CN1269480C - Orally disintegrating tablet of loratadine and its preparation method - Google Patents
Orally disintegrating tablet of loratadine and its preparation method Download PDFInfo
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- CN1269480C CN1269480C CN 200410027019 CN200410027019A CN1269480C CN 1269480 C CN1269480 C CN 1269480C CN 200410027019 CN200410027019 CN 200410027019 CN 200410027019 A CN200410027019 A CN 200410027019A CN 1269480 C CN1269480 C CN 1269480C
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- loratadine
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- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 title claims abstract description 98
- 229960003088 loratadine Drugs 0.000 title claims abstract description 98
- 238000002360 preparation method Methods 0.000 title claims abstract description 41
- 239000006191 orally-disintegrating tablet Substances 0.000 title abstract 4
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 62
- 238000000034 method Methods 0.000 claims abstract description 30
- 238000001035 drying Methods 0.000 claims abstract description 12
- 239000004480 active ingredient Substances 0.000 claims abstract description 3
- 239000000203 mixture Substances 0.000 claims description 53
- 239000002671 adjuvant Substances 0.000 claims description 28
- 239000000945 filler Substances 0.000 claims description 28
- 239000000314 lubricant Substances 0.000 claims description 20
- 210000000214 mouth Anatomy 0.000 claims description 20
- 239000008187 granular material Substances 0.000 claims description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 14
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 14
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 14
- 108010011485 Aspartame Proteins 0.000 claims 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 description 12
- 239000000605 aspartame Substances 0.000 claims description 12
- 235000010357 aspartame Nutrition 0.000 claims description 12
- 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 description 12
- 229960003438 aspartame Drugs 0.000 claims description 12
- 239000011230 binding agent Substances 0.000 claims description 12
- 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 10
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 10
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- 229940085605 saccharin sodium Drugs 0.000 claims description 10
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 10
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 10
- 239000008107 starch Substances 0.000 claims description 10
- 235000019698 starch Nutrition 0.000 claims description 10
- 239000004383 Steviol glycoside Substances 0.000 claims description 9
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 9
- 229930006000 Sucrose Natural products 0.000 claims description 9
- 229930182488 steviol glycoside Natural products 0.000 claims description 9
- 235000019411 steviol glycoside Nutrition 0.000 claims description 9
- 150000008144 steviol glycosides Chemical class 0.000 claims description 9
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- 239000004386 Erythritol Substances 0.000 claims description 8
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 8
- 239000007864 aqueous solution Substances 0.000 claims description 8
- 210000000988 bone and bone Anatomy 0.000 claims description 8
- 238000004132 cross linking Methods 0.000 claims description 8
- 235000019414 erythritol Nutrition 0.000 claims description 8
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 8
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- 238000012216 screening Methods 0.000 claims description 8
- 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 claims description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 7
- 239000000741 silica gel Substances 0.000 claims description 7
- 229910002027 silica gel Inorganic materials 0.000 claims description 7
- 239000000243 solution Substances 0.000 claims description 7
- 239000000600 sorbitol Substances 0.000 claims description 7
- 235000010356 sorbitol Nutrition 0.000 claims description 7
- 229920002907 Guar gum Polymers 0.000 claims description 6
- 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 6
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 6
- 235000010489 acacia gum Nutrition 0.000 claims description 6
- 239000001785 acacia senegal l. willd gum Substances 0.000 claims description 6
- 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 6
- 239000000665 guar gum Substances 0.000 claims description 6
- 235000010417 guar gum Nutrition 0.000 claims description 6
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- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 6
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 6
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 6
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- 235000010447 xylitol Nutrition 0.000 claims description 6
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 6
- 229960002675 xylitol Drugs 0.000 claims description 6
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims description 4
- 229920002261 Corn starch Polymers 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 108010010803 Gelatin Proteins 0.000 claims description 4
- 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 4
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims description 4
- 229920000881 Modified starch Polymers 0.000 claims description 4
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 4
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 claims description 4
- 239000008120 corn starch Substances 0.000 claims description 4
