CN104069077A - Preparation method of clarithromycin tablet - Google Patents
Preparation method of clarithromycin tablet Download PDFInfo
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- CN104069077A CN104069077A CN201410222520.7A CN201410222520A CN104069077A CN 104069077 A CN104069077 A CN 104069077A CN 201410222520 A CN201410222520 A CN 201410222520A CN 104069077 A CN104069077 A CN 104069077A
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- 229960002626 clarithromycin Drugs 0.000 title claims abstract description 21
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 title claims abstract description 21
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 16
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims abstract description 10
- 229920002774 Maltodextrin Polymers 0.000 claims abstract description 10
- 239000005913 Maltodextrin Substances 0.000 claims abstract description 10
- 229930195725 Mannitol Natural products 0.000 claims abstract description 10
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- 229940035034 maltodextrin Drugs 0.000 claims abstract description 10
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- 235000010355 mannitol Nutrition 0.000 claims abstract description 10
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- Medicinal Preparation (AREA)
Abstract
The invention relates to a medicinal preparation containing clarithromycin. The recipe of the medicinal preparation comprises 8% of clarithromycin, 10% of 2,3-dichloropyridine, 40-45% of mannitol, 15-20% of starch, 3-6% of maltodextrin, 6% of low substituted hydroxy propyl cellulose, 15% of microcrystalline cellulose, 1% of acetamido sulfamic acid, 1-3% of ammonium glycyrrhetate and 1% of magnesium stearate.
Description
Technical field
The present invention relates to the preparation field of pharmaceutical preparation, be specifically related to the preparation method of clarithromycin oral tablet.
Background technology
Pharyngitis is the modal disease of puzzlement modern life, is pharyngeal mucous membrane, submucous tissue and adenoid diffuse inflammation, is often a part for upper respiratory tract infection.Be divided into clinically acute and chronic two kinds.Acute pharyngitis is many in autumn and winter and at the end of winter and the beginning of spring morbidity.Pathological changes ordinary wave and whole pharyngeal cavity, also can limit to a place.Can be caused by virus, antibacterial and physical chemical factor and high temperature, dust, fumagine, irritative gas etc.Antibacterial infects taking gram-positive coccis such as streptococcus, staphylococcus and Diplococcus pneumoniaes as main.Wherein serious with A group group B streptococcus causer, antibacterial or toxin enter blood, can cause the purulent lesion of organ at a distance, are called acute septic pharyngitis.Oral or injection antibiotics infection control for treatment.
The chronic pharyngitis course of disease is very long, and symptom stubbornness, often by due to local infection or general pathological changes secondary, taking chronic disease, acute attack is as its feature repeatedly, and in many cases, acute attack is to be infected and caused by antibacterial, therefore, suitable antibacterial therapy contributes to control acute symptom.
Acute tonsillitis is the non-specific acute inflammation of one of very common palatine tonsil, often with pharyngeal mucous membrane to a certain degree and swallow adenoid acute inflammation.Main Pathogenic Bacteria is streptococcus, staphylococcus, Diplococcus pneumoniae.Adenovirus also can cause primary disease.Antibacterial and virus mixed infection are quite a few to be seen.Antibacterial may be extraneous intrusion, may be also the antibacterial being hidden in tonsillar crypts, when Abwehrkraft des Koepers is because of cold, and humidity, overworked, have a delicate constitution, when the factor such as tobacco and wine are excessive, harmful gas stimulation reduces suddenly, due to bacterial reproduction is strengthened.Acute tonsillitis is acute attack repeatedly on chronic tonsil basis often.Clinical manifestation aversion to cold, high heat, pharyngalgia, aggravate while swallowing etc., can the concurrent rheumatic fever relevant with hemolytic streptococcal infection, the multiple general disease such as acute glome-rulonephritis, myocarditis, arthritis.Treatment adopts pain relieving to bring down a fever, oral or injection antibiotics infection control.
Treatment antibacterial infects the pharyngitis, tonsillitis and the oral cavity infection that cause, often selects the antibiotics of resisting gram-positive bacteria, and the antibiotics of the anti-gram negative bacteria of part also has therapeutical effect.Clarithromycin is macrolide antibiotics, and mechanism of action is by the connection of block cell nucleoprotein 50S subunit, and Profilin is synthesized and generation bacteriostasis.This product has inhibitory action to gram positive bacteria as staphylococcus aureus, streptococcus, streptococcus pneumoniae etc., part gram-negative bacteria, if hemophilus influenza, bordetella pertussis, Diplococcus gonorrhoeae, legionella pneumophilia and part anaerobe are as bacteroides fragilis, peptostreptococcus, propionibacterium acnes etc. also have inhibitory action, is also had to inhibitory action to mycoplasma in addition.This product feature is that antibacterial activity is in vitro similar to erythromycin, but as stronger than erythromycin in the antibacterial activity of staphylococcus aureus, streptococcus, hemophilus influenza etc. to part antibacterial in vivo.Between clarithromycin and erythromycin, there is cross resistance.Be applicable to the caused following infection of clarithromycin sensitive organism: upper respiratory tract infection: tonsillitis, pharyngitis, sinusitis; Lower respiratory infection: acute bronchitis, acute episode of chronic bronchitis and pneumonia; Skin soft-tissue infection: impetigo, erysipelas, folliculitis, furuncle and wound infection; Urethritis and cervicitis etc. that acute otitis media, mycoplasma pneumoniae pneumonia, chlamydia trachomatis cause.Also combine the treatment for Mycobacterium avium infection, helicobacter pylori infections for infection with legionella, or with other drug.The preparation that oneself of this medicine succeeds in developing has tablet, capsule, and granule, injection etc., all adopt the whole body administrations such as oral or injection.While using inconvenience, administration in view of injection, be easy to cause local pain reaction.The oral absorption such as tablet are slower, distributed medicine is diluted in blood after entering blood by whole body, make medicine lower at the blood drug level of diseased region, and it is also longer to reach time of effective blood drug concentration at diseased region, affects its effective antibacterial efficacy.
