CN108096206A - A kind of tenofovir disoproxil fumarate tablet and preparation method thereof - Google Patents
A kind of tenofovir disoproxil fumarate tablet and preparation method thereof Download PDFInfo
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- CN108096206A CN108096206A CN201810103835.8A CN201810103835A CN108096206A CN 108096206 A CN108096206 A CN 108096206A CN 201810103835 A CN201810103835 A CN 201810103835A CN 108096206 A CN108096206 A CN 108096206A
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- disoproxil fumarate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
Abstract
The invention belongs to biomedicine technical fields, and in particular to a kind of tenofovir disoproxil fumarate tablet, the tablet supplementary material are：Tenofovir disoproxil fumarate, cross-linked carboxymethyl cellulose, microcrystalline cellulose, pre-paying starch, magnesium stearate, slow-release material are methacrylic acid methyl acrylate copolymer and chitosan；The tablet is based on compound controlled slowly releasing adjuncts, filler, disintegrant, lubricant is added in be prepared, wherein compound slow controlled release raw material is made of methacrylic acid methyl acrylate copolymer and chitosan, after preparation being prepared into filler, disintegrant, lubricant, on the basis of reaching and at the uniform velocity controlling the requirement of release, while ensure that the tablet impurity content is stablized.
Description
Technical field
The invention belongs to biomedicine technical fields, and in particular to a kind of tenofovir disoproxil fumarate tablet and its
Preparation method.
Background technology
Tenofovir piece main component is tenofovir disoproxil fumarate.Tenofovir disoproxil fumarate is applicable in
It is shared in other antiretroviral drugs, treatment HIV-1 infection.
Tenofovir disoproxil fumarate is a kind of open nucleoside phosphine diester analogue of adenosine monophosphate, and fumaric acid replaces
Nuo Fuwei dipivoxils are tenofovir firstly the need of the hydrolysis through diester, then form two by the phosphorylation of cellular enzymes
Phosphoric acid tenofovir.Diphosphonic acid tenofovir with natural substrate 5'- deoxyadenosine triphosphates by competing, and whole with DNA
DNA chain is terminated after conjunction, so as to inhibit the activity of HIV-1 reverse transcriptase.Diphosphonic acid tenofovir to mammalian DNA polymerases α,
β and mitochondria DNA polymerase γ is weak inhibitor.
Tenofovir is had evaluated in lymph matricyte system, primary monocyte/macrophage and peripheral blood lymphocytes
Anti- laboratory and the activity for being clinically separated HIV-1 Strain.EC50 (50% effective concentration) values of tenofovir 0.04 μM-
Between 8.5 μM.Tenofovir and nucleoside reverse transcriptase inhibitors (Abacavir, deglycoside, Lamivudine, stavudine,
Zalcitabine, Zidovudine), non-nucleoside reverse transcriptase inhibitor (delavirdine, efavirenz, nevirapine), protease suppression
In the research of preparation (anpunave, indinavir, Nai Feinawei, Ritonavir, inverase) drug combination, discovery has synergy
Or synergistic effect.Tenofovir also has antiviral activity to hypotype A, B, C, D, E, F, G, O of HIV-1 in cell culture
(EC50 values are between 0.5 μM -2.2 μM), have to HIV-2 different activity due to Strain (EC50 values 1.6 μM -4.9 μM it
Between).
In analysis as defined in testing program, carry relevant with Abacavir/emtricitabine/lamivudine resistance
M184V is mutated the patient of HIV-1, and the virological response of tenofovir disoproxil fumarate is not reduced.Have with it is neat more
In the case that husband determines drug resistance related mutation, M184V has no effect on what HIV-1RNA treated tenofovir disoproxil fumarate
Average response.HIV-1RNA reactions persistently existed during 48 weeks in these patients.
Therefore, the novel formulation using tenofovir disoproxil fumarate as active ingredient is researched and developed, there is important clinical
Meaning.
