CN1295469A - Hydroxypylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings - Google Patents

Hydroxypylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings Download PDF

Info

Publication number
CN1295469A
CN1295469A CN 99804552 CN99804552A CN1295469A CN 1295469 A CN1295469 A CN 1295469A CN 99804552 CN99804552 CN 99804552 CN 99804552 A CN99804552 A CN 99804552A CN 1295469 A CN1295469 A CN 1295469A
Authority
CN
China
Prior art keywords
compositions
agent
additive
substrate
coating
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
Application number
CN 99804552
Other languages
Chinese (zh)
Inventor
郭建华
韦尔丁·W·哈克姆
乔治·W·斯金纳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hercules LLC
Original Assignee
Hercules LLC
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hercules LLC filed Critical Hercules LLC
Publication of CN1295469A publication Critical patent/CN1295469A/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Cosmetics (AREA)

Abstract

A composition comprising hydroxypropylcellulose and at least one anionic polymer, such as sodium carboxymethylcellulose and the use of aqueous solutions thereof for coating substrates such as tablets, granules, beads, etc.

Description

Hydroxypropyl cellulose and anionic polymer compositions and as the purposes of pharmaceutical film coating
Invention field
The present invention relates to film and form compositions, more particularly, the present invention relates to contain the compositions of hydroxypropyl cellulose and sodium carboxymethyl cellulose.
Background of invention
With the polymer film forming compositions tablet, granule and pearl being carried out coating is that pharmaceutical field is known.Except pharmacy books, handbook and scientific and technical literature, the patent documentation in this field comprises: United States Patent (USP) NO.4931286 discloses the high glaze tablet, it contains the active component in the binding agent skeleton of being present in as label, and Polyethylene Glycol (PEG) plasticizer, this label has the outermost layer coating of sodium carboxymethyl cellulose (SCMC), and wherein the substitution value of sodium carboxymethyl cellulose (DS) is 150-400 for its degree of polymerization of 0.2-14 (DP).The outermost layer coating is applied by aqueous solution by spray coating.This tablet has higher gloss than other cellulosic polymer.So just there is no need increases gloss by other coating.In addition, only need sodium carboxymethyl cellulose very in a small amount, therefore bringing unexpected reduction effect aspect cost of material and processing time.Moreover the sodium carboxymethyl cellulose film dissolves sooner such as the film of hydroxypropyl methylcellulose etc., so the dissolving of unlikely interference coated tablet Chinese medicine.
Oneself is used to contain the moisture film coating like a bomb hydroxypropyl cellulose, to improve utilization (the The Use of Klucel hydroxy-propylcellulose (HPC) of hydroxypropyl methylcellulose, to increase the Utility of hydroxy propylmethyl-cellulose (HPMC) in Aqueous Film Coating (strengthening the application of hydroxypropyl methylcellulose in containing the moisture film coating, AqualonTechnical Bulletin VC-556A) with the Klucel hydroxypropyl cellulose.Hydroxypropyl methylcellulose has high tensile and low-down rate elongation.When the Klucel HPC with high rate elongation joined in traditional hydroxypropyl methylcellulose film coating, the pliability of this film and the cohesiveness of substrate increased greatly.
U.S. Patent No. 4316884 discloses indoprofen and can use to the people with the safety that improves at its effective antiinflammatory dosage, and the activity of indoprofen prolongs greatly by the indoprofen microcyst microgranule in the solid protection coating of cellulose ether such as ethyl cellulose.
Summary of the invention
The invention provides a kind of compositions, wherein contain hydroxypropyl cellulose and at least a anionic polymer, for example, the carboxylate of cellulosic carboxymethyl ester salt, methacrylate polymer and copolymer, carboxy vinyl polymer and copolymer, alginate, pectinic acid salt, pectate, carrageenin, agar and polysaccharide.
A kind of compositions also is provided, has wherein contained substrate and coating, this coating contains hydroxypropyl cellulose and at least a anionic polymer.
The method of coating substrate also is provided, and this method comprises the aqueous solution of (a) preparation hydroxypropyl cellulose and anionic polymer and (b) described solution is coated on the substrate.
In this article the term of Shi Yonging " basically by ... form " refer to that described component is essential, but can also contain other component that does not hinder the advantage of being recognized of the present invention.
