CN103156822A - Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof - Google Patents
Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof Download PDFInfo
- Publication number
- CN103156822A CN103156822A CN201310114152XA CN201310114152A CN103156822A CN 103156822 A CN103156822 A CN 103156822A CN 201310114152X A CN201310114152X A CN 201310114152XA CN 201310114152 A CN201310114152 A CN 201310114152A CN 103156822 A CN103156822 A CN 103156822A
- Authority
- CN
- China
- Prior art keywords
- preparation
- diclofenac sodium
- osmotic pump
- controlled release
- pump type
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Images
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a diclofenac sodium osmotic-pump controlled-release preparation and a preparation method thereof. The preparation is composed of an osmotic pump tablet core and a semipermeable controlled-release coating coated outside the tablet core, wherein the osmotic pump tablet core comprises a main drug, permeable active substances, a binding agent, a cosolvent, a filler and a lubricant; and the semipermeable controlled-release coating comprises a coating material, a pore-forming agent and a plasticizer. The invention also relates to a preparation method of the osmotic-pump preparation. The preparation technique is simple, and adopts a conventional tablet preparation method; the tablet core is pressed by a conventional method without determining the punching surface; and by using the osmotic pressure between the inner and outer sides of the semipermeable membrane as driving force, the preparation releases the drug at zero-level release rate to maintain the stable blood concentration in vivo, has the characteristics of moderate drug in-vivo action time and low side effect, and can not easily generate drug resistance after repeated administration. The invention can reduce the drug taking frequency, and enables the drug absorption to be free from the influence of food intake and in-vivo environment, thereby enhancing the compliance of the patient.
Description
Technical field
The invention belongs to technical field of medicine, relate to diclofenac sodium osmotic pump type controlled release preparation and preparation method thereof.
Background technology
Diclofenac sodium is third generation NSAID (non-steroidal anti-inflammatory drug), and in body, Cycloxygenase suppresses arachidonic synthetic to this product by suppressing, and makes the synthetic minimizing of prostaglandin; Simultaneously, it also can promote arachidonic acid to be combined with triglyceride, reduces the arachidonic acid concentration of endocellular liberation, and indirectly suppresses the synthetic of leukotriene, thereby plays rheumatism, antiinflammatory, pain relieving and refrigeration function.Be usually used in clinically antiinflammatory and the analgesia of osteoarthritis, bursitis, rheumatic arthritis, tendinitis and other joint or periarticular disease.Its antiinflammatory, refrigeration function are strong 9 times than indometacin, than the strong 26-50 of aspirin doubly.Have in similar drugs because of it that good effect, side effect are little, prolonged application is without advantages such as savings property, now use more than 40 countries and regions, be one of world's best-selling drugs.
The diclofenac sodium oral absorption is fast, complete; Reduce absorbance with food with clothes.Average 1～2 hour peaking of blood drug level auf nuechternen Magen einnehmen, 6 hours peakings when taking with food is same, the short (T of biological half-life
1/2Be 1.5h), plasma protein binding rate is 99%.
Because its biological half-life is short, want to keep its effective blood drug concentration, common oral preparation needs frequent drug administration, and blood concentration fluctuation is large, and patient dependence is poor, is unfavorable for clinical treatment; Though its slow releasing preparation is taken rear blood concentration fluctuation and is improved, belong to non-zero order and discharge, still not ideal enough.Existing dosage form can not adapt to needs clinically far away, and exploitation controlled release preparation once-a-day meets the needs of clinical development.Take the osmotic pump type controlled release tablets of osmotic pressure as main release power, can keep constant permeable pressure head in external setting-up time in tablet, for discharging, the medicine zero level of meeting water dissolution or even suspendible in tablet provides constant release power.The constant release of medicine has effectively been avoided the peak valley phenomenon of blood drug level in body, when keeping medicine and effectively treating concentration, has overcome the drug side effect that causes because of peak concentration.
