CN101259112A - Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof - Google Patents
Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof Download PDFInfo
- Publication number
- CN101259112A CN101259112A CNA2008100597248A CN200810059724A CN101259112A CN 101259112 A CN101259112 A CN 101259112A CN A2008100597248 A CNA2008100597248 A CN A2008100597248A CN 200810059724 A CN200810059724 A CN 200810059724A CN 101259112 A CN101259112 A CN 101259112A
- Authority
- CN
- China
- Prior art keywords
- controlled release
- osmotic pump
- sarpogrelate hydrochloride
- single layer
- preparation
- 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)
Abstract
The invention relates to the medicine technical filed, in particular to a monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride and a preparation method thereof, which is characterized by lasting drug effect, constant curative effect, slight toxic and side effect. The monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride comprises by weight percentage of 1 to 40 percent of sarpogrelate hydrochloride, 30 to 90 percent of auxiliary material that can promote osmosis, 1 to 40 percent of membrane material that performs controlled release and the rest is other auxiliary material; the diameter of a small drug release hole is 0.1 to 2.0 mm. The preparation method comprises: a certain amount of drug according to the prescription is mixed with an adhesive, a bulking agent and a co-penetrant which are respectively ground and screened, prepared into soft material and palletized, dried and particle finished and then added with a lube and pressed to obtain tablet core. Coating liquid is prepared and the tablet core coated, after coating, drying is done to solidify the coating membrane, and then one side of coated tablet is provided with the small drug release hole, thus obtaining an osmotic pump controlled release tablet. The monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride of the invention has the advantages of reducing times of dosage, promoting the compliance of sufferers and satisfying the requirements of clinical medication.
Description
Technical field
The present invention relates to medical technical field, exactly it is a kind of medicine-sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations that improves the ischemic symptoms such as ulcer, pain and creeping chill that chronic arteria occlusion disease causes and preparation method thereof.
Background technology
Sarpogrelate hydrochloride (English name: sarpogrelate hydrochloride) be the 5-HT receptor blocking agent of the former research and development of MIT, cardiovascular drugs.Listing in 93 years clinically is used to improve the ischemic symptoms such as ulcer, pain and creeping chill that chronic arteria occlusion disease causes.
Its pharmacological action characteristics are: 1. suppress the platelet aggregation effect: 5-hydroxy tryptamine (5-HT) receptor of this product selectivity antagonism platelet and blood vessel, suppress platelet aggregation.This product suppresses the platelet aggregation that collagen causes separately, and its IC50 is 4.5 μ mol/L, when adding collagen and 5-HT, then can stronger inhibition platelet aggregation, and IC50 is 0.1 μ mol/L.Oral hydrochloride Sarpogrelate conventional tablet can significantly suppress to add 5-HT and collagen-induced platelet aggregation, this agglutinative inhibitory action is occurred than very fast, and the back 1.5h that takes medicine can reach summit, and sustainable 4～6h, and compendency is and replys tendency behind the 12h.2. this product suppresses the vasoconstriction that 5-HT and platelet aggregation cause: the 5-HT of low concentration can cause the contractile response of blood vessel, in addition, also can cause the contractile response of blood vessel when platelet aggregation.This product have with drug level increase to 5-HT and the caused vasoconstriction effect of platelet aggregation, simultaneously this product vascular smooth muscle that also can suppress to cause with platelet aggregation shrinks.3. anti thrombotic action: clinical trial shows, this product can suppress the animal model that tremulous pulse injects the rat artery obliterans that lauric acid causes.4. improve the body circulation: the minimizing that this product is propped up blood flow to the lower limb side that is caused by 5-HT has good improvement effect, and strengthens with dosage.
