CN1203856C - Dispersion tablet of vasilowy hydrochlaride and its prepn. method - Google Patents
Dispersion tablet of vasilowy hydrochlaride and its prepn. method Download PDFInfo
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- CN1203856C CN1203856C CN 03125292 CN03125292A CN1203856C CN 1203856 C CN1203856 C CN 1203856C CN 03125292 CN03125292 CN 03125292 CN 03125292 A CN03125292 A CN 03125292A CN 1203856 C CN1203856 C CN 1203856C
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- Prior art keywords
- dispersible tablet
- polyvinylpyrrolidone
- sodium
- preparation
- hypromellose
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- 238000000034 method Methods 0.000 title abstract 3
- 239000006185 dispersion Substances 0.000 title description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 32
- 239000007919 dispersible tablet Substances 0.000 claims abstract description 24
- 238000002360 preparation method Methods 0.000 claims abstract description 20
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 16
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 15
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 15
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 15
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 12
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 12
- 239000008187 granular material Substances 0.000 claims abstract description 11
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 11
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 11
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 11
- 229960003943 hypromellose Drugs 0.000 claims abstract description 11
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims abstract description 10
- 108010011485 Aspartame Proteins 0.000 claims abstract description 9
- 239000000605 aspartame Substances 0.000 claims abstract description 9
- 235000010357 aspartame Nutrition 0.000 claims abstract description 9
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims abstract description 9
- 229960003438 aspartame Drugs 0.000 claims abstract description 9
- 235000019700 dicalcium phosphate Nutrition 0.000 claims abstract description 9
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 8
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims abstract description 8
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 8
- 229950005770 hyprolose Drugs 0.000 claims abstract description 8
- 239000011734 sodium Substances 0.000 claims abstract description 8
- 229910052708 sodium Inorganic materials 0.000 claims abstract description 8
- 229940013618 stevioside Drugs 0.000 claims abstract description 8
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims abstract description 8
- 235000019202 steviosides Nutrition 0.000 claims abstract description 8
- 229920002472 Starch Polymers 0.000 claims abstract description 7
- 239000008107 starch Substances 0.000 claims abstract description 7
- 235000019698 starch Nutrition 0.000 claims abstract description 7
- HDOVUKNUBWVHOX-QMMMGPOBSA-N Valacyclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCOC(=O)[C@@H](N)C(C)C)C=N2 HDOVUKNUBWVHOX-QMMMGPOBSA-N 0.000 claims description 27
- 229940093257 valacyclovir Drugs 0.000 claims description 26
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 15
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 15
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 15
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 15
- 239000000203 mixture Substances 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 15
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 11
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 11
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 10
- 230000001476 alcoholic effect Effects 0.000 claims description 10
- 239000000741 silica gel Substances 0.000 claims description 10
- 229910002027 silica gel Inorganic materials 0.000 claims description 10
- 239000000243 solution Substances 0.000 claims description 10
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 8
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 8
- 238000001035 drying Methods 0.000 claims description 8
- 229940085605 saccharin sodium Drugs 0.000 claims description 8
- 206010013786 Dry skin Diseases 0.000 claims description 7
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 7
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 claims description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 239000007864 aqueous solution Substances 0.000 claims description 5
- 239000007779 soft material Substances 0.000 claims description 5
- 239000003826 tablet Substances 0.000 abstract description 10
- 239000003814 drug Substances 0.000 abstract description 6