Detailed Description Of The Invention
Have now found that the compositions of hydroxypropyl cellulose and anionic polymer such as sodium carboxymethyl cellulose, have film forming characteristics.The film of these compositionss shows good tensile and rate elongation and the film coating of high glaze is provided.
Be applicable to that anionic polymer of the present invention is cellulosic carboxymethyl ester salt, the carboxylate of preferred SCMC, methacrylate polymer and copolymer, carboxy vinyl polymer and copolymer, alginate, pectinic acid salt, pectate, carrageenin, agar and polysaccharide.
The substitution value (DS) that is applicable to sodium carboxymethyl cellulose of the present invention is at least 0.2, and preferably is at least about 0.5.It is about 2.5 that the substitution value of sodium carboxymethyl cellulose can be as high as, and preferably is no more than about 0.9.It is about 100 that the degree of polymerization of sodium carboxymethyl cellulose (DP) is at least, preferably at least about 200.The degree of polymerization of sodium carboxymethyl cellulose can preferably be no more than about 1000 up to about 4000.
The weight average molecular weight that is suitable for hydroxypropyl cellulose of the present invention is at least about 80000.The molecular weight of hydroxypropyl cellulose can preferably be no more than about 95000 up to about 1150000.
The substitution value of sodium carboxymethyl cellulose is to be provided by carboxymethyl group with the 3.0 total substitution values as obtainable male caproic acid (androhexoic) site.Sodium carboxymethyl cellulose is the cellulose gum that is provided with trade name Aqualon_SCMC by Hercules Incoporated.Purity is all requirements that 99.5% free flowing powder meets American Pharmacopeia.
Hydroxypropyl cellulose is the cellulose gum that is provided with trade name Klucel_ hydroxypropyl cellulose by Hercules Incoporated.It meets all requirements of American Pharmacopeia as free flowing powder.
The weight ratio of hydroxypropyl cellulose and sodium carboxymethyl cellulose was at least about 1: 20, preferably at least about 1: 4.Hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose can reach about 20: 1, preferably is no more than about 4: 1.
Plasticizer also can optionally be present in the compositions of the present invention.Suitable plasticizer is ethanolamine, ethylene glycol, glycerol, 1,2,6-hexanetriol, list, two and glyceryl triacetate, 1,5-pentanediol, sorbitol, Polyethylene Glycol (weight average molecular weight is no more than about 600), propylene glycol and trimethylolpropane.Preferred plasticizer is a Polyethylene Glycol, and preferably its molecular weight is about 400.When plasticizer existed, it accounted for 1% of total composition weight at least, preferably at least about 5.5%.When plasticizer existed, it is about 50% that its percent that accounts for total composition weight can reach, and preferably is no more than about 20%.
Compositions of the present invention is particularly suitable for the coating as substrate, for example, and the coating of tablet, granule, pearl etc.The specific area of using is to contain the medicinal substrate of medicine active component such as the coating of tablet, maybe can be used for new pharmaceutical dosage form.This type of can use plasticizer such as the Polyethylene Glycol compatible with medicine in using.
As required with in order to improve practicality, value and the simplicity of preparation or coated tablet, granule, pearl and other novel pharmaceutical formulations type, in this coated composition, also can mix other component, for example active medicine component, active cosmetic component, nourishing additive agent, plasticizer, opacifying agent, surfactant, stabilizing agent, silicon dioxide, polysiloxanes, antiseptic, surface conditioning agent, correctives, cross-linking agent and other polymer.
The representative types of active medicine comprises antacid, anti-inflammatory substance (includes but not limited to nonsteroidal anti-inflammatory agent, NSAIDs, vasodilation, coronary vasodilator diastole agent, cerebral vasodilator and peripheral vasodilation agent), anti-infective, psychosis, antimanic drugs, analeptic, antihistaminic, cathartic, Decongestant, vitamin, the gastrointestinal tract tranquilizer, antidiarrhea agent, anti-anginal drug, anti-arrhythmic, antihypertensive, vasoconstrictor and migraine treatment agent, anticoagulant and antithrombotic drug, analgesic, antipyretic, sleeping pill, tranquilizer, Bendectin, antinanseant, anticonvulsant, neuromuscular drug, high or low blood glucose medicine, thyroid and antithyroid drug, diuretic, anti-spasmodics, uterine relaxant, mineral and nourishing additive agent, appetrol, the anabolism medicine, promoting erythrocyte generates medicine, antiasthmatics, expectorant, cough medicine, mucolytic, anti-hyperuricemia medicine, and the other medicines or the material that act locally on the oral cavity, for example, local analgesia agent, local anesthetic, polypeptide drugs, inverase, chemotherapy and antineoplastic agent etc.
