CN101461788A - Phloroglucine orally disintegrating tablet and preparation method thereof - Google Patents
Phloroglucine orally disintegrating tablet and preparation method thereof Download PDFInfo
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- CN101461788A CN101461788A CNA2007101725183A CN200710172518A CN101461788A CN 101461788 A CN101461788 A CN 101461788A CN A2007101725183 A CNA2007101725183 A CN A2007101725183A CN 200710172518 A CN200710172518 A CN 200710172518A CN 101461788 A CN101461788 A CN 101461788A
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- Prior art keywords
- phloroglucinol
- content
- orally disintegrating
- tablet
- disintegrating tablet
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000006191 orally-disintegrating tablet Substances 0.000 title claims abstract description 33
- QCDYQQDYXPDABM-UHFFFAOYSA-N phloroglucinol Chemical compound OC1=CC(O)=CC(O)=C1 QCDYQQDYXPDABM-UHFFFAOYSA-N 0.000 title claims abstract description 30
- 229960001553 phloroglucinol Drugs 0.000 title claims abstract description 29
- 238000002360 preparation method Methods 0.000 title claims abstract description 23
- JPYHHZQJCSQRJY-UHFFFAOYSA-N Phloroglucinol Natural products CCC=CCC=CCC=CCC=CCCCCC(=O)C1=C(O)C=C(O)C=C1O JPYHHZQJCSQRJY-UHFFFAOYSA-N 0.000 claims abstract description 28
- 239000003826 tablet Substances 0.000 claims abstract description 28
- 238000000034 method Methods 0.000 claims abstract description 22
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 14
- 239000007884 disintegrant Substances 0.000 claims abstract 3
- 239000003795 chemical substances by application Substances 0.000 claims description 19
- 239000011230 binding agent Substances 0.000 claims description 15
- 239000000314 lubricant Substances 0.000 claims description 15
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid group Chemical group C(CC(O)(C(=O)O)CC(=O)O)(=O)O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 9
- 239000003086 colorant Substances 0.000 claims description 8
- 239000000945 filler Substances 0.000 claims description 8
- 239000008187 granular material Substances 0.000 claims description 7
- 239000007779 soft material Substances 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 239000000463 material Substances 0.000 claims description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 5
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 108010011485 Aspartame Proteins 0.000 claims description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 3
- 229930195725 Mannitol Natural products 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 3
- 239000000605 aspartame Substances 0.000 claims description 3
- 235000010357 aspartame Nutrition 0.000 claims description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical group OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 3
- 229960003438 aspartame Drugs 0.000 claims description 3
- 239000008101 lactose Substances 0.000 claims description 3
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 3
- 239000000594 mannitol Substances 0.000 claims description 3
- 235000010355 mannitol Nutrition 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- 239000011975 tartaric acid Substances 0.000 claims description 3
- 235000002906 tartaric acid Nutrition 0.000 claims description 3
- 235000005979 Citrus limon Nutrition 0.000 claims description 2
- 244000131522 Citrus pyriformis Species 0.000 claims description 2
- 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 description 2
- 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 description 2
- 239000000796 flavoring agent Substances 0.000 claims description 2
- 235000019634 flavors Nutrition 0.000 claims description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- -1 pH regulators Substances 0.000 claims description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
- 238000010298 pulverizing process Methods 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 235000003599 food sweetener Nutrition 0.000 claims 4
- 239000003765 sweetening agent Substances 0.000 claims 4
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 claims 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 2
- 239000003205 fragrance Substances 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 239000000729 antidote Substances 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 claims 1
- 239000007968 orange flavor Substances 0.000 claims 1
- 239000007967 peppermint flavor Substances 0.000 claims 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims 1
- 229940083542 sodium Drugs 0.000 claims 1
- 235000015424 sodium Nutrition 0.000 claims 1
- UJMBCXLDXJUMFB-GLCFPVLVSA-K tartrazine Chemical group [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1\N=N\C1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-GLCFPVLVSA-K 0.000 claims 1
