CN103156814B - A kind of Azithromycin enteric composition and preparation method - Google Patents
A kind of Azithromycin enteric composition and preparation method Download PDFInfo
- Publication number
- CN103156814B CN103156814B CN201110408338.7A CN201110408338A CN103156814B CN 103156814 B CN103156814 B CN 103156814B CN 201110408338 A CN201110408338 A CN 201110408338A CN 103156814 B CN103156814 B CN 103156814B
- Authority
- CN
- China
- Prior art keywords
- enteric
- coating
- weight portion
- azithromycin
- thing
- 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.)
- Active
Links
Abstract
The present invention discloses Azithromycin enteric composition of a kind of energy rapid dispersion release medicine in intestinal and preparation method thereof.The raw material of this pharmaceutical composition consists of: azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, hypromellose, sodium lauryl sulphate, polyethylene pyrrole alkane ketone, magnesium stearate etc.The preparation method of Azithromycin enteric tablet of the present invention, for medicine and pharmaceutical excipient are carried out tabletting after treatment, is carried out enteric coating by label and is formed.Azithromycin enteric composition of the present invention; well can be protected under gastric acid condition; available protecting medicine is from the destruction of gastric acid; and (phosphate buffer PH6.8) can reach the feature of dispersible tablet under intestinal juice condition; rapid delivery of pharmaceuticals in intestinal, improves bioavailability.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition and preparation method thereof, particularly a kind of can Azithromycin enteric composition and preparation method thereof of rapid dispersion release medicine in intestinal.
Background technology
Azithromycin is a kind of fifteen-membered ring macrolide antibiotics derived by erythromycin, and this kind of nitrogenous 15 membered ring compounds have stronger alkalescence, and have larger activity to many gram negative bacilli, concentration is higher in the tissue, and Half-life in vivo is long.On Antibacterial Mechanism, have common point with erythromycin, be all combined by ribosome 50S subunit in bacterial cell, hinder antibacterial to turn peptide process, suppression depends on the synthesis of the protein of RNA and reaches antibacterial action.But due to the change of structure, azithromycin has antimicrobial spectrum widely than erythromycin, multiple gram positive coccus, mycoplasma, chlamydia and legionella pneumophilia can be suppressed, especially to some important gram negative bacilli such as hemophilus influenzas etc., there is good antibacterial activity, compensate for the deficiency of Macrolide to haemophilus effect difference.Be mainly used in the transmissible disease caused by the respiratory tract caused by sensitive organism, skin soft-tissue infection and chlamydia.Current azithromycin is sure to occupy medicine tap in macrolide with the advantage of himself uniqueness.
Current azithromycin listing dosage form is more, has conventional tablet, dispersible tablet, capsule, granule, dry suspension, enteric coatel tablets, injection etc.A large amount of research data document shows that azithromycin is unstable under gastric acid environment in the recent period, 30min degraded 68% in 0.1mol/L hydrochloric acid solution, cause bioavailability on the low side, and the side reaction of this kind of macrolide antibiotics ubiquity gastrointestinal, the discomfort such as easily cause that patient vomits, main cause is its stimulation to stomach.For reducing medicine to the stimulation of stomach, and ensure that azithromycin avoids the destruction of gastric acid, the enteric coated preparation of this medicine becomes development trend.
The patent application of this medicament enteric-coated formulation aspect is more at present, domestic had Azithromycin enteric sheet and enteric coated capsule listing, but such enteric coated preparation discharged slow, usually there is bioavailability in body lower, absorb poor at colon site, the deficiency of the aspects such as onset is slow, the invention of relevant Azithromycin enteric casing preparation patent, but still bioavailability may be caused on the low side.