- 238000005516 engineering process Methods 0.000 abstract description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 4
- ZCDDBUOENGJMLV-QRPNPIFTSA-N Valacyclovir hydrochloride Chemical compound Cl.N1C(N)=NC(=O)C2=C1N(COCCOC(=O)[C@@H](N)C(C)C)C=N2 ZCDDBUOENGJMLV-QRPNPIFTSA-N 0.000 abstract description 3
- 229940079593 drug Drugs 0.000 abstract description 3
- 238000004519 manufacturing process Methods 0.000 abstract description 3
- 238000004090 dissolution Methods 0.000 abstract description 2
- 239000000945 filler Substances 0.000 abstract description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 abstract 1
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 abstract 1
- 229920000084 Gum arabic Polymers 0.000 abstract 1
- 241000978776 Senegalia senegal Species 0.000 abstract 1
- 239000000205 acacia gum Substances 0.000 abstract 1
- 235000010489 acacia gum Nutrition 0.000 abstract 1
- XAAHAAMILDNBPS-UHFFFAOYSA-L calcium hydrogenphosphate dihydrate Chemical compound O.O.[Ca+2].OP([O-])([O-])=O XAAHAAMILDNBPS-UHFFFAOYSA-L 0.000 abstract 1
- 229940041616 menthol Drugs 0.000 abstract 1
- 229940049703 saccharin sodium dihydrate Drugs 0.000 abstract 1
- 229940064636 valacyclovir hydrochloride Drugs 0.000 abstract 1
- 229960004150 aciclovir Drugs 0.000 description 9
- MKUXAQIIEYXACX-UHFFFAOYSA-N aciclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCO)C=N2 MKUXAQIIEYXACX-UHFFFAOYSA-N 0.000 description 9
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 6
- 241000701022 Cytomegalovirus Species 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- 230000002155 anti-virotic effect Effects 0.000 description 2
- 239000003443 antiviral agent Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 2
- 239000010452 phosphate Substances 0.000 description 2
- 230000026731 phosphorylation Effects 0.000 description 2
- 238000006366 phosphorylation reaction Methods 0.000 description 2
- 230000003612 virological effect Effects 0.000 description 2
- -1 6-oxo-2-amino-1,6-dihydro-9H-purine-9-yl Chemical group 0.000 description 1
- 206010059313 Anogenital warts Diseases 0.000 description 1
- 102000016928 DNA-directed DNA polymerase Human genes 0.000 description 1
- 108010014303 DNA-directed DNA polymerase Proteins 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- 208000001688 Herpes Genitalis Diseases 0.000 description 1
- 208000009889 Herpes Simplex Diseases 0.000 description 1
- 208000007514 Herpes zoster Diseases 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 102000006601 Thymidine Kinase Human genes 0.000 description 1
- 108020004440 Thymidine kinase Proteins 0.000 description 1
- 241000934136 Verruca Species 0.000 description 1
- 108020005202 Viral DNA Proteins 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 208000000260 Warts Diseases 0.000 description 1
- 238000005260 corrosion Methods 0.000 description 1
- 230000007797 corrosion Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 201000004946 genital herpes Diseases 0.000 description 1
- 208000002672 hepatitis B Diseases 0.000 description 1
- 238000005213 imbibition Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 238000009434 installation Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
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- 238000002054 transplantation Methods 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Images
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a valaciclovir hydrochloride dispersible tablet and a preparation method thereof. The dispersible tablet contains 22.1 to 56.2 wt% of valacyclovir hydrochloride, 28.3 to 67.3 wt% of filler starch, cellulose microcrystalline and/or calcium hydrogenphosphate dihydrate, 4.3 to 20.3 wt% of sodium carboxyl methylstarch, hyprolose, crosslinked polyvinylpyrrolidone and/or crosslinked carmethose, 0.13 to 1.4 wt% of polyvinylpyrrolidone or hypromellose, 0.9 to 8.1 wt% of saccharin sodium dihydrate, aspartame or stevioside, 0 to 0.7 wt% of menthol, 0.25 to 1 wt% of magnesium stearate, and 0.25 to 2.3 wt% of talc powder or gum arabic. Because the dispersible tablet of the present invention has the unique properties of short disintegration time, good dispersed state, rapid dissolution of drugs, high biologic utilization degree, convenient administration, etc., the process technology of the dispersible tablet is the same as the process technology of the general non-coated tablet. No special equipment is needed and the production cost is lower. The dispersible tablet of the present invention can be entirely disintegrated and dispersed in water of the indoor temperature within 3 minutes, and the granules can pass through a No. 2 sieve.