Summary of the invention
The objective of the invention is to overcome the deficiency that exists in existing preparation technique, a kind of diclofenac sodium osmotic pump type controlled release preparation is provided, it is mainly diclofenac sodium mono-layer osmotic pump sheet, can effectively adjust drug release rate, obtain comparatively steady and effective blood drug level, thereby reduce drug side effect and medicining times, improve patient compliance.
Purpose of the present invention can reach by following measures: the present invention includes the label that contains diclofenac sodium and be wrapped in the label semi-transparent coating membrane of controlled release of drug release hole in addition, described coating membrane weight is the 3%-10% of label weight; Described drug release hole is in tablet surface one or both sides laser boring and/or machine drilling.
Described label comprises following composition, to account for the percentage ratio of label gross weight:
Described semi permeability film coating liquid consists of:
Described osmotic pressure active substance comprises macromolecular substances and small-molecule substance: macromolecular substances is any in polyoxyethylene, arabic gum, polyvinylpyrrolidone or hypromellose; Small-molecule substance is one or more in sucrose, lactose, glucose, potassium chloride, sodium chloride, mannitol, sorbitol.
Described binding agent: be one or more in water, ethanol, polyvidone.
Described cosolvent: be one or more in sodium carbonate, sodium bicarbonate, sodium stearyl fumarate, sodium lauryl sulphate.
Described filler: be selected from one or more in starch, lactose, microcrystalline Cellulose, amylum pregelatinisatum.
Described lubricant is: one or more of Pulvis Talci, magnesium stearate, micropowder silica gel, hydrogenated vegetable oil, Polyethylene Glycol apoplexy due to endogenous wind.
Described semipermeable membrane coating material is: one or more in cellulose acetate, ethyl cellulose, acrylic resin, acetylbutyrylcellulose, polyvinyl alcohol.Porogen is selected: a kind of in PEG400, PEG1500, PEG4000, PEG6000.Plasticizer is selected: one or more in glycerol, propylene glycol, Polyethylene Glycol, phthalic acid ester, triglyceride.
Described punching technology is that the hole that one or two diameter is the 0.2-1.4 millimeter is beaten in laser boring or machine drilling.
Diclofenac sodium osmotic pump tablet preparation method is as follows:
(1) supplementary material is crossed respectively 100 mesh sieves, and the supplementary material except lubricant is crossed 60 mesh sieve mix homogeneously, the soft material processed take the 10%PVP ethanol solution as binding agent, and 20 mesh sieves are granulated, 40 ℃ of dryings, 18 mesh sieve granulate add lubricant to be pressed into label.
(2) semipermeable membrane coating material and plasticizer, porogen are dissolved in solvent, magnetic agitation makes it to become uniform solution; Label is put coating pan with the certain pressure spray coating, art for coating: spray velocity 3-4ml/min, 40-50 ℃ of coating kettle temperature, coating pan rotating speed 30-35r/min, coating to the label 3%-10% that increases weight puts coated tablet and removes residual solvent in air dry oven, solidifies 12 hours;
(3) use laser or mechanical means to prepare the aperture of a diameter 0.2-1.4 millimeter in one or both sides, gained coated tablet surface, namely get the diclofenac sodium osmotic pump type controlled release tablets.
Advantage of the present invention is: the film control techniques of application of advanced, diclofenac sodium is made mono-layer osmotic pump type controlled release tablet.Compare with ordinary preparation, this preparation only needed be administered once in one day, and effect is lasting, stable curative effect, and toxic and side effects is little, reduces medicining times, improves patient's compliance.Said preparation is not affected by the factors such as gastrointestinal motility, pH value, gastric emptying, and the hook good relationship is released in the inside and outside.
Description of drawings
Fig. 1 is the 24 hours cumulative release percent-time graphs of release in vitro according to the diclofenac sodium osmotic pump tablet of embodiment 1 preparation.