Patent CN1602888A (publication date on April 6th, 2005) discloses Azithromycin enteric casing preparation and preparation method thereof, the soft just granule after drying of the conventional preparation of the method is as starting material, enteric coatedly after tabletting make enteric coatel tablets for Opadry-93018359, or Starting Particle is filled in enteric capsule shell, because of the impact by Opadry material and enteric capsule shell, the method may cause bioavailability too low.Patent 1569021A discloses a kind of Azithromycin enteric casing preparation and preparation method thereof; it adopts conventional material and preparation method carry out the granulation of core material or make micropill; this method can cause its release slow; particularly make micropill and make enteric coated preparation more later; the drug release process of micropill can be increased, affect drug absorption.The selection of its enteric material can cause medicine to arrive intestinal release later not in time, and bioavailability may be caused too low.Patent CN101991544 discloses a kind of Azithromycin enteric dry suspension and preparation method thereof; this patent is put in coating granulator by azithromycin granule; carry out enteric coating again after carrying out isolation coat to granule, the enteric coated particles of gained adds a large amount of correctivess and suspending agent etc. and mixes and get final product.Although likely improve drug release rate; accelerate drug effect and improve bioavailability; but because the specific surface area of this technique drug particles is too large; complicated process of preparation; need relatively large use coating material, and coatings protect is incomplete, there is bitterness; a large amount of correctivess and suspending agent need be added, there is the shortcoming that medicine can not be effectively protected in gastric acid and dosage is larger.
Therefore, still need a kind of new Azithromycin enteric casing preparation at present, both can not produce stomach stimulates, the advantageous feature that can possess again dispersible tablet namely in intestinal disintegrate rapidly, absorb fast, bioavailability is high.
Summary of the invention
The object of the present invention is to provide a kind of Azithromycin enteric composition, another object of the present invention is the preparation method providing a kind of Azithromycin enteric composition.
The present invention seeks to be achieved through the following technical solutions
The raw material of pharmaceutical composition of the present invention consists of:
Azithromycin 100 weight starch 0 ~ 50 weight portion
Lactose 0 ~ 30 weight portion microcrystalline Cellulose 0 ~ 70 weight portion
Carboxymethylstach sodium 0 ~ 20 weight portion cross-linking sodium carboxymethyl cellulose 0 ~ 30 weight portion
Polyvinylpolypyrrolidone 0 ~ 30 weight portion hypromellose 0 ~ 30 weight portion
Sodium lauryl sulphate 0 ~ 3 weight account polyethylene pyrrole alkane ketone 0 ~ 10 weight portion
Micropowder silica gel 0 ~ 50 weight portion magnesium stearate 0.5 ~ 5 weight portion.
The preferred weight proportioning of above-mentioned raw materials is as follows:
Azithromycin 100 parts by weight of lactose 10 ~ 30 weight portion microcrystalline Cellulose 40 ~ 60 weight portion
Carboxymethylstach sodium 3 ~ 15 weight portion cross-linking sodium carboxymethyl cellulose 5 ~ 20 weight portion
Hypromellose 10 ~ 30 weight portion sodium lauryl sulphate 0.5 ~ 2.5 weight portion
Polyethylene pyrrole alkane ketone 4 ~ 10 weight portion magnesium stearate 0.5 ~ 3 weight portion.
The preferred weight proportioning of above-mentioned raw materials is as follows:
Azithromycin 100 parts by weight of lactose 18 ~ 22 weight portion
Microcrystalline Cellulose 45 ~ 55 weight portion carboxymethylstach sodium 8 ~ 10 weight portion
Hypromellose 25 ~ 30 weight portion sodium lauryl sulphate 1 ~ 2 weight portion
Polyethylene pyrrole alkane ketone 6 ~ 8 weight portion magnesium stearate 1 ~ 2 weight portion.
The preferred weight proportioning of above-mentioned raw materials is as follows:
Azithromycin 100 parts by weight of lactose 20 weight portion
Microcrystalline Cellulose 50 weight portion carboxymethylstach sodium 9 weight portion
Hypromellose 27.5 weight portion sodium lauryl sulphate 1.5 weight portion
Polyethylene pyrrole alkane ketone 7 weight portion magnesium stearate 1.5 weight portion.
Get combinations thereof raw material, add customary adjuvant, conveniently technique, make tablet.
Enteric coatel tablets made by the material that pharmaceutical composition of the present invention adds following weight portion:
Enteric material contains thing 10 weight portion admittedly, antiplastering aid 2 ~ 10 weight portion, plasticizer 1 ~ 7 weight portion.
