CN1709273A - Roxhthromycin soft capsule and its preparing method - Google Patents
Roxhthromycin soft capsule and its preparing method Download PDFInfo
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- CN1709273A CN1709273A CN 200410041018 CN200410041018A CN1709273A CN 1709273 A CN1709273 A CN 1709273A CN 200410041018 CN200410041018 CN 200410041018 CN 200410041018 A CN200410041018 A CN 200410041018A CN 1709273 A CN1709273 A CN 1709273A
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- roxithromycin
- soft capsule
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- antioxidant
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Abstract
The present invention relates to a roxithromycin soft capsule and its preparation method. In the invented roxithromycin soft capsule its liquid medicine contains roxithromycin with effective dose and medicinal auxiliary material. Said medicinal auxiliary material includes dilutent, antioxidant, solubilizing agent, solubility promoter and pH regulator. In the liquid medicine of every standard capsule 0.01-0.25g of roxithromycin is contained. Besides, said invention also provides the concrete steps of its preparation process.
Description
Technical field:
The futuramic Roxithromycin dosage form of the present invention soft capsule belongs to medical technical field.
Background technology:
Roxithromycin is the derivant of Erythromycin A, is a relative newer semi-synthetic macrolide antibiotics.At first go on the market in France in October, 1987.At present, use each big and medium-sized cities of China.Antibacterial range and erythromycin are close.Characteristics are stable to acid, and can be absorbed by gastrointestinal rapidly, have higher blood drug level, and antibacterial action is strong than erythromycin, and medicine is long action time in vivo, and the half-life (blood drug level reduces the time of half) is than long 8～10 times of erythromycin.Mainly discharge with the original shape medicine, do not have the property accumulated, took medicine in per 12 hours and just can keep effective blood drug concentration 1 time by excrement and urine.Major defect is the careful usefulness of hepatic insufficiency person.
Roxithromycin mainly acts on: 1. be used for the upper and lower respiratory tract infection due to Diplococcus pneumoniae, Hemolytic streptococcus, hemophilus influenza, mycoplasma, chlamydia, the legionella.2. be used for the treatment of acute pharyngitis, laryngitis, tonsillitis, sinusitis, and eye conjunctivitis of causing of chlamydia, oral cavity infection etc.3. be used for the treatment of urinary tract and genital infection due to the chlamydia, as urethritis, cervicitis, vaginitis etc.4. be used for the treatment of the skin infection that streptococcus or staphylococcus cause.As erysipelas, cellulitis, furuncle and phyma, lymphangitis etc.Points for attention: Roxithromycin is a kind of service time of short macrolide antibiotics, and its untoward reaction found gradually, as common feel sick, digestive tract reactions such as stomachache, diarrhoea.Because the Roxithromycin flavor is extremely bitter, domestic commercially available Roxithromycin dry suspension taste is also bitter, and the child is difficult for accepting, and develops a kind of new dosage form that is applicable to child's oral administration and necessitates.
Roxithromycin soft capsule of the present invention has following advantage:
Soft capsule improves bitterness----pharmaceutical pack is rolled in the capsule, covers the bitterness of medicine, is suitable for the child and uses.
Making things convenient for the soft capsule volume of medication----10mg of the present invention～250mg specification is 0.1～0.6ml, and wherein the soft capsule of 0.1～0.2ml is suitable for the child and uses.
Improve stability-pharmaceutical pack is rolled in the capsule, avoided the influence of moisture, air, light; Adopt non-aqueous solvent systems simultaneously, avoid the hydrolysis and the oxidation of medicine, protection reaches stablizes medicine.
Medicine is rapid-action in vivo--and-medicine dissolution discharges with breaking of capsule shells at gastrointestinal tract in The suitable solvent, and the medicine in the solution disperses rapidly and absorbs, and is rapid-action.
Therefore developing this product has great social significance and good market prospect.
Summary of the invention:
The novel form that the purpose of this invention is to provide a kind of Roxithromycin its objective is to make Roxithromycin can be prepared into soft capsule, can improve its curative effect in the treatment virus infection.
