machine, injection concentration is 5% binder solution, up to the abundant moistening of celphere;
2.: will be behind benproperine phosphate and the adjuvant powder mix homogeneously add and handle in the above-mentioned coating machine and obtain ganoid pastille micropill (also can directly make) by the pastille mixture, 5% binder solution is continued to spray in the pastille micropill parcel back that finishes, and the pastille micropill after will wrapping up then places 25～80 ℃ drying baker inner drying 3～12 hours;
3.: in proper amount of solvent, stirring state adds the slow-release material mix homogeneously down and makes sustained release coating liquid;
4.: the benproperine phosphate pastille micropill that drying is good is reentered into the coating machine, and the sustained release coating liquid that even injection has prepared carries out Cotton seeds, makes slow-release micro-pill;
5.: slow-release micro-pill placed 50～80 ℃ common electrical drying baker inner drying 3～12 hours;
6.: measure the content and the dissolution of slow-release micro-pill, the hard capsule of packing into and being made by common osseocolla material detects and promptly makes benproperine phosphate slow releasing capsule of the present invention after qualified.
In 4., the material bed tempertaure during coating is controlled at 20～50 ℃.
The invention provides the dosage regimen of taking twice medicine in a day, have the benproperine phosphate medicine in the said composition at least, for the patient of needs, this slow releasing preparation is suitable for oral.Preferred this pharmaceutical composition micropill form.This pharmaceutical composition also can above coloring agent.
The present invention is owing to adopted macromolecular material, as hydroxypropyl methylcellulose, polyvidone, sodium carboxymethyl cellulose, ethyl cellulose etc., be wrapped in outside the pastille micropill, form semi-permeable release membranes, delay the release of benproperine phosphate, make blood concentration fluctuation little, more steady, the half-life prolongs, and valid density is kept the longer time, have more long-lasting, thereby reduced the dosage and the number of times of medication.Therefore slow releasing preparation of the present invention can the prolong drug holdup time in vivo, and the release of control medicine reduces medicining times, reduces toxic and side effects, improves curative effect.Especially for the outpatient of oral administration, take medicine twice every day, the blood drug level that can remain valid in 12 hours, and have best bioavailability.
The benproperine phosphate medicine can continue to discharge by gastrointestinal tract the time in the medicine of the present invention, can not produce that to block the drug release that membrane pores caused incomplete because of chyme, and the rate of release of pharmaceutical compositions is controlled easily, technology is simpler, operate simple and feasible, guarantee the quality of product easily, production cost is also little, the cycle of producing is short, and is good in economic efficiency.
Specific embodiment:
Embodiment one: per 1000 benproperine phosphate slow releasing capsule contain following material:
Benproperine phosphate 27.0g ethyl cellulose 30.0g
Dextrin 76.0g sugar 80.0g
PVP 20.0g magnesium stearate 1.5g
HPMC 10.0g
1, precision takes by weighing PVP, and water is mixed with 5% binder solution, and is standby;
2, sugar, dextrin are made the ball core, get benproperine phosphate, adding PVP (binding agent) solution is an amount of, and the hydrojet coating is drying to obtain the pastille micropill;
3, getting above-mentioned pastille micropill puts in the coating pan, pot Revolution Per Minute 10～20 changes, kettle temperature is 40～50 ℃, the uninterrupted spray coating solution (aqueous suspension of ethyl cellulose, commodity are called Sulisi, Surelease) to the pastille micropill, evenly wrap one deck slow release film-coat, be drying to obtain slow-release micro-pill;
4, detect after with the slow-release micro-pill hard capsule of packing into.
After testing, the release scope of the slow releasing preparation release of benproperine phosphate is that the release dose is 20～45% of a labelled amount in 2 hours; Discharging dose in 4 hours is 50～70% of labelled amount; Discharge dose in 8 hours greater than 75% of labelled amount.
Embodiment two: per 1000 benproperine phosphate slow releasing capsule contain following material:
Benproperine phosphate 52.7g acrylic resin 40.0g
Starch 90.0g sugar 40.0g
PVP 20.0g Pulvis Talci 2.3g
Preparation method is the same.
Embodiment three: per 1000 benproperine phosphate slow releasing capsule contain following material:
Benproperine phosphate 80.0g ethyl cellulose 28.0g
Dextrin 60.0g starch 55.0g
PVP 20.0g Pulvis Talci 2.5g
HPMC 10.0g
Preparation method is the same.
Claims (5)
1, a kind of drug effect discharges uniform benproperine phosphate slow-releasing agent, consist predominantly of benproperine phosphate and corresponding auxiliary material, it is characterized in that above-mentioned medicament is a kind of slow releasing capsule based on slow-release micro-pill, its slow-release micro-pill comprises and contains as the pastille micropill of the benproperine phosphate of active component and be coated on the sustained release coating layer that pastille micropill skin has slow releasing function, and above-mentioned adjuvant comprises and mixes the auxiliary material of back composition pastille micropill with benproperine phosphate and have the slow-release material of slow releasing function.
2, a kind of drug effect according to claim 1 discharges uniform benproperine phosphate slow-releasing agent, it is characterized in that benproperine phosphate in the above-mentioned slow-release micro-pill: auxiliary material: slow-release material (weight ratio) is 1: 1.5～4: 0.5～1.5.
3, a kind of drug effect according to claim 1 discharges uniform benproperine phosphate slow-releasing agent, it is characterized in that above-mentioned pastille micropill is made up of benproperine phosphate and auxiliary material, these auxiliary material are meant one or more in Carboxymethyl cellulose sodium, hydroxypropyl emthylcellulose, sodium alginate, arabic gum, starch, sugar and the dextrin.
4, a kind of drug effect according to claim 1 discharges uniform benproperine phosphate slow-releasing agent, the slow-release material that it is characterized in that above-mentioned sustained release coating layer is meant in acrylic resin, hydroxypropyl emthylcellulose, ethyl cellulose and the polyvinylpyrrolidone any one to multiple, also comprises a kind of to other multiple adjuvants in triethyl citrate, Pulvis Talci, magnesium stearate, Polyethylene Glycol, diethyl phthalate and the dibutyl sebacate in this sustained release coating layer.
5, discharge uniform benproperine phosphate slow-releasing agent according to the described a kind of drug effect of claim 1 to 4, the optimum content that it is characterized in that the benproperine phosphate in its simple grain capsule is 52.7mg or this numerical value 0.5～2 times.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510034600 CN1864692A (en) | 2005-05-17 | 2005-05-17 | A drug action released evenly sustained release capsule of benproperine phosphate |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510034600 CN1864692A (en) | 2005-05-17 | 2005-05-17 | A drug action released evenly sustained release capsule of benproperine phosphate |
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| CN1864692A true CN1864692A (en) | 2006-11-22 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104546733A (en) * | 2013-10-21 | 2015-04-29 | 广东东阳光药业有限公司 | Benproperine taste-masking pellet |
-
2005
- 2005-05-17 CN CN 200510034600 patent/CN1864692A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104546733A (en) * | 2013-10-21 | 2015-04-29 | 广东东阳光药业有限公司 | Benproperine taste-masking pellet |
| CN104546733B (en) * | 2013-10-21 | 2019-04-19 | 广东东阳光药业有限公司 | A kind of benproperine odor-masking pellet |
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Open date: 20061122 |