The specific embodiment
Embodiment 1
Core formulation (1000)
Coating fluid prescription:
Embodiment 2
Core formulation (1000)
Coating fluid prescription:
Embodiment 3
Core formulation (1000)
Coating fluid prescription:
Preparation technology: supplementary material is crossed respectively 100 mesh sieves, and the supplementary material except Pulvis Talci is crossed 60 mesh sieve mix homogeneously, the soft material processed take the 10%PVP ethanol solution as binding agent, and 20 mesh sieves are granulated, 40 ℃ of dryings, 18 mesh sieve granulate add Pulvis Talci to be pressed into label.Cellulose acetate, plasticizer and porogen are dissolved in solvent, label is carried out coating, increase weight to desired thickness, solidified 12 hours in 40 ℃.Then the small delivery aperture for preparing 1 millimeter of a diameter in coated tablet one side laser boring namely gets diclofenac sodium mono-layer osmotic pump type controlled release tablet.
Claims (11)
1. diclofenac sodium osmotic pump type controlled release preparation is characterized in that: this medicine is by the label that comprises diclofenac sodium and is wrapped in the outer semi permeability film coating with one or two drug release hole of label and consists of,
Described label comprises following composition, to account for the percentage ratio of label gross weight:
Described semi permeability film coating liquid consists of:
Coating material 2%-10% (w/v, mg/ml)
Plasticizer 3%-15% (w/v, mg/ml)
Porogen 10%-40% (w/v, mg/ml)
The film coating weightening finish is the heavy 3%-10% of sheet
Described drug release hole is in label one or both sides machine drilling or laser boring.
2. diclofenac sodium osmotic pump type controlled release preparation according to claim 1 is characterized in that: described osmo active substance comprises one or more in any and small-molecule substance sucrose in macromolecular substances polyoxyethylene, arabic gum, polyvinylpyrrolidone or hypromellose, lactose, glucose, potassium chloride, sodium chloride, mannitol, sorbitol.
3. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: described binding agent is one or more in water, ethanol, polyvidone.
4. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: described cosolvent is one or more in sodium carbonate, sodium bicarbonate, sodium stearyl fumarate, sodium lauryl sulphate.
5. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: described filler is selected from one or more in starch, lactose, microcrystalline Cellulose, amylum pregelatinisatum.
6. diclofenac sodium osmotic pump type controlled release preparation according to claim 1 is characterized in that: described lubricant is one or more of Pulvis Talci, magnesium stearate, micropowder silica gel, hydrogenated vegetable oil, Polyethylene Glycol apoplexy due to endogenous wind.
7. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: described semipermeable membrane coating material is selected from one or more in cellulose acetate, ethyl cellulose, acrylic resin, acetylbutyrylcellulose, polyvinyl alcohol.
8. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: described plasticizer is selected from one or more in glycerol, propylene glycol, Polyethylene Glycol, phthalic acid ester, triglyceride.
9. diclofenac sodium osmotic pump type controlled release preparation according to claim 1 is characterized in that: described porogen is selected from a kind of in PEG400, PEG1500, PEG4000, PEG6000.
10. diclofenac sodium osmotic pump type controlled release preparation according to claim 1, it is characterized in that: the hole of one or two diameter 0.2-1.4 millimeter is beaten in described laser boring or machine drilling.
