CN1857289A - Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process - Google Patents
Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process Download PDFInfo
- Publication number
- CN1857289A CN1857289A CN 200610044432 CN200610044432A CN1857289A CN 1857289 A CN1857289 A CN 1857289A CN 200610044432 CN200610044432 CN 200610044432 CN 200610044432 A CN200610044432 A CN 200610044432A CN 1857289 A CN1857289 A CN 1857289A
- Authority
- CN
- China
- Prior art keywords
- salt
- arbitrary proportion
- mesh sieves
- acid
- aminoacid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Abstract
The present invention discloses a kind of dispersed compound tablet of glycyrrhizic acid and its salt. The dispersed compound tablet consists of: glycyrrhizic acid or its salt or its lipoid ligand, amino acid, antioxidant stabilizer, disintegrating agent, filler, adhesive, lubricant, surfactant in certain weight proportion. The present invention also discloses the preparation process of the dispersed compound tablet. Compared with available tablet of glycyrrhizinate, the dispersed compound tablet has the advantages of fast acting, high bioavailability, less side effect, convenient taking, etc.
Description
Technical field
The present invention relates to a kind of dispersible tablet and preparation method thereof, relate in particular to dispersible tablet of a kind of compound glycyrrbizic acid and salt thereof and preparation method thereof, belong to medical technical field.
Background technology
Glycyrrhizic acid claims glycyrrhizin again, is the main active of Radix Glycyrrhizae, mainly contains two kinds of configurations of α and β.Have antiviral, antiinflammatory, antiallergic action, immunomodulating, protection hepatocyte isoreactivity, be used for the treatment of multiple diseases such as chronic hepatitis, erythra clinically, received good efficacy.
The preparation listing of at present both at home and abroad existing glycyrrhizic acids and salt thereof has the folk prescription tablet, also by the compound injection of forming with aminoacid.The therapeutic effect of folk prescription glycyrrhizunate tablet is often not as compound preparation, and the heavy slightly patient of child, old man and the state of an illness is difficult for swallowing than big tablet.The problem that the compound glycyrrbizic acid saline injection exists is medication inconvenience, and patient's compliance is low.
Summary of the invention
At the deficiencies in the prior art, the object of the present invention is to provide the dispersible tablet of a kind of compound glycyrrbizic acid and salt thereof.This compound dispersed tablet agent have protect the liver, effect such as antiinflammatory, antiallergic, detoxifcation, and have rapid-action, side effect is little, bioavailability height, but advantages such as life-time service easy to use.
Another object of the present invention is to provide the preparation method of the dispersible tablet of a kind of compound glycyrrbizic acid and salt thereof.
Another purpose of the present invention is to provide the new dosage form of a kind of compound glycyrrbizic acid and salt thereof.
The dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof, form by following component:
Glycyrrhizic acid or glycyrrhetate or its lipid ligand, aminoacid, and antioxidative stabilizer, two or more in disintegrating agent, filler, binding agent, lubricant, the surfactant or whole; Wherein, described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 20～110: 10～370: 1～15: 20～70: 15～25: 10～15: 1～2.5: 1～5.
Wherein: described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is preferably: 30～45: 30～55: 5～12: 20～40: 18～23: 10～13: 2～2.5: 1～4.
Wherein: described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant most preferably is: 35: 50: 8.82: 20: 20: 10: 2.5: 3.