- 239000008273 gelatin Substances 0.000 claims description 4
- 229920000159 gelatin Polymers 0.000 claims description 4
- 235000019322 gelatine Nutrition 0.000 claims description 4
- 235000011852 gelatine desserts Nutrition 0.000 claims description 4
- -1 oven dry Substances 0.000 claims description 4
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- 239000002002 slurry Substances 0.000 claims description 4
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- 244000144730 Amygdalus persica Species 0.000 claims description 3
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- 239000004925 Acrylic resin Substances 0.000 claims description 2
- 229920000178 Acrylic resin Polymers 0.000 claims description 2
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 claims description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 2
- 240000000851 Vaccinium corymbosum Species 0.000 claims description 2
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- 230000008014 freezing Effects 0.000 abstract 1
- 238000007710 freezing Methods 0.000 abstract 1
- 238000004108 freeze drying Methods 0.000 description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 12
- 239000003814 drug Substances 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
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- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
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- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical group CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
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- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
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- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 1
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- 239000007884 disintegrant Substances 0.000 description 1
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- GDCRSXZBSIRSFR-UHFFFAOYSA-N ethyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.CCOC(=O)C=C GDCRSXZBSIRSFR-UHFFFAOYSA-N 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The present invention discloses a loratadine orally disintegrating tablet used for treating anaphylactic diseases and a preparation method thereof. The loratadine orally disintegrating tablet comprises loratadine active ingredients and medical acceptable auxiliary material. The loratadine orally disintegrating tablet is characterized in that the weight percentage of loratadine is from 2 to 25%, and the weight percentage of the auxiliary material is from 75 to 98%; the auxiliary material contains disintegrating agents, bulk additive, corrigent and sweetening agents, wherein the weight percentage of the disintegrating agents is from 5 to 40%, the weight percentage of the bulk additive is from 10 to 60%, the weight percentage of the corrigent is from 0.1 to 1%, and the weight percentage of the sweetening agents is from 1 to 30%. The preparation method can adopt a freezing drying method, a powder pressing tablet method and a wet granulation pressing tablet method. According to the different preparation methods, the partial auxiliary material or the whole auxiliary material which has various purposes can be selected from the ingredients. Compared with other loratadine preparations, the present invention has the advantages of rapid disintegration, convenient administration and good mouth feel. Various ingredients and preparation methods can be selected. A market prospect is wide.
Description
Technical field the present invention relates to a kind of medicine of taking convenience and improves method for making, especially for oral loratadine disintegrating tablet for the treatment of anaphylactic disease and preparation method thereof.
Background technology is according to the Epidemiological study of countries in the world, and allergic rhinitis is a kind of modal allergic disease, and its morbidity crowd is up to 10-20%, some area even up to 30%, and also sickness rate all is in many countries and increases trend.The urticaria majority is caused by allergy, belong to corium paraphilia reaction (usually owing to take medicine or the endogenous allergy causes) and be characterized in that temporary erythema appears in part or whole skin or mucosa, welt, edema, and with serious pruritus, there is the crowd of 15-20% once suffering from urticaria in life, but only about 5% goes to see a doctor.Therefore allergic diseases such as allergic rhinitis and urticaria are very common clinically, and sickness rate is higher, has greatly influenced people's quality of life.Although medicine is more at present, the clinical evaluation curative effect is unsatisfactory.
Histamine H
1Receptor antagonist is used for clinical existing more than 40 year history, is widely used in alleviating seasonal or permanent rhinitis and urticaria.But classical histamine H
1Receptor antagonist has tangible sedation and anti-acetylcholine effect, has limited its application.In recent years, constantly there is antihistaminic of new generation to come out, is characterized in that antihistamine effect is reliable, especially little to central nervous system's side effect.In a series of chemical compounds, loratadine is a better kind.
Loratadine, chemical name 4-(8-chloro-5,6-dihydro-11H-benzo [5,6] ring heptan is [1,2-b] pyridine-11-subunit also)-1-piperidine carboxylate, as oral long-acting tricyclic antidepressants antihistaminic, it is rapid-action, effect is strong, to the periphery histamine H
1Receptor has high selectivity, to the H of nervus centralis
1A little less than the receptor affinity, to acetylcholinergic receptor or α
1Adrenoreceptor works hardly.