The content of the invention
For these reasons, applicant tests by repeatedly creative, and research obtains a kind of new fumaric acid and replaces promise good fortune
Wei dipivoxil tablet, the tablet are based on compound controlled slowly releasing adjuncts, add in filler, disintegrant, lubricant and are prepared into
It arrives, wherein compound slow controlled release raw material is made of methacrylic acid-acrylic acid methyl terpolymer and chitosan, with filling
After agent, disintegrant, lubricant are prepared into preparation, on the basis of reaching and at the uniform velocity controlling the requirement of release, ensure that the tablet impurity contains
Amount is stablized.
The present invention is as follows by technical solution.
A kind of tenofovir disoproxil fumarate tablet, the tablet supplementary material are：Tenofovir disoproxil fumarate,
Cross-linked carboxymethyl cellulose, microcrystalline cellulose, pre-paying starch, magnesium stearate, slow-release material are methacrylic acid-acrylic acid first
Ester copolymer and chitosan.
A kind of tenofovir disoproxil fumarate tablet, wherein：300 weight of tenofovir disoproxil fumarate
Measure part, cross-linked carboxymethyl cellulose 75-85 parts by weight, microcrystalline cellulose 115-125 parts by weight, pre-paying starch 48-52 weight
Part, magnesium stearate 25-27 parts by weight, methacrylic acid-acrylic acid methyl terpolymer and chitosan 115-125 weight
Part.
A kind of tenofovir disoproxil fumarate tablet, wherein：300 weight of tenofovir disoproxil fumarate
Measure part, 80 parts by weight of cross-linked carboxymethyl cellulose, 120 parts by weight of microcrystalline cellulose, 50 parts by weight of pre-paying starch, magnesium stearate
26 parts by weight, 120 parts by weight of methacrylic acid-acrylic acid methyl terpolymer and chitosan.
A kind of tenofovir disoproxil fumarate tablet, wherein methacrylic acid-acrylic acid methyl terpolymer
Weight ratio with chitosan is：11：1.
A kind of tenofovir disoproxil fumarate tablet, wherein methacrylic acid-acrylic acid methyl terpolymer
Weight ratio with chitosan is：23：1.
A kind of preparation method of tenofovir disoproxil fumarate tablet is：
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains tablet.
Specific embodiment
Technical scheme is illustrated with specific embodiment below, but protection scope of the present invention is without being limited thereto.
Content described in this specification embodiment is only enumerating to the way of realization of inventive concept, protection of the invention
Scope is not construed as being only limitted to the concrete form that embodiment is stated, protection scope of the present invention is also and in art technology
Personnel conceive according to the present invention it is conceivable that equivalent technologies mean.Although embodiment of the invention below is retouched
It states, but the invention is not limited in above-mentioned specific embodiments and applications field, following specific embodiments is only to show
It is meaning property, guiding rather than restricted.Those of ordinary skill in the art under the enlightenment of this specification and are not taking off
In the case of the scope protected from the claims in the present invention, a variety of forms can also be made, these belong to the present invention
The row of protection.
The following experiments of the present invention are on the basis of multiple creative experiment, with the claimed technical solution of the present invention
Based on, the conclusive experiment of the research staff of summary.
Experiment 1
Disintegration time limited, friability test
Test 1 group：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, lactose 120g, starch
50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl terpolymer 120g.
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, lactose, starch,
Size controlling crosses 60 mesh sieves in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer；
(2) starch adds water, is prepared into 10% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, lactose, magnesium stearate, metering system are taken
In acid-methyl acrylate copolymer input granulator, it is uniformly mixed, adds in the aqueous suspension of starch, pelletize, dry, tabletting obtains
To 1000, tablet.
Test 2 groups：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, mannitol 120g form sediment
Powder 50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl terpolymer 120g.
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, mannitol, shallow lake
Powder, size controlling cross 60 mesh sieves in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer；
(2) starch adds water, is prepared into 10% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, mannitol, magnesium stearate, methyl-prop are taken
In olefin(e) acid-methyl acrylate copolymer input granulator, it is uniformly mixed, adds in the aqueous suspension of starch, pelletize, dry, tabletting,
Obtain 1000, tablet.
