CN1513439A - Slow release medicine of pseudo-ephedrine hydrochloride - Google Patents
Slow release medicine of pseudo-ephedrine hydrochloride Download PDFInfo
- Publication number
- CN1513439A CN1513439A CNA031318428A CN03131842A CN1513439A CN 1513439 A CN1513439 A CN 1513439A CN A031318428 A CNA031318428 A CN A031318428A CN 03131842 A CN03131842 A CN 03131842A CN 1513439 A CN1513439 A CN 1513439A
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- CN
- China
- Prior art keywords
- solid dispersion
- slow releasing
- pseudoephedrine hydrochloride
- preparation
- pseudoephedrine
- Prior art date
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Abstract
A slow-release pseudoephedrine hydrochloride in the form of capsule, tablet, suspension, dripping pill, or powder is prepared from the pseudoephedrine hydrochloride (10-80 wt.%) and at least one pharmacologically receptable slow releasing material as skeleton (20-90 wt.%).
Description
Technical field
The present invention relates to a kind of pseudoephedrine hydrochloride slow release medicine.
The prospect technology
Pseudoephedrine hydrochloride (d-pesudoephedine hydrochloride PE-HCL) is a kind of sympathomimetic amine, mainly act on neuro alpha-receptor, oral PE-HCL is a kind of very effectively mucosa Decongestant, be mainly used in clinically because of the acute and chronic that flu, respiratory tract infection etc. cause, the treatment of allergic rhinitis, its central nervous system's (CNS) side effect is more much smaller than the ephedrine hydrochloride that similar curative effect is arranged, phenylpropanolamine etc.Pseudoephedrine hydrochloride is become different compound preparations with antipyretic analgesic, antihistaminic, eliminating phlegm and stopping cough medicine compatibility abroad, be widely used in the treatment flu, and use as the nonprescription drugs (OTC) of safety.Pseudoephedrine hydrochloride has multiple dosage forms such as tablet, capsule, syrup, slow releasing tablet, slow-release micro-pill, and the common single dose of quick releasing formulation is 30mg, need take every day 2～3 times.
Summary of the invention
The main slow release formulation of commercially available pseudoephedrine hydrochloride has slow-release micro-pill, slow releasing tablet.Slow-release micro-pill leans on repeatedly bundled slow-releasing clothing film to reach the purpose of controlled release drug rate of release more, slow releasing tablet mostly is hydrogel matrix tablet, when preparation requires multiple drug release rate, then need to prepare slow-release micro-pill or the preparation multilamellar compressed tablets or the clad sheet of multiple rate of release, the production routine complexity that the preparation method of these several dosage forms relates to, technic index require high, the preparation apparatus expensive, numerous domestic producer generally is difficult to satisfy its every specification requirement.
The technical problem to be solved in the present invention is problems such as existing pseudoephedrine hydrochloride class slow releasing pharmaceutical complex manufacturing, production cost height.
For addressing the above problem, the present invention adopts following technical scheme:
Utilize solid dispersions technique that a kind of pharmaceutical formulation that continue to discharge effective ingredient that has is provided, pseudoephedrine hydrochloride as active component, and is contained at least a pharmaceutically acceptable sustained-release materials as framework material.
Its principle is: pseudoephedrine hydrochloride is very easily water-soluble, utilizes the water-insoluble adjuvant the bigger principal agent of dissolubility in the water to be reached the purpose of control drug release speed by solid dispersions technique.(SolidDispersion SD) means that medicine is dispersed in system in the solid carrier material with forms such as microgranule, crystallite or molecularities to solid dispersion.
The content range of active component of the present invention is 10～80% (weight), and the content range of pharmaceutically acceptable framework material is 20～90% (weight).
The preferred content of each composition of the present invention is: the content range of active component is 15～50% (weight), and the content range of pharmaceutically acceptable framework material is 30～75% (weight).