In the dispersible tablet of above-mentioned compound glycyrrbizic acid and salt thereof, described glycyrrhizic acid or its salt comprise α configuration and beta comfiguration, and described glycyrrhetate is one of potassium salt, ammonium salt, magnesium salt, sodium salt, zinc salt of glycyrrhizic acid; Described aminoacid is that arbitrary proportion mixes between one of glycine, L-cysteine hydrochloride, methionine, lysine, arginine, Aspartic Acid or its both or the many persons; Described antioxidative stabilizer is that arbitrary proportion mixes between one of vitamin C, sodium sulfite, sodium sulfite or its both or the many persons; Described disintegrating agent is that arbitrary proportion mixes between one of hydroxypropyl starch, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, soluble starch or its both or the many persons; Described filler is that arbitrary proportion mixes between one of lactose, mannitol, sorbitol, starch, modified starch, dextrin, calcium sulfate, microcrystalline Cellulose or its both or the many persons; Described binding agent is that arbitrary proportion mixes between one of polyvinylpyrrolidone, hypromellose, methylcellulose, sodium carboxymethyl cellulose, starch slurry, syrup, rubber cement or its both or the many persons; Described lubricant is that arbitrary proportion mixes between one of magnesium stearate, calcium stearate, Polyethylene Glycol, micropowder silica gel, Pulvis Talci or its both or the many persons; Described surfactant is that arbitrary proportion mixes between one of Stepanol MG, sodium lauryl sulphate, Polysorbate, poloxamer or its both or the many persons.
Wherein: described glycyrrhetate is the potassium salt or the ammonium salt of glycyrrhizic acid preferably; Described aminoacid preferably between both or the many persons of one of glycine, L-cysteine hydrochloride, methionine or its arbitrary proportion mix; Described antioxidative stabilizer is one of vitamin C, sodium sulfite or its arbitrary proportion mixing between the two preferably; Described disintegrating agent preferably between both or the many persons of one of hydroxypropyl starch, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, carboxymethylcellulose calcium, soluble starch or its arbitrary proportion mix; Described filler preferably between both or the many persons of one of lactose, mannitol, sorbitol, starch, microcrystalline Cellulose or its arbitrary proportion mix; Described binding agent preferably between both or the many persons of one of polyvinylpyrrolidone, hypromellose, methylcellulose, syrup or its arbitrary proportion mix; Described lubricant preferably between both or the many persons of one of magnesium stearate, calcium stearate, micropowder silica gel or its arbitrary proportion mix; Described surfactant is one of Stepanol MG, sodium lauryl sulphate or its arbitrary proportion mixing between the two preferably.
In the dispersible tablet of above-mentioned compound glycyrrbizic acid and salt thereof: described glycyrrhetate is potassium glycyrrhizana preferably further; Described aminoacid further preferably one of glycine, methionine or its both mix by equal proportion.
Wherein: described potassium glycyrrhizana most preferably is glycyrrhizic acid list potassium or glycyrrhizic acid dipotassium.
Wherein: described aminoacid most preferably is that glycine mixes by 1: 1 weight proportion with methionine.
The weight portion that weight proportion of the present invention relates to can be the known mass units of field of medicaments such as μ g, mg, g, kg.
Component in the dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof: glycyrrhizic acid or glycyrrhetate or glycyrrhizinate lipid ligand, aminoacid, antioxidative stabilizer, disintegrating agent, filler, binding agent, lubricant and surfactant all adopt the raw material that meets medicinal standard or can be used for pharmaceutical production.
The preparation method of the dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof, finish by following steps:
(1) takes by weighing respectively by weight ratio and pulverize the back and, take by weighing in proportion simultaneously through super-dry, pulverizing and through the filler and the binding agent of 150 mesh sieves screening through the glycyrrhizic acid of 200 mesh sieves screening or glycyrrhetate or glycyrrhizinate lipid ligand, aminoacid, antioxidative stabilizer;
(2) above-mentioned supplementary material is placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulate with 20 mesh sieves at granulator then;
(3) again the granule that makes is placed granulator to carry out granulate to remove oversized particles with 16 mesh sieves; add through super-dry, pulverizing and through disintegrating agent, lubricant and the surfactant of 150 mesh sieves screening in described ratio subsequently; mix homogeneously; at last that the granule that is up to the standards is heavy according to the sheet that the granule content of measuring calculates, on tablet machine, carry out the dispersible tablet that tabletting is made compound glycyrrbizic acid and salt thereof.
The lipid ligand of glycyrrhizic acid of the present invention and salt thereof can prepare by literature method.
In the preparation method of the dispersible tablet of above-mentioned compound glycyrrbizic acid and salt thereof: the composition of the easy oxidation deterioration of end-on air; should adopt the specific process protection as L-cysteine hydrochloride etc.; separately its coating is granulated as alcoholic solution with convention amount cellulose family binding agent, and then with other granule mixing film-making.
