CN103638020A - Novel pharmaceutical composition for treating gout - Google Patents
Novel pharmaceutical composition for treating gout Download PDFInfo
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- CN103638020A CN103638020A CN201310710777.2A CN201310710777A CN103638020A CN 103638020 A CN103638020 A CN 103638020A CN 201310710777 A CN201310710777 A CN 201310710777A CN 103638020 A CN103638020 A CN 103638020A
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Abstract
The invention belongs to the field of medical technology, and relates to a novel pharmaceutical composition for treating gout, which is prepared by the existing preparation process by taking febuxostat and diacerein as active ingredients accompanied by a pharmaceutically acceptable medicinal carrier. With a synergistic effect, the pharmaceutical composition provided by the invention is convenient to be applied to a patient, and can reduce the formation of uric acid from the source and prevent the pain of the patient caused by a gout attack resulting from early deposition of uric acid.
Description
Technical field
The invention belongs to medical technical field, particularly, relate to a kind of new pharmaceutical composition for the treatment of gout, said composition comprises a kind of xanthine oxidase (XO) inhibitor Febustat and a kind of osteoarthritis IL-1 inhibitor diacerein.
Background technology
Gout (metabolic arthritis) is a kind of because of purine metabolism obstacle, makes uric acid accumulation and the disease that causes, belongs to arthritic a kind of, claims again metabolic arthritis.Due to uric acid excessive concentration in blood of human body, at soft tissue, form acicular crystal in as membrana articulata or tendon, cause health immune system overreaction (sensitivity) and the inflammation that causes suffering.
Morbidity and the living standard of gout are closely related, and China's living standards of the people were lower in the past, and the animal food in diet is less, thereby the prevalence of gout is lower, are considered to a kind of rare disease always, are called as in the past " emperor is sick ".Analysis report according to Chinese disease in 2004 and health survey center shows, due to the raising of modern life level, the foods such as the meat, drinks of purine are rich in the too much absorption of people, and the gout of today has been no longer emperors' patent.According to statistics, at present China's Patients with Hyperuricemia number has reached 1.2 hundred million, and wherein patient with gout surpasses 7,500 ten thousand people, and just with annual 9.7% annual rate of growth, increases sharply.Gout has become China inferior to the second largest metabolism class disease of diabetes, the health of wantonly engulfing people.
In the control procedure of gout, need being used in conjunction with of multiclass medicine, in view of the pathogenesis of gout, at present the main flow medicine of gout be take and suppressed the synthetic and antiinflammatory of uric acid as main.
Suppress at present uric acid synthetic drug, main flow medicine has Febustat, allopurinol, alloxanthine alcohol etc., and the mechanism of action is to suppress the activity of xanthine oxidase, and hypoxanthine, the synthetic uric acid of xanthine are obstructed.The Febustat tablet of Japanese Di Ren drugmaker (trade name: ULORIC) obtain FDA approval on February 13rd, 2009 and go on the market in the U.S. wherein, firstly over 40 years to get permission treatment with the new drug of hyperuricemia patient with gout, curative effect is better than allopurinol, and untoward reaction is relatively light.Febustat is 3.1 kind new medicines at present at home, and the conceptual phase of domestic enterprise mostly is clinical front and back.
And at present main anti-inflammatory drug, thereby what from the generation of source inflammation-inhibiting, improve state of an illness medicine is mainly IL-1 inhibitor, its main flow medicine has: diacerein etc., the mechanism of action is from the source of cartilage degradation reaction, to suppress the cascade of response of inflammation of IL-1 induction, thereby stop cartilage destroyed, there is the cartilage of promotion simultaneously and synthesize and repair.
Mechanism of action based on above-mentioned two kinds of medicines, on the basis of a large amount of clinical investigations and animal model test, for convenience of clothes for patients, use, performance drug synergism, in the present invention, Febustat and diacerein are combined to use, be prepared into compositions, can reduce from source the formation of uric acid, can prevent again the misery that early stage, uric acid deposition caused gout to be shown effect bringing to patient.
Summary of the invention
The object of this invention is to provide a kind of pharmaceutical composition that Febustat and diacerein exist to work in coordination with ratio that contains, be used for the treatment of gout.
