CN1562046A - Adefovir dipivoil dispersion tablet and preparing method - Google Patents
Adefovir dipivoil dispersion tablet and preparing method Download PDFInfo
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- CN1562046A CN1562046A CN 200410012867 CN200410012867A CN1562046A CN 1562046 A CN1562046 A CN 1562046A CN 200410012867 CN200410012867 CN 200410012867 CN 200410012867 A CN200410012867 A CN 200410012867A CN 1562046 A CN1562046 A CN 1562046A
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- adefovir ester
- dispersible tablet
- lactose
- magnesium stearate
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Abstract
A dispersing tablet of adefovirdipivoxil ester is prepared from adefovirdipivoxil ester, pregelatinized starch, microcrystalline fibres, lactose, carboxymethyl starch sodium, sodium laurylsulfate, and magnesium stearate through respective sieving, proportionally mixing and die pressing.
Description
Technical field
The present invention relates to the adefovirdipivoxil ester formulation, particularly contain dispersible tablet of adefovir ester and preparation method thereof.
Background technology
Adefovir ester (adefovir dipivoxil is called for short AD) chemistry is by name: two (pivaloyloxymethoxy) phosphonium mesitoyl methoxies of 9-[2-[] ethyl] adenine is a kind of multiple crystal formation of having of water and unformed curing material of being insoluble in.Adefovir ester can be used for treating human or animal's retroviral infection (HIV, SIV, FIV), dna virus infection (people's cytomegalovirus or herpesvirus, as HSV1 or HSV2), hepatitis B virus or other hepatitis viruss etc., lamivudine and the drug-fast HBV Strain of famciclovir are all had very strong inhibitory action, are a kind of novel antiviral drugs.Starrett etc., J Med.Chem., 1994,37:1857-1864; Starrett etc., Antiviral Res., 1992,19:267-273; Benzaria etc., J.Med.Chem., 1996,39:4958～4965; Zhang Yong etc., Shenyang Pharmaceutical University's journal, 2001,18 (2): 95-97; Report is all arranged.European patent EP 481214; Chinese patent CN1435420A, CN1330547A, CN1374314A, CN1251592A, CN1425673A all have report to dosage forms such as the conventional tablet of adefovir ester, capsule, powder, granule, pill, pastes, but do not see the report for dispersible tablet.
Existing adefovir ester tablet mainly is the conventional tablet made from wet granulation, and it is not high in intravital bioavailability of people and trap; The preparation process complexity, labour, time, equipment, energy resource consumption are bigger; Production efficiency is low; Need production site bigger; Be unfavorable for industrialized great production.And dispersible tablet formulation can effectively remedy these defectives, improves bioavailability and trap.
Summary of the invention
The invention provides a kind of dispersible tablet formulation that forms with the mixing compression by adefovir ester and pharmaceutical excipient.Pharmaceutical excipient mixes directly compression with special ratios and makes dispersible tablet formulation.
Technical scheme of the present invention:
The adefovir ester dispersible tablet, the content range of each component is as follows: adefovir ester 1%-20% (weight) pregelatinized Starch 10%-20% (weight), microcrystalline Cellulose 25%-50% (weight), lactose 10%-30% (weight), carboxymethyl starch sodium 10%-30% (weight), sodium lauryl sulphate 0.5%-3% (weight), magnesium stearate 0.5%-3% (weight).
The adefovir ester dispersible tablet, the content range of each component can also be: adefovir ester 5%-15% (weight), pregelatinized Starch 12%-18% (weight), microcrystalline Cellulose 30%-40% (weight), lactose 14%-26% (weight), carboxymethyl starch sodium 15%-25% (weight), sodium lauryl sulphate 1%-2.5% (weight), magnesium stearate 1%-2.5% (weight).
Preferred version:
Adefovir ester 8.3% (weight), microcrystalline Cellulose 33.4% (weight), pregelatinized Starch 16.6% (weight), lactose 16.6% (weight), carboxymethyl starch sodium 21.7% (weight), sodium lauryl sulphate 1.7% (weight), magnesium stearate 1.7% (weight).
