CN1223116A - Enteric soluble azithromycin preparation - Google Patents
Enteric soluble azithromycin preparation Download PDFInfo
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- CN1223116A CN1223116A CN 98110020 CN98110020A CN1223116A CN 1223116 A CN1223116 A CN 1223116A CN 98110020 CN98110020 CN 98110020 CN 98110020 A CN98110020 A CN 98110020A CN 1223116 A CN1223116 A CN 1223116A
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- azithromycin
- enteric
- capsule
- preparation
- composition
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Abstract
The present invention relates to an enteric coated azithromycin tablet preparation, including medicine core, isolating layer and coating layer, in which the medicine core component contains azithromycin, starch and low-substituted hydroxypropylcellulose, the isolating layer component mainly contains hydroxypropyl methylcellulose and Tween-80, and its coating layer component mainly contains Oubadai or acrylic resin No.2 and No.3. As compared with general azithro-mycin tablet and capsule preparation, it possesses the following advantages: it is stable in gastric juice, can be quickly dissolved and absorbed in intestinal tract, and its bioavailability is high, etc.
Description
The present invention relates to the azithromycin enteric coated preparation, belong to the Western medicine preparation technical field.
Azithromycin is a kind of macrolide antibiotics, the clinical various bacterial respiratory tracts of treatment, skin, soft tissue and the urogenital infections of being widely used in.Common dosage form is oral formulations such as conventional tablet, capsule, syrup.Recent research shows azithromycin degraded 68% in 30 minutes in 0.1 N HCl medium, degraded in 70 minutes reaches 84%, (PH=1.3) degraded 35.0% in 15 minutes in simulated gastric fluid, degraded 57% in 30 minutes, prove absolutely that azithromycin is in the gastric acid instability, degradation speed is fast, medicine under one's belt major part be damaged, obviously influence clinical efficacy.Reported in literature is arranged, and the bioavailability of azithromycin oral formulations is about 37%, and the interior ED50 protection dosage that the golden Portugal bacterium of mice is infected of body is 60mg/kg, is about 5 times of drug administration by injection dosage.And external clinical multiple strain bacteriostatic test, consumption equates with the injection azithromycin, ordinary preparation also is described because of stomach acids destroy, affects the treatment.
The objective of the invention is provides a kind of and can avoid stomach acids destroy with topic at above-mentioned, dissolves rapidly at intestinal, absorption, azithromycin enteric coated preparation that bioavailability is high, comprises tablet, capsule (microcapsule, capsule).
Technical essential of the present invention is on the basis of common oral preparation (tablet, capsule), selected for use hydroxypropyl emthylcellulose to pack contagion gown, avoid alkaline azithromycin and outer enteric material to react to each other, influence disintegrate, select dissolved enteric material acroleic acid resin, Opadry, Hydroxypropyl Methylcellulose Phathalate in the PH5-6.8 scope for use, pack enteric coating and form.Enteric coated preparation of the present invention is kept perfectly the human stomach behind the oral administration, does not leak medicine, and after entering pylorus, PH (5 o'clock, enteric coating dissolves rapidly, disintegrate, discharge the azithromycin medicine, intestinal absorbs rapidly, thereby reaches the purpose that improves bioavailability and curative effect.
Azithromycin enteric coated preparation of the present invention, comprise medicine inner core, sealing coat, enteric layers, it is characterized in that enteric coated preparation comprises tablet and capsule (pellet capsule), the label composition of tablet is azithromycin 100-250g, starch 20-60mg, low-substituted hydroxypropyl cellulose 10-30mg, the composition of sealing coat is hydroxypropyl emthylcellulose 2-6mg, tween 80 1-4mg, the composition of enteric layers are Opadry 8-16mg; The ball core composition of capsule (pellet capsule) is azithromycin 100-250mg, lactose 350-450mg, microcrystalline Cellulose 70-130mg, the composition of sealing coat is hydroxypropyl emthylcellulose 5-15mg, tween 80 7-10mg, the composition of enteric layers is acroleic acid resin II 10-18mg, acroleic acid resin III 9-15mg, diethyl phthalate 5-15mg.Azithromycin enteric agents tablet, enteric layers also can adopt Hydroxypropyl Methylcellulose Phathalate.