Utilize the dispersible tablet of the compound glycyrrbizic acid of method of the present invention preparation and salt thereof to compare and have following advantage with existing folk prescription oral formulations and compound injection:
(1) added aminoacid such as glycine and methionine in the prescription, than folk prescription oral formulations better efficacy, side effect is lower, can suppress or alleviate owing to giving for a long time the unusual pseudo-aldosterone disease that causes of electrolyte metabolism that glycyrrhizic acid causes in a large number.
(2) because tablet is in dry anhydrous state all the time, and packing is tight, avoids contacting with air, thereby more stable than injection.
(3) produce, transport, preserve, carry and use more convenient.
(4) compliance of patient's medication is stronger.Because injection is not suitable for long-term prescription, and patient's compliance is relatively poor, and tablet can long-term prescription, thereby is applicable to that more the chronic takes for a long time, treats more convenient.
(5) make dispersible tablet and both can swallow, can take after mixing it with water again, thereby be specially adapted to old man, child and the patient of tablet difficulty that swallows.
The dispersible tablet of using compound glycyrrbizic acid of the present invention and salt thereof can obviously alleviate hepatocyte qualitative change and necrosis, alleviates matter inflammatory reaction between hepatocyte, suppresses hepatocyte fibroplasia, thereby reduces the incidence rate of liver cirrhosis and promote hepatocellular regeneration.This pharmaceutical composition also can suppress the activation of fibrinolysin system, stops the promotion of serum to capillary permeability, suppresses the hyperfunction of membrane permeability, and the effect that suppresses granuloma formation is arranged, and retardance anaphylaxis disease is also had inhibitory action.
In the component of the dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof: glycyrrhizic acid or glycyrrhetate or glycyrrhizinate lipid ligand are hydrolyzed to glucuronic acid and enoxolone by glycuronidase in vivo, steroid metabolism enzyme (Δ 5-β-reductase) in enoxolone and the liver has stronger affinity, thereby hinder the deactivation of hydrocortisone and aldosterone, so tangible 17-hydroxy-11-dehydrocorticosterone sample and aldosterone sample effect are arranged, use the back to show tangible 17-hydroxy-11-dehydrocorticosterone sample effect, as antiinflammatory, antiallergic, protecting film structure, immunomodulating and the metabolism of promotion bile pigments etc.; Glycyrrhizic acid or glycyrrhetate or glycyrrhizinate lipid ligand are decomposed into enoxolone and glucuronic acid at liver in addition, can combine with toxicant and a Detoxication.
Glycine has detoxifcation, anti-allergy action, can offset the side effect of glycyrrhizic acid water-sodium retention simultaneously.
Methionine is a kind of essential amino acids, can synthesize choline and creatine in human body; Choline is a kind of anti-fattyliver substance, and to the toxic hepatitis that is caused by arsenical, barbiturate, carbon tetrachloride etc., methionine has treatment and liver function protecting effect; The L-cysteine hydrochloride can be exchanged into methionine in vivo, and the L-cysteine hydrochloride also can alleviate potential aldosterone sample effect of glycyrrhizic acid or glycyrrhetate or glycyrrhizinate lipid ligand and hormonelike side effect.
The application of antioxidative stabilizer can keep the finished product preparation of the dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof to have stability in the useful life.
Utilize the dispersible tablet of compound glycyrrbizic acid of the present invention and salt thereof; by glycyrrhizic acid or glycyrrhetate or the different separately effect that stresses such as glycyrrhizinate lipid ligand, aminoacid; replenish mutually and act synergistically on body; give full play to antiinflammatory, antiallergic, protecting film structure, regulate effects such as immunity and antiviral, the clinical practice checking obtains excellent curative.
The specific embodiment
Further describe the present invention below in conjunction with embodiment, understand the present invention and advantage and effect, but described embodiment only is used to illustrate the present invention rather than restriction the present invention in order to more deep.