Pharmaceutical excipient of the present invention can comprise diluent, absorbent, wetting agent, binding agent, disintegrating agent, lubricant, correctives, aromatic and coloring agent etc., typical as: pregelatinized Starch, microcrystalline Cellulose, lactose, carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate, aspartame etc.
The used pharmaceutical excipient of adefovir ester dispersible tablet of the present invention can also be adefovir ester 1%-20% (weight); Disintegrating agent 10%-50% (weight); Lubricant 0.5%-3% (weight); Filler 30%-70% (weight).
Adefovir ester in the preparation of the present invention is a crystal formation or armorphous.
Crystal type adefovir ester in the preparation of the present invention is anhydrous crystal or water-containing crystal or other solvent version.Can be: anhydrous crystal shape, two crystalline hydrates, methanol solvate shape etc.
The preparation method of adefovir ester dispersible tablet of the present invention makes through following steps:
A: get adefovir ester and cross 100 mesh sieves;
B: get it filled and mixed 60 mesh sieves,, directly be pressed into dispersible tablet with the adefovir ester mix homogeneously with excipient pregelatinized Starch, microcrystalline Cellulose, lactose, carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate.
Adefovir ester dispersible tablet provided by the invention, with the prescription mobility of particle ideal that this scheme is made, compressibility is more satisfactory, hardness (kg/cm
2) be 6, friability is 0.1%, and be 2min disintegration, and dissolution (45min) is 94.71%, meets the regulation of the relevant dispersible tablet of pharmacopeia disintegration, and every index is all desirable.Carry out the dissolution test according to two appendix XC second methods of Chinese Pharmacopoeia version in 2000: the 500ml distilled water, 75rpm, 37 ± 0.5 ℃, in 30min, stripping quantity is measured in sampling, result of the test shows, 6 dissolutions in 30min meet the regulation of two relevant dissolutions of appendix XC of pharmacopeia all more than 90%, and this prescription can be used as the prescription of adefovir ester dispersible tablet.
For determining the flowability of this prescription powder, measured the angle of repose of three sample powder.Through three times angle of repose a measure, the average a value of result is 43.60 °, is slightly less than 45 °, this prescription and the preparation technology who is adopted are mixed into the mobile relatively good of powder, can satisfy dispersible tablet and prepare requirement.
The disintegration of adefovir ester dispersible tablet formulation disclosed by the invention and dissolution are all preferable, absorb soon the bioavailability height in the body; Can swallow, chew, contain and suck, also can put in the water take separately after disperseing or with fruit juice, milk with clothes, easily accepted by the child.
The present invention also provides a kind of adefovir ester and pharmaceutical excipient is mixed the preparation technology that directly compression forms dispersible tablet.Adefovir ester does not contact with water or organic solvent in this technical process, has avoided the brilliant phenomenon of contingent commentaries on classics.And preparation process is simple relatively, and labour, time, equipment, energy resource consumption are less, and the production efficiency height helps industrialized great production.
Adefovir ester disclosed by the invention disperses preparation technology simple, has saved the general required operation of tablet such as granulation, drying; Energy-conservation, save time serialization that helps producing and automatization.
The present invention also provides a kind of adefovirdipivoxil acid dispersible tablet formulation that can be used for using to cat, Canis familiaris L., horse, rabbit and other animal.
The specific embodiment
Following embodiment further specifies this rather than limits the scope that embodiment does not limit the present invention in any way of the present invention.
Embodiment 1:
Adefovir ester 8.3% (weight)
Pregelatinized Starch 16.7% (weight)
Microcrystalline Cellulose 33.3% (weight)
Lactose 16.6% (weight)
Carboxymethyl starch sodium 21.7% (weight)
Sodium lauryl sulphate 1.7% (weight)
Magnesium stearate 1.7% (weight)
Get the adefovir ester of recipe quantity, cross 100 mesh sieves, other gets lactose, microcrystalline Cellulose, pregelatinized Starch, its Starch Sodium of carboxylic first, magnesium stearate, the sodium lauryl sulphate of recipe quantity and crosses 60 mesh sieves, mix homogeneously, get the adjuvant with adefovir ester equivalent, cross 60 mesh sieve mix homogeneously, measure content with the method that equivalent is progressively increased, direct powder compression makes 1000 of adefovir ester dispersible tablets.