Preferred weight proportioning is as follows: enteric material contains thing 10 weight portion admittedly, antiplastering aid 6 weight portion, and plasticizer 4 weight portion or enteric material are admittedly containing thing 10 weight portion, antiplastering aid 3 weight portion, plasticizer 6 weight portion or enteric material contain thing 10 weight portion admittedly, antiplastering aid 9 weight portion, plasticizer 2 weight portion.
Described enteric material is methacrylic acid and ethyl acrylate copolymer (especially strange L30D-55 or claim Eudragit L100-55) or methacrylic acid and methylmethacrylate copolymer (especially strange L100) or two kinds of mixture containing thing admittedly.
Described antiplastering aid is one or more in Pulvis Talci, magnesium stearate or micropowder silica gel.
Described plasticizer is one or more in triethyl citrate, SA dibutyl ester, propylene glycol.
The concrete preparation technology of medicinal composition tablets of the present invention is as follows:
A. the making step of label: a. gets azithromycin, starch, lactose, microcrystalline Cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, hypromellose, micropowder silica gel, crosses 80 ~ 120 mesh sieves, mix homogeneously respectively; B. get polyethylene pyrrole alkane ketone join in the solution of 50% ethanol, to make containing polyethylene pyrrole alkane ketone be the concentration of 5%, and add sodium lauryl sulphate and dissolve, as binding agent; C. be used for by binding agent making soft ability in a, 16 ~ 24 mesh sieves are granulated, and granule puts 50 ~ 70 DEG C of drying 2 ~ 4h, and 18 ~ 24 mesh sieves are granulated, additional 0 ~ 12 weight portion micropowder silica gel, 0 ~ 5 weight portion hypromellose and magnesium stearate mixing, and tabletting, obtains label;
B. the making step of enteric coating: a. gets enteric material, antiplastering aid and plasticizer, add water and stir evenly, be mixed with the coating solution containing enteric material (admittedly containing thing) 10% ~ 20%, or add alcoholic solution and be mixed with suspendible coating solution containing enteric material (admittedly containing thing) 3% ~ 10%; B. get label set high effect coating pan in carry out coating, coating weight gain is 2% ~ 12%.
The preferred preparation technology of medicinal composition tablets of the present invention is as follows:
A. the making step of label: a. gets azithromycin, starch, lactose, microcrystalline Cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, hypromellose, micropowder silica gel, crosses 100 mesh sieves, mix homogeneously respectively; B. get polyethylene pyrrole alkane ketone join in the solution of 50% ethanol, to make containing polyethylene pyrrole alkane ketone be the concentration of 5%, and add sodium lauryl sulphate and dissolve, as binding agent; C. be used for by binding agent making soft ability in a, 20 mesh sieves are granulated, and granule puts 60 DEG C of dry 3h, and 20 mesh sieves are granulated, additional 0 ~ 6 weight portion micropowder silica gel and magnesium stearate mixing, and tabletting, obtains label;
B. the making step of enteric coating: a. gets enteric material, antiplastering aid and plasticizer, add water and stir evenly, be mixed with the coating solution containing enteric material (admittedly containing thing) 15%, or add alcoholic solution and be mixed with suspendible coating solution containing enteric material (admittedly containing thing) 6%; B. get label set high effect coating pan in carry out coating, coating weight gain is 5%.
Azithromycin enteric composition of the present invention; well can be protected under gastric acid condition; available protecting medicine is from the destruction of gastric acid; and (phosphate buffer PH6.8) can reach the feature of dispersible tablet under intestinal juice condition; rapid delivery of pharmaceuticals in intestinal, improves bioavailability.With the Azithromycin enteric tablet that the inventive method is obtained, taking convenience, covers bad bitterness, increases medicine stability, can not be subject to stomach acids destroy by available protecting medicine in the hydrochloric acid solution of 0.1mol/L, can rapid delivery of pharmaceuticals in simulated intestinal fluid.
Following experimental example and embodiment are used for further illustrating but are not limited to the present invention.