Oral cavity disintegration tablet is the novel solid preparation of foreign study exploitation in recent ten years, refers in the oral cavity to be disintegratable or complete molten tablet in 1 minute.This dosage form mainly is to select suitable fast disintegrant, by the existing certain rigidity of its tablet of making, certain sedimentation is arranged again, do not need water when taking or only need low amounts of water, also need not to chew, medicine places on the tongue, meet saliva dissolving or disintegrate rapidly, medicine borrows swallowing act to go into the stomach onset.Oral cavity disintegration tablet is compared with conventional tablet, and a kind of new instructions of taking can be provided, and can make things convenient for patient's medication, especially as dysphagia person (as old man, child), or patient's medication of water inconvenience under the special environment.
At present tablet, capsule, chewable tablet, Sublingual tablet, dispersible tablet, the syrup of the existing loratadine in domestic market go on the market or develop, and also do not have the oral cavity disintegration tablet dosage form.Chinese patent 95193578 discloses a kind of medicament and manufacture method thereof that contains loratadine and effervescent system, characteristic at loratadine hydrophobic active substance, select surfactant or emulsifying agent for use, make itself and active material particle relatively independent, and be dispersed in the effervescent system, thereby improved the common bad suspension of loratadine effervescent tablet, avoided blistered side effect.The loratadine effervescent tablet that relates in this invention need be placed in a large amount of water when taking, and drink after being separated into uniform solution, and preparation process need divide multistep obtain solution system, and need drying under reduced pressure to remove to desolvate, and method is complicated.
Summary of the invention the purpose of this invention is to provide a kind of oral loratadine disintegrating tablet, and not only disintegrate is rapid for it, is beneficial to absorption, and onset is faster, and preparation method is simple, good mouthfeel, taking convenience.
The technical scheme that technical solution problem of the present invention is adopted is, a kind of oral loratadine disintegrating tablet, comprise loratadine active ingredient and medicinal acceptable auxiliary, the percentage by weight that it is characterized in that loratadine is 2-25%, the percentage by weight of adjuvant is 75-98%, adjuvant contains disintegrating agent, filler, correctives, sweeting agent, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of filler is 10-60%, the percentage by weight of correctives is 0.1-1%, and the percentage by weight of sweeting agent is 1-30%.
Described oral loratadine disintegrating tablet preferably contains the loratadine that percentage by weight is 5-20%, the adjuvant of 80-95%.
The present invention is according to the difference of preparation method, can select for use in the component in the various uses adjuvant partly or entirely.
When the percentage by weight of loratadine less than 15% the time, the adjuvant of described oral loratadine disintegrating tablet can contain odor mask, also can not contain odor mask; When the percentage by weight of loratadine greater than 15% the time, the adjuvant of described oral loratadine disintegrating tablet also contains odor mask, odor mask is selected from a kind of or wherein several mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, guar gum, arabic gum, xanthan gum, paraffin, the Brazil wax, and accounting for the oral cavity disintegration tablet percentage by weight is 5-20%.
The adjuvant of described oral loratadine disintegrating tablet also contains lubricant, and lubricant is selected from a kind of or wherein several mixture in micropowder silica gel, magnesium stearate, the Pulvis Talci, and accounting for the oral cavity disintegration tablet percentage by weight is 0.5-5%.
The adjuvant of described oral loratadine disintegrating tablet also contains binding agent, binding agent is selected from a kind of or wherein several mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, the povidone solution, and accounting for the total formulation weight percentage ratio of oral cavity disintegration tablet is 1-5%.
The disintegrating agent of described oral loratadine disintegrating tablet is selected from a kind of or wherein several mixture in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Novagel RCN-15 (mixture of 85% microcrystalline Cellulose and 15% guar gum), carboxymethylcellulose calcium, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, the corn starch.
The filler of described oral loratadine disintegrating tablet is selected from a kind of or wherein several mixture in lactose, microcrystalline Cellulose, pregelatinized Starch, mannitol, sorbitol, xylitol, the erythritol.