Embodiment 1
With 1000 compound glycyrrbizic acid list potassium dispersible tablets is benchmark, take by weighing 35g glycyrrhizic acid list potassium, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 20g microcrystalline Cellulose and the 10g polyvidone of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through 20g carboxymethyl starch sodium and the 2.5g magnesium stearate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound glycyrrbizic acid list potassium dispersible tablets at last.
Embodiment 2
With 1000 compound glycyrrbizic acid list potassium dispersible tablets is benchmark, take by weighing 35g glycyrrhizic acid list potassium, 350g glycine, 8.82g vitamin C and the 0.25g sodium sulfite pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 20g pregelatinized Starch and the 10g hypromellose of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add the 17.5g L-CYSTEAMINE HCL granulates that makes with an amount of cellulose family binding agent alcoholic solution subsequently; add through super-dry, pulverizing and through the 20g low-substituted hydroxypropyl cellulose 2.5g calcium stearate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound glycyrrbizic acid list potassium dispersible tablets at last again.
Embodiment 3
With 1000 compound glycyrrbizic acid list potassium dispersible tablets is benchmark, take by weighing 35g glycyrrhizic acid list potassium, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 25g microcrystalline Cellulose and the 10g starch slurry of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through 20g polyvinylpolypyrrolidone, 1.5g micropowder silica gel and the 1g magnesium stearate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound glycyrrbizic acid list potassium dispersible tablets at last.
Embodiment 4
With 1000 compound monoammonium glycyrrhizinate dispersible tablets is benchmark, take by weighing 35g monoammonium glycyrrhizinate, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 30g pregelatinized Starch and the 15g hypromellose of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through the 20g cross-linking sodium carboxymethyl cellulose 2.5g magnesium stearate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound monoammonium glycyrrhizinate dispersible tablets at last.
Embodiment 5
With 1000 compound monoammonium glycyrrhizinate dispersible tablets is benchmark, take by weighing 35g monoammonium glycyrrhizinate, 350g glycine, 8.82g vitamin C and the 0.25g sodium sulfite pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 15g microcrystalline Cellulose and the 10g hypromellose of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add the 17.5g L-CYSTEAMINE HCL granulates that makes with an amount of cellulose family binding agent alcoholic solution subsequently; add through super-dry, pulverizing and through 20g low-substituted hydroxypropyl cellulose and the 2.5g micropowder silica gel and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound monoammonium glycyrrhizinate dispersible tablets at last again.
Embodiment 6
With 1000 compound glycyrrbizic acid diammonium dispersible tablets is benchmark, take by weighing 35g monoammonium glycyrrhizinate, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 20g microcrystalline Cellulose and the 10g hypromellose of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through the 20g carboxymethyl starch sodium 2.5g magnesium stearate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound glycyrrbizic acid diammonium dispersible tablets at last.
Embodiment 7
Press literature method (comparison of the physicochemical property of glycyrrhizic acid and lipid ligand thereof and anti-hepatic injury effect, contemporary Chinese application pharmaceutical journal, 2000,17 (3): 241～242) preparation glycyrrhizinate lipid ligand.
With 1000 compound glycyrrbizic acid lipid ligand dispersible tablets is benchmark, take by weighing 105g glycyrrhizinate lipid ligand, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 20g microcrystalline Cellulose and the 10g hypromellose of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through 20g low-substituted hydroxypropyl cellulose, 1.5g micropowder silica gel and 1g calcium stearate, 3g sodium lauryl sulphate and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound glycyrrbizic acid lipid ligand dispersible tablets at last.
Embodiment 8
Press literature method (trial-production of monoammonium glycyrrhizinate liposome of salt and stability study, Chinese Journal of Pharmaceuticals, 2000,35 (4): 222～224) preparation monoammonium glycyrrhizinate lipid ligand.