Description
Technical field
The present invention relates to antiviral agents valaciclovir hydrochlordide dispersible tablet and preparation method thereof.
Background technology
Valaciclovir hydrochlordide is L-valine-2-[(6-oxo-2-amino-1,6-dihydro-9H-purine-9-yl) methoxyl group] the ethyl ester hydrochlorate.English Valaciclovir Hydrochloride by name.
Valaciclovir hydrochlordide (VACV) is a kind of than the higher antiviral agents of its female medicine acyclovir bioavailability, absorbs fully rapidly after it is oral, and is converted into the acyclovir (ACV) with antivirus action in vivo very soon.After ACV enters the cell of viral infection, by viral thymidine kinase and cell kinase phosphorylation, medicine is become activated form acyclovir triguaiacyl phosphate by phosphorylation at last, and the acyclovir triguaiacyl phosphate suppresses viral dna polymerase, stop viral DNA synthetic, show antivirus action.This product oral administration biaavailability is 3～5 times of ACV.Overcome the shortcoming that ACV takes inconvenience (oral, 5 times on the one), only need take 2 times in 1st.The oral administration of its doses is similar to the pharmacokinetic parameters of intravenous injection ACV.Therefore, its clinical use is more convenient, and patient's compliance is better.
This product is in the listing of dozens of country, be mainly used in the herpes simplex of treatment herpes zoster, skin and mucosa, comprise that genital herpes, hepatitis B, verruca plana, condyloma acuminatum and the prevention HIV patient who just sends out and recur, organ transplantation person's cytomegalovirus (CMV) infect.
External more at present to the dosage form research of this product, conventional tablet, capsule, injection, dry syrup, granule, collyrium (facing the time spent preparation), biologic adhesion preparation, gel etc. are arranged.Its conventional tablet generally uses in many countries, and its granule, capsule are also in Japan and China's listing.
(150～500mg), its ordinary tablet with larger volume can only be swallowed again, and this is had dysphagia person, makes troubles as child and gerontal patient because the single dose of this product is big.
Summary of the invention
It is flexible that problem to be solved by this invention provides a kind of taking convenience, both can suck clothes, swallow, and can add valaciclovir hydrochlordide dispersible tablet of taking after the aqueous dispersion and preparation method thereof again.
Technical scheme provided by the invention is: the valaciclovir hydrochlordide dispersible tablet, the valaciclovir hydrochlordide that contains 22.1～56.2wt%, 32.8 the filler starch of～67.3wt%, microcrystalline Cellulose and/or calcium hydrogen phosphate, 7.6 the carboxymethylstach sodium of～20.3wt%, hyprolose, crospolyvinylpyrrolidone and/or cross-linked carboxymethyl cellulose sodium, 0.13 the polyvinylpyrrolidone of～1.4wt% or hypromellose, 0.9 the saccharin sodium of～8.1wt%, aspartame or stevioside, the Mentholum of 0～0.7wt%, 0.25 the magnesium stearate of～1wt%, the Pulvis Talci of 0.25～2.3wt% or micropowder silica gel.
The present invention also provides the preparation method of above-mentioned dispersible tablet, get valaciclovir hydrochlordide, starch, microcrystalline Cellulose and/or calcium hydrogen phosphate, carboxymethylstach sodium, hyprolose, crospolyvinylpyrrolidone and/or cross-linked carboxymethyl cellulose sodium, saccharin sodium, aspartame or the stevioside mix homogeneously that sieves, polyvinylpyrrolidone or hypromellose are mixed with the aqueous solution or the alcoholic solution of 5～50 grams per liter solvents, add then and make soft material in the said mixture, 14～24 mesh sieves are granulated, 50～60 ℃ of dryings 4～6 hours, 14～24 mesh sieve granulate, add Mentholum, magnesium stearate, Pulvis Talci or micropowder silica gel, mix homogeneously, tabletting promptly get required dispersible tablet.