Therefore, the buccal lozenge of development clarithromycin, by oral cavity buccal, directly acts on diseased region with high concentration medicine, for the treatment of pharyngitis, pharyngoamygdalitis and oral diseases, can overcome above-mentioned shortcoming, and strong auxiliary treatment means is provided.
Summary of the invention
The object of this invention is to provide a kind of buccal lozenge taking clarithromycin as ingredient and preparation method thereof, medicine dissolves by sucking in intraoral saliva, enters around oral cavity, pharyngeal and pharyngeal tonsil position, brings into play its antibacterial action.
Clarithromycin ingredient prescription of the present invention is as follows:
Further, prescription of the present invention is preferably as follows:
The application's choice for use account for tablet weight than the maltodextrin of 1-4%, in tabletting process, there is sliver problem in it, in the time that the proportional numerical value of maltodextrin and oral cavity dispersible tablet gross weight is more than or equal to approximately 5%, sliver problem disappear.
The concrete selection of diluent used is also necessary for obtaining good hardness and dispersing characteristic.Diluent that previously may use, certified comprises lactose, Sorbitol and microcrystalline Cellulose.In the combination ratio of standard, the disintegration time of all above-mentioned diluent of mentioning except cellulose is all oversize, and that cellulosic shortcoming is mouthfeel is bad.In addition, if microcrystalline Cellulose usage ratio is too high, in conventional tabletting machine, there will be production problems.Why Here it is only has mannitol to be considered to be suitable for use as diluent.In use, preferably mean diameter is approximately 160 μ m to mannitol, and its ratio is about tablet weight than 40% to 45%, and tablet will occur good mechanical performance.
In the present invention, use conventional disintegrating agent, for example corn starch, polyvinylpolypyrrolidone and cross-linked carboxymethyl cellulose calcium, but through experimental demonstration, most disintegrating agent all can not obtain suitable disintegration time; In addition, corn starch causes obviously division or the high fragility of tablet making.Demonstration repeatedly by experiment, only has 2,3-dichloropyridine and low-substituted hydroxypropyl cellulose coupling can obtain the disintegrating agent of good result, in the time that the use amount of low-substituted hydroxypropyl cellulose is 6%, tests the tablet quality optimum obtaining.
The invention still further relates to the preparation method of described buccal above.The method is characterised in that and comprises following consecutive steps:
1) by the clarithromycin of recipe quantity, 2, the low-substituted hydroxypropyl cellulose of 3-dichloropyridine, mannitol, maltodextrin, starch and half recipe quantity is crossed 20 mesh sieves, adds appropriate water to mix, and obtains wet mixture;
2) microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate are crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes;
3) by step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Specific embodiment
Embodiment 1: prepare clarithromycin tablet
(1) prescription:
(2) preparation technology:
The low-substituted hydroxypropyl cellulose of the clarithromycin of recipe quantity, mannitol, maltodextrin, starch and half recipe quantity is crossed to 20 mesh sieves, add appropriate water to mix, obtain wet mixture; The low-substituted hydroxypropyl cellulose of the microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate and residue recipe quantity is crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes; By step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Embodiment 2: prepare clarithromycin tablet
(1) prescription:
(2) preparation technology:
By the clarithromycin of recipe quantity, 2, the low-substituted hydroxypropyl cellulose of 3-dichloropyridine, mannitol, maltodextrin, starch and half recipe quantity is crossed 20 mesh sieves, adds appropriate water to mix, and obtains wet mixture; The low-substituted hydroxypropyl cellulose of the microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate and residue recipe quantity is crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes; By step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Embodiment 3:
Contrast tablet 1
(1) prescription:
(2) preparation technology:
The polyvinylpolypyrrolidone of the clarithromycin of recipe quantity, mannitol, maltodextrin, starch and half recipe quantity is crossed to 20 mesh sieves, add appropriate water to mix, obtain wet mixture; The polyvinylpolypyrrolidone of the microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate and residue recipe quantity is crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes; By step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Contrast tablet 2
(1) prescription:
(2) preparation technology:
