CN1771961A - Oral Geftinat prepn - Google Patents
Oral Geftinat prepn Download PDFInfo
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- CN1771961A CN1771961A CN 200410094557 CN200410094557A CN1771961A CN 1771961 A CN1771961 A CN 1771961A CN 200410094557 CN200410094557 CN 200410094557 CN 200410094557 A CN200410094557 A CN 200410094557A CN 1771961 A CN1771961 A CN 1771961A
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Abstract
The present invention is oral Geftinat preparation. The oral Geftinat preparation has Geftinat as active component and pharmaceutically acceptable carrier. It is prepared through proper preparation into oral tablet, dispersive tablet, film coated tablet, sublingual tablet, oral disintegrated tablet, etc.
Description
Technical field
Oral Geftinat preparation of the present invention, the said preparation oral formulations that to be active component with the gefitinib make with suitable preparation technology; Said preparation also can comprise the medicine acceptable carrier in forming.
Technical background
U.S. tumour medicine consultative committee (ODAC) recommends to list gefitinib in quick approval plan to FDA (Food and Drug Adminstration) (FDA), this plan is that promising medicine of approval or method can be received treatment the patient who suffers from the threat to life disease early, according to this plan, a kind of medicine can promptly go through to be applied to clinical under the situation that all clinical trials are not finished as yet fully, but need be based upon the patient good therapeutic response occurs and in advance on the basis in respect of clinical effectiveness preferably, needs further to confirm clinical effectiveness and assessment long-term safety after the approval.FDA has ratified the clinical treatment that is used for nonsmall-cell lung cancer in latter stage at end of gefitinib in May, 2003.So far, gefitinib has been applied to the treatment of nonsmall-cell lung cancer in late period by the approval of states such as the U.S., Australia, Japan, Argentina, Singapore and Korea S.The oncology of Astrazeneca AB medical science chief inspector doctor GeorgeBlackledge says: " gefitinib is 80; 000 optional patients with advanced NSCLC of no therapeutic scheme has been brought hope; these clinical datas will encourage Astrazeneca AB to continue the biochemistry and the molecules research of medicine; to reach the optimum therapeutic response of gefitinib, improve patient's treatment.”
Gefitinib (Gefitinib, ZD1839, trade name: Iressa, IressaTM) molecular weight is low, be a kind of synthetic aniline quinazoline [4-(3-chloro-4-fluoroaniline)-7-methoxyl group-6 (the inferior propoxyl group of 3-isomery) quinazoline], selectivity suppresses the epidermal growth factor recipient tyrosine kinase activity.Be applicable to and treat local late period or the transitivity nonsmall-cell lung cancer (NSCLC) of previously accepting chemotherapy or being unsuitable for chemotherapy.Gefitinib is a kind of selectivity EGF-R ELISA (EGFR) tyrosine kinase inhibitor, and this enzyme is expressed in the solid tumor of epithelial origin usually.Inhibition for the EGFR tyrosine kinase activity can hinder growth of tumor, shifts and angiogenesis, and increases the apoptosis of tumor cell.In vivo, gefitinib extensively suppresses the tumor growth that xenotransplantation is derived and is in the human tumor cells of nude mice, and improves the anti-tumor activity of chemotherapy, radiotherapy and hormone therapy.In clinical experiment, confirmed the symptom of gefitinib to local late period or transitivity nonsmall-cell lung cancer tool objective antitumor reaction also can improvement disease association.Behind the PK (pharmacokinetic) profile intravenously administrable, gefitinib is cleaned up rapidly, and is widely distributed, and on average removing the half-life is 48 hours.Behind cancer patient's oral administration, absorb slowlyer, average t1/2 is that administration every day of 41 hours gefitinibs 2-8 occurs 1 time and doubly accumulates, and reaches stable state after 7-10 days administration.Medication at interval in 24 hours, the circulating plasma drug level generally maintains between 2-3 times.The outer data of metabolism body shows that the P450 isozyme that participates in the gefitinib oxidative metabolism has only CYP3A4.In vitro study shows the inhibition CYP2D6 enzyme that gefitinib may be limited.In a clinical trial, gefitinib and metoprolol (metoprolol, a kind of CYP2D6 zymolyte) share the effect that makes this group a spot of increasing (35%), and its actual