CN1615121A - Taste masking coating compositions - Google Patents
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- CN1615121A CN1615121A CNA998165883A CN99816588A CN1615121A CN 1615121 A CN1615121 A CN 1615121A CN A998165883 A CNA998165883 A CN A998165883A CN 99816588 A CN99816588 A CN 99816588A CN 1615121 A CN1615121 A CN 1615121A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules 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
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules 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
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules 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
- A61K9/5005—Wall or coating material
- A61K9/501—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules 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
- A61K9/5073—Microcapsules 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
- A61K9/5078—Microcapsules 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 with drug-free core
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Abstract
A coating composition is described for the film coating of pharmaceutical cores containing the drug, said composition comprising a suitable film forming material in combination with a high viscosity swellable polymer.
Description
FIELD OF THE INVENTION
The present invention relates to a kind ofly cover bitter effectively and the coated composition of the taste of good to eat medicine not.
The background of invention
Most prescriptions and nonprescription drugs are with tablet or capsule oral.But the age is in the patient at two ends, and for example child and old man usually are difficult to swallow these solid-state dosage forms.For these patients, medicine can be made chewable tablet or dispersible tablets or liquid dosage for example solution, emulsion and suspension.The medicament of these forms can make taste bud feel active constituents of medicine.When taking with the dosage form of these forms, some medicines are extremely bitter, and are therefore disagreeable to the taste.Thus, just need take measures to cover the taste of these medicines, to strengthen patient's compliance.
According to the literature, there are several technology to make liquid dosage good to eat.They comprise that use can feel the lower medicine parent difficulty soluble salt of degree of exposure in the oral cavity of form.The syrup that contains or do not contain flavoring agent usually is enough to cover the taste of medicine.But, the bitterness of part medicine clearly, to such an extent as to conventional method for example uses sweeting agent, aminoacid, flavouring agent and absorbent also not all right.If this medicine is widely used in treatment child or old man, this just especially is a problem.Therefore, just need a kind of method of research, can cover the taste of bitter medicine effectively.
US4808411 has described a kind of compositions of covering the medicine taste, and it contains erythromycin and derivant and carbomer.It is believed that amido and the gelling performance of the ion gravitation carbonyl of carbomer between and insoluble carbomer and the combination of drug-polymer coordination compound by erythromycin compounds.This has just formed the minimum dissolution of erythromycin complex in the non-ionic water medium, and medicine is enough emitted from coordination compound lentamente, to avoid obviously feeling in the oral cavity bitterness.At stomach-intestinal canal, ionic environment causes the release of erythromycin complex.Thus, by the availability of control free form medicine, just can cover the medicine taste.But this method only is suitable for covering the medicine that can form reversible coordination compound, has limited its application thus.
US4865851 has described the deoxycholic acid coordination compound of taste masking, and this drug particles has complete fat or fat blend coating, and described fat is water insoluble, and is used to cover the bitterness of deoxycholic acid when oral.But this coating significantly reduces dissolubility, and therefore, the bioavailability of deoxycholic acid suspension is remarkable lower than tablet form.
US5695784 has described the method for covering the bitter medicine taste, and wherein coated composition contains the quaternary ammonium compound of the cation copolymer of dimethylaminoethyl methacrylate and neutral methacrylate, neutral polymethyl methacrylate and/or ethyl ester compound, polymethylacrylic acid or ethyl cellulose and triethyl citrate and optional hydroxypropyl emthylcellulose.This coated composition need come taste masking effectively with number of polymers.
The general introduction of invention
The present invention relates to a kind of coated composition and be applied to the nuclear outside that medical compounds constitutes, cover the drug coating preparation of compositions method of medical compounds taste effectively.This nuclear mainly can contain primary medicine grain, granule, crystal, ball or or even the form such as the tablet of unit dose.This coating comprises film forming polymer of shape and high viscosity polymers capable of swelling, and also optional other suitable components that comprise coating comprise lubricant, plasticizer and agent delivery (channeling agent).
The compositions of film forming polymer and polymers capable of swelling has the performance of barrier in film, control is suitable for the initial drug release of taste masking, and can not compromise medicine in the release of conventional immediate release dosage form in specified time limit.For very bitter medicine, can adopt conventional coating polymer, on micronucleus, use high to 80% polymer.The so few polymer of the compositions enough 10-15% of energy of the present invention is equivalent to the used solid amount of 20-30%, just obtains the degree of same taste masking.Just can form the repeatability of uniform coating thickness, processing, rate of dissolution faster thus, can not sacrifice bioavailability simultaneously.It also makes processing cost suitable, and is simultaneously consuming time few.