Osmotic pump preparation belongs to the slow/controlled release preparation in the pharmaceutical preparation, is a class preparation made from the osmotic pressure principle.The Oros sheet causes people's common concern with its unique release mode and stable rate of releasing drug, is ideal a kind of slow/controlled release preparation in the controlled release formulations for oral administration so far.Osmotic pump tablet release principle: osmotic pump tablet size and form are identical with conventional tablet, solid drugs and excipient are pressed into the core of medicine, outsourcing one deck can be permeable insoluble polymer film-coat, on film, open an aperture (or add water solublity porogen) and make with laser or mechanical force.When medicine enters in the gastrointestinal tract, the clothing film optionally makes water penetrate dissolved substance, the tablet internal penetration is pressed be higher than outside gastro-intestinal Fluid, and medicine can not see through coating membrane and discharges, and drug solution can only slowly release in aperture.Therefore, osmotic pump preparation has the function that continues slow control drug release, and the rate of release of medicine is constant, be not subjected to the influence of gastrointestinal tract pH environment, gastrointestinal motility etc., drug absorption speed mainly is subjected to the drug releasing rate restriction, therefore the blood concentration fluctuation scope is little, avoids producing the blood drug level peak valley phenomenon, can reduce side effects of pharmaceutical drugs.
The Oros type preparation of having researched and developed at present has single chamber and multicell osmotic pump preparation.The elementary osmotic pump sheet comprises plain edition, has semipermeability and enteric solubility mixing coating material-type, has different permeability multiple coatings membranous type and have multilayer materials coating type etc.; The multicell osmotic pump preparation comprises the osmotic pumps with similar piston motive force additive component, the two-chamber osmotic pump with soft membrane and miniature osmotic pumps etc.Oral slow/controlled release osmotic pump preparation can reduce the medication number of times because taking convenience, and curative effect is lasting, and is safe and reliable and enjoy people to favor.
The cardiovascular diseases is generally chronic disease, needs patient's long-term prescription.Listing dosage form sarpogrelate hydrochloride dosage form is a conventional tablet at present, and specification is the 100mg/ sheet, and dosage regimen is 3 times/day.Patient's administration number of times every day is frequent, forgets easily or slips, and causes missing medicine time or medicining times and reduces, and blood concentration fluctuation is big in the blood, and medicine is accumulated easily, patient's administration poor compliance.Therefore, this sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations will allow the patient to be administered once every day, and carry out drug dose design and drug release rate designs according to the osmotic pump preparation design principle, for improving patient's medication compliance, reduce simultaneously farthest individual patient difference, prolong the release of active substance and be different from ordinary preparation.
Summary of the invention
The objective of the invention is that a kind of convenient drug administration, effect are lasting in order to provide, stable curative effect, sarpogrelate hydrochloride single layer osmotic pump controlled release tablet that toxic and side effects is little.
The object of the present invention is achieved like this:
Preparation of the present invention contains following component by weight percentage:
Sarpogrelate hydrochloride 1-40%
Play short chemosmotic adjuvant 30-90%
Play the coating membrane material 1-40% of controlled release effect
Other adjuvant surplus
Small delivery aperture aperture 0.1-2.0mm
Wherein the pharmaceutical salts of sarpogrelate hydrochloride is a hydrochlorate, and playing short chemosmotic adjuvant is sodium chloride and/or potassium chloride and/or citric acid and/or sodium citrate and/or lactose and/or mannitol and/or fructose and/or sucrose and/or sodium hydrogen phosphate and/or polyoxyethylene and/or arabic gum and/or hypromellose and/or methyl starch sodium and/or low-substituted hydroxypropyl cellulose and/or cross-linking sodium carboxymethyl cellulose and/or crospolyvinylpyrrolidone and/or polyvinylpyrrolidone and/or carbopol.
The membrane material that plays the controlled release effect is cellulose acetate and/or ethyl cellulose and/or acrylic resin and/or hydroxypropyl emthylcellulose and/or polyethylene and/or polyethylene glycols.
The drug release hole of the one or both sides of coated tablet is laser boring or mechanical punching, and the small delivery aperture aperture can be 0.1-2.0mm.