Embodiment 2:
Adefovir ester 4.2% (weight)
Pregelatinized Starch 19.2% (weight)
Microcrystalline Cellulose 43.3% (weight)
Lactose 16.6% (weight)
Carboxymethyl starch sodium 13.3% (weight)
Sodium lauryl sulphate 1.7% (weight)
Aspartame is an amount of
Magnesium stearate 1.7% (weight)
Get the adefovir ester of recipe quantity, cross 100 mesh sieves, other gets sweet mistake 60 mesh sieves of lactose, microcrystalline Cellulose, pregelatinized Starch, its Starch Sodium of carboxylic first, magnesium stearate, sodium lauryl sulphate, A Siba of recipe quantity, mix homogeneously, get the adjuvant with adefovir ester equivalent, cross 60 mesh sieve mix homogeneously, measure content with the method that equivalent is progressively increased, direct powder compression makes 1000 of adefovir ester dispersible tablets.
Embodiment 3:
Adefovir ester 8.7% (weight)
Pregelatinized Starch 14.4% (weight)
Microcrystalline Cellulose 39.2% (weight)
Lactose 21.2% (weight)
Carboxymethyl starch sodium 13.9% (weight)
Sodium lauryl sulphate 1.7% (weight)
Sunset yellow is an amount of
Magnesium stearate 0.9% (weight)
Get the adefovir ester of recipe quantity, cross 100 mesh sieves, other gets lactose, microcrystalline Cellulose, pregelatinized Starch, its Starch Sodium of carboxylic first, magnesium stearate, sodium lauryl sulphate, the sunset yellow of recipe quantity and crosses 60 mesh sieves, mix homogeneously, get the adjuvant with adefovir ester equivalent, cross 60 mesh sieve mix homogeneously, measure content with the method that equivalent is progressively increased, direct powder compression makes 1000 of adefovir ester dispersible tablets.
Embodiment 4:
Adefovir ester 1% (weight)
Pregelatinized Starch 19.4% (weight)
Microcrystalline Cellulose 45.3% (weight)
Lactose 17.6% (weight)
Carboxymethyl starch sodium 13.3% (weight)
Sodium lauryl sulphate 1.7% (weight)
Sunset yellow is an amount of
Magnesium stearate 1.7% (weight)
Get the adefovir ester of recipe quantity, cross 100 mesh sieves, other gets lactose, microcrystalline Cellulose, pregelatinized Starch, its Starch Sodium of carboxylic first, magnesium stearate, sodium lauryl sulphate, the sunset yellow of recipe quantity and crosses 60 mesh sieves, mix homogeneously, get the adjuvant with adefovir ester equivalent, cross 60 mesh sieve mix homogeneously, measure content with the method that equivalent is progressively increased, direct powder compression makes 1000 of adefovir ester dispersible tablets.
Embodiment 5:
Adefovir ester 20% (weight)
Pregelatinized Starch 10% (weight)
Microcrystalline Cellulose 40% (weight)
Lactose 18% (weight)
Carboxymethyl starch sodium 11% (weight)
Sodium lauryl sulphate 0.5% (weight)
Sunset yellow is an amount of
Magnesium stearate 0.5% (weight)
Get the adefovir ester of recipe quantity, cross 100 mesh sieves, other gets lactose, microcrystalline Cellulose, pregelatinized Starch, its Starch Sodium of carboxylic first, magnesium stearate, sodium lauryl sulphate, the sunset yellow of recipe quantity and crosses 60 mesh sieves, mix homogeneously, get the adjuvant with adefovir ester equivalent, cross 60 mesh sieve mix homogeneously, measure content with the method that equivalent is progressively increased, direct powder compression makes 1000 of adefovir ester dispersible tablets.