The correctives of described oral loratadine disintegrating tablet is selected from a kind of or wherein several mixture in Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, blue berry, Fructus Musae, Fructus Ananadis comosi, honey peach, the maltose essence.
The sweeting agent of described oral loratadine disintegrating tablet is selected from a kind of or wherein several mixture in saccharin sodium, sucrose, aspartame, the steviol glycosides; Simultaneously, a kind of or wherein several mixture of saccharin sodium, aspartame, steviol glycosides is not more than percentage by weight 5%.
The preparation method of oral loratadine disintegrating tablet can be freeze-drying, powder pressing method, wet granule compression tablet method.Concrete method for making is as follows:
Freeze-drying: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, filler, correctives, sweeting agent, the percentage by weight of loratadine is 2-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of filler is 10-60%, the percentage by weight of correctives is 0.1-1%, and the percentage by weight of sweeting agent is 1-30%.The main method step is: with loratadine and disintegrating agent, filler, correctives, sweeting agent mix homogeneously, and add the suitable quantity of water dilution, fully mixing places suitable sheet shape mould, puts into the freeze dryer lyophilization, is shaped to the material bone dry.
Freeze-drying: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, odor mask, filler, correctives, sweeting agent, the percentage by weight of loratadine is 15-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of odor mask is 5-20%, the percentage by weight of filler is 10-60%, and the percentage by weight of correctives is 0.1-1%, and the percentage by weight of sweeting agent is 1-30%.The main method step is: the aqueous solution of loratadine and odor mask is even, and add disintegrating agent, filler, correctives, sweeting agent, and add the suitable quantity of water dilution, abundant mixing, place suitable sheet shape mould, put into the freeze dryer lyophilization, be shaped to the material bone dry.
Powder pressing method: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, filler, sweeting agent, correctives, lubricant, the percentage by weight of loratadine is 2-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of filler is 10-60%, the percentage by weight of correctives is 0.1-1%, and the percentage by weight of sweeting agent is 1-30%, and the percentage by weight of lubricant is 0.5-5%.The main method step is: disintegrating agent, filler, sweeting agent, correctives are sieved, and with the loratadine mix homogeneously, tabletting is shaped behind the adding lubricant.
Powder pressing method: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, odor mask, filler, correctives, sweeting agent, lubricant, the percentage by weight of loratadine is 15-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of odor mask is 5-20%, and the percentage by weight of filler is 10-60%, and the percentage by weight of correctives is 0.1-1%, the percentage by weight of sweeting agent is 1-30%, and the percentage by weight of lubricant is 0.5-5%.The main method step is: loratadine added the aqueous solution of odor mask, mixed 1-2 hour, and in 40 ℃ of dryings 12 hours, crushing screening behind the bone dry; With disintegrating agent, filler, sweeting agent, correctives sieve with crushing screening after loratadine carry out mix homogeneously, add lubricant after tabletting be shaped.
The wet granule compression tablet method: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, filler, correctives, sweeting agent, lubricant, binding agent, the percentage by weight of loratadine is 2-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of filler is 10-60%, and the percentage by weight of correctives is 0.1-1%, and the percentage by weight of sweeting agent is 1-30%, the percentage by weight of lubricant is 0.5-5%, and the percentage by weight of binding agent is 1-5%.The main method step is: with loratadine and part disintegrating agent, filler, correctives, sweeting agent, mix homogeneously, adds suitable amount of adhesive system soft material, granulates, and oven dry, granulate adds surplus disintegrating agent and lubricant, the tabletting shaping.
The wet granule compression tablet method: component comprises loratadine active component and adjuvant, adjuvant comprises disintegrating agent, odor mask, filler, correctives, sweeting agent, lubricant, binding agent, the percentage by weight of loratadine is 15-25%, the percentage by weight of disintegrating agent is 5-40%, the percentage by weight of odor mask is 5-20%, the percentage by weight of filler is 10-60%, the percentage by weight of correctives is 0.1-1%, the percentage by weight of sweeting agent is 1-30%, the percentage by weight of lubricant is 0.5-5%, and the percentage by weight of binding agent is 1-5%.The main method step is: loratadine added the aqueous solution of odor mask, mixed 1-2 hour, and in 40 ℃ of dryings 12 hours, crushing screening behind the bone dry; With the loratadine behind the crushing screening and part disintegrating agent, filler, rectify and hide agent, sweeting agent mix homogeneously, add suitable amount of adhesive system soft material, granulate, oven dry, granulate adds surplus disintegrating agent and lubricant, the tabletting shaping.