Multiple polymers can both be used for forming film.The non-limitative example of these film forming polymers can be classified as acrylic polymer, cellulosic polymer or polyvinyl.Used acrylic polymer is to be the polymer of trade mark with Eudragit available from Rohm Pharma.Preferred acrylic polymer can be with the methacrylic acid copolymer of Eudragit L and the sale of Eudragit S trade mark and polyethyl acrylate-methyl methacrylate of selling with Eudragit NE trade mark.
The film former of useful cellulose membrane comprises alkylcellulose, for example methyl or ethyl cellulose and hydroxy alkyl cellulose (for example hydroxypropyl cellulose or hydroxypropyl emthylcellulose).The polymer that forms the alkylcellulose film comprises that Dow Chemicals is with trade mark Methocel E
TMWith the polymer of Surelease sale and the Aquacoat of FMC.The example that forms the polymer of vinyl film comprises polyvinyl acetate or polyvinyl acetate phthalic acid ester.The dry weight of the film forming polymer that uses reaches as high as 30% of the nuclear weight of wanting taste masking.
Can be used for comprising carbopol, high viscosity glue, carrageenin, high viscosity polyvinyl or high-viscosity cellulose polymer, for example Methocel with the polymers capable of swelling of film forming polymer combination
TMK series polymer (trade mark Dow Chmeical).The content of polymers capable of swelling can be the 0.1-20% of film forming polymer dry weight.
Described coated composition can be chosen wantonly and comprise acceptable excipient on the pharmacology that is conventionally used as agent delivery, for example starch, lactose or (PEG) Polyethylene Glycol.The content of this agent delivery can be up to 100% of film forming polymer dry weight, and is preferred 60%, or more preferably up to 30%.
Described coated composition also contains lubricant, and it is as caking inhibiter (for example Pulvis Talci, silicon dioxide colloid and magnesium stearate) and pharmaceutically acceptable plasticizer (for example triethyl citrate, Polyethylene Glycol, glyceryl monostearate, glyceryl triacetate, triethyl group citric acid acetas, triethyl citrate, dibutyl phthalate and dibutyl sebacate).The content of lubricant can be up to 200% of film forming polymer dry weight, more preferably up to 100% of film forming polymer dry weight.The content of plasticizer can be up to 40% of film forming polymer dry weight.The formulation that is wrapped can be chosen wantonly and at high temperature finish processed.
Polymer total amount in the coating is up to 30% of medicine nuclear weight, or preferably more, and 10% of medicine nuclear weight just is enough to cover the bitterness of highly water soluble drugs.
By the present composition obtain want taste masking be wrapped granule can with food or beverage blends, can be used for preparing oral liquid suspension, but but maybe can be mixed with routine oral full wafer chewable tablet or dispersible tablet.In making tablet or liquid suspension process, can use well-known pharmaceutically acceptable composition in the conventional industry.For being used for suspension, particle mean size is preferably less than 50 orders (297 microns).Described medicine can be chosen wantonly and at first be mixed with ball, sheet or capsule, can wrap up then, with taste masking.
The following examples further specify the present invention, but do not limit the scope of the invention.
Detailed description of the invention
Embodiment 1
Table 1.1 shows the coated composition of the taste that is used for covering multiple medicine nuclear:
Table 1.1
| Composition | Use amount (g) | Dry weight (g) |
| Eudragit?L30D | ????333.33 | ????100.0 |
| Carbomer (Aqueous Carbopol 971P dispersion liquid 1%w/w) | ????200.0 | ????2.0 |
| Pulvis Talci USP (Pulvis Talci aqueous dispersions 30%w/w) | ????40.80 | ????102.0 |
| Polyethylene Glycol USNF (PEG1500) | ????15.3 | ????15.3 |
| Purified water USP peak | ????1000.00 | ????- |
In order to prepare coating solution, stir in following 30 minutes talcous aqueous dispersions (30%w/w) is joined in the aqueous dispersions of 1%w/w carbopol.At last, stirring adds carbopol-Pulvis Talci dispersion liquid in plastifying (using PEG1500) Eudragit dispersion in 30-40 minute down.