Experimental example 1: release experiment in acid
Measure with reference to Chinese Pharmacopoeia 2010 editions two (annex XC second method), with the hydrochloric acid solution 900ml of 0.1mol/L for dissolution medium, temperature (37 ± 0.5 DEG C), rotating speed 50r/min.Medicinal composition tablets of the present invention 6 prepared by Example 11 is put in stripping rotor respectively and is measured, draw solution 10ml after 2h, getting subsequent filtrate adopts high performance liquid chromatography to carry out the assay of azithromycin, another precision takes azithromycin reference substance, the solution product liquid in contrast of 0.2mg/ml is made with mobile phase dilution, be measured in the same method, calculate release, should 10% be less than by release regulation in the acid of Chinese Pharmacopoeia enteric coated preparation.Its chromatographic condition is: be filler with octadecylsilane chemically bonded silica; With phosphate buffer (get 0.05mol/L dipotassium hydrogen phosphate solution, the phosphoric acid solution with 20% regulates pH value to 8.2) ,-acetonitrile (45: 55) is mobile phase; Determined wavelength is 210nm; Flow velocity: 1.0ml/min; Sample size: 20 μ l; Measurement result is: the release of azithromycin of the present invention in acid after 2h is 2.1%.
Experimental example 2: the release experiment in artificial enteric liquid
A, the release medium in release experiment in acid (experimental example 1) is changed into simulated intestinal fluid (phosphate buffer PH6.8), other experimental techniques remain unchanged, and investigate and contrast the release profiles of other Azithromycin enteric sheets in simulated intestinal fluid.Experimental result is as follows:
B, the release medium in release experiment in acid is changed into phosphate buffer PH7.8 ~ 8.0, and (get dipotassium hydrogen phosphate 5.59g and potassium dihydrogen phosphate 0.41g, 1000ml is made in the dilution that is dissolved in water, and to obtain final product.), other experimental techniques remain unchanged, and investigate and contrast the release profiles of other Azithromycin enteric sheets in simulated intestinal fluid.Experimental result is as follows:
Experimental example 3: finely dispersed test in simulated intestinal fluid
With reference to the assay method of Chinese Pharmacopoeia dispersed homogeneous degree, medicinal composition tablets of the present invention 6 prepared by Example 11, put in 250ml beaker, add simulated intestinal fluid (phosphate buffer PH6.8) 100ml or phosphate buffer (PH7.8 ~ 8.0) 100ml of 15 ~ 25 DEG C, jolt 3min, investigate and whether all disintegrate also can pass through No. two sieves, and compare with commercially available enteric coatel tablets and dispersible tablet.Experimental result is as follows:
Illustrate that azithromycin of the present invention can reach the requirement of dispersible tablet under the condition of simulated intestinal fluid (phosphate buffer PH6.8) and phosphate buffer (PH7.8 ~ 8.0), more can disperse than other enteric coatel tablets, fast release thing.
Following embodiment all can realize the effect described in above-mentioned experimental example.
Embodiment 1:
Core formulation and preparation:
Azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium are crossed 100 mesh sieves respectively, mix homogeneously; The solution of 5% made by polyvidone 50% ethanol; After the soft ability of 5%PVP alcoholic solution system, 18 ~ 24 mesh sieves are granulated, and granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Get enteric material, antiplastering aid and plasticizer, add water and stir evenly, with the abundant homogenize 20min of high speed shear refiner, be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 15.9%, get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 2:
Core formulation and preparation:
Azithromycin, micropowder silica gel, microcrystalline Cellulose, carboxymethylstach sodium, polyvidone are crossed 100 mesh sieves respectively, mix homogeneously; After the soft ability of 50% alcoholic solution system, 18 ~ 24 mesh sieves are granulated, and granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Get in enteric material solution 500g dissolving, add triethyl citrate, in addition Pulvis Talci is poured in remaining solvent, shear 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 3:
Core formulation and preparation:
Azithromycin, starch, microcrystalline Cellulose, micropowder silica gel are crossed 100 mesh sieves respectively, mix homogeneously (inside adding micropowder silica gel 140g); Sodium lauryl sulphate makes the solution of 0.5% with 50% ethanol and after making soft ability with it, 18 ~ 24 mesh sieves are granulated, and granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, additional micropowder silica gel (60g) and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Get in enteric material solution 500g dissolving, add triethyl citrate, in addition Pulvis Talci is poured in remaining solvent, shear 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 2%.