Though any active medicine compatible with hydroxypropyl cellulose and anionic polymer mixture and other tablet component physicochemical property all is fine, the example of given activity medicine comprises aluminium hydroxide, andrographolide, dexamethasone, aspirin, acetaminophen, ibuprofen, isosorbide, dinitrate, nicotinic acid, tetracycline, ampicillin, dexbrompheniramine, chlorphenamine, albuterol, isoephedrine, loratadine, tea alkali, ascorbic acid, tocopherol, Benadon, methoclopramide, magnesium hydroxide, verapamil, procainamide hydrochloride, Propranolol, captopril, Ergotamine, flurazepam, diazepam, lithium carbonate, insulin, furosemide, hydrochlorothiazide, guaifenesin, dextromethorphan and benzocaine.
The preparation that contains NSAIDs can also contain (comprising the acetaminophen among the application) other pharmaceutically active component that often uses with NSAID of therapeutic dose, it includes but not limited to Decongestant or bronchodilator (isoephedrine for example, phenylpropanolamine, phenylephrine and pharmaceutical salts thereof), cough medicine is (as caramiphen, dextromethorphan and pharmaceutical salts thereof), antihistaminic is (as chlorphenamine, the bromo pheniramine, dexchlorpheniramine, dexbrompheniramine, triprolidine, doxylamine, tripelennamine, Cyproheptadine, pyrilamine, hydroxyzine, promethazine, azatadine and pharmaceutical salts thereof), non-sedative antihistamine medicine (acrivastine for example, astemizole, cetirizine, ketotifen, loratadine, temelastine, terfenadine (comprising the U.S. Patent No. 4254129 and the 4285957 disclosed metabolite that are incorporated herein by reference) and pharmaceutical salts thereof), muscle relaxant (glyceryl list ether (glycerylmonether) SMRs for example, methocarbamol, mephenesin, the mephenesin carbamate, cyclobenzaprine, chlorzoxazone, mephenesin acid succinate, chlorphenesin carbamate or its pharmaceutical salts) and adjuvant (as diphenhydramine, caffeine, xanthine derivative (comprise that U.S. Patent No. 4558051 is disclosed, be introduced into as a reference) and pharmaceutical salts thereof), the cooperative programs of nourishing additive agent and any said medicine.Said medicine can be united with acetaminophen and treated allergy, cough, flu, flu sample and/or the flu-like symptom that mammal comprises the people.But, these medicines can be used as the auxiliary agent of sleeping peacefully (as diphenhydramine) or for other purpose and acetaminophen mixed.
Anionic polymer, as sodium carboxymethyl cellulose, crosslinked in the presence of some polyvalent cation.Sodium carboxymethyl cellulose (SCMC) is an anionic water-soluble polymer.The physicochemical property of SCMC makes its application very wide, as food, medicine and personal nursing.Aqueous solution with some multivalent salts treatment S CMC causes its precipitation.But, in SCMC solution, discharge polyvalent cation such as Al gradually + 3, it is uniform crosslinked that polymer molecule has been produced by carboxymethyl group.Prepared gel like this.The character of this gel depends on the amount of cross-linking agent existence, the concentration and the DP of polymer molecule successively.The speed dependent that produces gel is in A1 + 3Ionic dissociation enters the speed of this water system.The final mass of gel and gel time can be controlled by changing viscosity grade and the amount of used SCMC, the ratio of polyvalent cation and the pH of medium.
At coated composition with at substrate (tablet for example, granule and pearl etc.) in the active component of blending can be medical active component such as sleeping pill, tranquilizer, town's epilepsy agent, awakening agents (awakening agent), anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, add pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
Coated composition and substrate (as tablet, granule, pearl etc.) can contain cosmetic active agent such as breath freshening chemical compound such as menthol and be usually used in other correctives and the spice of oral hygiene, and the quaternary ammonium base that is used for tooth and oral cavity cleaning etc.Can improve the effect of spice with spice promoter such as tartaric acid, citric acid, vanillin etc.