Use the oral loratadine disintegrating tablet of freeze-drying preparation, place lingual surface to dissolve rapidly, disintegration time was less than 10 seconds, use the oral cavity disintegration tablet of pressed powder and wet granule compression tablet gained, enter the oral cavity based on disintegrate, disintegration time is less than 40 seconds, the equal good mouthfeel of all components, acidity, sugariness suit no grittiness.
Be the key index of estimating the oral cavity disintegration tablet dosage form disintegration, because the oral cavity disintegration tablet dosage form is not taken in pharmacopeia as yet at present, the disintegration time mensuration method is not clearly stipulated, recommends assay method as follows:
Get both ends open glass-tube (diameter 1.5cm), an end is sealed 24 eye mesh screens, drops into tablet, puts into the 50ml graduated cylinder that 37 ℃ of water of 2ml are housed, leave standstill 1min after, add the flushing of 3ml water, answer the noresidue granule.
Good effect of the present invention: the present invention is according to the difference of preparation method, rationally select for use in the component in the above various uses adjuvant partly or entirely, provide that a kind of component is reasonable, method simple, the oral loratadine disintegrating tablet of taking convenience and preparation method thereof.With adapting to the sudden of anaphylactic disease, make things convenient for patient's medication under various environment, on instructions of taking, change traditional application method, make oral administration not need water, and, be that disintegrate is molten entirely in 40 seconds because disintegrate is rapid, can quicken stripping, be beneficial to absorption, onset is faster, compares prior dosage form and preparation method, have outstanding characteristics and significant advantage, will bring good economic benefit and social benefit.
The following embodiment of the specific embodiment is used for specifically setting forth the present invention, but the present invention is not construed as limiting.
Oral loratadine disintegrating tablet of the present invention comprises loratadine active component and medicinal acceptable auxiliary, and adjuvant can contain the mixture of disintegrating agent, filler, odor mask, correctives, sweeting agent, lubricant, binding agent.Its component composition can be:
Loratadine: 2-25%; Disintegrating agent: 5-40%; Filler: 10-60%; Lubricant: 0.5-5%; Odor mask: 5-20%; Correctives: 0.1-1%; Sweeting agent: 1-30%; Binding agent: 1-5%.
Preferred ingredient is to contain the loratadine that percentage by weight is 5-20%, the adjuvant of 80-95%.
In the specific implementation, according to the difference of preparation method, in the component in the above various uses adjuvant of optional usefulness partly or entirely.
Embodiment 1 oral loratadine disintegrating tablet and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 2
Polyvinylpolypyrrolidone 5
Microcrystalline Cellulose pH301 30
Lactose 30
Sucrose 25
Saccharin sodium 2
Eudragit E udragit L30D-55 5.5
Flavoring orange essence 0.5
Preparation method:
Loratadine is added in the Eudragit L30D-55 suspension, add appropriate amount of deionized water, stir, add polyvinylpolypyrrolidone, microcrystalline Cellulose, lactose, sucrose, saccharin sodium and flavoring orange essence successively, the limit edged stirs, be heated to 30～40 ℃, mixed 1 hour, and became uniform suspension, be poured in the suitable mould and carry out lyophilization, lyophilizing is shaped and finishes back press seal, packing.
The obtained freeze-drying goods are by aforementioned disintegration time mensuration method, and disintegration is qualified; And short texture is put good mouthfeel on the tongue, and disintegrate is molten entirely rapidly, and disintegration time is 6 seconds.