Embodiment 4:
Core formulation and preparation:
Azithromycin, starch, lactose, microcrystalline Cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, hypromellose are crossed 100 mesh sieves respectively, mix homogeneously; The soft ability of povidone solution system of 50% alcoholic solution preparation 5%, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g water, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, magnesium stearate is poured in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 18%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 5:
Core formulation and preparation:
Azithromycin, starch, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate are crossed 100 mesh sieves respectively, mix homogeneously; The soft ability of povidone solution system of 50% alcoholic solution preparation 5%, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g ethanol, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, magnesium stearate is poured in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 6:
Core formulation and preparation:
Azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate are crossed 100 mesh sieves respectively, mix homogeneously; The soft ability of 50% alcoholic solution system, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g water, with the abundant homogenize 10min of high speed shear refiner, adds SA dibutyl ester, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 16%.Get label set high effect coating pan in carry out coating, control coating weight gain be 7%.
Embodiment 7:
Core formulation and preparation:
Azithromycin, starch, carboxymethylstach sodium, sodium lauryl sulphate, micropowder silica gel are crossed 100 mesh sieves respectively, mix homogeneously; The soft ability of povidone solution system of 50% ethanol preparation 5%, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g water, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 16%.Get label set high effect coating pan in carry out coating, control coating weight gain be 6%.
Embodiment 8:
Core formulation and preparation:
Get azithromycin, starch, lactose, microcrystalline Cellulose, polyvinylpolypyrrolidone and cross 100 mesh sieves respectively, mix homogeneously; The soft ability of 50% alcoholic solution system, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel, hypromellose and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g95% ethanol, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly.Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 9:
Core formulation and preparation:
Get azithromycin, starch, lactose, microcrystalline Cellulose, polyvinylpolypyrrolidone and cross 100 mesh sieves respectively, mix homogeneously; The soft ability of 50% alcoholic solution system, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel, hypromellose and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Get enteric material, antiplastering aid and plasticizer, add water and stir evenly, with the abundant homogenize 20min of high speed shear refiner, be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 15.9%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 10:
Core formulation and preparation:
Get azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, cross-linking sodium carboxymethyl cellulose and cross 100 mesh sieves respectively, mix homogeneously; The soft ability of sodium dodecyl sulfate solution system of 50% ethanol preparation 0.75%, soft just with 18 ~ 24 mesh sieves granulations, granule puts 60 DEG C of drying 2 ~ 4h, 18 ~ 24 mesh sieve granulate, and additional micropowder silica gel, polyvinylpolypyrrolidone and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g solvent, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly, be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 10%.
Embodiment 11:
Core formulation and preparation:
Get azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, hypromellose and cross 100 mesh sieves respectively, mix homogeneously; Get recipe quantity polyethylene pyrrole alkane ketone and sodium lauryl sulphate be added to as the soft ability of binding agent system in 50% alcoholic solution of 140ml, softly just granulate with 20 mesh sieves, granule puts 60 DEG C of dry 3h, 20 mesh sieve granulate, and additional magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g solvent, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min; By two liquid mixing, fully stir evenly; Be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 15%; Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 12:
Core formulation and preparation:
Get azithromycin, starch, lactose, microcrystalline Cellulose, polyvinylpolypyrrolidone and cross 100 mesh sieves respectively, mix homogeneously; The soft ability of 50% alcoholic solution system, soft just with 18 mesh sieves granulations, granule puts 65 DEG C of dry 4h, 18 mesh sieve granulate, and additional micropowder silica gel, hypromellose and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g95% ethanol, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, is poured into by Pulvis Talci in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly, be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Embodiment 13:
Core formulation and preparation:
Azithromycin, starch, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate are crossed 100 mesh sieves respectively, mix homogeneously; The soft ability of povidone solution system of 50% alcoholic solution preparation 5%, soft just with 24 mesh sieves granulations, granule puts 55 DEG C of dry 2h, 24 mesh sieve granulate, and additional micropowder silica gel and magnesium stearate mixing, tabletting, obtains label.