Medicinal soft capsule of the present invention is characterized in that: Roxithromycin is scattered in the The suitable solvent makes.Wherein solvent can be Macrogol 200-1000, propylene glycol, glycerol, soybean oil, Oleum Gossypii semen, Oleum Arachidis hypogaeae semen, Oleum Sesami, Semen Maydis oil, olive oil, oleic acid etc.; Also can add solubilizing agent, cosolvent, antioxidant, pH regulator agent etc.
1, soft capsule of the present invention also can be selected following adjuvant for use: diluent is as Macrogol 200-1000, propylene glycol, glycerol, Oleum Gossypii semen, Oleum Arachidis hypogaeae semen, Oleum Sesami, Semen Maydis oil, olive oil, oleic acid etc.; Solubilizing agent is as Tweens, pluronic F-68, polyoxyethylene ether Oleum Ricini, polyvidone, sodium cholate, sodium lauryl sulphate etc.; Antioxidant is as propyl gallate, di-tert-butyl hydroxy-methylbenzene (BHT), butylated hydroxyarisol (BHA), vitamin E, ascorbyl palmitate, sodium sulfite, sodium sulfite, sodium pyrosulfite, sodium thiosulfate, glycine, methionine, lysine, valine, arginine, leucine, isoleucine, tryptophan, glutathion etc.Cosolvent is as sodium sulfite, sodium carbonate, sodium bicarbonate, potassium dihydrogen phosphate, Ammonium biphosphate etc.; Amides compound such as carbamide, acetamide, nicotiamide, thiourea, Benzoylamide etc., amino acids such as arginine, aspartic acid, serine, glycine, methionine, histidine, glutamic acid, isoleucine, threonine, cysteine, cystine, tryptophan, phenylalanine, lysine, the chemical compound of hydroxyl or carboxyl such as sucrose, glucose, fructose, xylose, mannose, citric acid and sodium salt thereof, lactic acid, sodium salicylate etc.The pH regulator agent is tartaric acid, citric acid, glycine, cysteine, lactic acid etc.
The ratio of gelatin, glycerol and water can suitably be regulated in the glue shell, is advisable 1: 0.3～0.4: 0.7～1.4 as gelatin/glycerin/water three's ratio, also can add other compositions in the glue shell, as antiseptic: P-hydroxybenzoic acid first, second, third, butyl ester etc.; Plasticizer such as sorbitol etc.; Stabilizing agent such as arabic gum etc.; Opacifier is as titanium dioxide, barium sulfate, precipitated calcium carbonate etc.; Antioxidant such as amino acids; Pigment such as sunset yellow, lemon yellow, light blue, carmine etc.
Soft consumption with each composition of wafer is among the present invention: the mixed system 0.1-0.5ml of diluent such as Polyethylene Glycol (200-1000) and propylene glycol, suitable consumption are 0.1-0.4ml; The consumption of solubilizing agent such as Tween 80 is 0.0%--30.0%, and suitable consumption is 1.0%--20.0%; The consumption of cosolvent such as polyvidone is 1.0%--100.0%, and suitable consumption is 10.0%-50.0%; The consumption of antioxidant is 0.001--0.5%, and suitable consumption is 0.01%--0.1%, and the consumption of pH regulator agent is 1.0%--20.0%, and suitable consumption is 2.0%--10.0%.
The amount of application of Chinese medicine of the present invention can be according to variations such as the type of patient age, body weight, body surface area, the disease of being treated and the orders of severity, and its daily dose can be 10-500mg.Can use by one or many.
The following examples can make those skilled in the art more fully understand the present invention, but do not limit the present invention in any way.
Embodiment 1
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 50mg gelatin 46.00%
PEG400 0.18ml glycerol 17.82%
Propylene glycol 0.02ml water 36.18%
Tartaric acid 10mg
It is an amount of to get dehydrated alcohol, adds PEG400, propylene glycol, tartaric acid mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 50mg.