The present invention is on the basis of a large amount of clinical investigations, pass through animal model experiment, be surprised to find: Febustat and diacerein have beyond thought synergism with the ratio composition pharmaceutical composition of 1:0.2～5, the preparation administration artifact availability that makes like this its compositions make is high, makes both can effectively bring into play therapeutical effect.
Pharmacological experiment study below shows: the compositions of Febustat and diacerein has synergism aspect reduction uric acid in serum concentration and treatment gouty arthritis.
1 experiment material
1.1 medicines and reagent
Febustat, white powder, Hubei China biological medicine Science and Technology Ltd. of WorldCom provides.With 0.5% sodium carboxymethyl cellulose (CMC-Na), be configured to before use the suspendible medicinal liquid of desired concn, for animal gastric infusion.
Diacerein, yellow or yellowish-brown powder, biological medicine science and technology (Wuhan) company limited of Sino-U.S. China WorldCom provides.With 0.5% sodium carboxymethyl cellulose, be configured to before use the suspendible medicinal liquid of desired concn, for animal gastric infusion.
1.2 animal
Kunming mouse, Military Medical Science Institute's Experimental Animal Center provides.
1.3 instruments and consumptive material
LD-6M vertical low speed large capacity refrigerated centrifuge, Sichuan Shu Ke Instrument Ltd. produces;
722 grating spectrophotometers, Shanghai Tianxiang optical instrument company limited produces;
K608-100 uric acid detects assay kit, and the prompt Science and Technology Ltd. of Amy produces.
2 methods and result
2.1 get 160 of Kunming mouses, and body weight is 160～180g, are divided at random 5 groups, 10 every group.Be respectively blank group, model control group, Febustat low dose group, in Febustat, dosage is 1 group, in Febustat, dosage is 2 groups, Febustat high dose group, diacerein low dose group, in diacerein, dosage is 1 group, in diacerein, dosage is 2 groups, diacerein high dose group, Febustat and diacerein composition low dose group, in Febustat and diacerein composition, dosage is 1 group, in Febustat and diacerein composition, dosage is 2 groups, in Febustat and diacerein composition, dosage is 3 groups, in Febustat and diacerein composition, dosage is 4 groups, Febustat and diacerein composition high dose group.
2.2 respectively to each group mouse stomach administration, the mice of 4 dosage groups of Febustat is the Febustat of gastric infusion corresponding dosage respectively, 4 dosage group mices of diacerein are the diacerein of gastric infusion corresponding dosage respectively, and the mice of Febustat and 6 dosage groups of diacerein composition is the Febustat of the corresponding dosage of administration simultaneously and the compositions that diacerein is made respectively.Blank group and model control group mice give respectively isometric normal saline.Every day 1 time, continuous 7 days.
2.3 the 7th days, l hour before last administration, got and respectively organizes the left back ankle joint of mice and make a clear horizontal line with marking pen, with toes capacity measurer, measured rat toes volume.Except blank group, all the other each groups give oxonic acid potassium salt 300mg/kg Mus lumbar injection.
After 2.41 hours, respectively organize gastric infusion, and carry out sterile working, except matched group, to the left back toes of each group mice, inject respectively 10% micro-crystal type uric acid sodium suspension 0.1mL(phosphate buffer preparation), after injection, 1h, 2h, 3h, 4h, 5h measure rat toes volume, and calculate paw swelling.Simultaneously after last administration, during 1h, by each group mice, at Mus tail, get hematometry blood uric acid.
2.5 paw swellings and uric acid level are measured
Each time point foot volume ﹣ swelling front foot volume after paw swelling=swelling
By the mouse blood of obtaining, centrifugal, prepare serum, get serum kit measurement uric acid level
2.6 interpretation
From table 1 data analysis: Febustat is when medication separately: low dosage can obviously reduce rat blood serum the concentration (P<0.05) of uric acid.Uric acid concentration in the reduction rat blood serum of middle dosage and high dose group energy highly significant (P<0.05,0.01).But the low middle high dose group of Febustat does not all have obvious inhibitory action (p<0.05,0.01) to rat paw edema acute inflammatory reaction in 1-5 hour.Diacerein is when independent medication: low dose group can significantly suppress the rat paw edema degree (P<0.05) of 2～3h, and middle dosage group and high dose group can significantly suppress the rat paw edema degree (P<0.05,0.01) of each time point of 2～5h.But the low middle high dose group of diacerein does not all obviously reduce uric acid concentration in rat blood serum (p<0.05).When Febustat and diacerein composite reagent: low dose group can be aided the rat paw edema degree (P<0.05) that suppresses 2～3h, can obviously reduce again uric acid concentration in rat blood serum (P < 0.05).Middle dosage group and high dose group all can significantly suppress the rat paw edema degree (P<0.05,0.01) of each time point of 2～5h, the uric acid concentration (P<0.01) in simultaneously also can the reduction rat blood serum of highly significant.