Test 3 groups：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, mannitol 120g, hydroxyl
Third cellulose 50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl terpolymer 120g.
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, mannitol, hydroxypropyl
Cellulose, size controlling cross 60 mesh sieves in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer；
(2) hydroxypropylcellulose adds water, is prepared into 10% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, mannitol, magnesium stearate, methyl-prop are taken
In olefin(e) acid-methyl acrylate copolymer input granulator, it is uniformly mixed, adds in the aqueous suspension of hydroxypropylcellulose, pelletize, do
Dry, tabletting obtains 1000, tablet.
Friability, disintegration time limited detection (according to Chinese Pharmacopoeia 2015 editions) are carried out to above-mentioned tablet, testing result is shown in Table 1：
The different tablet testing results of table 1
Result of the test：It is above-mentioned experiments have shown that, adjust the species of filler and adhesive etc. in tablet, the friability of the tablet
States Pharmacopoeia specifications are not met with disintegration time limited, and applicant continues to test.
Experiment 2
Dissolution Rate Testing
Test 1 group：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, microcrystalline cellulose
120g, pregelatinized starch 50g, magnesium stearate 26g, polyvinyl chloride 120g.
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling cross 60 mesh sieves in 100 mesh, magnesium stearate, polyvinyl chloride；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, poly- is taken
It in vinyl chloride input granulator, is uniformly mixed, adds in the aqueous suspension of pregelatinized starch, pelletize, dry, tabletting obtains tablet
1000.
Test 2 groups：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, microcrystalline cellulose
120g, pregelatinized starch 50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl esters 120g.
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling cross 60 mesh sieves in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl esters；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base acrylic acid-acrylic acid methyl esters input granulator, it is uniformly mixed, adds in the aqueous suspension of pregelatinized starch, pelletize, it is dry,
Tabletting obtains 1000, tablet.
Test 3 groups：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, microcrystalline cellulose
120g, pre-paying starch 50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl terpolymer 110g and chitosan
10g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 1000, tablet.
Friability, disintegration time limited detection (according to Chinese Pharmacopoeia 2015 editions) are carried out to above-mentioned tablet, testing result is shown in Table 2：
The different tablet testing results of table 2
Conclusion (of pressure testing)：It is above-mentioned experiments have shown that, after adjusting filler and adhesive in preparation prescription, friability and disintegration
Time limit meets the requirements.
Above-mentioned tablet is subjected to dissolution rate detection experiment：
This product is taken, according to dissolution rate and drug release determination method (four general rules of Chinese Pharmacopoeia version in 2015,0,931 first method), with
0.1mol/L hydrochloric acid solutions 900ml is dissolution medium, and rotating speed is 50 turns per minute, operates in accordance with the law, after 30 minutes, solution is taken to filter
It crosses, precision measures subsequent filtrate 5ml, puts 50mL volumetric flasks, with 0.1mol/L hydrochloric acids to scale, shakes up, molten as test sample
Liquid；Another precision takes tenofovir disoproxil fumarate reference substance 33.0mg, puts 100ml volumetric flasks, molten with 0.1mol/L hydrochloric acid
It solves and is diluted to scale.Precision measures 5ml, puts 50mL volumetric flasks, with 0.1mol/L hydrochloric acids to scale, shakes up, as right
According to product solution.Above two solution is taken, according to UV-VIS spectrophotometry (four general rules 0401 of Chinese Pharmacopoeia version in 2015),
Absorbance is measured at the wavelength of 260nm, calculates the stripping quantity of every.
Result of the test is shown in Table 3：
The different Dissolution of Tablet inspection results (%) of table 3
Conclusion (of pressure testing)：Tablet of the polyvinyl chloride for slow-release material is used, phenomenon of burst release occurs in 4h, therefore, it is impossible to adopt
It is used by the use of the auxiliary material of polyvinyl chloride as slow-release tablet agent of the present invention.