Above-mentioned preparation polyvinylpyrrolidone or the used ethanol of hypromellose alcoholic solution are the ethanol water of 20～50% (volume ratios).
Advantage of the present invention and good effect
Dispersible tablet of the present invention is because of having disintegration time weak point, good dispersing state, special performances such as the medicine stripping is rapid, bioavailability is high, taking convenience, and its production technology is identical with common non-coated tablet, does not need special installation, and production cost is lower.The tablet that the water soluble drug that content of dispersion is bigger is made, its disintegrate mechanism is corrosion, but not imbibition.Dispersible tablet of the present invention in the water of room temperature (15～25 ℃ or 19～21 ℃), all disintegrates, dispersion within 3 minutes, granule can sieve by No. 2.Therefore, as can be seen, also can be developed into dispersible tablet by the suitable bigger water soluble drug of prescription design content of dispersion.
Description of drawings
Accompanying drawing is the valaciclovir hydrochlordide dispersible tablet of the present invention's preparation and the stripping curve figure of commercially available ordinary tablet.
The specific embodiment
Embodiment 1 per 1000 consumptions
Valaciclovir hydrochlordide 200g
Microcrystalline Cellulose 530g
Hyprolose 40
Cross-linked carboxymethyl cellulose sodium 66g (intragranular respectively adds 33g outward)
Stevioside 40g
Polyvinylpyrrolidone (k30) 7g
Mentholum 3g
Pulvis Talci 11g
Magnesium stearate 5g
The preparation of valaciclovir hydrochlordide dispersible tablet
Cross-linked carboxymethyl cellulose sodium of getting valaciclovir hydrochlordide, microcrystalline Cellulose, hyprolose, stevioside and half amount of recipe quantity sieves, mix homogeneously, polyvinylpyrrolidone is made into the aqueous solution of 50 grams per liter solvents, add in the said mixture and make soft material, crossing 14 mesh sieves granulates, 50～60 ℃ of dryings 4 hours add Mentholum, Pulvis Talci, magnesium stearate and residue cross-linked carboxymethyl cellulose sodium mix homogeneously, tabletting promptly.
Embodiment 2 per 1000 consumptions
Valaciclovir hydrochlordide 500g
Microcrystalline Cellulose 200g
Starch 100g
Cross-linked carboxymethyl cellulose sodium 70g
Saccharin sodium 23g
Hypromellose 2g
Pulvis Talci 16g
Magnesium stearate 4g
The preparation of valaciclovir hydrochlordide dispersible tablet
Valaciclovir hydrochlordide, microcrystalline Cellulose, starch, cross-linked carboxymethyl cellulose sodium, the saccharin sodium of getting recipe quantity sieves, mix homogeneously, hypromellose is made into the aqueous solution of 5 grams per liters, add in the said mixture and make soft material, crossing 24 mesh sieves granulates, 50～60 ℃ of dryings 4 hours add Pulvis Talci, magnesium stearate mix homogeneously, tabletting promptly.
Embodiment 3 per 1000 consumptions
Valaciclovir hydrochlordide 500g
Microcrystalline Cellulose 700g
Crospolyvinylpyrrolidone 64g (grain is outer to add)
Saccharin sodium 23g
Polyvinylpyrrolidone (k30) 5g
Mentholum 5g
Micropowder silica gel 4g
Magnesium stearate 4g
Annotate: polyvinylpyrrolidone is made into the alcoholic solution of 30 grams per liter solvents, and solvent adopts the ethanol water of 50% volume ratio.
The preparation of valaciclovir hydrochlordide dispersible tablet
Valaciclovir hydrochlordide, microcrystalline Cellulose, the saccharin sodium of getting recipe quantity sieves, mix homogeneously, polyvinylpyrrolidone is made into the alcoholic solution of 30 grams per liter solvents with the ethanol of 50% volume ratio, add in the said mixture and make soft material, crossing 14 mesh sieves granulates, 50～60 ℃ of dryings 6 hours add Mentholum, micropowder silica gel, magnesium stearate and crospolyvinylpyrrolidone mix homogeneously, tabletting promptly.