2.7 experiment conclusion:
Uricopoiesis depressant Febustat and diacerein form compound recipe, can reduce hyperuricemia mice serum uric acid level, can obviously suppress the acute inflammatory reaction that micro-crystal type uric acid sodium suspension causes rat paw edema simultaneously, have resist inflammation on repercussive function.Test shows: Febustat and diacerein drug ratio are in 1:(0.2～5) time the pharmaceutical composition that forms, there is obvious synergism, most preferably be 1:0.5～1:1.5, can reduce uric acid in serum level, can effectively suppress acute inflammatory reaction again, there is resist inflammation on repercussive function, can reduce from source the formation of uric acid, can prevent again the misery that early stage, uric acid deposition caused gout to be shown effect bringing to patient.
The object of this invention is to provide a kind of pharmaceutical composition that is used for the treatment of gout, be included in Febustat and the diacerein of the treatment effective dose of preparing in pharmaceutically acceptable pharmaceutical carrier.Wherein, the ratio of weight and number of Febustat and diacerein is 1:(0.2～5).
Pharmaceutical composition provided by the invention is comprised of Febustat and diacerein and pharmaceutically acceptable pharmaceutical carrier; Febustat wherein: diacerein: the ratio of weight and number of acceptable pharmaceutical carrier is 1:(0.2～5): (0.5～100), is preferably 1:(0.5～1.5): (1～50).
Pharmaceutical composition of the present invention comprises: various oral solid preparations, liquid agent.Preferably active component and any one or more pharmaceutically acceptable carrier are fully mixed and made into oral solid preparation.Preferred oral solid formulation is various tablets, granule, capsule, drop pill or pill.Liquid preparation is wherein pharmaceutically common dosage form, includes but not limited to injection, syrup, Emulsion, suspensoid etc.Because be easy to administration, tablet, granule and capsule represent the oral presented in unit dosage form of most convenient.
Pharmaceutical composition of the present invention also comprises also can comprise other pharmaceutically acceptable carrier additives, type for described interpolation does not have concrete restriction, it can be additive conventional in this area, specifically be selected from pharmaceutically acceptable solvent, propellant, solubilizing agent, cosolvent, emulsifying agent, coloring agent, adhesive, disintegrating agent, filler, lubricant, wetting agent, osmotic pressure regulator, stabilizing agent, fluidizer, correctives, antiseptic, suspending agent, coating material, aromatic, anti-adhesive, integrated agent, penetration enhancer, pH value regulator, buffer agent, plasticizer, surfactant, foaming agent, defoamer, thickening agent, inclusion agents, wetting agent, absorbent, diluent, flocculating agent and deflocculant, filter aid, discharge blocker etc.Consumption and combining form for other additives do not have any restriction.
In pharmaceutical composition of the present invention, pharmaceutically suitable carrier is excipient conventional in pharmacy, comprising: filler, for example, lactose, sucrose, starch, microcrystalline Cellulose, pregelatinized Starch, sorbitol or calcium phosphate etc. and their mixture; Binding agent: for example, syrup, gelatin, hyprolose, polyvinylpyrrolidone (PVP), PEG (Macrogol 4000 or 6000), starch or dextrin; Disintegrating agent: for example, microcrystalline Cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose or crospolyvinylpyrrolidone; Lubricant: for example, magnesium stearate, Pulvis Talci; High-molecular bone frame material: for example, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, ethyl cellulose, Brazil wax, hydrogenated vegetable oil or acrylic resin; Filmogen: for example, hydroxypropyl emthylcellulose, polyvinylpyrrolidone or acrylic resin etc.For injection, can select as caffolding agent mannitol, glycine, solubilizing agent propylene glycol, antioxidant sodium pyrosulfite etc.