Embodiment 2 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 15
Mannitol 10
Pregelatinized Starch 10
Guar gum 5
Arabic gum 10
Erythritol 30
Microcrystalline Cellulose 10
Sucrose 9.8
Vanilla 0.2
Preparation method:
Loratadine is added in the mixed liquor of guar gum and arabic gum, add suitable quantity of water, stir, add mannitol, erythritol and sucrose, to dissolving fully, add pregelatinized Starch, microcrystalline Cellulose and vanilla, the limit edged stirs, and mixes 1 hour, become uniform suspension, be poured in the suitable mould and carry out lyophilization, lyophilizing is shaped and finishes back press seal, packing.
The obtained freeze-drying goods are by aforementioned disintegration time mensuration method, and disintegration is qualified; And short texture is put good mouthfeel on the tongue, and disintegrate is molten entirely rapidly, and disintegration time is 5 seconds.
Embodiment 3 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 20
Gelatin 20
Xylitol 10
Aspartame 4.9
Novagel?RCN-15 40
Cross-linking sodium carboxymethyl cellulose 5
Honey peach essence 0.1
Preparation method:
Loratadine, gelatin, xylitol, aspartame, cross-linking sodium carboxymethyl cellulose, RCN-15 in the component are suspended in the water, stirred 1 hour, make suspension, be poured in the suitable mould, carry out lyophilization, lyophilizing is shaped and finishes back press seal, packing.
The obtained freeze-drying goods are by aforementioned disintegration time mensuration method, and disintegration is qualified; And short texture is put good mouthfeel on the tongue, and disintegrate is molten entirely rapidly, and disintegration time is 4 seconds.
Embodiment 4 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 8
Cross-linking sodium carboxymethyl cellulose 5
Starch 23
Sorbitol 33
Steviol glycosides 0.5
Sucrose 29.5
Flavoring pineapple essence 0.5
Micropowder silica gel 0.5
Preparation method:
100 mesh sieves are crossed in loratadine, sorbitol, steviol glycosides, sucrose, micropowder silica gel respectively, earlier with loratadine and steviol glycosides, sucrose, flavoring pineapple essence, micropowder silica gel mix homogeneously, progressively increase and mix with cross-linking sodium carboxymethyl cellulose, starch, sorbitol equivalent again, placed three-dimensional mixer 15 minutes, abundant mix homogeneously, tabletting is shaped.
The every index of gained sheet all meets the pharmacopeia regulation, and by aforementioned disintegration time mensuration method, disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 25 seconds.
Embodiment 5 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 23.5
Magnesiumaluminumsilicate 10
Low-substituted hydroxypropyl cellulose 27
Lactose 3
Mannitol 31.5
Fructus Citri Limoniae essence 1
Aspartame 2.5
Magnesium stearate 1.5
Preparation method:
Loratadine is added in the aqueous solution of Magnesiumaluminumsilicate, mix,, or to bone dry, pulverize, cross 100 mesh sieves in 40 ℃ of dryings 12 hours; Low-substituted hydroxypropyl cellulose, lactose, mannitol are crossed 100 mesh sieves, and with Fructus Citri Limoniae essence, aspartame, the magnesium stearate equivalent mix homogeneously that progressively increases, with the pretreatment powder mixing of loratadine, direct compression is shaped then.
The every index of gained sheet all meets the pharmacopeia regulation, and by aforementioned assay method, disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 30 seconds.
Embodiment 6 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 10
Carboxymethyl starch sodium 15
Microcrystalline Cellulose 25
Erythritol 40
Maltose essence 0.8
Saccharin sodium 4.2
Pulvis Talci 5
Preparation method:
Loratadine, carboxymethyl starch sodium, microcrystalline Cellulose, erythritol are crossed 100 sieves, and with maltose essence, saccharin sodium, the Pulvis Talci equivalent mix homogeneously that progressively increases, direct compression is shaped.
The every index of gained sheet all meets the pharmacopeia regulation, presses preceding method and measures, and disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 28 seconds.
Press component and preparation method in the present embodiment, composition is simple, technological operation is easy, compares lyophilization and the wet granulation technology step is less, production cost is low, and disintegrate is rapid, sugariness, acidity optimum, no grittiness, good mouthfeel is preferred ingredient and preparation method.