- 229960000943 tartrazine Drugs 0.000 claims 1
- 235000012756 tartrazine Nutrition 0.000 claims 1
- 239000004149 tartrazine Substances 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 abstract description 15
- 230000000694 effects Effects 0.000 abstract description 6
- 239000000843 powder Substances 0.000 abstract description 6
- 210000003296 saliva Anatomy 0.000 abstract 1
- 238000005550 wet granulation Methods 0.000 abstract 1
- ADZXDFALMZGPTN-UHFFFAOYSA-M Diponium bromide Chemical compound [Br-].C1CCCC1C(C(=O)OCC[N+](CC)(CC)CC)C1CCCC1 ADZXDFALMZGPTN-UHFFFAOYSA-M 0.000 description 19
- 239000003814 drug Substances 0.000 description 8
- 238000005516 engineering process Methods 0.000 description 8
- 238000005259 measurement Methods 0.000 description 8
- 238000004519 manufacturing process Methods 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 238000001035 drying Methods 0.000 description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 210000002460 smooth muscle Anatomy 0.000 description 4
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- 208000002193 Pain Diseases 0.000 description 3
- 230000006835 compression Effects 0.000 description 3
- 238000007906 compression Methods 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- 235000009854 Cucurbita moschata Nutrition 0.000 description 2
- 240000001980 Cucurbita pepo Species 0.000 description 2
- 235000009852 Cucurbita pepo Nutrition 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- 208000007101 Muscle Cramp Diseases 0.000 description 2
- 208000005392 Spasm Diseases 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 238000004132 cross linking Methods 0.000 description 2
- 238000007922 dissolution test Methods 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 238000012856 packing Methods 0.000 description 2
- 210000000582 semen Anatomy 0.000 description 2
- 235000020354 squash Nutrition 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 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 description 1
- WQNHWIYLCRZRLR-UHFFFAOYSA-N 2-(3-hydroxy-2,5-dioxooxolan-3-yl)acetic acid Chemical compound OC(=O)CC1(O)CC(=O)OC1=O WQNHWIYLCRZRLR-UHFFFAOYSA-N 0.000 description 1
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 1
- 229930003347 Atropine Natural products 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 206010013786 Dry skin Diseases 0.000 description 1
- 239000001329 FEMA 3811 Substances 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 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 description 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- 206010038419 Renal colic Diseases 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 235000010358 acesulfame potassium Nutrition 0.000 description 1
- 229960004998 acesulfame potassium Drugs 0.000 description 1
- 239000000619 acesulfame-K Substances 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 229910052934 alunite Inorganic materials 0.000 description 1
- 239000010424 alunite Substances 0.000 description 1
- 150000008064 anhydrides Chemical class 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 1
- 229960000396 atropine Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000003445 biliary tract Anatomy 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 230000009084 cardiovascular function Effects 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 230000003153 cholinolytic effect Effects 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 210000003298 dental enamel Anatomy 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 210000002249 digestive system Anatomy 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000011010 flushing procedure Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 230000036543 hypotension Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000012982 microporous membrane Substances 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- ITVGXXMINPYUHD-CUVHLRMHSA-N neohesperidin dihydrochalcone Chemical compound C1=C(O)C(OC)=CC=C1CCC(=O)C(C(=C1)O)=C(O)C=C1O[C@H]1[C@H](O[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 ITVGXXMINPYUHD-CUVHLRMHSA-N 0.000 description 1
- 229940089953 neohesperidin dihydrochalcone Drugs 0.000 description 1
- 235000010434 neohesperidine DC Nutrition 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000009702 powder compression Methods 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000007898 rapid-disintegration tablet Substances 0.000 description 1
- 229940085605 saccharin sodium Drugs 0.000 description 1
- 239000004576 sand Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 230000002048 spasmolytic effect Effects 0.000 description 1