Embodiment 4 per 1000 consumptions
Valaciclovir hydrochlordide 150g
Microcrystalline Cellulose 210g
Crospolyvinylpyrrolidone 44g (intragranular respectively adds 22g outward)
Stevioside 18g
Hypromellose 1.5g
Mentholum 1.5g
Pulvis Talci 10g
Magnesium stearate 2g
Annotate: hypromellose is made into the aqueous solution of 10 grams per liter solvents.
Preparation method is with embodiment 1.Wherein drying condition is 50～60 ℃, 6 hours.
Embodiment 5 per 1000 consumptions
Valaciclovir hydrochlordide 300g
Microcrystalline Cellulose 200g
Calcium hydrogen phosphate 200g
Carboxymethylstach sodium 44g
Crospolyvinylpyrrolidone 66g (intragranular respectively adds 33g outward)
Aspartame 24g
Polyvinylpyrrolidone (k30) 3g
Mentholum 3g
Micropowder silica gel 8g
Magnesium stearate 4g
Annotate: polyvinylpyrrolidone is made into the alcoholic solution of 10 grams per liter solvents, and solvent adopts the ethanol water of 20% volume ratio.
Preparation technology: with embodiment 1.Wherein be that 24 mesh sieves are granulated, 50～60 ℃ of dryings 6 hours, 24 mesh sieve granulate.
According to above-mentioned prescription, prepared dispersible tablet, measure its dissolution, draw stripping curve, and compare with commercially available ordinary tablet.The results are shown in accompanying drawing, wherein " ▲ " is commercially available ordinary tablet stripping curve, and " ■ " is self-control dispersible tablet stripping curve.As seen the dispersible tablet stripping is obviously accelerated than commercially available ordinary tablet.
Embodiment 6 per 1000 consumptions
Valaciclovir hydrochlordide 300g
Microcrystalline Cellulose 150g
Calcium hydrogen phosphate 250g
Hyprolose 60g
Cross-linked carboxymethyl cellulose sodium 70g (intragranular respectively adds 35g outward)
Aspartame 24g
Polyvinylpyrrolidone (k90) 11
Micropowder silica gel 10g
Magnesium stearate 5g
Annotate: polyvinylpyrrolidone is made into the alcoholic solution of 20 grams per liter solvents, and solvent adopts the ethanol water of 90% volume ratio.
Preparation method is with embodiment 1.
Embodiment 7 per 1000 consumptions
Valaciclovir hydrochlordide 400g
Microcrystalline Cellulose 250g
Calcium hydrogen phosphate 250g
Carboxymethylstach sodium 50g
Cross-linked carboxymethyl cellulose sodium 90g (intragranular respectively adds 45g outward)
Aspartame 24
Polyvinylpyrrolidone (k90) 6
Magnesium stearate 5
Annotate: polyvinylpyrrolidone is made into the alcoholic solution of 30 grams per liter solvents, and solvent adopts the ethanol water of 40% volume ratio.
Preparation method is with embodiment 1.
Embodiment 8 per 1000 consumptions
Valaciclovir hydrochlordide 150g
Microcrystalline Cellulose 100g
Calcium hydrogen phosphate 100g
Carboxymethylstach sodium 22g
Crospolyvinylpyrrolidone 34g (intragranular respectively adds 17g outward)
Aspartame 12g
Polyvinylpyrrolidone (k30) 1.5g
Mentholum 1.5g
Micropowder silica gel 5g
Magnesium stearate 2g
Annotate: polyvinylpyrrolidone is made into the alcoholic solution of 10 grams per liter solvents, and solvent adopts the ethanol water of 70% volume ratio.
Preparation method is with embodiment 1.Wherein be that 24 mesh sieves are granulated, 50～60 ℃ of dryings 6 hours, 24 mesh sieve granulate.