Above-mentioned adjuvant is pharmaceutical carrier, expanding material, suspensoid, permeation-promoter, porogen, binding agent, lubricant, antiplastering aid, semipermeable membrane material, plasticizer, lucifuge agent, solvent.Pharmaceutical carrier, expanding material, suspensoid can adopt polyoxyethylene, arabic gum, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carbopol etc.Permeation-promoter can adopt citric acid, sodium citrate, sodium chloride, potassium chloride, lactose, mannitol, fructose, sucrose etc.; Binding agent can adopt polyvinylpyrrolidone, hypromellose etc.; Wetting agent can adopt the ethanol-water solution of water, dehydrated alcohol, various concentration; Lubricant can adopt stearic acid, magnesium stearate, Pulvis Talci, micropowder silica gel etc.; Porogen can be sucrose, mannitol, Polyethylene Glycol (Macrogol 200, PEG400, polyethylene glycol 1500, Macrogol 4000, polyethylene glycol 6000), carbamide etc.; Plasticizer can adopt Methyl Benzene-o-dicarboxylate and/or citrate, ethyl phthalate, citric acid three ester, Polyethylene Glycol; Opacifier can adopt titanium dioxide, Pulvis Talci, silicon dioxide etc.; Membrane material can adopt cellulose acetate, polyethylene, ethyl cellulose, acrylic resin etc.; Solvent can adopt acetone, dehydrated alcohol, ethanol, water etc.
The dosage form of above-mentioned preparation can be tablet, coating type, capsule, soft capsule.The preparation method of osmotic pump preparation of the present invention has: medicine and binding agent, filler, the short penetrating agent pulverize separately of recipe quantity are sieved, behind the mix homogeneously, with the soft ability of binding agent system, the granulation of sieving, oven for drying, granulate sieves, add lubricant, behind the mix homogeneously, tabletting obtains label.Filmogen and plasticizer are dissolved in the solvent as coating solution, label is put in the coating pan, carry out coating, after coating finishes, dry in the drying baker, coating membrane is solidified, prepare a suitable small delivery aperture in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Advantage of the present invention is: compare with ordinary preparation, that this preparation only needs be administered once, act in one day is lasting, stable curative effect, toxic and side effects are little.Controlled release preparation of the present invention will be used to improve the ischemic symptoms such as ulcer, pain and creeping chill that chronic arteria occlusion disease causes clinically.
Description of drawings:
Fig. 1 is the drug release curve chart according to the sarpogrelate hydrochloride single layer core controlled release tablet of embodiment 1 preparation
Fig. 2 is the drug release curve chart according to the sarpogrelate hydrochloride single layer core controlled release tablet of embodiment 2 preparations
The specific embodiment:
Embodiment 1:
Label is formed:
Sarpogrelate hydrochloride 25%
Polyoxyethylene (molecular weight 300,000) 42.5%
Citric acid 32.0%
Magnesium stearate 0.5%
The semipermeable membrane coating solution is formed:
Cellulose acetate 2.0%
PEG400 0.16%
Acetone solvent
Preparation method: medicine and citric acid, the polyoxyethylene pulverize separately of recipe quantity are crossed 100 mesh sieves, behind the mix homogeneously, with the soft ability of starch slurry system, cross 18 orders and granulate, 60 ℃ of oven for drying are crossed 20 mesh sieve granulate, add lubricant again, behind the mix homogeneously, direct compression obtains label.Cellulose acetate and plasticizer P EG400 are dissolved in the acetone soln as coating solution, label is put in the coating pan, the coating temperature is carried out coating for 40-60 ℃, after coating finishes, coated tablet is dry in 40 ℃ of drying baker, coating membrane is solidified, prepare the small delivery aperture of a 0.5mm in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Embodiment 2:
Label is formed:
Sarpogrelate hydrochloride 20%
Polyoxyethylene (molecular weight 300,000) 15%
Citric acid 64.5%
Magnesium stearate 0.5%
The semipermeable membrane coating solution is formed:
Cellulose acetate 2.5%
PEG400 0.25%
Acetone solvent