Acceptable framework material is selected from cellulose ether and/or cellulose esters on the said medicine: comprise ethyl cellulose (EC), cellulose acetate-butyrate, cellulose acetate phthalate ester (CAP), Hydroxypropyl Methylcellulose Phathalate (HPMCP), Ka Baibo (Carbopol, Carbomer); Crylic acid resin: comprise Eudragit E, L, S, RL, RS etc., homemade II number, III number, IV polyacrylic resin; Lipid: comprise the glyceride type of cholesterol, cupreol, stearic acid, stearyl alcohol, tripalmitin, cholesterol ester stearic acid, castor oil hydrogenated, Cera Flava, babassu ester, microwax and other fatty acid etc.Preferably ethyl cellulose, polyacrylic resin class, Ka Baibo, stearic acid, castor oil hydrogenated.
Can add some water-soluble substanceses such as polyethylene glycols (PEG), polyvinylpyrrolidone (PVP), polyoxyethylene (PEG), sodium lauryl sulphate (SLS) and saccharide etc. in addition and regulate drug release rate as perforating agent.
Preparation method of the present invention can be according to the difference of framework material and is different, comprise following several: (1) solvent precipitation: in the alcoholic solution of pseudoephedrine hydrochloride, add carrier mass (cellulose family, crylic acid resin), stir, on boiling water bath, boil off ethanol, formed solid is pulverized, promptly.(2) fusion method: with pseudoephedrine hydrochloride and carrier mixing (lipid), be heated to fusion with water-bath or oil bath, stirring makes and is uniformly dispersed, cooling rapidly, promptly.
The pseudoephedrine hydrochloride solid dispersion that the present invention makes can be used for preparing multiple slow release formulation, because each solid dispersion granule all is an independent sustained-release administration unit, the preparation chance liquid of being made by the solid dispersion granule promptly collapses the diffusing multiple dose unit delivery system that is, can avoid single dose units release preparation to take the local irritant influence in back, can avoid occurring " dose dumping " risk of (referring to that the release active compound in the slow-releasing agent gets too fast) equally.And be far from the repeatedly slow-release micro-pill complexity of coating of its preparation technology.The solid dispersion granule can directly be made capsule, or is pressed into tablet or multilamellar matrix tablet, or makes suspensoid, long-acting drop pill.Speed, slow-releasing granules that other drug powder or other method of perhaps mixing made can directly be made capsule or tablet with multiple drug release rate.
The specific embodiment
Embodiment 1:
A kind of average loading amount is the pseudoephedrine sustained-release capsule of 240mg, presses the lek number and feeds intake:
Pseudoephedrine hydrochloride 60g
Polyacrylic resin II 60g
Polyacrylic resin III 120g
1000
Take by weighing pseudoephedrine hydrochloride, polyacrylic resin by recipe quantity, add the alcoholic solution of 50ml95%, stirring boils off solvent after making dissolving fully, and 0 ℃ of cooling 10min takes out solid matter, smashes, and it is encapsulated to get 24～30# sieve granule.The rate of release data are as follows:
Time (h) release (%)
0.5 60.21
1 73.68
2 80.24
4 88.28
6 96.58
Embodiment 2:
A kind of average loading amount is the pseudoephedrine sustained-release capsule of 120mg, presses the lek number and feeds intake:
Pseudoephedrine hydrochloride 60g
Ethyl cellulose 60g
Make 1000
Take by weighing pseudoephedrine hydrochloride, ethyl cellulose by recipe quantity, add the alcoholic solution of 50ml 95%, stirring boils off solvent after making dissolving fully, and 0 ℃ of cooling 10min takes out solid matter, smashes, and it is encapsulated to get 24～30# sieve granule.The rate of release data are as follows:
Time (h) release (%)
0.5 29.35
1 44.10
2 49.24
4 50.16
6 51.78
Embodiment 3:
The pseudoephedrine slow releasing tablet that a kind of average loading amount is 182mg, press the lek number and feed intake:
Pseudoephedrine hydrochloride 60g
Polyacrylic resin II 60g
Hydroxypropyl methylcellulose HPMC K4M 30g
Lactose 30g
Magnesium stearate 2g
Make 1000