Embodiment 2
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 50mg gelatin 46.00%
PEG400 0.14ml glycerol 17.82%
Propylene glycol 0.06ml water 36.18%
Tartaric acid 15mg
It is an amount of to get dehydrated alcohol, adds PEG400, propylene glycol, tartaric acid mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 50mg.
Embodiment 3
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 50mg gelatin 46.00%
PEG400 0.1ml glycerol 17.82%
Glycerol 0.02ml water 36.18%
Tartaric acid 5mg
It is an amount of to get dehydrated alcohol, adds PEG400, glycerol, tartaric acid mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 50mg.
Embodiment 4
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 50mg gelatin 46.00%
PEG400 0.1ml glycerol 17.82%
Propylene glycol 0.02ml water 36.18%
Tartaric acid 5mg
30 POVIDONE K 30 BP/USP 30 30mg
Butylated hydroxyarisol (BHA) 0.01mg
It is an amount of to get dehydrated alcohol, adds PEG400, propylene glycol, tartaric acid, polyvidone, BHA mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 50mg.
Embodiment 5
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 125mg gelatin 46.00%
PEG400 0.4ml glycerol 17.82%
Propylene glycol 0.04ml water 36.18%
Tween 80 0.02ml
Tartaric acid 5mg
Di-tert-butyl hydroxy-methylbenzene (BHT) 0.01mg
It is an amount of to get dehydrated alcohol, adds PEG400, propylene glycol, tartaric acid, Tween 80, BHT mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 125mg.
Embodiment 6
The Roxithromycin soft capsule
Prescription: every of content contains the glue shell
Roxithromycin 250mg gelatin 46.00%
PEG400 0.4ml glycerol 17.82%
Glycerol 0.04ml water 36.18%
Tartaric acid 20mg
Di-tert-butyl hydroxy-methylbenzene (BHT) 0.02mg
It is an amount of to get dehydrated alcohol, adds PEG400, glycerol, tartaric acid, BHT mix homogeneously; Roxithromycin is dissolved in wherein, removes ethanol, get settled solution with reduction vaporization under the 50-60 ℃ of condition; This solution is made soft capsule.Every contains Roxithromycin 250mg.
Claims (8)
1, a kind of Roxithromycin soft capsule and preparation method thereof is characterized in that, medicinal liquid contains the Roxithromycin and the pharmaceutic adjuvant of effective dosage, and pharmaceutic adjuvant comprises diluent, antioxidant, solubilizing agent, cosolvent, pH regulator agent etc.By the normal capsules grain, contain Roxithromycin 0.01～0.25 gram in every medicinal liquid.
2, Roxithromycin soft capsule as claimed in claim 1 is characterized in that, described diluent is one or more in vegetable oil, glycerol, propylene glycol, Polyethylene Glycol (molecular weight 200-1000), the mineral oil.
3, Roxithromycin soft capsule as claimed in claim 1, it is characterized in that described antioxidant is one or more in propyl gallate, di-tert-butyl hydroxy-methylbenzene (BHT), butylated hydroxyarisol (BHA), vitamin E, ascorbyl palmitate, sodium sulfite, sodium sulfite, sodium pyrosulfite, sodium thiosulfate, glycine, methionine, lysine, valine, arginine, leucine, isoleucine, tryptophan, the glutathion.
4, Roxithromycin soft capsule as claimed in claim 1 is characterized in that, described solubilizing agent is Tween 80, pluronic F-68, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, polyvidone, sodium cholate, sodium lauryl sulphate etc.;
5, Roxithromycin soft capsule as claimed in claim 1 is characterized in that, described cosolvent is sodium sulfite, sodium carbonate, sodium bicarbonate, potassium dihydrogen phosphate, Ammonium biphosphate etc.; Amides compound such as carbamide, acetamide, nicotiamide, thiourea, Benzoylamide etc., amino acids such as arginine, aspartic acid, serine, glycine, methionine, histidine, glutamic acid, isoleucine, threonine, cysteine, cystine, tryptophan, phenylalanine, lysine, one or more in the chemical compound of hydroxyl or carboxyl such as sucrose, glucose, fructose, xylose, mannose, citric acid and sodium salt thereof, lactic acid, the sodium salicylate.