Embodiment 7 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 18
Xanthan gum 6
Sorbitol 40
Mannitol 20
Novagel?RCN-15 11.5
Aspartame 1
Strawberry essence 0.2
Magnesium stearate 3.3
Preparation method:
Loratadine is added in the aqueous solution of xanthan gum, mix,, or to bone dry, pulverize, cross 100 mesh sieves in 40 ℃ of dryings 12 hours; Sorbitol, mannitol, Novagel RCN-15 are crossed 100 mesh sieves, progressively increase and mix, placed three-dimensional mixer 15 minutes with strawberry essence, aspartame, magnesium stearate equivalent, mix homogeneously, direct compression is shaped.
The every index of gained sheet all meets the pharmacopeia regulation, and by aforementioned assay method, disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 22 seconds.
Embodiment 8 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 13.5
Carboxymethylcellulose calcium 8
Mannitol 42.5
Microcrystalline Cellulose 17
Steviol glycosides 2.6
Herba Menthae essence 0.4
Pulvis Talci 1
Starch slurry 5
Preparation method:
Loratadine, mannitol, 1/3 amount microcrystalline Cellulose, steviol glycosides, Herba Menthae essence are made soft material with the appropriate amount of starch slurry, cross 40 mesh sieves and granulate, 60 ℃ of dryings, to moisture be below 2%, add carboxymethylcellulose calcium, 2/3 amount microcrystalline Cellulose, Pulvis Talci, tabletting is shaped behind the mix homogeneously.
The every index of gained sheet meets the pharmacopeia regulation, and by aforementioned assay method, disintegration is qualified, and good looking appearance, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 35 seconds.
Embodiment 9 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 25
Arabic gum 15
Xylitol 30.5
Corn starch 18
Aspartame 2
Cross-linking sodium carboxymethyl cellulose 5
Grape essence 0.3
Polyvidone (75% ethanol liquid) 2.5
Magnesium stearate 1.7
Preparation method:
Loratadine is added in the aqueous solution of arabic gum, stirred 1 hour, in 40 ℃ of dryings 12 hours, pulverize, cross 100 mesh sieves, gained powder and xylitol, corn starch, aspartame, grape essence mix homogeneously, 75% ethanol liquid with polyvidone is binding agent system soft material, cross 40 mesh sieves and granulate, 60 ℃ of dryings are to moisture below 2%, granulate, add cross-linking sodium carboxymethyl cellulose, magnesium stearate, mix homogeneously, tabletting is shaped.
The every index of gained sheet all meets the pharmacopeia regulation, presses preceding method and measures, and disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 32 seconds.
Embodiment 10 oral loratadine disintegrating tablets and preparation method thereof
Component:
Composition (supplementary material) consumption (percentage by weight, %)
Loratadine 5
Low-substituted hydroxypropyl cellulose 33
Erythritol 47
Polyvinylpolypyrrolidone 5
Saccharin sodium 5
Flavoring orange essence 1
Micropowder silica gel 3
Sodium carboxymethyl cellulose (50% ethanol liquid) 1
Preparation method:
With loratadine and low-substituted hydroxypropyl cellulose, erythritol, saccharin sodium, flavoring orange essence mix homogeneously, 50% ethanol liquid with sodium carboxymethyl cellulose is binding agent system soft material, crossing 40 mesh sieves granulates, 60 ℃ of dryings, to moisture below 2%, granulate, add polyvinylpolypyrrolidone, micropowder silica gel, mix homogeneously, tabletting is shaped.
The every index of gained sheet all meets the pharmacopeia regulation, presses preceding method and measures, and disintegration is qualified, places oral cavity sugariness, aromaticity to suit no grittiness, disintegration time 36 seconds.