- 230000001148 spastic effect Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- RINCXYDBBGOEEQ-UHFFFAOYSA-N succinic anhydride Chemical class O=C1CCC(=O)O1 RINCXYDBBGOEEQ-UHFFFAOYSA-N 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- KPZTWMNLAFDTGF-UHFFFAOYSA-D trialuminum;potassium;hexahydroxide;disulfate Chemical compound [OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Al+3].[Al+3].[Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O KPZTWMNLAFDTGF-UHFFFAOYSA-D 0.000 description 1
- 210000003708 urethra Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
本发明公开了一种间苯三酚口腔崩解片及其制备方法。采用粉末湿法制粒压片法，制备了间苯三酚口腔崩解片，其包含治疗有效量的间苯三酚和可药用的赋形剂，所述的赋形剂中包括崩解剂，按片剂总重量计，间苯三酚的含量为15～30％，所述的赋形剂的含量为70～85％，所述的崩解剂的含量为3～23％。本发明的间苯三酚口腔崩解片硬度较高，制备工艺简单，疗效显著，在口腔内与唾液接触最快不到10秒的时间快速崩解，患者服用方便。The invention discloses a phloroglucinol orally disintegrating tablet and a preparation method thereof. Phloroglucinol orally disintegrating tablets were prepared by powder wet granulation tableting method, which contained a therapeutically effective amount of phloroglucinol and pharmaceutically acceptable excipients, including disintegrants in the excipients According to the total weight of the tablet, the content of phloroglucinol is 15-30%, the content of the excipient is 70-85%, and the content of the disintegrant is 3-23%. The orally disintegrating tablet of phloroglucinol of the present invention has high hardness, simple preparation process, remarkable curative effect, and disintegrates quickly in less than 10 seconds at the fastest contact with saliva in the oral cavity, and is convenient for patients to take.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, particularly a kind of Spaston orally disintegrating tablets and preparation method thereof.
Background technology
The pain that smooth muscle spasm causes is one of modal emergency case clinically, the acute spasmic pain that causes as digestive system and biliary tract dysfunction; Acute spastic urethra, bladder, renal colic; Gynecological's spasmic pain etc.External exploitation recently and in clinical practice novel non-atropine of close flesh, the pure flat sliding flesh spasmolytic of non-Semen Papaveris bases: phloroglucinol (Phloroglucinol, trade name: the rich Spasfon of this handkerchief), it can directly act on the smooth muscle of gastrointestinal tract and urogenital tract, remove smooth muscle spasm, and can not produce a series of cholinolytic sample side effect as atropic category, Semen Papaveris bases smooth muscle spasmolysis medicine, can not cause symptoms such as hypotension, heart rate quickening, arrhythmia, to not influence of cardiovascular function yet.Phloroglucinol is extremely important clinically.
The phloroglucinol dosage form has injection and oral cavity disintegration tablet at present.Drug administration by injection need medical personnel be assisted patient's poor compliance.
(Orally Disintegrating Tablet is a kind of new medicinal preparation that rises both at home and abroad in recent years ODT) to oral cavity disintegration tablet, and its characteristics are: do not need water or only need low amounts of water, also need not to chew, medicine places lingual surface, after the disintegrate, borrows swallowing act to go into the stomach onset rapidly.Can make things convenient for part patient medication, as dysphagia person (especially old man, child), or the medicine quick acting is wished in patient's medication and specific occasion under the special environment that can not obtain water.Oral cavity disintegration tablet is directed to special sufferer colony, and its exploitation is not subjected to the constraint of character of medicine own or pharmacological action, has bigger application prospect.
The method for preparing oral cavity disintegration tablet at present both at home and abroad has: lyophilization pressed disc method, direct powder compression and widely used at home powder wet method grain-making and squash method.The Orally disintegrating piece preparation method that present preceding two kinds of methods are comparative maturities, the oral cavity disintegration tablet quality of preparation is loose, and the disintegrate effect is relatively good, and disintegration is generally in 15 seconds.But there is deficiency in the both: the hardness of finished product is less, and crisp broken degree is higher, even through extra package, also is difficult to guarantee its outward appearance integrity when storing and transport; And preparation method all has specific characteristics, to process conditions and equipment requirements than higher.Adopt the oral cavity disintegration tablet of powder wet granule compression tablet method preparation, for obtaining quickly disintegrated effect, usually in prescription, add a large amount of disintegrating agent (addition inside and outside general the employing), the oral cavity rapid disintegration tablet porosity of pressing preparation is little, disintegrate is slow slightly, but preparation technology is simple, and mechanical strength is better.