Take by weighing pseudoephedrine hydrochloride, polyacrylic resin II number by recipe quantity, add the alcoholic solution of 50ml 95%, stir make dissolving fully after, boil off solvent, 0 ℃ of cooling 10min takes out solid matter, pulverizes, got 60# sieve fine powder and HPMC K4M, lactose, starch mix homogeneously, with 5%PVP K30 solution is binding agent, crosses 24# sieve series grain, 55 ℃ of baking 2h, behind the magnesium stearate mixing, compacting in flakes.The rate of release data are as follows:
Time (h) release (%)
0.5 18.73
1 35.10
2 60.42
4 80.36
6 88.47
Embodiment 4:
The pseudoephedrine compound sustained release capsules that a kind of average loading amount is 433mg, press the lek number and feed intake:
Pseudoephedrine hydrochloride 60g
Stearic acid 120g
Ka Baibo 934P 30g
Hydroxypropyl methylcellulose K100M 100g
Naproxen sodium 120g
Make 1000
Take by weighing pseudoephedrine hydrochloride, stearic acid by recipe quantity, 55 ℃ make fusion, after stirring makes mix homogeneously, natural cooling, smash, got 60# sieve fine powder and recipe quantity card primary ripple 934P, hydroxypropyl methylcellulose K100M mixing, with 7% ethyl cellulose alcoholic solution as binding agent, cross 24# sieve series grain, remove fine powder; Naproxen sodium is crossed 24# sieve series grain with the pure liquid system soft material of 2% PVP K30.Two kinds of granules are at 40 ℃ of baking 2h, and mixing is encapsulated in proportion.The rate of release data are as follows:
Release (%)
Time (h) pseudoephedrine hydrochloride naproxen sodium
0.5 30.17 78％
1 48.35 82％
2 63.41 87％
4 75.22 92％
6 81.47 97％
Embodiment 5:
The pseudoephedrine slow releasing tablet that a kind of average loading amount is 420mg, press the lek number and feed intake:
Pseudoephedrine hydrochloride 60g
Hydrogenated soya phosphatide 360g
Make 1000
Take by weighing pseudoephedrine hydrochloride, hydrogenated soya phosphatide by recipe quantity, mix homogeneously adds ethanol in the pasty state, fully stir evenly, and decompression, the solid that obtains is pulverized, and gets 24～30# sieve granule, and compacting is in flakes.The rate of release data are as follows:
Time (h) release (%)
1 12.44
2 17.24
4 26.01
8 45.65
12 62.53
Embodiment 6:
A kind of average loading amount is the pseudoephedrine sustained-release capsule of 90mg, presses the lek number and feeds intake:
Pseudoephedrine hydrochloride 60g
Castor wax 30g
1000
Take by weighing pseudoephedrine hydrochloride, castor wax by recipe quantity, mixing on boiling water bath, it is encapsulated that 18～24# sieve granule was got in the pulverizing of cooling back, high temperature fluidized processing.The rate of release data are as follows:
Time (h) release (%)
0.5 15.84
1 23.06
2 44.91
4 65.22
6 80.43
Claims (10)
1, a kind of slow releasing pharmaceutical that utilizes pseudoephedrine hydrochloride solid dispersion preparation, it is characterized in that be with pseudoephedrine hydrochloride as active component, and contain at least a pharmaceutically acceptable sustained-release materials as framework material.
2, the slow releasing pharmaceutical that utilizes the preparation of pseudoephedrine hydrochloride solid dispersion as claimed in claim 1 is characterized in that the weight content scope of active component is 10～80%, and the content range of pharmaceutically acceptable framework material is 20～90%.
3, the slow releasing pharmaceutical that utilizes the preparation of hydrochlorate pseudoephedrine solid dispersion as claimed in claim 2 is characterized in that the preferred weight content of each composition is an active component: 15～50%, 30～75% of pharmaceutically acceptable framework material.
4,, it is characterized in that described pharmaceutically acceptable framework material can be one or more of cellulose ether, cellulose esters, crylic acid resin, lipid as claim 1 or the 2 or 3 described slow releasing pharmaceuticals that utilize pseudoephedrine hydrochloride solid dispersion preparation.
5, the slow releasing pharmaceutical of the sour pseudoephedrine solid dispersion preparation of utilization as claimed in claim 4 is characterized in that described cellulose ether can be ethyl cellulose (EC), cellulose acetate-butyrate, Hydroxypropyl Methylcellulose Phathalate (HPMCP).
6, the slow releasing pharmaceutical of the sour pseudoephedrine solid dispersion preparation of utilization as claimed in claim 4 is characterized in that described cellulose esters can be cellulose acetate phthalate ester, Ka Baibo.