Compositions of the present invention is preferably given substrate such as tablet coating with the form of aqueous solution.
Method for optimizing with present composition coating substrate comprises the aqueous solution for preparing hydroxypropyl cellulose and anionic polymer such as sodium carboxymethyl cellulose, and this aqueous solution is coated on substrate.In this coated composition, also optionally there is above-mentioned plasticizer.When preparation sodium carboxymethyl cellulose, hydroxypropyl cellulose and aqueous solution of plasticizer, this solution can prepare or preparation respectively together.Suitable coat weight preferably account for coating substrate gross weight at least about 0.5%, more preferably at least about 0.75%.Coat weight accounts for the coated composition gross weight can preferably be no more than 2% up to about 10%.
The high glaze medicinal tablet generally contains at least a medicine activity component in the binding agent matrix core, this label has the coating of the plasticizer of anionic polymer such as sodium carboxymethyl cellulose, hydroxypropyl cellulose and selectivity existence.
Compositions of the present invention has industrial applicibility in each pharmaceutical preparation of system.
Provide the following example, just be used for illustrating rather than limiting the scope of the invention.Unless otherwise specified, all umber and percentage number average are by weight.Embodiment 1
In this embodiment, air suspension fluid column coating machine, Glatt GPCG5/9 is provided by Glatt Air Techniques, and its parameter is as follows:
Spray gun: port size, mm 1.2
Gasket ring, mm 3.0
Spray air pressure, crust 1.8
Peristaltic pump
Transport speed, g/ minutes 28
Post
The setting of intake air vibroshock is opened
The outlet air vibroshock is provided with, and % 45
In batches, kg 3
The intake air temperature, ℃ 60
Outlet air temperature, ℃ 48
By nozzle, this nozzle is contained in the center of product chambers bottom perforated plate with tablet aerated flow influencing meridian cylindrical shape coating partition wall.When tablet passed through spraying, they were by this aqueous solution coating.The perimeter of this partition wall is downward bed.This regional air flow remains almost weightless suspension with these tablets, so that they can move down fast, and in the opening of this coating partition wall base portion of the horizontal suction of energy.This process lasts till that tablet obtains till the required coating.
Stir down, the 24.8g sodium carboxymethyl cellulose (is derived from Hercules Inc., commodity are called Aqualon_7L2P CMC): and 24.8g hydroxypropyl cellulose (derive from Hercules Inc., commodity are called the Klucel_EF hydroxypropyl cellulose) is mixed with the 906.5g deionized water.Mixed last till obtain clear solution.In this solution, add 7.7g Polyethylene Glycol (derive from Union Carbide, be PEG 400) and mixed then up to obtaining uniform solution.Detect solution viscosity make detected value for 125 to 300 cps so that provide good coating with Glatt GPCG-5 coating machine.
2kg biconvex placebo tablet is added in the fluid bed, and heated 5 minutes.Then, this coating solution is coated on these tablets.The weight that increases is 1.9%.The disintegration time of these tablets is 4:00 minute.The gloss of these tablets is than the height with hydroxypropyl cellulose/the hydroxypropyl methylcellulose coating obtains.
ASTMD523-89 detects glossiness with multi-angle remission meter (Multi Angular Reflectometer).
Glossiness
20° 60° 80.5°
HPC/HPMC 1/1 13.7 30.9 43.1
HPC/CMC 1/1 8.1 26.9 51.2
HPC/CMC 2/1 15.0 54.2 90.8
HPC/CMC 1/2 36.3 68.8 89.3
PEG 400 accounts for 8.7% of polymer weight
Embodiment 2
Stir down, 24.8g Aqualon_7L2P sodium carboxymethyl cellulose is joined in the 595.2g deionized water, and 24.8g Klucel_EF hydroxypropyl cellulose and 235.2g deionized water is mixed.Mixed last till obtain clear solution.In these two solution, all add 3.9g Polyethylene Glycol (derive from Union Carbide, be PEG 400) and mixed then up to obtaining uniform solution.3.1g aluminum chloride is dissolved in the 50g deionized water, joins this solution in the hydroxypropyl cellulose solution and be blended into and obtain uniform solution.Detect solution viscosity make detected value for 125 to 175 cps so that provide good coating with Glatt GPCG-5 coating machine, tablet is added in the fluid bed, and heated 5 minutes.Begin to spray one deck sodium carboxymethyl cellulose, then spray one deck hydroxypropyl cellulose.These layers are alternative, and last one deck is a sodium carboxymethyl cellulose.The weight that increases is 1.7%.
The disintegration time of these tablets is 8:10 minute.