Present Spaston orally disintegrating tablets is prepared from the lyophilization pressed disc method, and drug effect is remarkable, however to process conditions and equipment requirements than higher, technology is special, development cost is higher, costs an arm and a leg, hardness is lower, is not easy to packing, stores and transportation.
Summary of the invention
Therefore, the technical problem to be solved in the present invention just provides a kind of new Spaston orally disintegrating tablets, this Spaston orally disintegrating tablets is guaranteeing under the respond well prerequisite of disintegrate, reach also that preparation technology is simple, production cost is lower, finished product hardness is higher, is convenient to packing, storage and requirements on transport.
The technical problem that the present invention also will solve provides the preparation method of described Spaston orally disintegrating tablets.
The inventor is in order to simplify the production technology of Spaston orally disintegrating tablets, reduce production cost, studied and adopted existing domestic powder wet method grain-making and squash method production technology commonly used to prepare Spaston orally disintegrating tablets, find out the prescription that is suitable for above-mentioned production technology, and make the oral cavity disintegration tablet that makes have good disintegrate effect.
Therefore, the present invention solves the problems of the technologies described above the technical scheme that is adopted: a kind of Spaston orally disintegrating tablets, can comprise the phloroglucinol and the pharmaceutically useful excipient for the treatment of effective dose, comprise disintegrating agent in the described excipient, by the tablet total weight amount, the content of phloroglucinol is 15～30%, and the content of described excipient is 70～85%, and the content of described disintegrating agent is 3～23%.
More excellent, the optional self-crosslinking polyvidone of described disintegrating agent (PVPP), cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium (CMS-Na) and low-substituted hydroxypropyl cellulose (L-HPC).
Preferable, described excipient also can comprise the excipient that other is pharmaceutically commonly used, for example filler, pH regulator agent, binding agent, sweeting agent, coloring agent, aromatic and lubricant etc. except disintegrating agent.
Wherein, described filler can be selected from mannitol, microcrystalline Cellulose (MCC), lactose, pregelatinized Starch, dextrin, sorbitol, Icing Sugar and glucose etc., preferred mannitol, microcrystalline Cellulose and lactose;
Described pH regulator agent is optional from organic acid, can be selected from citric acid, tartaric acid, succinic acid, lactic acid, glycolic, oxalic acid, gluconic acid, Citric anhydride, succinic anhydrides and winestone anhydride etc., and commonly used is citric acid and tartaric acid;
Described binding agent can be selected from PVP (polyvinylpyrrolidone) and starch, and consumption is an appropriate amount, and forming " agglomerating, promptly the loosing of touching of alunite " state with soft material is criterion;
Described sweeting agent can be selected from aspartame, aspartame, acesulfame potassium, saccharin sodium and Neohesperidin Dihydrochalcone Herba Menthae etc.;
Described coloring agent can be selected from lemon yellow and ferrum oxide etc.;
Described aromatic can be selected from Herba Menthae, Fructus Citri Limoniae essence, Herba Menthae essence and Fructus Citri tangerinae essence etc.;
Described lubricant can be selected from magnesium stearate, Pulvis Talci and Stepanol MG etc.
Preferable, by the tablet total weight amount, the content of described filler is 45～70%;
The content of described pH regulator agent is 0～3%;
The content of described binding agent is 0.5～3%;
The content of described sweeting agent is 0～5%;
The content of described coloring agent is 0～3%;
The content of described aromatic is 0～3%;
The content of described lubricant is 0.5～3%.