Experiment 3
Influence factor is tested
Take 3 groups of 2 groups of the experiment of experiment 2 and experiment；
Test 4 groups：Tenofovir disoproxil fumarate 300g, cross-linked carboxymethyl cellulose 80g, microcrystalline cellulose
120g, pre-paying starch 50g, magnesium stearate 26g, methacrylic acid-acrylic acid methyl terpolymer 115g and chitosan
5g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 1000, tablet.
It takes and 2 groups and 3 groups of preparations of experiment is tested in experiment 2, carry out influence factor experiment；
Content and method for detecting impurities are detected according to USP Method, and by Haikou City, medicine inspecting institute examines.
It the results are shown in Table 4, table 5, table 6.
The different preparation hot test results (60 DEG C) of table 4
The different preparation highlight test results of table 5
The different preparation highlight test results of table 6
Conclusion (of pressure testing)：By influence factor, experiments have shown that, 2 groups of preparations of experiment are single after 10 days high temperature and high wet test
Ester content, dimer content, total impurities content increase substantially, and the impurity for testing 3 groups and experiment 4 groups (Tablets) contains
Measure variable quantity very little, it is clear that adding in a certain amount of chitosan plays an important role of stability, therefore, in order to ensure that preparation produces
The superiority of the quality of product, applicant select a certain proportion of methacrylic acid-acrylic acid methyl terpolymer, chitosan
As slow-release material.
By above-mentioned experiments have shown that, chitosan, methacrylic acid-acrylic acid methyl terpolymer in Tablets
With disintegrant, filler, lubricant on the basis of dissolution rate is ensured, meanwhile, also ensure stability of active ingredient etc., because
This, the composition of invention formulation auxiliary material has important scientific meaning.
Prepare embodiment
Embodiment 1
Tenofovir disoproxil fumarate 3000g, cross-linked carboxymethyl cellulose 800g, microcrystalline cellulose 1200g are pre-payed
Change starch 500g, magnesium stearate 260g, methacrylic acid-acrylic acid methyl terpolymer 1150g and chitosan 50g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 10000, tablet.
Embodiment 2
Tenofovir disoproxil fumarate 3000g, cross-linked carboxymethyl cellulose 800g, microcrystalline cellulose 1200g are pre-payed
Change starch 500g, magnesium stearate 260g, methacrylic acid-acrylic acid methyl terpolymer 1100g and chitosan 100g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains tablet 10000.
Embodiment 3
Tenofovir disoproxil fumarate 15000g, cross-linked carboxymethyl cellulose 4000g, microcrystalline cellulose 6000g, in advance
Friendshipization starch 2500g, magnesium stearate 1300g, methacrylic acid-acrylic acid methyl terpolymer 5500g and chitosan
500g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 50000, tablet.
Embodiment 4
Tenofovir disoproxil fumarate 6000g, cross-linked carboxymethyl cellulose 1600g, microcrystalline cellulose 2400g, in advance
Friendshipization starch 1000g, magnesium stearate 520g, methacrylic acid-acrylic acid methyl terpolymer 2300g and chitosan
100g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 20000, tablet.
Embodiment 5
Tenofovir disoproxil fumarate 150g, cross-linked carboxymethyl cellulose 40g, microcrystalline cellulose 60g, pre-paying are formed sediment
Powder 25g, magnesium stearate 13g, methacrylic acid-acrylic acid methyl terpolymer 55g and chitosan 5g；
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose,
Pre-paying starch, size controlling is in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Cross 60 mesh sieves；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, first are taken
In base copolymer of acrylic acid and methyl acrylate, chitosan input granulator, it is uniformly mixed, adds in pregelatinized starch
Aqueous suspension is pelletized, dry, and tabletting obtains 500, tablet.
Supplementary material source of the present invention is as follows：
7 supplementary material source of table
The embodiment is including but not limited to above-mentioned.