The step of preparation nuclear particle:
Table 1.2
| Composition | Use amount (g) |
| Norfloxacin USP | ????260.0 |
| Microcrystalline Cellulose USNF (Avicl PH102) | ????88.0 |
| Pregelatinized starch USNF (starch 1500) | ????10.0 |
| Povidone USP (PVP K-30) | ????30.0 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????2.0 |
| Magnesium stearate USNF | ????0.75 |
Sift out the component (except Aerosil 200) of weighing from British Standard Sieve (BSS) #44, and in double cone mixer, mixed 10 minutes, add Aerosil 200 (down) then, remix 2 minutes from the BSS#60 sieve.Then, water is the mixture granulating, and in the tray exsiccator 60 ℃ of dryings 24 hours.The particle that obtains is sieved, obtain (BSS) #44/#85 part.
With the lubricated granule (150g) that forms of 0.5% magnesium stearate, and adopt Wurster coating machine (available from the Glatt GPCG-1 of German Glatt GmbH), with the coating solution spraying of preparation.The polymer total amount of the coating that uses is 12.0% of nuclear weight, and the solid amount that uses is 26% of nuclear weight.Only 12% coating polymer total amount just is enough to cover the bitterness of norfloxacin, provides the required best stripping of formulation (table 1.3) that discharges at once simultaneously.
Table 1.3
| Time (minute) | The medicine percentage rate USP pH of buffer 4.0 that discharges; 50rpm; 900ml | |
| Coating not | Coating | |
| ????5 | ????63.80 | ????2.30 |
| ????10 | ????95.73 | ????19.40 |
| ????15 | ????106.40 | ????38.30 |
| ????20 | ????- | ????54.23 |
| ????25 | ????- | ????66.37 |
| ????30 | ????- | ????82.17 |
Embodiment 2
In this embodiment, with the ibuprofen granulating, and as described below coating with taste masking.
Table 2.1
| Composition | Use amount (g) |
| Ibuprofen USP | ????260.0 |
| Microcrystalline Cellulose (Avicel PH102) | ????88.0 |
| Pregelatinized starch USNF (starch 1500) | ????10.0 |
| Povidone USP (PVP K-30) | ????30.0 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????2.0 |
| Magnesium stearate USNF | ????0.75 |
Sift out ibuprofen, Avicel 102, starch 1500 and the PVP K-30 of weighing from BSS#44, and in double cone mixer, mixed 10 minutes.Sieve Aerosil 200 down from BSS#60, and add in the interior mixture of double cone mixer remix 2 minutes.Water is the mixture granulating, and in the tray exsiccator 60 ℃ of dryings 4 hours.After BSS#44 and BSS#85 sieve, with the lubricated #44/85 part of magnesium stearate (0.75g) (150gm).Dry with the coating solution spraying of the described preparation of embodiment 1 (table 1.1) and lubricated granule (150.0g).The coating polymer (solid amount of use is 13%) that only accounts for nuclear weight 6% just is enough to cover the bitterness of ibuprofen.When coated granules stops 1.2 minutes in mouth, do not have any bitterness.This coating can the appreciable impact ibuprofen dissolubility, shown in table 2.2.
Table 2.2
| Time (minute) | The medicine percentage rate phosphate buffer pH7.2 that discharges; 150rpm; 900ml | |
| Coating not | Coating | |
| ????5 | ????54.30 | ????46.27 |
| ????10 | ????85.63 | ????76.03 |
| ????15 | ????94.06 | ????88.97 |
| ????20 | ????97.00 | ????93.37 |
| ????25 | ????97.40 | ????93.00 |
| ????30 | ????97.90 | ????94.70 |
Embodiment 3
Table 3.1
| Composition | Use amount (g) |
| Etodolac BP | ????200.0 |
| Microcrystalline Cellulose USNF (Avicel PH102) | ????148.0 |
| Pregelatinized starch USNF (starch 1500) | ????10.0 |
| Povidone USP (PVP K-30) | ????30.0 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????2.0 |
| Magnesium stearate USNF | ????0.75 |
Etodolac, Avicel PH102, starch 1500 and PVP K-30 mix in double cone mixer.The Aerosil 200 that sifts out from BSS#60 adds the mixture, mixes 2 minutes.Water is the mixture granulating, and 60 ℃ of dryings 4 hours.The dry material of crossing of sieve obtains the BSS#44/85 part, and lubricated with magnesium stearate (0.75g).Dry with the coating solution spraying of the described preparation of embodiment 1 (table 1.1) and lubricated granule (150.0g).The coating polymer total amount that only accounts for nuclear weight 12% just is enough to cover the bitterness of medicine.The solid amount that uses is 26%.Coated granules has the optimal dissolution degree, shown in table 3.2.