clinical meaning is not estimated as yet.Gefitinib does not show enzyme induction in zoopery, and other cytochrome P 450 enzymes is not had remarkable inhibitory action (external) yet.The site of three biotransformations is determined in the metabolism of gefitinib: the metabolism of N-propyl group morpholine class, the oxidation defluorination of substituent demethylation of methoxy and benzene halide base class on the quinazoline.The major metabolite that is separated in human plasma is the O-desmethyl gefitinib.It to the inhibitory action of EGFR stimulating cellular growth than gefitinib a little less than 14 times, therefore the clinical activity of gefitinib is not had obvious effect.The total blood plasma of removing gefitinib is cleaned up and is about 500mL/min.Main by defecate, about 4% by the form removing of kidney with prototype and metabolite.Special population: according to crowd's medication data, not finding has dependency between steady plasma-drug concentration and patient's age, body weight, sex, race or the inosine clearance rate.One comprises 41 routine entity tumors with hepatic metastases, and liver function is normal, gefitinib is estimated in the patient's of moderate or severe infringement the clinical research.Studies show that, behind the oral gefitinib dosage every day 250mg, reach stable state time, total plasma clearance and stable state drug exposure level (Cmaxss, AUC24ss) similar with moderate infringement group result in the liver function normal group.Routine from 4 because the Notes of Key Data stable state drug exposure level that the patient of the serious hepatic insufficiency that the liver transfer causes obtains is also similar to the liver function normal patient.Not in the liver function injury patient that liver cirrhosis or hepatitis cause to studying.The clinical preceding security document gefitinib relevant with the prescriber do not show the genotoxicity tendency.Be consistent with the pharmacological activity of gefitinib, when dosage was given to 20mg/kg/ days, lowered the fertility that can be observed Mus.Fetal development to Mus when device palace generation period giving high dose (30mg/kg/ days) does not have influence, but for rabbit, and 20mg/kg/ days and above dosage then can alleviate the weight of fetus.Between two species, all do not induce deformity.The dosage that awards 20mg/kg/ days at gestation and the farrowing interval of Mus can reduce the existence (seeing that gestation and suckling save) of young Mus.Divide the gefitinib of puerperium continuous 14 days oral carbon 14 labellings Mus, the concentration of radioactivity is higher than the concentration (seeing that gestation and suckling save) in the blood in the milk.Non-clinical (external) research data shows that gefitinib has and suppresses the cardiomotility process of repolarization probability of (as the QT interval).Its clinical meaning is not still known.The carcinogenic research of gefitinib is not carried out as yet.Gefitinib can be postponed the breast carcinoma zoopery of modern 2004 03 phases of combination of Chinese and Western medicine magazine U.S. of falling ill and be shown that a kind of lung cancer drugs gefitinib that is used for the treatment of can play preventive and therapeutic effect to breast carcinoma.According to the U.S. " national ICR magazine ", the research worker of U.S. Beile medical university at first uses gene technology to turn out the experimental mouse that easily suffers from breast cancer, and allows the experimental group mouse take gefitinib then, and the matched group mouse is only taken placebo.As a result, the matched group mouse has and can postpone breast carcinoma morbidity.Gefitinib (Gefitinib) shifts the brain of nonsmall-cell lung cancer has 2004 04 phase Cai Junming of curative effect China's pulmonary carcinoma magazine, the clear magnificent comparative analysis gefitinib in mound to different physical performance, previously different chemotherapy number of times, have or do not have the nonsmall-cell lung cancer patient's of brain metastatic lesion therapeutic outcome.Method always has 76 routine patients and participates in test.The disease of patient control rate is 63.2% (95%CI is 52.1%～74.3%) as a result, the median of no disease progression life cycle is 5.0 months (95%CI is 3.5～6.6 months), and the median of whole life cycle is 9.9 months (95%CI is 4.9～14.8 months).Wherein having the 57 routine patient's objective response raties that can measure focus is 33.3% (95%CI is 20.7%～46.0%).Have 21 routine patients to have appreciable intracranial