Claims (6)
1. a kind of tenofovir disoproxil fumarate tablet, it is characterised in that the tablet supplementary material is：Fumaric acid tenofovir
Dipivoxil, cross-linked carboxymethyl cellulose, microcrystalline cellulose, pre-paying starch, magnesium stearate, slow-release material are metering system
Acid-methyl acrylate copolymer and chitosan.
2. a kind of tenofovir disoproxil fumarate tablet according to claim 1, wherein：Fumaric acid tenofovir two
300 parts by weight of pyrrole furan ester, cross-linked carboxymethyl cellulose 75-85 parts by weight, microcrystalline cellulose 115-125 parts by weight, pre-paying are formed sediment
Powder 48-52 parts by weight, magnesium stearate 25-27 parts by weight, methacrylic acid-acrylic acid methyl terpolymer and chitosan
115-125 parts by weight.
3. a kind of tenofovir disoproxil fumarate tablet according to claim 1, wherein：Fumaric acid tenofovir two
300 parts by weight of pyrrole furan ester, 80 parts by weight of cross-linked carboxymethyl cellulose, 120 parts by weight of microcrystalline cellulose, 50 weight of pre-paying starch
Part, 26 parts by weight of magnesium stearate, 120 parts by weight of methacrylic acid-acrylic acid methyl terpolymer and chitosan.
4. according to a kind of tenofovir disoproxil fumarate tablet of claim 1-3 any one of them, wherein metering system
The weight ratio of acid-methyl acrylate copolymer and chitosan is：11：1.
5. according to a kind of tenofovir disoproxil fumarate tablet of claim 1-3 any one of them, wherein metering system
The weight ratio of acid-methyl acrylate copolymer and chitosan is：23：1.
6. according to a kind of tenofovir disoproxil fumarate tablet of claim 1-5 any one of them, it is characterised in that should
The preparation method of tablet is：
(1) tenofovir disoproxil fumarate crosses 40 mesh screens, spare；Cross-linked carboxymethyl cellulose, microcrystalline cellulose are pre-payed
Change starch, size controlling crosses 60 in 100 mesh, magnesium stearate, methacrylic acid-acrylic acid methyl terpolymer, chitosan
Mesh sieve；
(2) pre-paying starch adds water, is prepared into 12% suspension of concentration, spare；
(3) tenofovir disoproxil fumarate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, methyl-prop are taken
In olefin(e) acid-methyl acrylate copolymer, chitosan input granulator, it is uniformly mixed, the water for adding in pregelatinized starch mixes
Suspension is pelletized, dry, and tabletting obtains tablet.
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| CN201910029160.1A CN109432029B (en) | 2018-02-01 | 2019-01-12 | Tenofovir disoproxil fumarate tablet and preparation method thereof |
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2018
- 2018-02-01 CN CN201810103835.8A patent/CN108096206A/en active Pending
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2019
- 2019-01-12 CN CN201910029160.1A patent/CN109432029B/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1984640A (en) * | 2004-07-09 | 2007-06-20 | 吉里德科学公司 | Topical antiviral formulations |
| CN105395504A (en) * | 2015-11-26 | 2016-03-16 | 郑州瑞启生物技术有限公司 | Flunarizine hydrochloride matrix sustained-release tablets and preparing method thereof |
| CN105853380A (en) * | 2016-04-29 | 2016-08-17 | 广州白云山医药集团股份有限公司白云山制药总厂 | Fumaric-acid-tenofovir-dipivoxil tablet and preparing method thereof |
| CN106727437A (en) * | 2017-01-05 | 2017-05-31 | 蚌埠丰原涂山制药有限公司 | A kind of tenofovir disoproxil fumarate spansule and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 杜艺伟等: "富马酸替诺福韦二吡呋酯片处方开发研究", 《中国医药科学》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN109432029A (en) | 2019-03-08 |
| CN109432029B (en) | 2020-10-30 |
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