11. the preparation method of a diclofenac sodium osmotic pump type controlled release preparation as claimed in claim 1 is characterized in that it comprises the following steps:
(1) supplementary material is crossed respectively 100 mesh sieves, and the supplementary material except lubricant is crossed 60 mesh sieve mix homogeneously, the soft material processed take the 10%PVP ethanol solution as binding agent, and 20 mesh sieves are granulated, 40 ℃ of dryings, 18 mesh sieve granulate add lubricant to be pressed into label;
(2) semipermeable membrane coating material and plasticizer, porogen are dissolved in solvent, magnetic agitation makes it to become uniform solution; Label is put in coating pan with the certain pressure spray coating, art for coating: spray velocity 3-4ml/min, 40-50 ℃ of coating kettle temperature, coating pan rotating speed 30-35r/min, to label weightening finish 3%-10%, coated tablet is put removed residual solvent in air dry oven, solidified 12 hours;
(3) use laser or mechanical means to prepare the aperture of a diameter 0.2-1.4 millimeter in one or both sides, gained coated tablet surface, namely get the diclofenac sodium osmotic pump type controlled release tablets.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310114152XA CN103156822A (en) | 2013-04-03 | 2013-04-03 | Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310114152XA CN103156822A (en) | 2013-04-03 | 2013-04-03 | Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103156822A true CN103156822A (en) | 2013-06-19 |
Family
ID=48580690
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310114152XA Pending CN103156822A (en) | 2013-04-03 | 2013-04-03 | Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103156822A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105581993A (en) * | 2016-03-11 | 2016-05-18 | 常州欧法玛制药技术有限公司 | Aspirin osmotic pump controlled-release tablet and preparing method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101919860A (en) * | 2009-06-12 | 2010-12-22 | 鲁南制药集团股份有限公司 | Medicine composite containing pentoxifyllinum and diclofenac and application thereof |
-
2013
- 2013-04-03 CN CN201310114152XA patent/CN103156822A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101919860A (en) * | 2009-06-12 | 2010-12-22 | 鲁南制药集团股份有限公司 | Medicine composite containing pentoxifyllinum and diclofenac and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| 王宗春等: "双氯芬酸钠微孔渗透泵控释片的制备", 《中国医院药学杂志》 * |
| 赵学玲等: "微孔渗透泵片的药物传递机制", 《药学学报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105581993A (en) * | 2016-03-11 | 2016-05-18 | 常州欧法玛制药技术有限公司 | Aspirin osmotic pump controlled-release tablet and preparing method thereof |
| CN105581993B (en) * | 2016-03-11 | 2018-06-29 | 常州欧法玛制药技术有限公司 | A kind of aspirin osmotic pump controlled release tablet and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10507185B2 (en) | Composite structural material and pharmaceutical composition thereof | |
| JP2022104916A (en) | Self-regulating osmotic gastroretentive drug delivery systems | |
| CN103006612B (en) | Lisinopril controlled-release tablet and preparation method thereof | |
| CN113476421B (en) | Controlled release composition of febuxostat and preparation method thereof | |
| CN102307575B (en) | Aceclofenac-containing controlled-release oral drug preparations and their manufacturing process | |
| CN101259113B (en) | Etodolac osmotic pump type controlled-release preparation and preparation thereof | |
| CN102048701A (en) | Pitavastatin calcium enteric sustained-release micropill preparation and preparation method thereof | |
| JP2024054132A (en) | Sustained release compositions containing liothyronine - Patent Application 20070229933 | |
| CN111526872B (en) | Pharmaceutical composition and preparation method and application thereof | |
| CN103550183A (en) | Trimetazidine hydrochloride osmotic pump controlled-release tablet and preparation method thereof | |
| CN101249081A (en) | Administer orally controlled release drug administration pharmaceutical tablet | |
| CN102697761B (en) | Ibuprofen slow release solid composition and preparation method thereof | |
| CN103156822A (en) | Diclofenac sodium osmotic-pump controlled-release preparation and preparation method thereof | |
| CN102670575A (en) | Ketoprofen osmotic pump type controlled release preparation and preparation method thereof | |
| CN105769773A (en) | Loxoprofen sodium sustained-release pellet | |
| CN103169685B (en) | A kind of butylphenyl phthaleine controlled release preparation and preparation method thereof | |
| WO2018228440A1 (en) | Controlled release febuxostat composition and preparation method therefor | |
| CN104856971B (en) | A kind of pulse dual-release preparation and the preparation method and application thereof | |
| CN101584683A (en) | Metolazone slow-release capsule and method for preparing same | |
| CN107441055A (en) | A kind of preparation method of controlled release drug | |
| CN102319224A (en) | Compound methoxyphenamine rapid-release slow-release osmotic pump preparation | |
| CN103432130B (en) | Ketoprofen lansoprazole sustained-release pellets, as well as preparation method and preparation thereof | |
| CN102188405A (en) | New cavity administration preparation formulation | |
| CN102813638A (en) | Preparation method of dexketoprofen trometamol double-layer sustained-release tablets | |
| CN101259112A (en) | Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130619 |