Table 3.2
| Time (minute) | The medicine percentage rate phosphate buffer pH7.5 that discharges; 100rpm; 900ml | |
| Coating not | Coating | |
| ????5 | ????86.60 | ????29.70 |
| ????10 | ????91.37 | ????73.10 |
| ????15 | ????93.43 | ????88.00 |
| ????20 | ????94.00 | ????92.80 |
| ????25 | ????-- | ????94.40 |
| ????30 | ????-- | ????94.90 |
Embodiment 4
Table 4.1
| Composition | Use amount (g) |
| Acetaminophen USP | ????260.0 |
| Microcrystalline Cellulose USNF (Avicel PH102) | ????88.0 |
| Pregelatinized starch USNF (starch 1500) | ????10.0 |
| Povidone USP (PVP K-30) | ????30.0 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????2.0 |
| Magnesium stearate USNF peak | ????0.75 |
Acetaminophen, Avicel PH102, starch 1500 and PVP K-30 mix in double cone mixer.Sift out Aerosil 200 from BSS#60, and mixed 2 minutes.Water is the mixture granulating, and 60 ℃ dry 4-5 hour.With the lubricated 150g drying nest (BSS#44/85) of magnesium stearate (0.75g).Dry with the coating solution spraying of the described preparation of embodiment 1 (table 1.1) and lubricated granule (150g).Polymer total amount and the amount of solid used account for 8% and 17.5% of nuclear weight respectively, and this is enough to cover the bitterness of medicine, and does not influence dissolubility (table 4.2).
Table 4.2
| Time (minute) | The medicine percentage rate phosphate buffer pH5.8 that discharges; 50rpm; 900ml | |
| Coating not | Coating | |
| ????5 | ????76.10 | ????61.90 |
| ????10 | ????96.30 | ????86.60 |
| ????15 | ????96.90 | ????92.60 |
| ????20 | ????97.00 | ????94.10 |
| ????25 | ????97.40 | ????94.40 |
| ????30 | ????-- | ????94.90 |
Embodiment 5
| Composition | Use amount (g) |
| Cirramycin hydrochlorate USP (being equivalent to 200g cirramycin USP) | ????239.0 |
| Hydroxypropyl cellulose USNF (HPC-L) | ????11.2 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????0.75 |
| Microcrystalline Cellulose USNF (Celphere ) | ????100.0 |
| Pulvis Talci USP (Pulvis Talci aqueous liquid dispersion 30%w/w) | ????14.0 |
| Purified water USP peak | ????670.0 |
HPC-L is dissolved in the water, adds cirramycin hydrochlorate and Pulvis Talci then under the vigorous stirring, prepare dispersion liquid.Make the suspension homogenization reach 30 minutes, sieve and cover the 100g particle mean size be on 170 microns the microcrystalline cellulose spheres (Celphere , FMC Corp., USA).
Cambial step: Celphere pearl (100g) is added in the processing cavity of Wurster coating machine (available from the Glatt GPCG-1 of German GlattGmbH), and spray the drug suspension for preparing from the bottom with 5-9g/min speed.After spray finished, drying was loaded with the nuclear of medicine.
With the dry nuclear of crossing of the lubricated 150g of 0.75g Aerosil (going out) from the BSS#60 mesh sieve, and with the described coating solution spraying for preparing of following table 5.2.
Table 5.2
| Composition | Use amount (g) | Dry weight (g) |
| Eudragit?L30D | ????66.67 | ????20.0 |
| Carbomer (Carbopol 971P aqueous dispersions 1%w/w) | ????40.0 | ????0.40 |
| Polyethylene Glycol USNF (PEG 1500) | ????3.06 | ????3.06 |
| Lactose monohydrate USNF | ????2.04 | ????2.04 |
| Pulvis Talci USP (Pulvis Talci aqueous dispersions 40%w/w) | ????51.0 | ????20.4 |
| Purified water USP peak | ????200.0 | ????-- |
The polymer total amount of the coating that uses is 11.90% of nuclear weight, and the solid amount that uses is 27% of nuclear weight.Can cover the bitterness of cirramycin with the coating that applies, not influence dissolubility, shown in table 5.3.