Enteric coating:
Getting enteric material puts in 500g ethanol, with the abundant homogenize 10min of high speed shear refiner, adds triethyl citrate, continues to shear 20min, magnesium stearate is poured in addition in remaining solvent, shears 10min.By two liquid mixing, fully stir evenly, be mixed with the coating solution containing enteric material (polymer is admittedly containing thing) 6%.Get label set high effect coating pan in carry out coating, control coating weight gain be 5%.
Claims (4)
1. an Azithromycin enteric composition, is characterized in that the raw material of said composition consists of:
It is methacrylic acid and ethyl acrylate copolymer that described enteric material contains thing admittedly; Antiplastering aid is one or more in Pulvis Talci, magnesium stearate or micropowder silica gel; Plasticizer is one or more in triethyl citrate, dibutyl sebacate, propylene glycol;
The preparation method of described Azithromycin enteric composition is:
A. the making step of label: a. gets azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, hypromellose, crosses 100 mesh sieves, mix homogeneously respectively; B. get polyethylene pyrrole alkane ketone join in the solution of 50% ethanol, to make containing polyethylene pyrrole alkane ketone be the concentration of 5%, and add sodium lauryl sulphate and dissolve, as binding agent; C. binding agent is used for soft material processed in a, 20 mesh sieves are granulated, and granule puts 60 DEG C of dry 3h, and 20 mesh sieves are granulated, additional magnesium stearate mixing, and tabletting, obtains label;
B. the making step of enteric coating: a. gets enteric material admittedly containing thing, antiplastering aid and plasticizer, adds water and stirs evenly, and is mixed with containing enteric material admittedly containing the coating solution of thing 15%, or adds alcoholic solution and be mixed with containing enteric material admittedly containing the suspendible coating solution of thing 6%; B. get label set high effect coating pan in carry out coating, coating weight gain is 5%.
2. compositions as claimed in claim 1, is characterized in that:
3. compositions as claimed in claim 1, it is characterized in that enteric material admittedly containing thing 10 weight portion, antiplastering aid 6 weight portion, plasticizer 4 weight portion or enteric material are admittedly containing thing 10 weight portion, antiplastering aid 3 weight portion, plasticizer 6 weight portion or enteric material contain thing 10 weight portion admittedly, antiplastering aid 9 weight portion, plasticizer 2 weight portion.
4. the preparation method of compositions as claimed in claim 3, is characterized in that the method is:
A. the making step of label: a. gets azithromycin, lactose, microcrystalline Cellulose, carboxymethylstach sodium, hypromellose, crosses 100 mesh sieves, mix homogeneously respectively; B. get polyethylene pyrrole alkane ketone join in the solution of 50% ethanol, to make containing polyethylene pyrrole alkane ketone be the concentration of 5%, and add sodium lauryl sulphate and dissolve, as binding agent; C. binding agent is used for soft material processed in a, 20 mesh sieves are granulated, and granule puts 60 DEG C of dry 3h, and 20 mesh sieves are granulated, additional magnesium stearate mixing, and tabletting, obtains label;
B. the making step of enteric coating: a. gets enteric material admittedly containing thing, antiplastering aid and plasticizer, adds water and stirs evenly, and is mixed with containing enteric material admittedly containing the coating solution of thing 15%, or adds alcoholic solution and be mixed with containing enteric material admittedly containing the suspendible coating solution of thing 6%; B. get label set high effect coating pan in carry out coating, coating weight gain is 5%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110408338.7A CN103156814B (en) | 2011-12-09 | 2011-12-09 | A kind of Azithromycin enteric composition and preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110408338.7A CN103156814B (en) | 2011-12-09 | 2011-12-09 | A kind of Azithromycin enteric composition and preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103156814A CN103156814A (en) | 2013-06-19 |