Claims (81)

1. moisture coated composition that the high glaze coating is provided, it is made up of hydroxypropyl cellulose and at least a anionic polymer basically.
2. the compositions of claim 1, wherein anionic polymer is selected from the carboxylate of cellulosic carboxymethyl ester salt, methacrylate polymer and copolymer, carboxy vinyl polymer and copolymer, alginate, pectinic acid salt, pectate, carrageenin, agar and polysaccharide.
3. the compositions of claim 2, wherein anionic polymer is selected from cellulosic carboxymethyl ester salt.
4. the compositions of claim 3, wherein said cellulosic carboxymethyl ester salt is sodium carboxymethyl cellulose.
5. the compositions of claim 4, wherein the substitution value of sodium carboxymethyl cellulose is at least 0.2.
6. the compositions of claim 4, the substitution value of wherein said sodium carboxymethyl cellulose is no more than 2.5.
7. the compositions of claim 4, the degree of polymerization of wherein said sodium carboxymethyl cellulose is at least 100.
8. the compositions of claim 4, the degree of polymerization of wherein said sodium carboxymethyl cellulose is no more than about 4000.
9. the compositions of claim 2, wherein the molecular weight of hydroxypropyl cellulose is at least about 80000.
10. the compositions of claim 2, wherein the molecular weight of hydroxypropyl cellulose is no more than about 1150000.
11. the compositions of claim 2 wherein contains plasticizer.
12. the compositions of claim 4, wherein hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose was at least about 1: 20.
13. the compositions of claim 4, wherein hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose is no more than about 20: 1.
14. the compositions of claim 11, wherein the amount based on the weight plasticizer of total composition is at least about 1%.
15. the compositions of claim 11, wherein the amount based on the weight plasticizer of total composition is no more than about 50%.
16. the compositions of claim 2 wherein contains at least a additive, this additive is selected from cross-linking agent, medicine activity component, cosmetic active constituent and nourishing additive agent.
17. the compositions of claim 4, wherein the substitution value of sodium carboxymethyl cellulose for about 0.2 to about 2.5 degree of polymerization be about 100 to about 4000, the weight average molecular weight of hydroxypropyl cellulose is about 80000 to about 1150000, hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose is about 1: 20 to about 20: 1, and optionally containing additive, this additive is selected from plasticizer, cross-linking agent, medicine activity component, cosmetic active constituent and nourishing additive agent.
18. the compositions of claim 17, wherein the substitution value of sodium carboxymethyl cellulose is at least about 0.5.
19. the compositions of claim 17, wherein the substitution value of sodium carboxymethyl cellulose is no more than about 0.9.
20. the compositions of claim 17, wherein the degree of polymerization of sodium carboxymethyl cellulose is at least about 200.
21. the compositions of claim 17, wherein the degree of polymerization of sodium carboxymethyl cellulose is no more than about 1000.
22. the compositions of claim 17, wherein the molecular weight of hydroxypropyl cellulose is at least about 80000.
23. the compositions of claim 17, wherein the molecular weight of hydroxypropyl cellulose is no more than about 95000.
24. the compositions of claim 17 wherein contains plasticizer, this plasticizer is selected from ethanolamine, ethylene glycol, glycerol, 1,2,6-hexanetriol, list, two and glyceryl triacetate, 1,5-pentanediol, sorbitol, Polyethylene Glycol, propylene glycol and trimethylolpropane.
25. the compositions of claim 17, wherein hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose was at least about 1: 4.
26. the compositions of claim 17, wherein hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose is no more than about 4: 1.
27. the compositions of claim 17, wherein based on the weight of total composition, the amount of plasticizer is at least about 5.5%.
28. the compositions of claim 17, wherein based on the weight of total composition, the amount of plasticizer is no more than about 20%.
29. the compositions of claim 17, wherein the substitution value of sodium carboxymethyl cellulose for about 0.5 to about 0.9 degree of polymerization be about 200 to about 1000, the weight average molecular weight of hydroxypropyl cellulose is about 80000 to about 950000, hydroxypropyl cellulose: the weight ratio of sodium carboxymethyl cellulose is about 1: 4 to about 4: 1, and optionally contain additive, this additive is selected from cross-linking agent, medicine activity component, the cosmetic active constituent, nourishing additive agent and plasticizer, wherein plasticizer is selected from ethanolamine, ethylene glycol, glycerol, 1,2, the 6-hexanetriol, single, two and glyceryl triacetate, 1, the 5-pentanediol, sorbitol, Polyethylene Glycol, propylene glycol and trimethylolpropane.