Table 5.3
| Time (minute) | The medicine percentage rate 0.1N HCl that discharges; 75rpm; 900ml; USP instrument-2 | |
| Coating not | Coating | |
| ????5 | ????87.0 | ????7.20 |
| ????10 | ????97.8 | ????27.2 |
| ????15 | ????100.7 | ????46.3 |
| ????20 | ????- | ????62.90 |
| ????25 | ????- | ????76.0 |
| ????30 | ????- | ????85.1 |
Embodiment 6
Table 6.1 has been described another kind of coated composition, and it contains film forming polymer (ethyl cellulose) and polymers capable of swelling (carbopol).
Table 6.1
| Composition | Use amount (g) | Dry weight (g) |
| Ethyl cellulose aqueous dispersions USNF (Aquacoat ECD-30) | ????100.0 | ????30.0 |
| Carbomer (Carbopol 971P aqueous dispersions 1%w/w) | ????60.0 | ????0.60 |
| Triethyl citrate USNF | ????6.0 | ????-- |
| Pulvis Talci USP (Pulvis Talci aqueous dispersions 30%w/w) | ????30.0 | ????9.0 |
| Purified water USP peak | ????200.0 | ????-- |
In order to prepare coating solution, under agitation in 30 minutes, Pulvis Talci aqueous dispersions (30%w/w) is joined in the aqueous dispersions of 1% carbopol.At last, stir down in 30-40 minute, carbopol-Pulvis Talci dispersion liquid is added in the ethylcellulose dispersion of (triethyl citrate) of plasticising.
The prescription of use shown in table 6.2, preparation contains the nuclear of acetaminophen.
Table 6.2
| Composition | Use amount (g) |
| Acetaminophen USP | ????260.0 |
| Povidone USP (PVP K-30) | ????28.0 |
| Lactose monohydrate USNF | ????18.0 |
| Microcrystalline Cellulose USNF (Avicel PH101) | ????90.0 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????4.0 |
| Amount to | ????400.0 |
Acetaminophen, PVP K-30, lactose and Avicel PH101 mixed in double cone mixer 10 minutes.Then, water is they corning, and 60 ℃ of dryings are 4 hours in the tray exsiccator, and sieves and obtain BSS part #30/85.The granule that obtains like this is lubricated with Aerosil 200, and adopts Wurster coating machine (the Glatt GPCG-1 of German GmbH) the coating solution spraying that makes.The polymer total amount of the coating that uses is 12% of nuclear weight.This coating can be covered the stimulation taste of acetaminophen effectively, also provides desired dissolution and distributes, shown in table 6.3.
Table 6.3
| Time (minute) | The medicine percentage rate phosphate buffer pH5.8 that discharges; 50rpm; 900ml | |
| Coating not | Coating | |
| ????5 | ????90.1 | ????23.7 |
| ????10 | ????97.7 | ????62.4 |
| ????15 | ????97.9 | ????88.0 |
| ????20 | ????98.1 | ????98.2 |
| ????25 | ????98.3 | ????98.9 |
| ????30 | ????-98.4 | ????99.3 |
Embodiment 7
Embodiment relates to and coated composition identical shown in the table 6.1, and wherein ethyl cellulose and carbopol were with 100: 2 mixed.The drug particles that coating is crossed is made of cirramycin alkali, and its component is shown in table 7.1.
Table 7.1
| Composition | Use amount (g) |
| Cirramycin USP | ????50.0 |
| Lactose monohydrate USNF | ????3.5 |
| Povidone USP (PVP K-30) | ????5.5 |
| Microcrystalline Cellulose USNF (Avicel PH101) | ????17.5 |
| Silicon dioxide colloid USNF (Aerosil 200) | ????00.75 |
| Amount to | ????77.25 |
Cirramycin, lactose, Avicel PH101 and the PVP K-30 of weighing are sifted out from BSS#44, and in the double cone blender, do and mix.With granulating mixture, form the cohesive material with enough water.This wet stock is at tray exsiccator inner drying, and sifts out from BSS#30, stays on the BSS#85.With the lubricated dry material of crossing of the Aerosil that sifts out (sifting out from BSS#60), the Glatt GPCG-1 Wurster that packs into then is with ethyl cellulose-carbopol solution (shown in table 6.1) coating.