and the outer focus of cranium simultaneously among the 76 routine patients, wherein 17 examples (81.0%) have identical intracranial and the outer tumor response of cranium to gefitinib, do not influence survival time of patients and the brain transfer occurs.Preliminary report China pulmonary carcinoma 2004 04 phases of magazine Jiang state of the nonsmall-cell lung cancer of failing behind gefitinib (Iressa) treatment operation, radiotherapy, the chemotherapeutic treatment, Hong Xiaonan treats intractable nonsmall-cell lung cancer (NSCLC) patient's initial experience with gefitinib (Iressa).Method 55 routine intractable NSCLC enter research, are the case of modern oncotherapy means treatment back failure such as operation, radiotherapy, chemotherapy.Wherein the tumor of 5 examples is confined in the thoracic cavity, and 50 examples have had metastasis.Iressa dosage is 250mg/ time, and is oral, every day 1 time.The middle bit time that full group is taken medicine is 4 months.The main toxic and side effects of result is an erythra, betides 26 routine patients, account for complete group 47%.Other side effect has diarrhoea 4 examples (7%), 4 examples (7%) of feeling sick, stomatocace, alopecia, each 1 example (2%) of gastrorrhagia.Above-mentioned toxic and side effects is all not serious, and the patient all can tolerate.Gefitinib (Iressa) the treatment recurrent nonsmall-cell lung cancer Liu Lun rising sun, Lee is 2004 04 phase gefitinibs (Iressa) of people China pulmonary carcinoma magazine treatment recurrent nonsmall-cell lung cancer patient's clinical efficacy.Method 29 examples enter this research through the nonsmall-cell lung cancer of chemicotherapy treatment failure, and wherein 3 routine tumors are confined in the thoracic cavity, the existing metastasis of 26 examples.Iressa dosage is 250mg/ time, and is oral, every day 1 time.The middle bit time that full group is taken medicine is 5 months.The main toxic and side effects of result is an erythra, has 12 examples erythra take place, account for complete group 41.4%.Other side effect has diarrhoea 2 examples, bradycardia 1 example, transaminase's 1 example that raises.Obtain after the treatment and alleviate 1 example fully, part is alleviated 7 examples, stablizes 12 examples, makes progress 9 examples.Full group effective percentage is 27.59%, and disease control rate is 68.97%.
Summary of the invention
The oral ordinary tablet that oral Geftinat preparation of the present invention is active component with the gefitinib to be made with suitable preparation technology, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.; Said preparation also can comprise the medicine acceptable carrier in forming.
The preparation technology of oral Geftinat preparation of the present invention: gefitinib is added suitable adjuvant uniform mixing, the disk that forms by preparation technique compacting or the solid preparation of special-shaped sheet can be made oral ordinary tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet etc.
The preparation technology of oral Geftinat preparation of the present invention: gefitinib is added suitable adjuvant such as diluent, fluidizer, disintegrating agent etc. make uniform powder or grain packing in Capsules, can make hard capsule.
The preparation technology of invention oral Geftinat preparation: with one or more gefitinib sustained-releases, rapid release, controlled release piller, filling or mixing back filling can be made slow release, rapid release, controlled release capsule in Capsules separately.
Adjuvant in the pharmaceutical preparation of the present invention has filler, binding agent, surfactant, wetting agent, wetting agent, disintegrating agent helps and collapses agent, suspending agent, fluidizer, lubricant, correctives, absorbent, suspensoid, coating material, coating material, coating material, slow-release material, rapid release material, controlled-release material or the like.
Filler in the pharmaceutical preparation of the present invention includes but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium carbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose etc.
Binding agent in the pharmaceutical preparation of the present invention includes but not limited to starch, pregelatinized Starch, gelatin, dextrin, maltose dextrin, sucrose, arabic gum, polyvinylpyrrolidone, various viscosity methylcellulose, low viscosity carboxymethyl cellulose, various viscosity ethyl cellulose, various viscosity polyvinyl alcohol, polyethylene glycol 6000, the following hydroxypropyl emthylcellulose of 50MPAS etc.