Preparation method: medicine and citric acid, the polyoxyethylene pulverize separately of recipe quantity are crossed 100 mesh sieves, behind the mix homogeneously, with the soft ability of starch slurry system, cross 18 orders and granulate, 60 ℃ of oven for drying are crossed 20 mesh sieve granulate, add lubricant again, behind the mix homogeneously, direct compression obtains label.Cellulose acetate and plasticizer P EG400 are dissolved in the acetone soln as coating solution, label is put in the coating pan, the coating temperature is carried out coating for 40-60 ℃, after coating finishes, coated tablet is dry in 40 ℃ of drying baker, coating membrane is solidified, prepare the small delivery aperture of a 0.5mm in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Embodiment 3:
Label is formed:
Sarpogrelate hydrochloride 30%
Polyoxyethylene (molecular weight 300,000) 50%
Lactose 19.5%
Magnesium stearate 0.5%
The semipermeable membrane coating solution is formed:
Cellulose acetate 3.0%
PEG400 0.3%
Acetone: isopropyl alcohol (4: 1) solvent
Preparation method: with the medicine of recipe quantity with cross 100 mesh sieves with lactose, polyoxyethylene pulverize separately, behind the mix homogeneously, add lubricant again, behind the mix homogeneously, direct compression obtains label.Cellulose acetate and plasticizer P EG 400 are dissolved in the acetone soln as coating solution, label is put in the coating pan, the coating temperature is carried out coating for 40-60 ℃, after coating finishes, coated tablet is dry in 40 ℃ of drying baker, coating membrane is solidified, prepare the small delivery aperture of a 0.5mm in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Embodiment 4:
Label is formed:
Sarpogrelate hydrochloride 20%
Citric acid 79.5%
Magnesium stearate 0.5%
The semipermeable membrane coating solution is formed:
Cellulose acetate 3.0%
PEG400 0.3%
Acetone: isopropyl alcohol (4: 1) solvent
Preparation method: medicine and citric acid, the polyoxyethylene pulverize separately of recipe quantity are crossed 100 mesh sieves, behind the mix homogeneously, with the soft ability of starch slurry system, cross 18 orders and granulate, 60 ℃ of oven for drying are crossed 20 mesh sieve granulate, add lubricant again, behind the mix homogeneously, direct compression obtains label.Cellulose acetate and plasticizer P EG400 are dissolved in the acetone soln as coating solution, label is put in the coating pan, the coating temperature is carried out coating for 40-60 ℃, after coating finishes, coated tablet is dry in 40 ℃ of drying baker, coating membrane is solidified, prepare the small delivery aperture of a 0.5mm in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Claims (6)
1. sarpogrelate hydrochloride single layer osmotic pump sheet, it is characterized in that: said preparation contains following composition by weight percentage:
Sarpogrelate hydrochloride 1-40%
Play short chemosmotic adjuvant 30-90%
Play the membrane material 1-40% of controlled release effect
Other adjuvant surplus
Small delivery aperture aperture 0.1-2.0mm
2. sarpogrelate hydrochloride single layer core osmotic pump controlled release tablet according to claim 1 is characterized in that: the pharmaceutical salts of sarpogrelate hydrochloride is a hydrochlorate.
3. sarpogrelate hydrochloride single layer osmotic pump controlled release tablet according to claim 1 is characterized in that: playing short chemosmotic adjuvant is sodium chloride and/or potassium chloride and/or citric acid and/or sodium citrate and/or lactose and/or mannitol and/or fructose and/or sucrose and/or sodium hydrogen phosphate and/or polyoxyethylene and/or arabic gum and/or hypromellose and/or methyl starch sodium and/or low-substituted hydroxypropyl cellulose and/or cross-linking sodium carboxymethyl cellulose and/or crospolyvinylpyrrolidone and/or polyvinylpyrrolidone and/or carbopol.
4. according to claims 1 described sarpogrelate hydrochloride single layer osmotic pump controlled release tablet, it is characterized in that: the membrane material that plays the controlled release effect is cellulose acetate and/or ethyl cellulose and/or acrylic resin and/or hydroxypropyl emthylcellulose and/or polyethylene and/or polyethylene glycols.
5. according to claims 1 described sarpogrelate hydrochloride single layer osmotic pump controlled release tablet, it is characterized in that: the drug release hole of the one or both sides of coated tablet is laser boring or mechanical punching, and the small delivery aperture aperture can be 0.1-2.0mm.