In a preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 80 weight portions;
Single water and milk sugar of 116 weight portions;
The cross-linking sodium carboxymethyl cellulose of 20 weight portions;
The magnesium stearate of 4 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 160 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 120 weight portions;
Single water and milk sugar of 184 weight portions;
The cross-linking sodium carboxymethyl cellulose of 30 weight portions;
The magnesium stearate of 6 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 40 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 60 weight portions;
Single water and milk sugar of 82 weight portions;
The cross-linking sodium carboxymethyl cellulose of 15 weight portions;
The magnesium stearate of 3 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80 weight portions;
The diacerein of 100 weight portions;
The mannitol of 50 weight portions;
The pregelatinized Starch of 150 weight portions;
The polyvinylpolypyrrolidone of 15 weight portions;
The micropowder silica gel of 3 weight portions (silicon dioxide);
The magnesium stearate of 2 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 160 weight portions;
The diacerein of 100 weight portions;
The mannitol of 75 weight portions;
The pregelatinized Starch of 235 weight portions;
The polyvinylpolypyrrolidone of 22.5 weight portions;
The micropowder silica gel of 4.5 weight portions (silicon dioxide);
The magnesium stearate of 3 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 40 weight portions;
The diacerein of 100 weight portions;
The mannitol of 37.5 weight portions;
107.5 the pregelatinized Starch of weight portion;
11.25 the polyvinylpolypyrrolidone of weight portion;
The micropowder silica gel of 2.25 weight portions (silicon dioxide);
The magnesium stearate of 1.5 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80 weight portions;
The diacerein of 100 weight portions;
Single water and milk sugar of 150 weight portions;
The corn starch of 50 weight portions;
The PVP K30 of 4 weight portions;
The cross-linking sodium carboxymethyl cellulose of 12 weight portions;
The Pulvis Talci of 4 weight portions
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 160 weight portions;
The diacerein of 100 weight portions;
Single water and milk sugar of 235 weight portions;
The corn starch of 75 weight portions;
The PVP K30 of 6 weight portions;
The cross-linking sodium carboxymethyl cellulose of 18 weight portions;
The Pulvis Talci of 6 weight portions;
The magnesium stearate of 5.4 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 108 weight portions;
Single water and milk sugar of 206.1 weight portions;
The cross-linking sodium carboxymethyl cellulose of 27 weight portions;
The hyprolose of 13.5 weight portions;
The magnesium stearate of 5.4 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 160 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 108 weight portions;
Single water and milk sugar of 126.1 weight portions;
The cross-linking sodium carboxymethyl cellulose of 27 weight portions;
The hyprolose of 13.5 weight portions.
The magnesium stearate of 5.4 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 40 weight portions;
The diacerein of 100 weight portions;
The microcrystalline Cellulose of 54 weight portions;
Single water and milk sugar of 59.8 weight portions;
The cross-linking sodium carboxymethyl cellulose of 13.5 weight portions;
The hyprolose of 6.25 weight portions.
The magnesium stearate of 2.7 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80 weight portions;
The diacerein of 100 weight portions;
The sucrose of 2000 weight portions;
The mannitol of 805 weight portions;
The magnesium stearate of 15 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 160 weight portions;
The diacerein of 100 weight portions;
The sucrose of 2000 weight portions;
The mannitol of 725 weight portions;
The magnesium stearate of 15 weight portions.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 40 weight portions;
The diacerein of 100 weight portions;
The sucrose of 1000 weight portions;
352.5 the mannitol of weight portion;
7.5 the magnesium stearate of weight portion.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 40mg;
The diacerein of 50mg;
The propylene glycol of 20mL;
The sodium sulfite of 0.2g;
The water for injection of 790mL.
In another preferred embodiment of the present invention, described in contain Febustat and diacerein compositions comprise:
The Febustat of 80mg;
The diacerein of 50mg;
The propylene glycol of 20mL;
The sodium sulfite of 0.2g;
The water for injection of 790mL.
The described compositions that contains Febustat and diacerein can be prepared into various solid dosage formss, and described solid preparation is pharmaceutically common dosage form, includes but not limited to tablet, granule, capsule etc.
The preparation method of the described composition tablet that contains Febustat and diacerein, adopts conventional method for preparing tablet thereof all can realize, and comprises wet granule compression tablet method, dry granulation tabletting method or direct powder compression method.
The described composition capsule that contains Febustat and diacerein, the preparation method of its content, adopts conventional preparation method of granules all can realize, and comprises wet granulation process, dry granulation method or powder direct mixing method.
The preparation method of the described composition granule that contains Febustat and diacerein, adopts conventional preparation method of granules all can realize, and comprises wet granulation process, dry granulation method.
Pharmaceutical composition of the present invention reduces fast and obviously the metabolic arthritis level in serum, can effectively suppress acute inflammatory reaction again, there is resist inflammation on repercussive function, can reduce from source the formation of uric acid, can prevent again the misery that early stage, uric acid deposition caused gout to be shown effect bringing to patient.
The specific embodiment
Describe embodiments of the invention below in detail, it should be noted that the embodiment the following describes is exemplary, only for explaining the present invention, and can not be interpreted as limitation of the present invention.In addition, if do not clearly not stated, all reagent of adopting are in the following embodiments can be buied on market, or can be synthetic according to text or known method, for the reaction condition of not listing, be also that those skilled in the art easily obtain.
One aspect of the present invention provides a kind of compositions containing Febustat diacerein, comprising: the diacerein of the Febustat of 40-80 weight portion and 50-100 weight portion.
In the present invention, for Febustat, not having any restriction, can be any pharmaceutically useful Febustat and salt thereof.
In the present invention, for diacerein, not having any restriction, can be any pharmaceutically useful diacerein and salt thereof.
In the present invention, in Febustat and diacerein composition solid preparation, the weight of contained Febustat and diacerein does not limit, and it can be the common dose scope of Febustat and diacerein clinically.In a preferred embodiment of the invention, every portion is 40mg containing contained Febustat in Febustat diacerein composition, and the weight of diacerein is 50mg.In another preferred embodiment of the present invention, every portion is 40mg containing contained Febustat in Febustat diacerein composition, and the weight of diacerein is 100mg.In another preferred embodiment of the present invention, every portion is 80mg containing contained Febustat in Febustat diacerein composition, and the weight of diacerein is 50mg.In another preferred embodiment of the present invention, every portion is 80mg containing contained Febustat in Febustat diacerein composition, and the weight of diacerein is 100mg.
In compositions of the present invention, also can comprise other pharmaceutically acceptable additives.Type for described additive does not have concrete restriction, can be additive conventional in this area, specifically be selected from one or more of pharmaceutically acceptable filler, pharmaceutically acceptable disintegrating agent, pharmaceutically acceptable binding agent and pharmaceutically acceptable lubricant.In the present invention, the consumption for other additives does not have any restriction.In a preferred embodiment of the present invention, the content of described additive is 100-5000 weight portion.
In the present invention, for the type of pharmaceutically acceptable filler, do not have any restriction, it can be filler conventional in this area.In a preferred embodiment of the present invention, described filler is selected from pregelatinized Starch, lactose, mannitol, microcrystalline Cellulose and their mixture.In another preferred embodiment of the present invention, described filler is single water and milk sugar, microcrystalline Cellulose and their mixture.In the present invention, for the consumption of filler, do not have any restriction, it can be the conventional amount used in this area.In an example of the present invention, the consumption of described filler is 100-5000 weight portion, is preferably 150-4000 weight portion, and 220-3000 weight portion more preferably, in 100 weight portion diacereins.
In the present invention, for the type of described disintegrating agent, without any restriction, it can be pharmaceutically acceptable conventional disintegrating agent.In a preferred embodiment of the present invention, described disintegrating agent is selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and their mixture.In the present invention, the content of described disintegrating agent should be preferably 10-50 weight portion at 5-100 weight portion, and 12-30 weight portion more preferably, in 100 weight portion diacereins.
In the present invention, for the type of described binding agent, without any restriction, it can be pharmaceutically acceptable conventional binding agent.In a preferred embodiment of the present invention, described binding agent is selected from water or PVP K30.
In the present invention, for the type of pharmaceutically acceptable lubricant, do not have any restriction, it can be lubricant conventional in this area.In a preferred embodiment of the present invention, described lubricant is selected from magnesium stearate.In the present invention, for the consumption of lubricant, do not have any restriction, it can be the conventional amount used in this area.In an example of the present invention, the consumption of described lubricant is 0-50 weight portion, is preferably 0-30 weight portion, and 0-15 weight portion more preferably, in 100 weight portion diacereins.
In the present invention, term used " pharmaceutically acceptable additive " refers to the additive of pharmaceutically acceptable reinforcement preparation characteristic.Examples of such additives is well-known to those skilled in the art, comprises filler, disintegrating agent, binding agent, lubricant and other.Wherein filler is lactose, pregelatinized Starch and microcrystalline Cellulose etc.Disintegrating agent is cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone and carboxymethyl starch sodium etc.Binding agent is water, PVP K30 etc.Lubricant is magnesium stearate etc.
Below by specific embodiment, further describe the present invention, but do not limit the scope of the invention.
Embodiment 1
Febustat and diacerein tablet formulation 1
Embodiment 2
Febustat and diacerein tablet formulation 2
Embodiment 3
Febustat and diacerein tablet formulation 3
Embodiment 4
Febustat and diacerein tablet formulation 4
The preparation method of embodiment 1-4: the Febustat and the diacerein that take recipe quantity, microcrystalline Cellulose, single water and milk sugar and cross-linking sodium carboxymethyl cellulose, mix homogeneously after sieving respectively, add purified water appropriate, make soft material, cross 20 mesh sieves and make wet granular, 60 degree are dried, cross 20 order granulate, then add magnesium stearate to mix, compacting in flakes.
Embodiment 5
Febustat and diacerein tablet formulation 5
Embodiment 6
Febustat and diacerein tablet formulation 6
Embodiment 7
Febustat and diacerein tablet formulation 7
The preparation method of embodiment 5-7: the Febustat and the diacerein that take recipe quantity, mannitol, pregelatinized Starch and polyvinylpolypyrrolidone, cross respectively mix homogeneously after 80 mesh sieves, add purified water appropriate, make soft material, cross 24 mesh sieves and make wet granular, 60 degree are dried, cross 20 order granulate, then add micropowder silica gel (silicon dioxide) and magnesium stearate to mix, compacting in flakes.
Embodiment 8
Febustat and diacerein tablet formulation 8
Embodiment 9
Febustat and diacerein tablet formulation 9
The preparation method of embodiment 8-9: the Febustat and the diacerein that take recipe quantity, single water and milk sugar, corn starch and cross-linking sodium carboxymethyl cellulose (1), cross respectively mix homogeneously after 80 mesh sieves, 5% PVP K30 aqueous solution is appropriate, makes soft material, crosses 20 mesh sieves and makes wet granular, 60 degree are dried, cross 18 order granulate, then add cross-linking sodium carboxymethyl cellulose (2) and Pulvis Talci to mix, compacting in flakes.
Embodiment 10
Febustat and diacerein capsule prescription 10
Embodiment 11
Febustat and diacerein capsule prescription 11
Embodiment 12
Febustat and diacerein capsule prescription 12
The preparation method of embodiment 10-12: the Febustat and the diacerein that take recipe quantity, single water and milk sugar, microcrystalline Cellulose and cross-linking sodium carboxymethyl cellulose, cross respectively mix homogeneously after 80 mesh sieves, and 2.5% hyprolose aqueous solution is appropriate, make soft material, cross 40 mesh sieves and make wet granular, 60 degree are dried, and cross 40 order granulate, add again magnesium stearate to mix, with No. 2 capsules, filled capsules, loading amount is 270mg.
Embodiment 13
Febustat and diacerein granule prescription 13
Embodiment 14
Febustat and diacerein granule prescription 14
Embodiment 15
Febustat and diacerein granule prescription 15
The preparation method of embodiment 13-15: the Febustat and the diacerein that take recipe quantity, sucrose, mannitol, mix homogeneously after sieving respectively, obtains Febustat and diacerein compound, adds purified water appropriate, make soft material, 28 orders sieve and make wet granular, and 60 degree are dry, cross 22 order granulate, obtain, loading amount is 1500mg/ bag.
Febustat and diacerein injection prescription 16
| Form | Every bottle of consumption |
| Febustat | 40mg |
| Diacerein | 50mg |
| Propylene glycol | 20mL |
| Sodium sulfite | 0.2g |
| Water for injection | Add to 1000ml |
Embodiment 17
Febustat and diacerein injection prescription 17
| Form | Every bottle of consumption |
| Febustat | 80mg |
| Diacerein | 50mg |
| Propylene glycol | 20mL |
| Sodium sulfite | 0.2g |
| Water for injection | Add to 1000ml |
The preparation method of embodiment 16-17: the Febustat and the diacerein that take recipe quantity are added in 60-80 ℃ of water, add propylene glycol, stirs, both are all dissolved, be cooled to 40-50 ℃, regulate pH value to 4.0-9.0, add active carbon, stir 15min, standing filtration, add antioxidant, then add water for injection to full dose, stir, fine straining is to qualified, embedding, autoclaving, obtains.
Although illustrated and described embodiments of the invention above, be understandable that, above-described embodiment is exemplary, can not be interpreted as limitation of the present invention, those of ordinary skill in the art can change above-described embodiment within the scope of the invention in the situation that not departing from principle of the present invention and aim, modification, replacement and modification.
Claims (9)
1. treat a new pharmaceutical composition for gout, be included in Febustat and the diacerein of the treatment effective dose of preparing in pharmaceutically acceptable pharmaceutical carrier.
2. pharmaceutical composition according to claim 1, is characterized in that, the ratio of weight and number of described Febustat and diacerein is 1:0.2～1:5, is preferably 1:0.5～1:1.5.
3. pharmaceutical composition according to claim 1, it is characterized in that, this pharmaceutical composition also comprises other pharmaceutically acceptable carrier additives, concrete is to be selected from pharmaceutically acceptable solvent, propellant, solubilizing agent, cosolvent, emulsifying agent, coloring agent, adhesive, disintegrating agent, filler, lubricant, wetting agent, osmotic pressure regulator, stabilizing agent, fluidizer, correctives, antiseptic, suspending agent, coating material, aromatic, anti-adhesive, integrated agent, penetration enhancer, pH value regulator, buffer agent, plasticizer, surfactant, foaming agent, defoamer, thickening agent, inclusion agents, wetting agent, absorbent, diluent, flocculating agent and deflocculant, filter aid, discharge blocker etc.
4. according to the pharmaceutical composition described in claim 1-3, it is characterized in that, described compositions can be prepared into solid preparation or liquid preparation.
5. pharmaceutical composition according to claim 4, is characterized in that, described solid preparation is pharmaceutically common dosage form, includes but not limited to tablet, granule, capsule.
6. pharmaceutical composition according to claim 4, is characterized in that, described liquid preparation is pharmaceutically common dosage form, includes but not limited to injection, syrup, Emulsion, suspensoid.
7. the application of the pharmaceutical composition described in claim 1-4 in the medicine of preparation treatment hyperuricemia and its relevant various diseases.
8. application as claimed in claim 6, wherein said hyperuricemia comprises constitutional and secondary hyperuricemia.
9. application as claimed in claim 6, wherein said various diseases comprise acute and chronic gout, gouty arthritis, gouty nephropathy and renal calculus.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310710777.2A CN103638020A (en) | 2013-12-20 | 2013-12-20 | Novel pharmaceutical composition for treating gout |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310710777.2A CN103638020A (en) | 2013-12-20 | 2013-12-20 | Novel pharmaceutical composition for treating gout |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769766A (en) * | 2016-03-24 | 2016-07-20 | 长沙佰顺生物科技有限公司 | Topiroxostat nano-emulsion and preparation method of topiroxostat nano-emulsion |
| CN105832729A (en) * | 2016-05-30 | 2016-08-10 | 青岛云天生物技术有限公司 | Pharmaceutical composition for treating hyperuricemia and application of pharmaceutical composition for treating hyperuricemia |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103429236A (en) * | 2011-03-11 | 2013-12-04 | 安成生物科技股份有限公司 | Methods and compositions for treating hyperuricemia and metabolic disorders associated with hyperuricemia |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103429236A (en) * | 2011-03-11 | 2013-12-04 | 安成生物科技股份有限公司 | Methods and compositions for treating hyperuricemia and metabolic disorders associated with hyperuricemia |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769766A (en) * | 2016-03-24 | 2016-07-20 | 长沙佰顺生物科技有限公司 | Topiroxostat nano-emulsion and preparation method of topiroxostat nano-emulsion |
| CN105832729A (en) * | 2016-05-30 | 2016-08-10 | 青岛云天生物技术有限公司 | Pharmaceutical composition for treating hyperuricemia and application of pharmaceutical composition for treating hyperuricemia |
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