Disintegrating agent in the pharmaceutical preparation of the present invention includes but not limited to starch, pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure lignocellulose, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, ion exchange resin, methylcellulose, sodium carboxymethyl cellulose etc.
Lubricant in the pharmaceutical preparation of the present invention includes but not limited to magnesium stearate, calcium stearate, zinc stearate, Pulvis Talci, glyceryl monostearate, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, triacetyl glycerine, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium chloride, sodium laurylsulfate, magnesium laurylsulfate etc.
Surfactant in the pharmaceutical preparation of the present invention comprises but is not limited to sodium lauryl sulphate, smelting Luo Shamu, Tween 80, bromination hexadecane trimethylamine, sodium laurylsulfate, stearyl alcohol sodium sulfonate, polyoxyethylene high fatty alcohol, sucrose ester, sorbitol fatty ester, soybean phospholipid etc.
Correctives in the pharmaceutical preparation of the present invention includes but not limited to steviosin, fructose, glucose, high fructose syrup, Mel, aspartame, protein sugar, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, phyllodulcin, Sodium Cyclamate, flavoring banana essence, flavoring pineapple essence, Fructus Citri tangerinae essence, Herba Menthae essence, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence, rose essence etc.
The adjuvant material that pharmaceutical preparation of the present invention is used can be any material that can play slow releasing function.These coating materials include but not limited to cellulose and derivatives class thereof, crylic acid resin, ethene polymers etc.
The used coating material of pharmaceutical preparation of the present invention includes but not limited to gelatin, arabic gum, carboxymethyl cellulose, polyvinyl alcohol, polyacrylic acid, hydroxyethyl-cellulose, polylactic acid, ethyl cellulose, polyethylene, polyamide, stearic acid, celluloid, tristerin, Lac, Cellulose Acetate Phthalate.
Used slow release, rapid release, the controlled release matrix material of pharmaceutical preparation of the present invention includes but not limited to that Brazil wax, castor oil hydrogenated, Semen Ricini are cured, hydrogenated soya phosphatide, Lac, gelatin, sodium alginate, chitosan, amylopectin, agar, carrageenin, guar gum, cellulose derivative, crylic acid resin, polyethylene kind, macromolecular material etc.
Oral formulations of the present invention with gefitinib as active constituents of medicine, their content can be the 1--99% of preparation total amount, other composition is medicine acceptable auxiliary or slow-release material, and the content of these medicine acceptable auxiliary or slow-release material can be the 1--99% of preparation total amount.
For each medicament, as each sheet or each capsules, the effective dose of its active constituents of medicine can be 1-1000mg, wherein, gefitinib can be 5-800mg, and preferred gefitinib can be 10-500mg, and preferred gefitinib can be 15-400mg, particularly preferred gefitinib can be 25-300mg, and the most reasonable preferred gefitinib can be 50--250mg.
The present invention can prepare by the following method: (for example slow releasing tablet)
Gefitinib is mixed with pharmaceutical composition respectively, thereby obtain preferred the processing and processing characteristics, operable medicinal ingredient comprises binding agent, filler, lubricant, disintegrating agent and other pharmaceutic adjuvants.
With preferred gefitinib respectively with mix homogeneously such as one or more slow-release materials, filler, disintegrating agent, add a certain amount of binder solution respectively, wet granulation, the granule flood of gained is separately done to a certain degree, add lubricant, be pressed into the tablet of certain specification and size, granule mixes with above-mentioned slow releasing tablet of pressing, and is pressed into double-layer sustained release tablets.
In preparation process, also can with gefitinib together with above-mentioned various composition mix homogeneously, through suitably handling, be pressed into single that is fit to specification and size.
The present invention can prepare by the following method: (for example slow releasing capsule)
Gefitinib is mixed with suitable component respectively, comprise mix homogeneously such as binding agent, filler,, make the core piller through handling.The piller of gained is used for further processing.
Preferred gefitinib is dissolved in the appropriate solvent, adds suitable filler, binding agent etc. be made into coating solution,, the coating solution of above-mentioned preparation is wrapped in respectively on the celphere, obtain containing the pastille piller of gefitinib by fluidized bed coating.