6. according to claims 1 described sarpogrelate hydrochloride single layer osmotic pump controlled release tablet, it is characterized in that: medicine and binding agent, filler, the short penetrating agent pulverize separately of recipe quantity are sieved, behind the mix homogeneously, with the soft ability of binding agent system, the granulation of sieving, oven for drying, granulate sieves, add lubricant, behind the mix homogeneously, tabletting obtains label.Filmogen and plasticizer are dissolved in the solvent as coating solution, label is put in the coating pan, carry out coating, after coating finishes, dry in the drying baker, coating membrane is solidified, prepare a suitable small delivery aperture in coated tablet one side with laser or mechanical means then, promptly get the sarpogrelate hydrochloride single layer osmotic pump controlled release tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100597248A CN101259112A (en) | 2008-02-19 | 2008-02-19 | Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100597248A CN101259112A (en) | 2008-02-19 | 2008-02-19 | Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101259112A true CN101259112A (en) | 2008-09-10 |
Family
ID=39959946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008100597248A Pending CN101259112A (en) | 2008-02-19 | 2008-02-19 | Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101259112A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101933918A (en) * | 2010-09-08 | 2011-01-05 | 苏州世林医药技术发展有限公司 | Sarpogrelate hydrochloride sustained-release preparation and preparation method |
| CN102552165A (en) * | 2012-01-05 | 2012-07-11 | 金陵药业股份有限公司 | Sarpogrelate hydrochloride sustained release pellet and preparation method thereof |
-
2008
- 2008-02-19 CN CNA2008100597248A patent/CN101259112A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101933918A (en) * | 2010-09-08 | 2011-01-05 | 苏州世林医药技术发展有限公司 | Sarpogrelate hydrochloride sustained-release preparation and preparation method |
| CN102552165A (en) * | 2012-01-05 | 2012-07-11 | 金陵药业股份有限公司 | Sarpogrelate hydrochloride sustained release pellet and preparation method thereof |
| CN102552165B (en) * | 2012-01-05 | 2014-07-16 | 金陵药业股份有限公司 | Sarpogrelate hydrochloride sustained release pellet and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2593582T3 (en) | Coated tablet formulation and method | |
| KR0137731B1 (en) | Dossage form for a delayed drug delivery | |
| ES2392396T3 (en) | Osmotic diffusion / pumping drug delivery system combined | |
| CN100563638C (en) | Nifedipine controlled-release tablet and preparation method thereof | |
| CN101485644B (en) | Novel controlled release capsule and preparation method thereof | |
| CN101732275A (en) | Double-layer osmotic pump controlled release tablet of isosorbide mononitrate and preparation method thereof | |
| CN103417505A (en) | Huperzine A controlled release preparation having biphasic release behavior, and preparation method thereof | |
| CN103860504A (en) | Slow/controlled-release preparation of ticagrelor | |
| CN102626428B (en) | Ginkgo leaf extract osmotic pump controlled-release preparation and preparation method thereof | |
| CN101095681A (en) | Alfuzosin Hydrochloride permeating pump type controlled-release preparation and method for preparing the same | |
| KR20140131205A (en) | Pharmaceutical composition containing highly water-soluble drug for sustained release | |
| CN108338976A (en) | A kind of nifedipine double-layer osmotic pump tablet and preparation method thereof | |
| CN103550183A (en) | Trimetazidine hydrochloride osmotic pump controlled-release tablet and preparation method thereof | |
| CN100571783C (en) | Glipizide controlled release tablets and preparation method thereof | |
| CN102349880B (en) | Isradipine controlled-release tablets and preparation method thereof | |
| CN101259112A (en) | Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof | |
| CN105055360A (en) | Prazosin hydrochloride controlled-release tablet and preparation method thereof | |
| CN101342151A (en) | Isosorbide mononitrate osmotic pump type controlled release formulation and preparation method thereof | |
| CN103284974B (en) | Benzene ring nonyl ester double-layer osmotic pump controlled-release tablet and preparation method thereof | |
| CN101642443A (en) | Isosorbide mononitrate osmotic pump type controlled-release preparation and preparation method thereof | |
| CN103655508A (en) | Double-medicament-layer isosorbide mononitrate osmotic pump controlled release tablet and preparation method thereof | |
| CN102293760B (en) | Isosorbide mononitrate timing controlled release preparation and preparation method thereof | |
| CN101380313B (en) | Famotidine high density type gastric retention osmotic pump controlled release preparation and preparation method thereof | |
| CN101269056B (en) | Metoprolol salt oral administration impulse pellet preparation | |
| CN100376230C (en) | Timing slow-releasing micrpill and its preparation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20080910 |