With 1000 compound monoammonium glycyrrhizinate lipid ligand dispersible tablets is benchmark, take by weighing 105g monoammonium glycyrrhizinate lipid ligand, 25g glycine, 25g methionine and the 8.82g vitamin C pulverizing the back and screen respectively through 200 mesh sieves, take by weighing simultaneously through super-dry, pulverizing and through the 20g microcrystalline Cellulose and the 10g polyvidone of 150 mesh sieves screening, these supplementary materials are placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulates with 20 mesh sieves at oscillating granulator then; Place oscillating granulator to carry out granulate to remove oversized particles this granule with 16 mesh sieves; add subsequently through super-dry, pulverizing and through 20g cross-linking sodium carboxymethyl cellulose and 2.5g micropowder silica gel, 3g Stepanol MG and the mix homogeneously of 150 mesh sieves screening, the sheet that the granule that is up to the standards is calculated according to the granule content of measuring focuses on and carries out tabletting on the tablet machine and make 1000 compound monoammonium glycyrrhizinate lipid ligand dispersible tablets at last.
Embodiment 9
Unit is in kilogram, and by diammonium glycyrrhizinate: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 25: 40: 5: 30: 15: 10: 1.5: 3 amount takes by weighing each component respectively.Wherein: described aminoacid is glycine; Described antioxidative stabilizer is a vitamin C; Described disintegrating agent is a hydroxypropyl starch; Described filler is a lactose; Described binding agent is a polyvinylpyrrolidone; Described lubricant is a magnesium stearate; Described surfactant is a Stepanol MG.
The dispersible tablet for preparing the compound glycyrrbizic acid diammonium with following steps:
(1) takes by weighing respectively by weight ratio and pulverize the back and, take by weighing in proportion simultaneously through super-dry, pulverizing and through the filler and the binding agent of 150 mesh sieves screening through diammonium glycyrrhizinate, aminoacid, the antioxidative stabilizer of 200 mesh sieves screening;
(2) above-mentioned supplementary material is placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulate with 20 mesh sieves at granulator then;
(3) again the granule that makes is placed granulator to carry out granulate to remove oversized particles with 16 mesh sieves; add through super-dry, pulverizing and through disintegrating agent, lubricant and the surfactant of 150 mesh sieves screening in described ratio subsequently; mix homogeneously; at last that the granule that is up to the standards is heavy according to the sheet that the granule content of measuring calculates, on tablet machine, carry out the dispersible tablet that tabletting is made the compound glycyrrbizic acid diammonium.
Embodiment 10
Unit is in kilogram, and by glycyrrhizic acid list potassium: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 35: 50: 8.82: 20: 20: 10: 2.5: 3 amount takes by weighing each component respectively.Wherein: described aminoacid is that glycine mixes by 1: 1 weight proportion with methionine; Described antioxidative stabilizer is a vitamin C; Described disintegrating agent is that carboxymethyl starch sodium mixes by 1: 1 weight proportion with carboxymethylcellulose calcium; Described filler is that mannitol mixes by 1: 1 weight proportion with sorbitol; Described binding agent is that hypromellose mixes by 1: 1 weight proportion with methylcellulose; Described lubricant is that magnesium stearate is mixed by 1: 1 weight proportion with calcium stearate; Described surfactant is a sodium lauryl sulphate.
The dispersible tablet for preparing compound glycyrrbizic acid list potassium with following steps:
(1) takes by weighing respectively by weight ratio and pulverize the back and, take by weighing in proportion simultaneously through super-dry, pulverizing and through the filler and the binding agent of 150 mesh sieves screening through glycyrrhizic acid list potassium, aminoacid, the antioxidative stabilizer of 200 mesh sieves screening;
(2) above-mentioned supplementary material is placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulate with 20 mesh sieves at granulator then;
(3) again the granule that makes is placed granulator to carry out granulate to remove oversized particles with 16 mesh sieves; add through super-dry, pulverizing and through disintegrating agent, lubricant and the surfactant of 150 mesh sieves screening in described ratio subsequently; mix homogeneously; at last that the granule that is up to the standards is heavy according to the sheet that the granule content of measuring calculates, on tablet machine, carry out the dispersible tablet that tabletting is made compound glycyrrbizic acid list potassium.