The cross-linking sodium carboxymethyl cellulose of the clarithromycin of recipe quantity, mannitol, maltodextrin, starch and half recipe quantity is crossed to 20 mesh sieves, add appropriate water to mix, obtain wet mixture; The cross-linking sodium carboxymethyl cellulose of the microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate and residue recipe quantity is crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes; By step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Contrast tablet 3
(1) prescription:
(2) preparation technology:
The clarithromycin of recipe quantity, mannitol, maltodextrin, starch are crossed to 20 mesh sieves, add appropriate water to mix, obtain wet mixture; The microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate are crossed respectively to 20 mesh sieves, pour 3 dimension mixers into and mix 15 minutes; By step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
Embodiment 4: the inspection that is uniformly dispersed of tablet
Experimental technique: get respectively embodiment 1, embodiment 2, contrast tablet 1, contrast tablet 2, the prepared dispersible tablet of contrast tablet 3, according to dispersing uniformity inspection technique (two annex IA of Chinese Pharmacopoeia version in 2005) in the 100ml water of 20 DEG C ± 1 DEG C, jolting 3 minutes, all disintegrates by No. 2 sieves, its result of the test is in table 1:
Table 1. dispersing uniformity result
| Sample | Experimental result |
| Dispersible tablet prepared by embodiment 1 | 1 point of all disintegrate in 07 second, and by No. 2 sieves |
| Dispersible tablet prepared by embodiment 2 | 1 point of all disintegrate in 10 seconds, and by No. 2 sieves |
| Contrast tablet 1 | 1 point of all disintegrate in 45 seconds, part is by No. 2 sieves |
| Contrast tablet 2 | 2 points of all disintegrates in 05 second, part is by No. 2 sieves |
| Contrast tablet 3 | 2 points of part disintegrates in 20 seconds, part is by No. 2 sieves |
Experimental result shows that dispersible tablet prepared by the embodiment of the present invention 1, embodiment 2 is in the water of 20 DEG C ± 1 DEG C, and within 3 minutes, all disintegrates by No. 2 sieves, are better than other contrast tablets.
Embodiment 5: dissolution in vitro test
Experimental technique: get respectively embodiment 1, embodiment 2, contrast tablet 1, contrast tablet 2, the prepared dispersible tablet of contrast tablet 3, according to dissolution method (second annex XC the second method of Chinese Pharmacopoeia version in 2005), taking hydrochloric acid solution (9 → 1000) 1000ml as solvent, rotating speed is per minute 50 to turn, 37 DEG C ± 0.5 DEG C of temperature, measure, respectively at 5,10 in accordance with the law, 20,30,45,60min sampling.Ultraviolet visible spectrophotometry (second annex IV of Chinese Pharmacopoeia version in 2005) is measured trap in 258nm place, and calculates dissolution, and it the results are shown in Table 2:
The comparison of table 2. dissolution result
As seen from the above table, the dissolution in vitro of the embodiment of the present invention 1, embodiment 2 is better than the dissolution of other contrast tablets.
Claims (3)
1. contain a pharmaceutical preparation for clarithromycin, its prescription is as follows:
2. pharmaceutical preparation according to claim 1, is characterized in that prescription is as follows:
3. contain a pharmaceutical preparation for clarithromycin, its preparation technology comprises the following steps:
A, the low-substituted hydroxypropyl cellulose of the clarithromycin of recipe quantity, mannitol, maltodextrin, starch and half recipe quantity is crossed to 20 mesh sieves, add appropriate water to mix, obtain wet mixture;
B, by the microcrystalline Cellulose of recipe quantity, acesulfame potassium, ammonium glycyrrhizinate respectively cross 20 mesh sieves, pour into 3 dimension mixers mix 15 minutes;
C, by step 1) with step 2) mixture, pour into 3 dimension mixers mix 30 minutes; Continue to add the magnesium stearate of recipe quantity, mix 2-3 minute; Be dried, cross 20 mesh sieves in 40-60 DEG C; Pour material in tablet machine tabletting, maintenance tablet hardness is 20-40N.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6284270B1 (en) * | 1999-08-04 | 2001-09-04 | Drugtech Corporation | Means for creating a mass having structural integrity |
| CN102526752A (en) * | 2011-06-15 | 2012-07-04 | 上海现代制药股份有限公司 | Bitterness-eliminated medicinal preparation |
-
2014
- 2014-05-21 CN CN201410222520.7A patent/CN104069077A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6284270B1 (en) * | 1999-08-04 | 2001-09-04 | Drugtech Corporation | Means for creating a mass having structural integrity |
| CN102526752A (en) * | 2011-06-15 | 2012-07-04 | 上海现代制药股份有限公司 | Bitterness-eliminated medicinal preparation |
Non-Patent Citations (2)
| Title |
|---|
| 无: "2,3-Dichloropyridine", 《M A T E R I A L S A F E T Y D A T A S H E E T》 * |
| 无: "2,3-Dichloropyridine", 《MATERIAL SAFETY DATA SHEET》 * |
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