Better, described Spaston orally disintegrating tablets is by the tablet total weight amount, can contain following component: phloroglucinol 15～25%, filler 55～70%, disintegrating agent 7.5～11.5%, sweeting agent 1.5～3.5%, aromatic 1～2%, coloring agent 1～1.5%, pH regulator agent 1～2%, binding agent 0.8～1.5%, lubricant 0.8～1.5%.
The present invention also provides a kind of preparation method of described Spaston orally disintegrating tablets, and it can adopt existing conventional powder wet granule compression tablet method, can comprise following steps:
A) phloroglucinol and various excipient are pulverized;
B) take by weighing described each material and mix homogeneously except that binding agent and lubricant, add binding agent then and make soft material, and then make wet granular;
C) behind the described wet grain drying, add lubricant, compacting in flakes behind the mixing.
Preferable, after pulverizing, each material described in the step a) can cross 80 eye mesh screens.
Soft material described in the step b) can be crushed to wet granular by 20 mesh sieves.
Behind the wet grain drying described in the step c), add lubricant, available tablet machine compacting in flakes.
Major advantage of the present invention is:
1) adopt powder wet granule compression tablet method, simple to process conditions and equipment requirements, can adopt domestic existing manufacturing technique, production cost is lower;
2) finished product hardness higher (usually 10-20N) is difficult for crisp brokenly, can tolerate the various processing under the routine operation condition and its character is not produced bigger influence, also need not pass through extra package, the outward appearance integrity in the time of just can keeping storing and transporting.
3) disintegrate effect is better, reaches the disintegrate requirement of oral cavity disintegration tablet, and the external test disintegration time can be controlled in 30 seconds, mostly less than 10 seconds, and can be than the superior less than 5 seconds.
4) taste good, no grains of sand sense and bad mouthful/smell flavor.
5) contain the pH regulator agent in the oral cavity disintegration tablet of the present invention, make it behind intraoral disintegration, form weakly acidic condition, be beneficial to medicine and see through the mucosa absorption, improve bioavailability.
The specific embodiment
Further specify the present invention with embodiment below, the condition that other not concrete experiment conditions that indicate are advised according to routine or manufacturer, but the present invention is not so limited.Remove explanation in addition, otherwise % is weight percentage.
Embodiment 1
According to the form below takes by weighing each component, progressively increases method with phloroglucinol and each the adjuvant mix homogeneously except that binding agent and lubricant by equivalent.The mixture of gained is crossed 40 mesh sieves twice, and the gained material is placed appropriate containers.In described container, add the PVP aqueous solution of binding agent 5% (g/100ml), make soft material.Described soft material is crushed to wet granular by 20 mesh sieves.Described wet granular is placed in the dried enamel tray, and puts into the air blast thermostatic drying chamber together, 50 ℃ of dryings 2 hours.The weight of weighing dried particles adds lubricant, with the tablet machine compacting in flakes, obtains containing the oral cavity disintegration tablet of phloroglucinol behind the mixing.
Measure the hardness of slice, thin piece with hardness tester, and measure granularity situation, disintegration time and the dissolution of prepared oral cavity disintegration tablet, the results are shown in following table according to following method.
The granularity inspection technique:
1 of oral cavity disintegration tablet is placed the 2ml distilled water, should disintegrate in 1 minute, whether the granule after the disintegrate is observed all by 30 eye mesh screens with the suitable quantity of water flushing.
Slaking test:
The mensuration of disintegration time is carried out according to two appendix XA of Pharmacopoeia of People's Republic of China version in 2005 method disintegration.Sieve aperture internal diameter 2mm adds baffle plate, comes and goes frequency per minute 30-35 time.
Dissolution test:
Carry out dissolution test according to two appendix X of Pharmacopoeia of the People's Republic of China version in 2005 C dissolution method.Oral cavity disintegration tablet is put into 900 ml distilled waters under constant temperature and stable the stirring, in the time of the 15th minute, get 5 milliliters of samples.With 0.45 micron filtering with microporous membrane sample, measure stripping medicament contg with the HPLC method then, calculate stripping percent according to total dose again.Stir speed (S.S.) is 50 rev/mins, and thermostat temperature is 37 ± 0.5 ℃.