The preparation method of azithromycin enteric coated preparation of the present invention adopts conventional method pharmacy thing inner core and packs sealing coat, enteric layers.
Azithromycin enteric coated preparation of the present invention compares as conventional tablet, the capsule of enteric coated tablet with existing clinical use; Have characteristics stable in gastric acid.In simulated gastric fluid (containing protease) and 0.1M hydrochloric acid solution, placed conventional tablet, capsule only surplus 5.6% and 2.3% and enteric coated tablet 98.5% keeps 1 hour.Azithromycin enteric coated preparation of the present invention.Bioavailability is also apparently higher than ordinary preparation.Experimental result is as follows:
4 of men's health volunteers are all normal through health check-up and liver, kidney function test.Every experimenter all accepts 2 administrations: promptly single agent is oral azithromycin capsule (0.25g/ grain on an empty stomach, U.S. Pifzer company product) and enteric azithromycin capsule (0.25g/ grain, self-control, lot number 970509) the inherent different time of each 500mg 0-144h after taking medicine is got blood, measure with microbial method, undertaken by the big plate disperse of the agar-agar method of Bennet etc., the test bacterium is a Sarcina lutea, read the result with the standard curve method survey, lowest detection is limited to 0.005mg/L.
The blood drug level data that record are carried out every pharmacokinetic parameter calculating with the 3P87 program on the NEC microcomputer, it the results are shown in Table 1.
The human bioavailability of two kinds of azithromycin preparations of table 1
| ????Cmax ????(mg/L) | Tmax (h) | T1/2 (h) | AUCO-∞ (h.mg/L) |
| Capsule 0.4 enteric coated micropill 0.56 | ?2.64 ?3.2 | ?1.08 ?1.2 | ?6.4 ?8.9 |
The result confirms that this enteric coated micropill and the relative bioavailability of conventional capsule comparison are 139%.
Azithromycin enteric coated preparation of the present invention relatively has in gastric juice stablely with common azithromycin tablet, capsule, and the intestinal dissolving advantage that infiltration rate is fast, bioavailability is high, and common process preparation easily realize suitability for industrialized production.
The embodiment of the invention:
1 of example 1 enteric azithromycin
(1) label
1000 consumptions of writing out a prescription
Azithromycin 250g
Starch 40g
Low-substituted hydroxypropyl cellulose 20%
Preparation: take by weighing azithromycin, starch, low-substituted hydroxypropyl cellulose pulverize separately and cross 80 mesh sieves, claim sample, mixing, in right amount with the ethanol water (80%) of 2% hydroxypropyl emthylcellulose by recipe quantity, the system soft material is crossed 16 mesh sieves, granulate, 50-60 ℃ dried quick-fried, with 18 mesh sieve granulate.Measure granule content, tabletting, that is, every heavy 312mg contains azithromycin 250mg.
(2) sealing coat
Prescription
Hydroxypropyl emthylcellulose 2g
Tween 80 1g
Ethanol 80m1
Water 20m1
Dosing: get the recipe quantity hydroxypropyl emthylcellulose and be dispersed in the quantitative ethanol, after stirring evenly, add suitable quantity of water, it is standby that dissolving is evenly crossed 100 order nylon mesh to clear and bright solution.
Preparation: get 500g azithromycin sheet, place coating pan to start 30 ℃ of back preheating label temperature, adjusting rotating speed is 5-8 rev/min, and with hydroxypropyl methyl ethanol water spray coating, every weightening finish 6mg takes out then in 40 ℃ of following dried overnight with first gas spray gun.
(3) enteric coating
Prescription:
Opadry OY-P 15g
Ethanol 80ml
Water 20ml
The all same sealing coat of dosing and coating, the every about 12mg of weightening finish takes out 40 ℃ of dried overnight promptly then.
Example 2 enteric azithromycin micropills
(1) micropill prescription
Azithromycin 250g
Lactose 400g
Microcrystalline Cellulose 100g
Preparation: three kinds of raw materials of duty, adjuvant, make with 2% polyvinylpyrrolidone aqueous solution, diameter is 0.5-0.7mm.