Claims (5)
1. an adefovir ester dispersible tablet is characterized in that the content range of each component is as follows: adefovir ester 1%-20% (weight), pregelatinized Starch 10%-20% (weight), microcrystalline Cellulose 25%-50% (weight), lactose 10%-30% (weight), carboxymethyl starch sodium 10%-30% (weight), sodium lauryl sulphate 0.5%-3% (weight), magnesium stearate 0.5%-3% (weight).
2. dispersible tablet according to claim 1 is characterized in that the content of each component consists of: 5%-15% (weight), pregelatinized Starch 12%-18% (weight), microcrystalline Cellulose 30%-40% (weight), lactose 14%-26% (weight), carboxymethyl starch sodium 15%-25% (weight), sodium lauryl sulphate 1%-2.5% (weight), magnesium stearate 1%-2.5% (weight).
3. according to the described dispersible tablet of claim 1--2, it is characterized in that the content of each component consists of: adefovir ester 8.3% (weight), pregelatinized Starch 16.6% (weight), microcrystalline Cellulose 33.4% (weight), lactose 16.6% (weight) % (weight), carboxymethyl starch sodium 21.7% (weight), sodium lauryl sulphate 1.7% (weight), magnesium stearate 1.7% (weight).
4. according to the preparation method of the described dispersible tablet of claim 1-3, it is characterized in that it comprises the following steps: to get adefovir ester and crosses 100 mesh sieves; Other gets pregelatinized Starch, microcrystalline Cellulose, lactose, carboxymethyl starch sodium, sodium lauryl sulphate, magnesium stearate and crosses 60 mesh sieves; With the adefovir ester mixing, powder directly is pressed into dispersible tablet.
5. according to the described dispersible tablet of claim 1-3, wherein said adefovir ester can be crystalline state or amorphous.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200410012867 CN1562046A (en) | 2004-03-19 | 2004-03-19 | Adefovir dipivoil dispersion tablet and preparing method |
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| CN 200410012867 CN1562046A (en) | 2004-03-19 | 2004-03-19 | Adefovir dipivoil dispersion tablet and preparing method |
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| CN1562046A true CN1562046A (en) | 2005-01-12 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100333719C (en) * | 2005-10-18 | 2007-08-29 | 安微济人药业有限公司 | Hyperlipemia-treating Chinese traditional medicinal tablet and its preparation process |
| CN100353943C (en) * | 2005-07-04 | 2007-12-12 | 广州固志医药科技有限公司 | Fleroxacin lactate dispersion tablet, and its prepn. method |
| CN103083339A (en) * | 2011-11-08 | 2013-05-08 | 广州白云山制药股份有限公司广州白云山制药总厂 | Adefovir dipivoxil pharmaceutical composition |
| CN114224858A (en) * | 2021-12-29 | 2022-03-25 | 辰欣药业股份有限公司 | Adefovir dipivoxil tablet and preparation method thereof |
-
2004
- 2004-03-19 CN CN 200410012867 patent/CN1562046A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100353943C (en) * | 2005-07-04 | 2007-12-12 | 广州固志医药科技有限公司 | Fleroxacin lactate dispersion tablet, and its prepn. method |
| CN100333719C (en) * | 2005-10-18 | 2007-08-29 | 安微济人药业有限公司 | Hyperlipemia-treating Chinese traditional medicinal tablet and its preparation process |
| CN103083339A (en) * | 2011-11-08 | 2013-05-08 | 广州白云山制药股份有限公司广州白云山制药总厂 | Adefovir dipivoxil pharmaceutical composition |
| CN103083339B (en) * | 2011-11-08 | 2014-05-28 | 广州白云山制药股份有限公司广州白云山制药总厂 | Adefovir dipivoxil pharmaceutical composition |
| CN114224858A (en) * | 2021-12-29 | 2022-03-25 | 辰欣药业股份有限公司 | Adefovir dipivoxil tablet and preparation method thereof |
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