As claim 1 described Roxithromycin soft capsule, it is characterized in that 6, described pH regulator agent is one or more in tartaric acid, citric acid, glycine, cysteine, the lactic acid.
7, Roxithromycin soft capsule as claimed in claim 1 is characterized in that, the content of each component in the described medicinal liquid:
Every of component
Roxithromycin 0.01-0.25g
Diluent 0.1-0.6ml
Antioxidant 0.001%-0.5%
Solubilizing agent 0.0%-30.0%
Cosolvent 1.0%-100.0%
PH regulator agent 1.0%--20.0%
8, the described Roxithromycin preparation of soft capsule of claim 1 method may further comprise the steps:
(1) gelatin places the glue jar, adds the purified water of solubilized gelatin amount, 70～80 ℃ of glue jar temperature, and the in-depth back adds glycerol, antiseptic, with the cologne earth toning, stirs, and is incubated set aside for use after the vacuumize degassing;
(2) solubilizing agent (or cosolvent), antioxidant, pH regulator agent, dehydrated alcohol are added in the diluent, Roxithromycin is dissolved in wherein, both mix homogeneously; 50-60 ℃ of reduction vaporization removed ethanol, gets settled solution;
(3) the above-mentioned medicinal liquid for preparing poured in the pellet processing machine, finalized the design, put drying, scrape promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410041018 CN1709273A (en) | 2004-06-18 | 2004-06-18 | Roxhthromycin soft capsule and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410041018 CN1709273A (en) | 2004-06-18 | 2004-06-18 | Roxhthromycin soft capsule and its preparing method |
Publications (1)
| Publication Number | Publication Date |
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| CN1709273A true CN1709273A (en) | 2005-12-21 |
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| CN 200410041018 Pending CN1709273A (en) | 2004-06-18 | 2004-06-18 | Roxhthromycin soft capsule and its preparing method |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266309A (en) * | 2011-07-12 | 2011-12-07 | 江苏黄河药业股份有限公司 | Novel roxithromycin capsule and preparation method thereof |
| CN102697753A (en) * | 2012-06-08 | 2012-10-03 | 浙江维康药业有限公司 | Roxithromycin compound and soft capsule preparation thereof |
| CN106138009A (en) * | 2016-07-29 | 2016-11-23 | 花园药业股份有限公司 | Roxithromycin capsules and preparation technology thereof |
| CN107951859A (en) * | 2017-12-25 | 2018-04-24 | 安徽永生堂药业有限责任公司 | A kind of roxithromycin soft capsule and preparation method thereof |
| CN108703955A (en) * | 2018-07-31 | 2018-10-26 | 荆楚理工学院 | A kind of minerals soft capsule and preparation method thereof |
-
2004
- 2004-06-18 CN CN 200410041018 patent/CN1709273A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266309A (en) * | 2011-07-12 | 2011-12-07 | 江苏黄河药业股份有限公司 | Novel roxithromycin capsule and preparation method thereof |
| CN102697753A (en) * | 2012-06-08 | 2012-10-03 | 浙江维康药业有限公司 | Roxithromycin compound and soft capsule preparation thereof |
| CN106138009A (en) * | 2016-07-29 | 2016-11-23 | 花园药业股份有限公司 | Roxithromycin capsules and preparation technology thereof |
| CN107951859A (en) * | 2017-12-25 | 2018-04-24 | 安徽永生堂药业有限责任公司 | A kind of roxithromycin soft capsule and preparation method thereof |
| CN108703955A (en) * | 2018-07-31 | 2018-10-26 | 荆楚理工学院 | A kind of minerals soft capsule and preparation method thereof |
| CN108703955B (en) * | 2018-07-31 | 2020-02-21 | 荆楚理工学院 | Mineral soft capsule and preparation method thereof |
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