The component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 2
Preparation method is with embodiment 1, and binding agent is mixed with 10% (g/100ml) aqueous solution and uses, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 3
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 4
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 5
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 6
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 7
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Embodiment 8
Preparation method is with embodiment 1, and the component and the measurement result of Spaston orally disintegrating tablets are as follows.
Claims (9)
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| CN2007101725183A CN101461788B (en) | 2007-12-18 | 2007-12-18 | Phloroglucine orally disintegrating tablet and preparation method thereof |
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| CN2007101725183A CN101461788B (en) | 2007-12-18 | 2007-12-18 | Phloroglucine orally disintegrating tablet and preparation method thereof |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101856324A (en) * | 2010-06-10 | 2010-10-13 | 南京生命能科技开发有限公司 | Method for preparing phloroglucinol injection |
| CN101874792B (en) * | 2009-12-25 | 2012-04-18 | 雷绍青 | Phloroglucinol oral disintegrating tablet and preparation method thereof |
| CN103054927A (en) * | 2013-01-31 | 2013-04-24 | 成都中医药大学 | Sore-throat-relieving buccal tablet and preparation method thereof |
| CN103120652A (en) * | 2012-12-30 | 2013-05-29 | 湖南湘药制药有限公司 | Phloroglucin orally disintegrating tablet and preparation method thereof |
| CN103622936A (en) * | 2013-12-09 | 2014-03-12 | 中国人民解放军广州军区武汉总医院 | Phloroglucinol film-coated tablet with antioxidative function and preparation method thereof |
| CN103735520A (en) * | 2014-01-20 | 2014-04-23 | 中国人民解放军广州军区武汉总医院 | Phloroglucinol granules and preparation method thereof |
| CN111419809A (en) * | 2020-04-26 | 2020-07-17 | 药源生物科技（启东）有限公司 | Sublingual tablet pharmaceutical composition for acute spastic pain and preparation method thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2709959B1 (en) * | 1993-09-14 | 1995-12-08 | Lafon Labor | New dosage form of phloroglucinol. |
| CN101209249A (en) * | 2006-12-26 | 2008-07-02 | 海南高升医药科技开发有限公司 | Spaston orally disintegrating tablets and preparation thereof |
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2007
- 2007-12-18 CN CN2007101725183A patent/CN101461788B/en not_active Expired - Fee Related
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101874792B (en) * | 2009-12-25 | 2012-04-18 | 雷绍青 | Phloroglucinol oral disintegrating tablet and preparation method thereof |
| CN101856324A (en) * | 2010-06-10 | 2010-10-13 | 南京生命能科技开发有限公司 | Method for preparing phloroglucinol injection |
| CN101856324B (en) * | 2010-06-10 | 2011-09-28 | 南京生命能科技开发有限公司 | Method for preparing phloroglucinol injection |
| CN103120652A (en) * | 2012-12-30 | 2013-05-29 | 湖南湘药制药有限公司 | Phloroglucin orally disintegrating tablet and preparation method thereof |
| CN103054927A (en) * | 2013-01-31 | 2013-04-24 | 成都中医药大学 | Sore-throat-relieving buccal tablet and preparation method thereof |
| CN103622936A (en) * | 2013-12-09 | 2014-03-12 | 中国人民解放军广州军区武汉总医院 | Phloroglucinol film-coated tablet with antioxidative function and preparation method thereof |
| CN103735520A (en) * | 2014-01-20 | 2014-04-23 | 中国人民解放军广州军区武汉总医院 | Phloroglucinol granules and preparation method thereof |
| CN111419809A (en) * | 2020-04-26 | 2020-07-17 | 药源生物科技（启东）有限公司 | Sublingual tablet pharmaceutical composition for acute spastic pain and preparation method thereof |
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| CN101461788B (en) | 2011-08-17 |
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