30. the compositions of claim 17, wherein plasticizer is a Polyethylene Glycol.
31. the plasticizer of claim 28, wherein the molecular weight of Polyethylene Glycol is about 400.
32. a compositions wherein contains substrate and contains the coating that right requires 1 described compositions.
33. a compositions wherein contains substrate and contains the coating that right requires 2 described compositionss.
34. a compositions wherein contains substrate and contains the coating that right requires 4 described compositionss.
35. a compositions wherein contains substrate and contains the coating that right requires 17 described compositionss.
36. a compositions wherein contains substrate and contains the coating that right requires 29 described compositionss.
37. the compositions of claim 32, wherein substrate contains medicine activity component.
38. the compositions of claim 33, wherein substrate contains medicine activity component.
39. the compositions of claim 34, wherein substrate contains medicine activity component.
40. the compositions of claim 35, wherein substrate contains medicine activity component.
41. the compositions of claim 36, wherein substrate contains medicine activity component.
42. the compositions of claim 32, wherein medicine activity component is selected from sleeping pill, tranquilizer, town's epilepsy agent, awakening agents, anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, adds pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
43. the compositions of claim 33, wherein medicine activity component is selected from sleeping pill, tranquilizer, town's epilepsy agent, awakening agents, anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, adds pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
44. the compositions of claim 34, wherein medicine activity component is selected from sleeping pill, tranquilizer, town's epilepsy agent, awakening agents, anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, adds pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
45. the compositions of claim 35, wherein medicine activity component is selected from sleeping pill, tranquilizer, town's epilepsy agent, awakening agents, anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, adds pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
46. the compositions of claim 36, wherein medicine activity component is selected from sleeping pill, tranquilizer, town's epilepsy agent, awakening agents, anti-psychoneurosis medicine, neuromuscular blocking agents, spasmolytic, antihistaminic, anti-allergic drug, cardiac tonic, anti-arrhythmic, diuretic, depressor, adds pressing, expectorant, thyroxine, gonadal hormone, antidiabetic drug, antineoplastic agent, antibiotic, chemotherapeutics and anesthetics.
47. the compositions of claim 32, wherein substrate contains the cosmetic active constituent.
48. the compositions of claim 34, wherein substrate contains the cosmetic active constituent.
49. the compositions of claim 34, wherein substrate contains the cosmetic active constituent, and this component is selected from the breath freshening chemical compound and is usually used in oral hygiene and other correctives and the spice of tooth and oral cavity cleaning, tartaric acid, citric acid and vanillin.
50. the compositions of claim 32, wherein substrate contains nourishing additive agent.
51. the compositions of claim 34, wherein substrate contains nourishing additive agent.
52. the compositions of claim 32, wherein coating contains at least a additive, and this additive is selected from cross-linking agent, pharmaceutically active component, cosmetic active constituent and nourishing additive agent.
53. the compositions of claim 33, wherein coating contains at least a additive, and this additive is selected from cross-linking agent, pharmaceutically active component, cosmetic active constituent and nourishing additive agent.
54. the compositions of claim 34, wherein coating contains at least a additive, and this additive is selected from cross-linking agent, pharmaceutically active component, cosmetic active constituent and nourishing additive agent.
55. the compositions of claim 35, wherein coating contains at least a additive, and this additive is selected from cross-linking agent, pharmaceutically active component, cosmetic active constituent and nourishing additive agent.