15% (solid amount of use is 34.35%) that the polymer total amount of using accounts for nuclear weight just is enough to cover the bitterness of cirramycin, and can obviously do not influence dissolution.
Table 7.2 shows and adopts USP instrument-2 coating to cross and not coated granule distribution of the dissolution in 900ml 0.1N hydrochloric acid under 75rpm.
Table 7.2
| Time (minute) | The medicine percentage rate 0.1NHCl that discharges; 75rpm; 900ml; USP instrument-II | |
| Coating not | Coating | |
| ????5 | ????83.3 | ????12.8 |
| ????10 | ????97.7 | ????31.7 |
| ????15 | ????97.8 | ????58.7 |
| ????20 | ????98.1 | ????70.8 |
| ????25 | ????- | ????82.6 |
| ????30 | ????- | ????95.2 |
Though described the present invention according to the specific embodiment, the those of ordinary skill in the industry can be understood some change and equivalent, and described change and equivalent all are in the scope of the present invention.
Claims (18)
1. the coated composition of the coating membrane of a medicine nuclear that is used to contain medicine, described compositions contains suitable film forming matter and high viscosity polymers capable of swelling and optional other are applicable to the mixture of the component of coating, and described other components comprise lubricant, plasticizer and agent delivery.
2. compositions as claimed in claim 1, wherein said film forming matter contain methacrylic acid copolymer, polymethacrylates-methylmethacrylate copolymer, alkylcellulose or their mixture.
3. compositions as claimed in claim 2, the dry weight of wherein used film forming polymer is up to 30% of nuclear weight.
4. compositions as claimed in claim 1, wherein said high viscosity polymers capable of swelling comprise carbopol, carrageenin, polyvinyl alcohol, cellulosic polymer or other suitable high viscosity glue.
5. compositions as claimed in claim 4, the content of wherein said polymers capable of swelling accounts for the 0.1-20%w/w of film forming polymer dry weight.
6. compositions as claimed in claim 4, wherein said high viscosity polymers capable of swelling is a carbopol.
7. compositions as claimed in claim 1, wherein said agent delivery comprise or are selected from lactose, starch, Pulvis Talci and composition thereof.
8. compositions as claimed in claim 7, the content of wherein said agent delivery is up to 100% of the polymer dry weight.
9. compositions as claimed in claim 8, the content of wherein said agent delivery is up to 60% of the polymer dry weight.
10. compositions as claimed in claim 9, the content of wherein said agent delivery is up to 30% of the polymer dry weight.
11. compositions as claimed in claim 1 wherein has lubricant, and is selected from Pulvis Talci, glyceryl monostearate, magnesium stearate, silicon oxide colloid and composition thereof.
12. compositions as claimed in claim 11, the content of wherein said lubricant is up to 200% of the film forming polymer dry weight.
13. compositions as claimed in claim 12, the content of wherein said lubricant is up to 100% of the film forming polymer dry weight.
14. compositions as claimed in claim 1, wherein said plasticizer joins in the film, and is selected from Polyethylene Glycol, acetylated monoglyceride, glyceryl monostearate, glyceryl triacetate, triethyl group citric acid acetas, triethyl citrate, dibutyl phthalate, dibutyl sebacate and composition thereof.
15. compositions as claimed in claim 14, the content of wherein said plasticizer is up to 40% of the film forming polymer dry weight.
16. compositions as claimed in claim 15, wherein said plasticizer are Polyethylene Glycol (PEG).
17. compositions as claimed in claim 1, the polymer dry weight that it contains accounts for the 0.5-30% of nuclear weight.
18. compositions as claimed in claim 14, but wherein said coated granule be mixed with dust, dry powder, liquitabs, suspension, emulsion or full wafer can be chewed or dispersible tablet or any other suitable peroral dosage form.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN454/DEL/99 | 1999-03-19 | ||
| IN454DE1999 IN191482B (en) | 1999-03-19 | 1999-03-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1615121A true CN1615121A (en) | 2005-05-11 |
Family
ID=11089863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA998165883A Pending CN1615121A (en) | 1999-03-19 | 1999-10-26 | Taste masking coating compositions |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1235556A4 (en) |
| CN (1) | CN1615121A (en) |
| AU (1) | AU6224699A (en) |
| BR (1) | BR9917219A (en) |
| IN (1) | IN191482B (en) |
| WO (1) | WO2000056266A2 (en) |
| ZA (1) | ZA200007724B (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN191239B (en) | 1999-06-11 | 2003-10-11 | Ranbaxy Lab Ltd | |
| DE19961897A1 (en) * | 1999-12-20 | 2001-06-28 | Basf Ag | Use of a film coating as a taste masking coating of pharmaceutical dosage forms |
| DK1411899T3 (en) * | 2001-08-01 | 2009-06-02 | Novartis Ag | Taste-masking composition |
| SI1476138T1 (en) | 2002-02-21 | 2012-07-31 | Valeant Internat Barbados Srl | Modified release formulations of at least one form of tramadol |
| US8323692B2 (en) | 2002-02-21 | 2012-12-04 | Valeant International Bermuda | Controlled release dosage forms |
| US20060233873A1 (en) * | 2003-01-24 | 2006-10-19 | Julien Meissonnier | Dispersion of taste masked crystals or granules of active substances, chewable soft capsules filled with said dispersion, and process for preparing same |
| US8889184B2 (en) * | 2006-09-07 | 2014-11-18 | Losan Pharma Gmbh | Particulate form of a pharmaceutical composition which is easy to swallow |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4321253A (en) * | 1980-08-22 | 1982-03-23 | Beatty Morgan L | Suspension of microencapsulated bacampicillin acid addition salt for oral, especially pediatric, administration |
| CH666405A5 (en) * | 1985-06-24 | 1988-07-29 | Ciba Geigy Ag | SOLID, DURABLE PHARMACEUTICAL FORMS WITH ELASTIC FILM COVER. |
| US4851226A (en) * | 1987-11-16 | 1989-07-25 | Mcneil Consumer Products Company | Chewable medicament tablet containing means for taste masking |
| IT1227899B (en) * | 1988-12-23 | 1991-05-14 | Poli Ind Chimica Spa | TOTAL OR PARTIAL COATING OF PHARMACEUTICAL ACTIVE SUBSTANCES AND RELATED COMPOSITIONS |
| US5527545A (en) * | 1989-09-18 | 1996-06-18 | Recordati S.A. Chemical And Pharmaceutical Company | Liquid-suspension controlled-release pharmaceutical composition |
| KR100193933B1 (en) * | 1990-07-20 | 1999-06-15 | 에밀리오 캠포레시, 존 페르구손 | Water-soluble complexes of bismuth and polyacrylates, preparation methods thereof, and pharmaceutical compositions for treating ulcerative colitis containing the complexes or other bismuth salts |
| IT1250421B (en) * | 1991-05-30 | 1995-04-07 | Recordati Chem Pharm | CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION WITH BIO-ADHESIVE PROPERTIES. |
| US5958459A (en) * | 1991-12-24 | 1999-09-28 | Purdue Pharma L.P. | Opioid formulations having extended controlled released |
| CA2137265C (en) * | 1992-06-04 | 2003-10-28 | Sanjay Bhardwaj | Palatable pharmaceutical compositions |
| DE19709532A1 (en) * | 1997-03-10 | 1998-09-17 | Basf Ag | Use of redispersible polymer powders or polymer granules for coating pharmaceutical or agrochemical dosage forms |
-
1999
- 1999-03-19 IN IN454DE1999 patent/IN191482B/en unknown
- 1999-10-26 EP EP99949283A patent/EP1235556A4/en not_active Withdrawn
- 1999-10-26 WO PCT/IB1999/001735 patent/WO2000056266A2/en not_active Application Discontinuation
- 1999-10-26 AU AU62246/99A patent/AU6224699A/en not_active Abandoned
- 1999-10-26 BR BR9917219-4A patent/BR9917219A/en not_active Application Discontinuation
- 1999-10-26 CN CNA998165883A patent/CN1615121A/en active Pending
-
2001
- 2001-09-19 ZA ZA200007724A patent/ZA200007724B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2000056266A3 (en) | 2002-07-04 |
| ZA200007724B (en) | 2002-06-12 |
| EP1235556A4 (en) | 2003-07-16 |
| BR9917219A (en) | 2002-04-23 |
| EP1235556A2 (en) | 2002-09-04 |
| IN191482B (en) | 2003-12-06 |
| WO2000056266A2 (en) | 2000-09-28 |
| AU6224699A (en) | 2000-10-09 |
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| C06 | Publication | ||
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| 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 |