(2) pack sealing coat
Prescription:
Hydroxypropyl emthylcellulose 2g
Tween 80 1g
Ethanol 80ml
Water 20ml
It is 50 rev/mins that preparation and coating are regulated the coating pan rotating speed with example 1, and pathogenic wind-warm is controlled at about 40 ℃, gap spraying sealing coat, and micropill increases weight 2%, is drying to obtain under taking out 40 ℃.
(3) enteric coating
Prescription:
Acroleic acid resin II 2.5g
Acroleic acid resin III 2.5g
Phthalic acid diethanol 2g
Ethanol 100ml
Preparation and the same sealing coat of coating, micropill weightening finish 4% is taken out 40 ℃ of following dryings and is sub-packed in capsule No. 0, and every contains azithromycin 250mg.
Example 3 enteric azithromycin sheets
(1) label
Prescription: 1000 consumptions
Azithromycin 100g
Starch 16g
Low-substituted hydroxypropyl cellulose 8g
Preparation:, contain azithromycin 100mg with example 1 every heavy 124mg.
(2) sealing coat
Prescription:
Hydroxypropyl emthylcellulose 2g
Tween 80 1g
Ethanol 80ml
Water 20ml
Dosing: with example 1
Preparation: with example 1: every weightening finish 4mg.
(3) enteric coating
Prescription:
Hydroxypropyl Methylcellulose Phathalate 5g
Ethanol 80ml
Water 20ml
The all same sealing coat of dosing and coating, every weightening finish 8mg takes out under 40 ℃ then, and dried overnight is promptly.
Claims (1)
1. azithromycin enteric coated preparation, comprise medicine inner core, sealing coat, enteric layers, it is characterized in that enteric coated preparation comprises tablet and capsule (pellet capsule), the label composition of tablet is azithromycin 100-250mg, starch 20-60mg, low-substituted hydroxypropyl cellulose 10-30mg, the composition of sealing coat is hydroxypropyl emthylcellulose 2-6mg, tween 80 1-4mg, and the composition of enteric layers is Opadry 8-16mg; The composition of the ball core of capsule (pellet capsule) is azithromycin 100-250mg, lactose 350-450mg, microcrystalline Cellulose 70-130mg, the composition of sealing coat is a hydroxypropyl emthylcellulose, 5-15mg, tween 80 7-10mg, the composition of enteric layers are acroleic acid resin II 10-18mg, acroleic acid resin III number, 9-15mg, diethyl phthalate 5-15mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98110020 CN1223116A (en) | 1998-01-14 | 1998-01-14 | Enteric soluble azithromycin preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98110020 CN1223116A (en) | 1998-01-14 | 1998-01-14 | Enteric soluble azithromycin preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1223116A true CN1223116A (en) | 1999-07-21 |
Family
ID=5220113
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 98110020 Pending CN1223116A (en) | 1998-01-14 | 1998-01-14 | Enteric soluble azithromycin preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1223116A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1127580A3 (en) * | 2000-02-23 | 2001-09-05 | Pfizer Products Inc. | Method of increasing the bioavailability and tissue penetration of azithromycin |
| CN102697749A (en) * | 2012-07-11 | 2012-10-03 | 上海新亚药业有限公司 | Preparation method of benazepril hydrochloride tablets |
| CN102908317A (en) * | 2011-08-01 | 2013-02-06 | 浙江丽水众益药业有限公司 | Macrolide antibiotics enteric-coated pellets and coating solution thereof |
-
1998
- 1998-01-14 CN CN 98110020 patent/CN1223116A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1127580A3 (en) * | 2000-02-23 | 2001-09-05 | Pfizer Products Inc. | Method of increasing the bioavailability and tissue penetration of azithromycin |
| CN102908317A (en) * | 2011-08-01 | 2013-02-06 | 浙江丽水众益药业有限公司 | Macrolide antibiotics enteric-coated pellets and coating solution thereof |
| CN102908317B (en) * | 2011-08-01 | 2014-08-20 | 浙江众益制药股份有限公司 | Macrolide antibiotics enteric-coated pellets and coating solution thereof |
| CN102697749A (en) * | 2012-07-11 | 2012-10-03 | 上海新亚药业有限公司 | Preparation method of benazepril hydrochloride tablets |
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| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |