CN104352463A - Ampicillin sodium dispersible tablet - Google Patents
Ampicillin sodium dispersible tablet Download PDFInfo
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- CN104352463A CN104352463A CN201410641924.XA CN201410641924A CN104352463A CN 104352463 A CN104352463 A CN 104352463A CN 201410641924 A CN201410641924 A CN 201410641924A CN 104352463 A CN104352463 A CN 104352463A
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- ampicillin
- clathrate
- dispersible tablet
- beta
- schardinger dextrin
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Abstract
The invention discloses a preparation method of an ampicillin sodium dispersible tablet. The preparation method comprises the following steps: firstly, preparing a clathrate compound from ampicillin sodium; and then preparing the dispersible tablet. The dispersible tablet comprises the following components in percentage by weight: 20% of PVP (polyvinyl pyrrolidone), 10% of mannitol, 2% of magnesium stearate, 1% of superfine silica powder and the balance of the clathrate compound of ampicillin sodium, wherein the weight ratio of ampicillin sodium to beta-cyclodextrin in the clathrate compound of ampicillin sodium is 2: 3. The ampicillin sodium dispersible tablet has the advantages of being fast to dissolve, quick to absorb, high in bioavailability, convenient to take and the like.
Description
Technical field
The present invention relates to a kind of animal-use drug, particularly relate to the preparation method of a kind of ampicillin sodium dispersible tablets.
Background technology
Ampicillin belongs to the Tri-Biocin of penicillin one class, may be used for intramuscular injection or intravenous injection.Main in order to treat the upper and lower respiratory tract infection, gastrointestinal infection, urinary tract infection, skin, soft tissue infection, meningitis, septicemia, endocarditis etc. caused by sensitive bacterial.This product is difficult to dissolve in methanol/ethanol, micro dissolution in water.
Dispersible tablet is put into after water can disintegrate rapidly, forms the ground suspension that is uniformly dispersed, has easy to use, the feature that bioavailability is high.The preparation method of dispersible tablet, working condition and production technology are simple, and instructions of taking is convenient, can swallow as conventional tablet, also can be distributed to wet suit and use.
Ampicillin is used for the treatment of animal body by the present invention, as the Bacillus pasteurii disease, pneumonia, mastitis, metritis, pyelonephritis, calf Hakuri, salmonella enteritis etc. of cattle; The bronchopneumonia, metritis, colt-ill, coltfoal streptococcus pneumonia, coltfoal enteritis etc. of horse; The enteritis of pig, pneumonia, erysipelas, metritis and piglet pujos blancos etc.; The mastitis of sheep, metritis and pneumonia etc.
Summary of the invention
The invention provides the preparation method of a kind of ampicillin sodium dispersible tablets; This dispersible tablet has the features such as solubility is good, good stability, and drug loading is high, safety of clinical trials is good.
Dispersible tablet is relative to conventional tablet, and in disintegrate medium, disintegration is less than 3 minutes, and the granule after disintegrate can all by No. 2 sieves, and compared with capsule preparations, it is rapid that dispersible tablet has stripping, absorb fast, the advantages such as bioavailability is high, taking convenience.
Clathrate has the following advantages: cover bad stink, reduces zest; Increase drug dissolution and bioavailability; Improve medicine stability.
Ampicillin is first prepared into clathrate by the application, and then prepared composition discrete piece, enclose and dispersion technology is united two into one, and plays the advantage of two aspects.
Ampicillin clathrate comprises active component and enclose material, and active component is ampicillin, and enclose material is alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more of hydroxypropylβ-cyclodextrin.The part by weight of active component and enclose material is 3:2-2:3.
The present invention also adopts the special adjuvant of dispersible tablet, and disintegrate is rapid, rapid-action.
The preparation method of ampicillin clathrate comprises:
(1) in water or aquiferous ethanol medium, by a certain percentage, by ampicillin and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, by ampicillin and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin; Or
(3) ampicillin and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, high energy milling is carried out in one or more reactions of hydroxypropylβ-cyclodextrin.