56. the compositions of claim 36, wherein coating contains at least a additive, and this additive is selected from cross-linking agent, pharmaceutically active component, cosmetic active constituent and nourishing additive agent.
57. the method for coating substrate, comprising (a) preparation contain right require 1 compositions aqueous solution and (b) described solution is coated on the substrate.
58. the method for coating substrate, comprising (a) preparation contain right require 2 compositionss aqueous solution and (b) described solution is coated on the substrate.
59. the method for coating substrate, comprising (a) preparation contain right require 4 compositionss aqueous solution and (b) described solution is coated on the substrate.
60. the method for coating substrate, comprising (a) preparation contain right require 17 compositionss aqueous solution and (b) described solution is coated on the substrate.
61. the method for coating substrate, comprising (a) preparation contain right require 29 compositionss aqueous solution and (b) described solution is coated on the substrate.
62. the method for claim 57, wherein substrate is selected from tablet, granule and pearl.
63. the method for claim 58, wherein substrate is selected from tablet, granule and pearl.
64. the method for claim 59, wherein substrate is selected from tablet, granule and pearl.
65. the method for claim 60, wherein substrate is selected from tablet, granule and pearl.
66. the method for claim 63, wherein said aqueous solution contains at least a additive, and this additive is selected from active medicine component, cross-linking agent, pigment, antioxidant, coloring agent, opacifying agent, surfactant, stabilizing agent, silicon dioxide, polysiloxanes, antiseptic, surface conditioning agent, correctives, cosmetic active constituent, nourishing additive agent and gives by other polymer of the substrate desirable characteristics of coating.
67. the method for claim 64, wherein said aqueous solution contains at least a additive, and this additive is selected from active medicine component, cross-linking agent, pigment, antioxidant, coloring agent, opacifying agent, surfactant, stabilizing agent, silicon dioxide, polysiloxanes, antiseptic, surface conditioning agent, correctives, cosmetic active constituent, nourishing additive agent and gives by other polymer of the substrate desirable characteristics of coating.
68. the method for claim 66, wherein additive is selected from multivalent ion salt.
69. the method for claim 67, wherein additive is selected from multivalent ion salt.
70. the method for claim 69, wherein multivalent ion salt is selected from aluminum salt, calcium salt, magnesium salt, iron salt, zinc salt, titanium salt and zirconates.
71. the method for claim 69, wherein multivalent ion salt is selected from aluminum salt and calcium salt.
72. the method for claim 50, wherein the aqueous solution of hydroxypropyl cellulose and sodium carboxymethyl cellulose prepares respectively, and the aqueous solution of hydroxypropyl cellulose contains at least a additive, and this additive is selected from active medicine component, cross-linking agent, pigment, antioxidant, coloring agent, opacifying agent, surfactant, stabilizing agent, silicon dioxide, polysiloxanes, antiseptic, surface conditioning agent, correctives, cosmetic active constituent, nourishing additive agent and gives by other polymer of the substrate desirable characteristics of coating.
73. the method for claim 72, wherein additive is selected from multivalent ion salt.
74. the method for claim 73, wherein multivalent ion salt is selected from aluminum salt, calcium salt, magnesium salt, iron salt, zinc salt, peptide salt and zirconates.
75. the method for claim 74, wherein multivalent ion salt is selected from aluminum salt and calcium salt.
76. the compositions of claim 32, wherein said coating account for composition total weight at least about 0.5% (weight).
77. the compositions of claim 34, wherein said coating account for composition total weight at least about 0.5% (weight).
78. the compositions of claim 32, wherein said coating are no more than about 10% (weight) of composition total weight.
79. the compositions of claim 34, wherein said coating are no more than about 10% (weight) of composition total weight.
80. the compositions of claim 35, wherein said coating account for composition total weight at least about 0.75% (weight).
81. the compositions of claim 35, wherein said coating are no more than about 2% (weight) of composition total weight.
CN 99804552 1998-12-31 1999-12-02 Hydroxypylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings Pending CN1295469A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22807598A 1998-12-31 1998-12-31
US09/228,075 1998-12-31