In addition, technologies such as available inert kind nuclear laminating method, powder lamination method, Ji Chu spheronization, preparation contains the core material of active substance, and the gained core pellet is used for further processing.Use suitable packaging technique, on above-mentioned core piller, slow-release material can be dispersed or dissolved in the water or in the appropriate organic solvent with one or more slow-release material separate application.With the slow-release micro-pill of gained, mix homogeneously is inserted capsule by a certain percentage, promptly gets slow releasing capsule.
In preparation process, also gefitinib can be included in the micropill, make the pastille piller, with gained piller bundled slow-releasing layer, at last the slow-release pill of gained is inserted capsule again, promptly get slow releasing capsule of the present invention.
The specific embodiment
Below in conjunction with embodiment the present invention is done further auspicious stating:
Embodiment 1: medicine is made preparation by gefitinib 50mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 2: medicine is made preparation by gefitinib 100mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 3: medicine is made preparation by gefitinib 150mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 4: medicine is made preparation by gefitinib 200mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 5: medicine is made preparation by gefitinib 250mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 6: medicine is made preparation by gefitinib 300mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 7: medicine is made preparation by gefitinib 350mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 8: medicine is made preparation by gefitinib 400mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
Embodiment 9: medicine is made preparation by gefitinib 450mg, is undertaken by oral formulations (conventional tablet, dispersible tablet, thin membrane coated tablet, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.) preparation technology's procedure operation.
In addition, make preparation by gefitinib and form and form packing, in clinical treatment, play a role.
The invention is not restricted to above-described embodiment.
Claims (7)
1, the new oral formulations of a kind of treatment nonsmall-cell lung cancer (NSCLC); The active constituents of medicine of said preparation is a gefitinib; The oral ordinary tablet that adjuvant is made by preparation technique, dispersible tablet, film coating, Sublingual tablet, oral cavity disintegration tablet, enteric coatel tablets, slow releasing tablet, fast-release tablet, controlled release tablet, hard capsule, enteric coated capsule, slow releasing capsule etc.; Also can comprise the medicine acceptable carrier in the composition of said preparation.
2, according to claims 1 described oral formulations; Gefitinib 1--1000mg.
3, according to claims 1 described oral formulations, it is characterized in that: get principal agent and mix with filler, disintegrating agent, surfactant, cosolvent, binding agent, guiding humid medium system soft material is granulated drying, granulate, add lubricant, tabletting is made oral ordinary tablet, should oral ordinary tablet, should oral ordinary tablet bag film-coat or enteric coating can further make Film coated tablets or enteric coatel tablets; Get principal agent and mix with filler, binding agent, guiding humid medium system soft material, granulation, drying, granulate add correctives, lubricant, tabletting, Sublingual tablet.Get principal agent and filler, disintegrating agent, help and collapse agent, surfactant, binding agent mix, and add correctives, lubricant, and tabletting is made dispersible tablet, oral cavity disintegration tablet; Get principal agent and slow release and/or rapid release and/or controlled-release material and mix, guiding humid medium system soft material is granulated, drying, and granulate adds lubricant, and tabletting is made slow releasing tablet, fast-release tablet, controlled release tablet.
4, oral formulations according to claim 1, it is characterized in that: get principal agent and mix with filler, disintegrating agent, surfactant, binding agent, guiding humid medium system soft material, granulate, be filled into Capsules, make hard capsule, the hard capsule of preparation is handled with the coating enteric material can further be made enteric coated capsule; Get principal agent and slow release and/or rapid release and/or controlled-release material and make one or more slow release and/or rapid release or controlled release piller, filled the Capsules sheet after filling or the mixing separately, make slow release and/or quick-release capsules or controlled release capsule.
5, the adjuvant of oral formulations according to claim 1: filler, binding agent are arranged, surfactant, wetting agent, wetting agent, disintegrating agent helps and collapses agent, suspending agent, fluidizer, lubricant, correctives, absorbent, suspensoid, coating material, coating material, coating material, slow-release material, rapid release material, controlled-release material etc.