Claims (3)
1. valaciclovir hydrochlordide dispersible tablet, contain the valaciclovir hydrochlordide of 22.1～56.2wt%, starch, microcrystalline Cellulose and/or the calcium hydrogen phosphate of 32.8～67.3wt%, 7.6 the carboxymethylstach sodium of～20.3wt%, hyprolose, crospolyvinylpyrrolidone and/or cross-linked carboxymethyl cellulose sodium, 0.13 the polyvinylpyrrolidone of～1.4wt% or hypromellose, 0.9 the saccharin sodium of～8.1wt%, aspartame or stevioside, the Mentholum of 0～0.7wt%, 0.25 the magnesium stearate of～1wt%, the Pulvis Talci of 0.25～2.3wt% or micropowder silica gel.
2. the preparation method of the described dispersible tablet of claim 1, get valaciclovir hydrochlordide, starch, microcrystalline Cellulose and/or calcium hydrogen phosphate, carboxymethylstach sodium, hyprolose, crospolyvinylpyrrolidone and/or cross-linked carboxymethyl cellulose sodium, saccharin sodium, aspartame or the stevioside mix homogeneously that sieves, polyvinylpyrrolidone or hypromellose are mixed with the aqueous solution or the alcoholic solution of 5～50 grams per liter solvents, add then and make soft material in the said mixture, 14～24 mesh sieves are granulated, 50～60 ℃ of dryings 4～6 hours, 14～24 mesh sieve granulate, add Mentholum, magnesium stearate, Pulvis Talci or micropowder silica gel, mix homogeneously, tabletting promptly get required dispersible tablet.
3. preparation method according to claim 2 is characterized in that: preparation polyvinylpyrrolidone or the used ethanol of hypromellose alcoholic solution are the ethanol water of 20～50% volume ratios.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03125292 CN1203856C (en) | 2003-08-19 | 2003-08-19 | Dispersion tablet of vasilowy hydrochlaride and its prepn. method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 03125292 CN1203856C (en) | 2003-08-19 | 2003-08-19 | Dispersion tablet of vasilowy hydrochlaride and its prepn. method |
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| CN1513454A CN1513454A (en) | 2004-07-21 |
| CN1203856C true CN1203856C (en) | 2005-06-01 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100435797C (en) * | 2005-05-10 | 2008-11-26 | 北京明新高科技发展有限公司 | Oral quick release preparation of indinavir, and preparing method |
| CN100435804C (en) * | 2005-05-10 | 2008-11-26 | 北京明新高科技发展有限公司 | Oral preparation of quick releasing stavudine, and producing method |
| CN101804037B (en) * | 2009-02-13 | 2014-05-28 | 北京以岭生物工程技术有限公司 | Acyclovir dispersible tablet and preparation method thereof |
| WO2013046453A1 (en) * | 2011-09-30 | 2013-04-04 | 持田製薬株式会社 | Easy-to-take solid preparation |
| CN103462918B (en) * | 2013-09-22 | 2015-12-02 | 南京正宽医药科技有限公司 | A kind of Valaciclovir hydrochloride tablet and preparation method thereof |
| CN105213898A (en) * | 2015-10-29 | 2016-01-06 | 青岛海之源智能技术有限公司 | A kind of valaciclovir hydrochlordide compound capsule and preparation method thereof |
| CN109662951A (en) * | 2018-12-31 | 2019-04-23 | 辰欣药业股份有限公司 | A kind of dispersion tablet of vasilowy hydrochlaride and its preparation process of high bioavilability |
| CN110693840A (en) * | 2019-09-19 | 2020-01-17 | 湖北科益药业股份有限公司 | High-utilization-degree valaciclovir hydrochloride dispersible tablet and preparation process thereof |
| CN113274356A (en) * | 2021-05-25 | 2021-08-20 | 丽珠集团丽珠制药厂 | Valaciclovir hydrochloride granules and preparation method thereof |
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2003
- 2003-08-19 CN CN 03125292 patent/CN1203856C/en not_active Expired - Lifetime
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| CN1513454A (en) | 2004-07-21 |
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