Publications (1)

Publication Number Publication Date
CN1295469A true CN1295469A (en) 2001-05-16

Family

ID=22855672

Family Applications (1)

Application Number Title Priority Date Filing Date
CN 99804552 Pending CN1295469A (en) 1998-12-31 1999-12-02 Hydroxypylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings

Country Status (10)

Country Link
EP (1) EP1058543A1 (en)
JP (1) JP2002534373A (en)
CN (1) CN1295469A (en)
AR (1) AR022118A1 (en)
AU (1) AU2037100A (en)
BG (1) BG104799A (en)
BR (1) BR9908394A (en)
CA (1) CA2322293A1 (en)
ID (1) ID26814A (en)
WO (1) WO2000040223A1 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102361652A (en) * 2009-03-25 2012-02-22 琳得科株式会社 Adhesion preventing composition, solid preparation and method for producing same
CN105640819A (en) * 2014-11-13 2016-06-08 广州十长生化妆品有限公司 Skin tendering smoothening whitening exfoliating microsphere and application thereof
CN106133046A (en) * 2014-03-24 2016-11-16 蓝宝迪有限公司 Wetting agent

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101171006B (en) * 2005-05-20 2010-12-01 第一三共株式会社 Film coated preparation
CN103520133B (en) * 2013-10-26 2015-02-04 中山市凯博思淀粉材料科技有限公司 Preparation method of starch-based soft capsules
WO2018195205A1 (en) 2017-04-18 2018-10-25 Sensient Colors Llc Dosage form coating composition and method of making and using the same

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57145817A (en) * 1981-03-05 1982-09-09 Satoru Yamazaki Remedy for peptic ulcer
US4931286A (en) * 1989-04-19 1990-06-05 Aqualon Company High gloss cellulose tablet coating
US5080717A (en) * 1991-01-24 1992-01-14 Aqualon Company Fluid suspensions of polysaccharide mixtures

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102361652A (en) * 2009-03-25 2012-02-22 琳得科株式会社 Adhesion preventing composition, solid preparation and method for producing same
CN102361652B (en) * 2009-03-25 2013-06-19 琳得科株式会社 Adhesion preventing composition, solid preparation and method for producing same
CN106133046A (en) * 2014-03-24 2016-11-16 蓝宝迪有限公司 Wetting agent
CN105640819A (en) * 2014-11-13 2016-06-08 广州十长生化妆品有限公司 Skin tendering smoothening whitening exfoliating microsphere and application thereof

Also Published As

Publication number Publication date
AU2037100A (en) 2000-07-24
JP2002534373A (en) 2002-10-15
CA2322293A1 (en) 2000-07-13
AR022118A1 (en) 2002-09-04
ID26814A (en) 2001-02-08
EP1058543A1 (en) 2000-12-13
BG104799A (en) 2001-05-31
WO2000040223A1 (en) 2000-07-13
BR9908394A (en) 2000-10-31

Similar Documents

Publication Publication Date Title
JP4919801B2 (en) Drug coating providing high drug loading and method for providing the same
JP2617109B2 (en) Formulation of sustained release drug for oral administration
EP0277127B1 (en) New drug preparation with controlled release of the active compound, and a method for the manufacture thereof
ES2304980T3 (en) SUSTAINED LIBERATION MATRIX SYSTEMS FOR HIGHLY SOLUBLE PHARMACOS.
JPH08501081A (en) Controlled release morphine formulation
PT642785E (en) HYDROGEL SYSTEMS OF HETROODISPERSO OF LIBERTACAO SUSTIDA
CZ298694A3 (en) Preparation containing morphine salt with controlled release
CN109044981A (en) A kind of Pregabalin intragastric floating slowly releasing piece and preparation method thereof
EP0616802B1 (en) Oral preparation for release in lower digestive tracts
CN1538837A (en) Swallow tablet comprising paracetamol
JPH08109126A (en) Impact-resistant enteric granule and tablet containing the same
CN1295469A (en) Hydroxypylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings
CN102178677B (en) Nifedipine double-layer osmotic pump medicinal composition and preparation technology thereof
CN102048730A (en) Levamlodipine besylate composition and preparation method thereof
CN108785268A (en) A kind of Betapace and preparation method thereof
WO2001026633A1 (en) Tablets coated with locust bean gum, guar gum or carrageenan gum
JPH0797330A (en) Oral depressant against cholesterol
JP4696210B2 (en) Sustained-release tablets containing isosorbide-5-mononitrate as an active ingredient and method for producing the same
WO2007143290A2 (en) Delayed-release compositions of extended release forms of venlafaxine
CN1403078A (en) Slow-releasing prepn containing p-acetamidophenol and opium
CN116098867A (en) Abiraterone polymeric micelle preparation and preparation method thereof
CN1483401A (en) Slow-released preparation
MXPA00008483A (en) Hydroxypropylcellulose and anionic polymer compositions and their use as pharmaceutical film coatings
ZA200504215B (en) Controlled-release compositions

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