6, the described filler of claim 5 includes but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium carbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose etc.Binding agent includes but not limited to starch, pregelatinized Starch, gelatin, dextrin, maltose dextrin, sucrose, arabic gum, polyvinylpyrrolidone, various viscosity methylcellulose, low viscosity carboxymethyl cellulose, various viscosity ethyl cellulose, various viscosity polyvinyl alcohol, polyethylene glycol 6000, the following hydroxypropyl emthylcellulose of 50MPAS etc.; Disintegrating agent includes but not limited to starch, pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure lignocellulose, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, ion exchange resin, methylcellulose, sodium carboxymethyl cellulose etc.; Lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, Pulvis Talci, glyceryl monostearate, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, triacetyl glycerine, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium chloride, sodium laurylsulfate, magnesium laurylsulfate etc.; Surfactant comprises but is not limited to sodium lauryl sulphate, smelting Luo Shamu, Tween 80, bromination hexadecane trimethylamine, sodium laurylsulfate, stearyl alcohol sodium sulfonate, polyoxyethylene high fatty alcohol, sucrose ester, sorbitol fatty ester, soybean phospholipid etc.; Correctives includes but not limited to steviosin, fructose, glucose, high fructose syrup, Mel, aspartame, protein sugar, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, phyllodulcin, Sodium Cyclamate, flavoring banana essence, flavoring pineapple essence, Fructus Citri tangerinae essence, Herba Menthae essence, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence, rose essence etc.
7, the described coating material of claim 5 includes but not limited to cellulose and derivatives class thereof, crylic acid resin, ethene polymers etc.Coating material includes but not limited to gelatin, arabic gum, carboxymethyl cellulose, polyvinyl alcohol, polyacrylic acid, hydroxyethyl-cellulose, polylactic acid, ethyl cellulose, polyethylene, polyamide, stearic acid, celluloid, tristerin, Lac, Cellulose Acetate Phthalate; Slow release, rapid release, controlled release matrix material include but not limited to that Brazil wax, castor oil hydrogenated, Semen Ricini are cured, hydrogenated soya phosphatide, Lac, gelatin, sodium alginate, chitosan, amylopectin, agar, carrageenin, guar gum, cellulose derivative, crylic acid resin, polyethylene kind, macromolecular material etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410094557 CN1771961A (en) | 2004-11-09 | 2004-11-09 | Oral Geftinat prepn |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410094557 CN1771961A (en) | 2004-11-09 | 2004-11-09 | Oral Geftinat prepn |
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| CN1771961A true CN1771961A (en) | 2006-05-17 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266300A (en) * | 2011-07-14 | 2011-12-07 | 广东药学院 | Gefitinib dispersible tablet and preparation method and application thereof |
| CN103845335A (en) * | 2014-03-24 | 2014-06-11 | 江苏奥赛康药业股份有限公司 | Gefitinib medicinal composition and tablet containing gefitinib medicinal composition |
| CN106913541A (en) * | 2015-12-25 | 2017-07-04 | 山东新时代药业有限公司 | A kind of Gefitinib tablet and preparation method thereof |
-
2004
- 2004-11-09 CN CN 200410094557 patent/CN1771961A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266300A (en) * | 2011-07-14 | 2011-12-07 | 广东药学院 | Gefitinib dispersible tablet and preparation method and application thereof |
| CN102266300B (en) * | 2011-07-14 | 2013-01-02 | 广东药学院 | Gefitinib dispersible tablet and preparation method and application thereof |
| CN103845335A (en) * | 2014-03-24 | 2014-06-11 | 江苏奥赛康药业股份有限公司 | Gefitinib medicinal composition and tablet containing gefitinib medicinal composition |
| CN103845335B (en) * | 2014-03-24 | 2016-07-13 | 江苏奥赛康药业股份有限公司 | Gefitinib pharmaceutical composition and the tablet containing this gefitinib pharmaceutical composition |
| CN106913541A (en) * | 2015-12-25 | 2017-07-04 | 山东新时代药业有限公司 | A kind of Gefitinib tablet and preparation method thereof |
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