7, the slow releasing pharmaceutical that utilizes pseudoephedrine hydrochloride solid dispersion preparation as claimed in claim 4 is characterized in that described crylic acid resin comprises Eudragit E, L, S, RL, RS etc., homemade II number, III number, IV polyacrylic resin.
8, the slow releasing pharmaceutical that utilizes the preparation of pseudoephedrine hydrochloride solid dispersion as claimed in claim 4 is characterized in that described lipid comprises the glyceride type of cholesterol, cupreol, stearic acid, stearyl alcohol, tripalmitin, cholesterol ester stearic acid, castor oil hydrogenated, Cera Flava, babassu ester, microwax and other fatty acid etc.
9, the slow releasing pharmaceutical that utilizes pseudoephedrine hydrochloride solid dispersion preparation as claimed in claim 4 is characterized in that described bone material preferably adopts ethyl cellulose or polyacrylic resin class, Ka Baibo, stearic acid, castor oil hydrogenated.
10, the slow releasing pharmaceutical that utilizes the preparation of pseudoephedrine hydrochloride solid dispersion as claimed in claim 2 is characterized in that described perforating agent can be polyethylene glycols, polyvinylpyrrolidone, polyoxyethylene, sodium lauryl sulphate and saccharide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031318428A CN1513439A (en) | 2003-06-05 | 2003-06-05 | Slow release medicine of pseudo-ephedrine hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031318428A CN1513439A (en) | 2003-06-05 | 2003-06-05 | Slow release medicine of pseudo-ephedrine hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1513439A true CN1513439A (en) | 2004-07-21 |
Family
ID=34239801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031318428A Pending CN1513439A (en) | 2003-06-05 | 2003-06-05 | Slow release medicine of pseudo-ephedrine hydrochloride |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1513439A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102357091A (en) * | 2011-08-29 | 2012-02-22 | 迪沙药业集团有限公司 | Chlocibutamine slow release pharmaceutical composition |
| CN108403674A (en) * | 2018-04-23 | 2018-08-17 | 常德职业技术学院 | A kind of anti-inflammatory sustained release preparation and preparation method thereof containing magnesium ion |
| CN110215521A (en) * | 2019-06-19 | 2019-09-10 | 江苏长泰药业有限公司 | Inhibit composition and its application that pseudoephedrine hydrochloride is extracted from solvent |
| CN114073689A (en) * | 2020-08-10 | 2022-02-22 | 江苏长泰药业有限公司 | Anti-extraction pharmaceutical composition and preparation thereof |
| CN114073690A (en) * | 2020-08-10 | 2022-02-22 | 江苏长泰药业有限公司 | Amino acid-containing anti-extraction pharmaceutical composition and preparation thereof |
-
2003
- 2003-06-05 CN CNA031318428A patent/CN1513439A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102357091A (en) * | 2011-08-29 | 2012-02-22 | 迪沙药业集团有限公司 | Chlocibutamine slow release pharmaceutical composition |
| CN102357091B (en) * | 2011-08-29 | 2015-12-09 | 迪沙药业集团有限公司 | A kind of Chlocibutamine slow release medicinal composition |
| CN108403674A (en) * | 2018-04-23 | 2018-08-17 | 常德职业技术学院 | A kind of anti-inflammatory sustained release preparation and preparation method thereof containing magnesium ion |
| CN110215521A (en) * | 2019-06-19 | 2019-09-10 | 江苏长泰药业有限公司 | Inhibit composition and its application that pseudoephedrine hydrochloride is extracted from solvent |
| CN114073689A (en) * | 2020-08-10 | 2022-02-22 | 江苏长泰药业有限公司 | Anti-extraction pharmaceutical composition and preparation thereof |
| CN114073690A (en) * | 2020-08-10 | 2022-02-22 | 江苏长泰药业有限公司 | Amino acid-containing anti-extraction pharmaceutical composition and preparation thereof |
| CN114073689B (en) * | 2020-08-10 | 2024-01-12 | 江苏长泰药业有限公司 | Extraction-preventing pharmaceutical composition and preparation thereof |
| CN114073690B (en) * | 2020-08-10 | 2024-01-12 | 江苏长泰药业有限公司 | Extraction-preventing pharmaceutical composition containing amino acid and preparation thereof |
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