Claims (4)
1. the preparation method of an oral loratadine disintegrating tablet contains loratadine active ingredient and medicinal acceptable auxiliary, and the percentage by weight of loratadine is 15-25%, and the percentage by weight of adjuvant is 75-85%; Adjuvant is selected from disintegrating agent, filler, correctives, sweeting agent, odor mask; Described disintegrating agent is selected from a kind of or wherein several mixture in the mixture, carboxymethylcellulose calcium, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, corn starch of polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, 85% microcrystalline Cellulose and 15% guar gum, and the percentage by weight of disintegrating agent is 5-40%; Described filler is selected from a kind of or wherein several mixture in lactose, pregelatinized Starch, mannitol, sorbitol, xylitol, the erythritol, and the percentage by weight of filler is 10-60%; Described correctives is selected from a kind of or wherein several mixture in Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, blue berry, Fructus Musae, Fructus Ananadis comosi, honey peach, the maltose essence, and the percentage by weight of correctives is 0.1-1%; Described sweeting agent is selected from a kind of or wherein several mixture in saccharin sodium, sucrose, aspartame, the steviol glycosides, the percentage by weight of sweeting agent is 1-30%, simultaneously, a kind of or wherein several mixture of saccharin sodium, aspartame, steviol glycosides is not more than total weight percent 5%; Described odor mask is selected from a kind of or wherein several mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, guar gum, arabic gum, xanthan gum, paraffin, the Brazil wax, and the percentage by weight of odor mask is 5-20%; The main method step is: loratadine added the aqueous solution of odor mask, mixed 1-2 hour, and in 40 ℃ of dryings 12 hours, crushing screening behind the bone dry; With disintegrating agent, filler, sweeting agent, correctives sieve with crushing screening after the loratadine mix homogeneously, add lubricant after tabletting be shaped.
2. method according to claim 1 is characterized in that adjuvant also contains lubricant, and lubricant is selected from a kind of or wherein several mixture in micropowder silica gel, magnesium stearate, the Pulvis Talci, and accounting for the oral cavity disintegration tablet percentage by weight is 0.5-5%.
3. method according to claim 2, it is characterized in that adjuvant also contains binding agent, binding agent is selected from a kind of or wherein several mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, the povidone solution, and accounting for the oral cavity disintegration tablet percentage by weight is 1-5%.
4. method according to claim 3, the main method step is: loratadine added the aqueous solution of odor mask, mixed 1-2 hour, in 40 ℃ of dryings 12 hours, crushing screening behind the bone dry; With the loratadine behind the crushing screening and part disintegrating agent, filler, correctives, sweeting agent mix homogeneously, add suitable amount of adhesive system soft material, granulate, oven dry, granulate adds surplus disintegrating agent and lubricant, the tabletting shaping.
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| CN 200410027019 CN1269480C (en) | 2004-04-24 | 2004-04-24 | Orally disintegrating tablet of loratadine and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200410027019 CN1269480C (en) | 2004-04-24 | 2004-04-24 | Orally disintegrating tablet of loratadine and its preparation method |
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| CN1269480C true CN1269480C (en) | 2006-08-16 |
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Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN100335055C (en) * | 2005-04-29 | 2007-09-05 | 邢为藩 | Pitavastatin soluble tablet composition and preparation method thereof |
| CN102048682B (en) * | 2009-10-31 | 2012-09-12 | 鲁南制药集团股份有限公司 | Loratadine cream and application thereof |
| CN103230378B (en) * | 2013-05-10 | 2014-12-10 | 青岛双鲸药业有限公司 | Method for preparing loratadine tablet |
| CN104490819A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Loratadine composition chewable tablets and preparation method thereof |
| CN105997909A (en) * | 2016-06-02 | 2016-10-12 | 中国药科大学 | Oral disintegrating tablet of obeticholic acid, and preparation method thereof |
| CN108926542A (en) * | 2017-05-26 | 2018-12-04 | 万特制药(海南)有限公司 | Loratadine tablet of Fast Stripping and preparation method thereof |
| CN107224439A (en) * | 2017-06-13 | 2017-10-03 | 江苏黄河药业股份有限公司 | It is a kind of to be used to treat oral loratadine disintegrating tablet of anaphylactia and preparation method thereof |
| CN109528666A (en) * | 2017-09-22 | 2019-03-29 | 万特制药(海南)有限公司 | Good Loratadine pharmaceutical composition of compressibility and preparation method thereof |
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