By the above-mentioned ampicillin clathrate prepared composition discrete piece prepared, described dispersible tablet comprises by weight, the disintegrating agent of 1-30%, the filler of 1-80%, the lubricant of 0.1-5%, the fluidizer of 0.1-5%, the flavouring agent of 0.1-5%, all the other are ampicillin clathrate.Particularly, disintegrating agent is polyvinylpolypyrrolidone or sodium carboxymethyl cellulose, and filler is microcrystalline Cellulose or mannitol, and lubricant is magnesium stearate or Pulvis Talci, and fluidizer is micropowder silica gel, and flavouring agent is cyclamate or fruit essence.Preferably, disintegrating agent is polyvinylpolypyrrolidone, and filler is mannitol, and the ratio of the two is 3:2, can significantly improve the preparation effect of dispersible tablet when adopting the adjuvant of this specific proportioning, accelerates disintegration rate.
Metering of the present invention is weight.
PVP20％；
Mannitol 10%;
Magnesium stearate 2%;
Micropowder silica gel 1%;
Flavouring agent 1%
Ampicillin clathrate surplus.
Detailed description of the invention
Embodiment 1: a kind of ampicillin sodium dispersible tablets
Ampicillin clathrate: beta-schardinger dextrin-is 2:3
The prescription of dispersible tablet is (by weight):
PVP20％；
Mannitol 10%;
Magnesium stearate 2%;
Micropowder silica gel 1%;
Cyclamate 1%
Ampicillin clathrate surplus.
Preparation method:
1. prepare ampicillin clathrate by the following method:
(1) in water or aquiferous ethanol medium, by a certain percentage, ampicillin and hydroxypropylβ-cyclodextrin are reacted, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, ampicillin and hydroxypropylβ-cyclodextrin are reacted; Or
(3) ampicillin and hydroxypropylβ-cyclodextrin react and carry out high energy milling.
2. by the polyvinylpolypyrrolidone of recipe quantity, mannitol, after cyclamate is mixed homogeneously by the equivalent method of progressively increasing with ampicillin clathrate, then adds magnesium stearate, micropowder silica gel, and mixing, tabletting, obtains ampicillin clathrate dispersible tablet.
Embodiment 2: a kind of ampicillin sodium dispersible tablets
Ampicillin clathrate: beta-schardinger dextrin-is 2:3
The prescription of dispersible tablet is (by weight):
Sodium carboxymethyl cellulose 20%;
Mannitol 10%;
Magnesium stearate 2%;
Micropowder silica gel 1%;
Cyclamate 1%;
Ampicillin clathrate surplus.
Preparation method:
1. prepare ampicillin clathrate by the following method:
(1) in water or aquiferous ethanol medium, by a certain percentage, ampicillin and hydroxypropylβ-cyclodextrin are reacted, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, ampicillin and hydroxypropylβ-cyclodextrin are reacted; Or
(3) ampicillin and hydroxypropylβ-cyclodextrin react and carry out high energy milling.
2. by the polyvinylpolypyrrolidone of recipe quantity, mannitol, after cyclamate is mixed homogeneously by the equivalent method of progressively increasing with ampicillin clathrate, then adds magnesium stearate, micropowder silica gel, and mixing, tabletting, obtains ampicillin clathrate dispersible tablet.
Embodiment 3: a kind of ampicillin sodium dispersible tablets
Ampicillin clathrate: beta-schardinger dextrin-is 2:3
The prescription of dispersible tablet is (by weight):
Sodium carboxymethyl cellulose 20%;
Mannitol 10%;
Magnesium stearate 2%;
Micropowder silica gel 1%;
Cyclamate 1%;
Ampicillin clathrate surplus.
Preparation method is the same
The analytical test result of ampicillin clathrate dispersible tablet prepared by the above embodiment of the present invention:
(1) weight differential of the ampicillin clathrate dispersible tablet of embodiment 1,2 preparation is little, and unilateral bright and clean, hardness is moderate, and mouthfeel is good.Ampicillin sodium dispersible tablets weight differential prepared by embodiment 3 is little, and unilateral injustice, hardness is little, and mouthfeel is slightly poor.
(2) ampicillin described in embodiment 1,2 and hydroxypropylβ-cyclodextrin are fully ground in 50% ethanol the even mastic of formation, after vacuum drying, obtain white powder, in the water of this powder, the ampicillin of the more non-enclose of solubility property improves 12 times.