| CN103156814B true CN103156814B (en) | 2015-11-25 |
Family
ID=48580683
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201110408338.7A Active CN103156814B (en) | 2011-12-09 | 2011-12-09 | A kind of Azithromycin enteric composition and preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103156814B (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107582538A (en) * | 2017-06-01 | 2018-01-16 | 合肥远志医药科技开发有限公司 | Azithromycin capsule and preparation method thereof |
| CN107281155B (en) * | 2017-06-06 | 2020-04-10 | 扬子江药业集团四川海蓉药业有限公司 | Azithromycin tablet and preparation method thereof |
| CN110882228A (en) * | 2019-11-29 | 2020-03-17 | 南京禾瀚医药科技有限公司 | Epiputidine enteric-coated preparation |
| CN111228233A (en) * | 2020-03-11 | 2020-06-05 | 正大青春宝药业有限公司 | Coating composition for preparing perhexiline enteric-coated tablets and application thereof |
| CN112656774A (en) * | 2020-12-26 | 2021-04-16 | 海南葫芦娃药业集团股份有限公司 | Azithromycin enteric capsule and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1569021A (en) * | 2004-04-23 | 2005-01-26 | 石家庄制药集团欧意药业有限公司 | Enteric-coated azithromycin preparation and its preparing process |
| CN1602888A (en) * | 2004-07-30 | 2005-04-06 | 浙江大德药业集团有限公司 | Azithromycin enteric casing preparation and its preparing process |
-
2011
- 2011-12-09 CN CN201110408338.7A patent/CN103156814B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1569021A (en) * | 2004-04-23 | 2005-01-26 | 石家庄制药集团欧意药业有限公司 | Enteric-coated azithromycin preparation and its preparing process |
| CN1602888A (en) * | 2004-07-30 | 2005-04-06 | 浙江大德药业集团有限公司 | Azithromycin enteric casing preparation and its preparing process |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103156814A (en) | 2013-06-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2093148C1 (en) | Composition exhibiting the delayed (prolonged) releasing | |
| RU2646825C2 (en) | Pharmaceutical form for drug delivery to the colon | |
| US20050025825A1 (en) | Tranexamic acid formulations with reduced adverse effects | |
| CN103156814B (en) | A kind of Azithromycin enteric composition and preparation method | |
| CN101969964A (en) | Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules | |
| CN104271113A (en) | A delayed release drug formulation | |
| CN103845335A (en) | Gefitinib medicinal composition and tablet containing gefitinib medicinal composition | |
| CN105979936A (en) | Pregabalin sustained-release preparation | |
| WO1997033574A1 (en) | Sustained-release metal valproate tablets | |
| CN103520169B (en) | Mirtazapine tablet and preparation method thereof | |
| CN101347413B (en) | Quetiapine sustained release tablets and method of preparing the same | |
| US20240082168A1 (en) | Controlled drug release formulation | |
| CN1771913B (en) | Emulifying solvent diffusing process for preparing taste masked micro ball | |
| CN105343028A (en) | Medicine composition with norfloxacin and method for preparing medicine composition | |
| CN105878256A (en) | Controlled-release preparation containing metformin hydrochloride and glimepiride and preparation method of controlled-release preparation | |
| CN100525760C (en) | Duloxetine hydrochloride sustained release medicine | |
| CN102552190A (en) | Ilaprazole enteric coated tablet and preparation method thereof | |
| WO2009101658A1 (en) | Timed-release pharmaceutical preparation | |
| CN103405395B (en) | Sodium picosulfate enteric-coated tablet and preparation method thereof | |
| CN102727496A (en) | Compound antituberculosis drug oral solid preparation and its preparation method | |
| RU2440104C2 (en) | Coating composition containing starch | |
| CN102397262B (en) | Amoxicillin sustained release solid medicinal composition and preparation method thereof | |
| CN1232386A (en) | Colonic delivery of weak acid drugs | |
| TW200932289A (en) | Enteric sustained-release coated core and pharmaceutical dosage form and manufacturing method thereof | |
| JP4864024B2 (en) | Timed release formulation |
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 |