Embodiment 11
Unit is in kilogram, and by glycyrrhizic acid list potassium: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 50: 70: 15: 60: 25: 15: 2.5: 5 amount takes by weighing each component respectively.Wherein: described aminoacid is that glycine mixes by 1: 1: 1 weight proportion with methionine, L-cysteine hydrochloride; Described antioxidative stabilizer is that vitamin C mixes by 1: 1 weight proportion with sodium sulfite; Described disintegrating agent is that crosslinked carboxymethyl fecula sodium mixes by 1: 1: 1 weight proportion with cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone; Described filler be modified starch with dextrin, calcium sulfate, microcrystalline Cellulose by 1: 1: 1: 1 weight proportion mixes; Described binding agent is that methylcellulose mixes by 1: 1: 1 weight proportion with sodium carboxymethyl cellulose, starch slurry; Described lubricant is that magnesium stearate is mixed by 1: 1 weight proportion with calcium stearate; Described surfactant is that sodium lauryl sulphate mixes by 1: 1 weight proportion with Stepanol MG.
The dispersible tablet for preparing compound glycyrrbizic acid list potassium with following steps:
(1) takes by weighing respectively by weight ratio and pulverize the back and, take by weighing in proportion simultaneously through super-dry, pulverizing and the filler and the binding agent that screen through 150 mesh sieves through glycyrrhizic acid list potassium, glycine and methionine, the antioxidative stabilizer of 200 mesh sieves screening;
(2) above-mentioned supplementary material is placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulate with 20 mesh sieves at granulator then;
(3) again the granule that makes is placed granulator to carry out granulate to remove oversized particles with 16 mesh sieves; add the L-CYSTEAMINE HCL granulates that makes with an amount of cellulose family binding agent alcoholic solution in described ratio subsequently; add again through super-dry, pulverizing and through disintegrating agent, lubricant and the surfactant mix homogeneously of 150 mesh sieves screening; at last that the granule that is up to the standards is heavy according to the sheet that the granule content of measuring calculates, on tablet machine, carry out the dispersible tablet that tabletting is made compound glycyrrbizic acid list potassium.
Claims (10)
1. the dispersible tablet of compound glycyrrbizic acid and salt thereof, it is characterized in that forming: glycyrrhizic acid or glycyrrhetate or its lipid ligand by following component, aminoacid, and antioxidative stabilizer, two or more in disintegrating agent, filler, binding agent, lubricant, the surfactant or whole; Wherein, described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 20～110: 10～370: 1～15: 20～70: 15～25: 10～15: 1～2.5: 1～5.
2. the dispersible tablet of compound glycyrrbizic acid according to claim 1 and salt thereof is characterized in that: described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 30～45: 30～55: 5～12: 20～40: 18～23: 10～13: 2～2.5: 1～4.
3. the dispersible tablet of compound glycyrrbizic acid according to claim 2 and salt thereof is characterized in that: described component glycyrrhizic acid or glycyrrhetate or its lipid ligand: aminoacid: antioxidative stabilizer: disintegrating agent: filler: binding agent: lubricant: the weight proportion of surfactant is: 35: 50: 8.82: 20: 20: 10: 2.5: 3.
4. according to the dispersible tablet of claim 1,2 or 3 described compound glycyrrbizic acids and salt thereof, it is characterized in that: described glycyrrhetate is one of potassium salt, ammonium salt, magnesium salt, sodium salt, zinc salt of glycyrrhizic acid; Described aminoacid is that arbitrary proportion mixes between one of glycine, L-cysteine hydrochloride, methionine, lysine, arginine, Aspartic Acid or its both or the many persons; Described antioxidative stabilizer is that arbitrary proportion mixes between one of vitamin C, sodium sulfite, sodium sulfite or its both or the many persons; Described disintegrating agent is that arbitrary proportion mixes between one of hydroxypropyl starch, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, soluble starch or its both or the many persons; Described filler is that arbitrary proportion mixes between one of lactose, mannitol, sorbitol, starch, modified starch, dextrin, calcium sulfate, microcrystalline Cellulose or its both or the many persons; Described binding agent is that arbitrary proportion mixes between one of polyvinylpyrrolidone, hypromellose, methylcellulose, sodium carboxymethyl cellulose, starch slurry, syrup, rubber cement or its both or the many persons; Described lubricant is that arbitrary proportion mixes between one of magnesium stearate, calcium stearate, Polyethylene Glycol, micropowder silica gel, Pulvis Talci or its both or the many persons; Described surfactant is that arbitrary proportion mixes between one of Stepanol MG, sodium lauryl sulphate, Polysorbate, poloxamer or its both or the many persons.