(3) dispersing uniformity experimental result display: according to the method for 2010 editions Chinese Pharmacopoeias two regulation, Example 1,2,3 each 6, puts in 250ml beaker, adds the water 100mL of about 20 DEG C, jolting 90 seconds, the whole disintegrate of embodiment 1,2 dispersible tablet also passes through No. two sieves.100% is shortened than 3 minute time limit of States Pharmacopoeia specifications.Embodiment 3 dispersible tablet jolting whole disintegrate by No. two sieves after 4 minutes.
(4) dissolution test result display: according to dissolution method (Chinese Pharmacopoeia 2010 editions two annex XC second methods), using 0.01mol/L hydrochloric acid solution 900ml as dissolution medium, rotating speed is 50 revs/min, operate in accordance with the law, every sheet stripping quantity is measured according to ultraviolet visible spectrophotometry, result be the stripping percentage rate of embodiment 1,2 dispersible tablet in 60 seconds at about 80-90%, substantially all strippings in 90 seconds.Embodiment 3 dispersible tablet after 3 minutes stripping percentage rate about 80%, basic all strippings in 5 minutes.Result shows, ampicillin clathrate dispersible tablet provided by the invention meets the regulation of Chinese Pharmacopoeia (2000 editions) about dispersible tablet.Vitamin C clathrate dispersible tablet has outstanding excellent water dissolubility and dispersion effect compared to ampicillin, and according to polyvinylpolypyrrolidone: mannitol is that clathrate dispersible tablet prepared by 3:2 has more outstanding excellent dispersion effect relative to the dispersible tablet of this special ratios non-.
Claims (2)
1. an ampicillin sodium dispersible tablets, is characterized in that the prescription of dispersible tablet is by weight:
PVP20％；
Mannitol 10%;
Magnesium stearate 2%;
Micropowder silica gel 1%;
Flavouring agent 1%;
Ampicillin clathrate surplus;
Wherein ampicillin in ampicillin clathrate: beta-schardinger dextrin-is 2:3.
2. the preparation method of ampicillin sodium dispersible tablets as claimed in claim 1, is characterized in that, comprise the steps:
1). prepare ampicillin clathrate:
(1) in water or aquiferous ethanol medium, in proportion, ampicillin and beta-schardinger dextrin-are reacted, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, ampicillin and beta-schardinger dextrin-are reacted; Or
(3) ampicillin and beta-schardinger dextrin-react and carry out high energy milling;
2). by the PVP of recipe quantity, mannitol, after cyclamate is mixed homogeneously by the equivalent method of progressively increasing with ampicillin clathrate, then adds magnesium stearate, micropowder silica gel, and mixing, tabletting, obtains ampicillin clathrate dispersible tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410641924.XA CN104352463A (en) | 2014-11-13 | 2014-11-13 | Ampicillin sodium dispersible tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410641924.XA CN104352463A (en) | 2014-11-13 | 2014-11-13 | Ampicillin sodium dispersible tablet |
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| Publication Number | Publication Date |
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| CN104352463A true CN104352463A (en) | 2015-02-18 |
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| CN201410641924.XA Pending CN104352463A (en) | 2014-11-13 | 2014-11-13 | Ampicillin sodium dispersible tablet |
Country Status (1)
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104887631A (en) * | 2015-05-19 | 2015-09-09 | 杨灵杰 | An ampicillin particle and a preparing method thereof |
| CN105200116A (en) * | 2015-09-25 | 2015-12-30 | 武汉科诺生物科技股份有限公司 | Method of quickly measuring content of Paenibacillus polymyxa in compound microbial agent |
-
2014
- 2014-11-13 CN CN201410641924.XA patent/CN104352463A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104887631A (en) * | 2015-05-19 | 2015-09-09 | 杨灵杰 | An ampicillin particle and a preparing method thereof |
| CN105200116A (en) * | 2015-09-25 | 2015-12-30 | 武汉科诺生物科技股份有限公司 | Method of quickly measuring content of Paenibacillus polymyxa in compound microbial agent |
| CN105200116B (en) * | 2015-09-25 | 2017-12-12 | 武汉科诺生物科技股份有限公司 | A kind of method of Paenibacillus polymyxa content in quick measure complex micro organism fungicide |
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Application publication date: 20150218 |