5. the dispersible tablet of compound glycyrrbizic acid according to claim 4 and salt thereof is characterized in that: described glycyrrhetate is the potassium salt or the ammonium salt of glycyrrhizic acid; Described aminoacid is that arbitrary proportion mixes between one of glycine, L-cysteine hydrochloride, methionine or its both or the many persons; Described antioxidative stabilizer is one of vitamin C, sodium sulfite or its arbitrary proportion mixing between the two; Described disintegrating agent is that arbitrary proportion mixes between one of hydroxypropyl starch, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, carboxymethylcellulose calcium, soluble starch or its both or the many persons; Described filler is that arbitrary proportion mixes between one of lactose, mannitol, sorbitol, starch, microcrystalline Cellulose or its both or the many persons; Described binding agent is that arbitrary proportion mixes between one of polyvinylpyrrolidone, hypromellose, methylcellulose, syrup or its both or the many persons; Described lubricant is that arbitrary proportion mixes between one of magnesium stearate, calcium stearate, micropowder silica gel or its both or the many persons; Described surfactant is one of Stepanol MG, sodium lauryl sulphate or its arbitrary proportion mixing between the two.
6. the dispersible tablet of compound glycyrrbizic acid according to claim 5 and salt thereof is characterized in that: described glycyrrhetate is a potassium glycyrrhizana; Described aminoacid be one of glycine, methionine or its both mix by equal proportion.
7. the dispersible tablet of compound glycyrrbizic acid according to claim 6 and salt thereof is characterized in that: described potassium glycyrrhizana is glycyrrhizic acid list potassium or glycyrrhizic acid dipotassium.
8. the dispersible tablet of compound glycyrrbizic acid according to claim 6 and salt thereof is characterized in that: described aminoacid is that glycine mixes by 1: 1 weight proportion with methionine.
9. the preparation method of the dispersible tablet of described compound glycyrrbizic acid of one of claim 1～3 and salt thereof, finish by following steps:
(1) takes by weighing respectively by weight ratio and pulverize the back and, take by weighing in proportion simultaneously through super-dry, pulverizing and through the filler and the binding agent of 150 mesh sieves screening through the glycyrrhizic acid of 200 mesh sieves screening or glycyrrhetate or glycyrrhizinate lipid ligand, aminoacid, antioxidative stabilizer;
(2) above-mentioned supplementary material is placed the mixer mix homogeneously, and tablet forming focuses on the Φ 15mm thin slice between 300～400mg, granulate with 20 mesh sieves at granulator then;
(3) again the granule that makes is placed granulator to carry out granulate to remove oversized particles with 16 mesh sieves; add through super-dry, pulverizing and through disintegrating agent, lubricant and the surfactant of 150 mesh sieves screening in described ratio subsequently; mix homogeneously; at last that the granule that is up to the standards is heavy according to the sheet that the granule content of measuring calculates, on tablet machine, carry out the dispersible tablet that tabletting is made compound glycyrrbizic acid and salt thereof.
10. the preparation method of the dispersible tablet of compound glycyrrbizic acid according to claim 9 and salt thereof; it is characterized in that: the L-cysteine hydrochloride composition of the easy oxidation deterioration of end-on air; separately its coating is granulated with the alcoholic solution of convention amount cellulose family binding agent, and then with other granule mixing film-making.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100444328A CN100386086C (en) | 2006-03-09 | 2006-03-09 | Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100444328A CN100386086C (en) | 2006-03-09 | 2006-03-09 | Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1857289A true CN1857289A (en) | 2006-11-08 |
| CN100386086C CN100386086C (en) | 2008-05-07 |
Family
ID=37296277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100444328A Expired - Fee Related CN100386086C (en) | 2006-03-09 | 2006-03-09 | Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100386086C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106214656A (en) * | 2016-08-31 | 2016-12-14 | 江苏鹏鹞药业有限公司 | The preparation of a kind of compound tablet of glycyrrhizin and test method of quality control |
| CN108210467A (en) * | 2018-02-05 | 2018-06-29 | 湖南博隽生物医药有限公司 | A kind of pharmaceutical composition for treating cardiovascular and cerebrovascular and preparation method thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002049607A2 (en) * | 2000-12-20 | 2002-06-27 | Firmenich Sa | Flavoured oral drug delivery system |
| CN1507862A (en) * | 2002-12-19 | 2004-06-30 | 洁 严 | Complex acetaminophen vitamin C dispersion tablet and preparing method thereof |
| CN100444846C (en) * | 2003-11-19 | 2008-12-24 | 山西亚宝药业集团股份有限公司 | Dispersion tablet contg. Gynostemma petaphylla total glucosides, and its prepn. method |
-
2006
- 2006-03-09 CN CNB2006100444328A patent/CN100386086C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106214656A (en) * | 2016-08-31 | 2016-12-14 | 江苏鹏鹞药业有限公司 | The preparation of a kind of compound tablet of glycyrrhizin and test method of quality control |
| CN108210467A (en) * | 2018-02-05 | 2018-06-29 | 湖南博隽生物医药有限公司 | A kind of pharmaceutical composition for treating cardiovascular and cerebrovascular and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100386086C (en) | 2008-05-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1954814A (en) | Medical composite with co-action for treating gout and its preparation method | |
| CN101862305B (en) | Ambroxol hydrochloride sustained-release pellet and preparation method | |
| CN1911954A (en) | Glycyrrhizic acid derivative having amino acid, its preparation method and medicinal composition containing them | |
| CN1742741A (en) | Medicinal composition containing amino glucose and calcium agent and vitamin D and use thereof | |
| CN102416003A (en) | Method for preparing entecavir tablets | |
| CN1903183A (en) | Dispersion tablets of telbivudine and its prepn. method | |
| CN1857289A (en) | Dispersed compound tablet of glycyrrhizic acid and glycyrrhizinate and its preparing process | |
| CN1989960A (en) | Andrographolide dispersed tablet | |
| CN1225464C (en) | Extraction technology of Hanbaicalein, medicinal composition and preparation technology of medicine | |
| CN1686151A (en) | Enteric dissolving preparation of compound glycyrrbizic acid and its salt and its preparation method | |
| CN1903208A (en) | Adefovir dipivoxil oral disintegration tablets medicine prepn., and prepn. method therefor | |
| CN1813769A (en) | Ciclesonide oral ulcer paster and its preparing method | |
| CN1408427A (en) | Reduced type glutathione lozenge | |
| CN1724034A (en) | Vagina effervescent tablets contg. callicarpa nudiflora, and its prepn. method | |
| CN1319533C (en) | Cefetamet pivoxil hydrochloride dispersion dispersion tablets and preparation method | |
| CN1704062A (en) | Sustained release tablet of oleanolic acid and its preparation method | |
| CN1839847A (en) | Tizanidine hydrochloride oral disintegrating tablet and preparation method thereof | |
| CN1709343A (en) | Medicinal composition for protecting liver, and its formulation preparing method | |
| CN1314400C (en) | Solid preparation taken through oral cavity of compound MEthoxyphEnaminE and preparation method | |
| CN101288651A (en) | Compound glycyrrhizin dispersible tablet and preparation method thereof | |
| CN1768751A (en) | Method for preparing 'Fen Ma Mei Yu' dispersible tablet | |
| CN1287797C (en) | Gancilorvir dispersable tablet and its preparation | |
| CN1857290A (en) | Oral disintegrant preparation of glycyrrihizic acid and glycyrrhizinate and its preparing process | |
| CN100335058C (en) | Composition and tablet of mifepristone and anorethidrane dipropionate | |
| CN1839835A (en) | Lacidipine pharmaceutical formulation preparing method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20080507 Termination date: 20100309 |