CN103156816A - Almotriptan drug absorbed through mouth mucosa - Google Patents
Almotriptan drug absorbed through mouth mucosa Download PDFInfo
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- CN103156816A CN103156816A CN 201110427472 CN201110427472A CN103156816A CN 103156816 A CN103156816 A CN 103156816A CN 201110427472 CN201110427472 CN 201110427472 CN 201110427472 A CN201110427472 A CN 201110427472A CN 103156816 A CN103156816 A CN 103156816A
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Abstract
Disclosed is an almotriptan drug absorbed through mouth mucosa. Malic acid almotriptan is an effective drug ingredient, and the almotriptan drug absorbed through mouth mucosa is jointly composed of malic acid almotriptan and auxiliary ingredients which are acceptable in a mouth mucosa drug, wherein the auxiliary ingredients comprise a disintegrating agent, a filling agent, a flavoring agent, a bonding agent, a mucosa sorbefacient and a lubricating agent. Preparation forms of specific drugs comprise sublingual tablets, lozenges, mouth and check lozenges, mouth disintegrating tablets, mouth adhering tablets and mouth pasting tablets and the like. The drug can be completely or mainly absorbed through mouth mucosa such as hypogloeeis mucosa and/or mouth and cheek mucosa and is non-irritant to a mouth. Bioavailability and a curative effect of the drug can be obviously improved, and the almotriptan drug absorbed through mouth mucosa can be taken conveniently, so that a patient is enabled to take the drug obediently.
Description
Technical field
The present invention relates to a kind of medicine of absorbed through oral mucosa, but be specifically a kind of Almogran medicine of absorbed through oral mucosa, comprise that Sublingual tablet, mouthful buccal tablet, buccal tablet, oral cavity disintegration tablet, oral cavity adhesion tablet and mouth paster etc. can be all or mainly by the pharmaceutical preparation of the oral mucosas such as hypoglossis mucous membrane and/or buccal mucosa absorption.
Background technology
Migraine is a kind of chronic neural blood vessel disorder disease, is take diffusivity or one-sided outbreak, sharp ache, repeatedly shows effect as a kind of common clinical, the frequently-occurring disease of feature.Migraine appears in the women in the whole world annual nearly 15%～18% and 6%～9% male; Be 4.2%～14.6% at the migrainous sickness rate of China.When migraine, the patient has a headache unbearably, feels sick, vomits, and can last for hours the even a few days, has a strong impact on patient's routine work and life.The triptan medicine is the migrainous medicine of a new generation's treatment, the exciting 5-HT of its selectivity
1B/D1Receptor, specificity is strong, and curative effect is clear and definite, since first triptan Medicine for treating migraine sumatriptan listing of in February, 1991, the first-line treatment medicine when such medicine has become acute migraine attack.
Almogran is the 5-HT receptor stimulating agent of a new generation, to intracranial vessel 5-HT
1B/D1Receptor has high selectivity.The contraction of its some intracranial vessel of energy selective control, and may interact with trigeminal vascular system, the plasma protein extravasation in the cerebral dura mater blood vessel suppressed after the stimulation trigeminal ganglion.To cause the convulsion effect little than other triptan medicines to coronarius for this product, stronger 25 times than sumatriptan to arteriocerebral effect.
At present, the Almogran preparation of listing is malic acid Almogran conventional tablet, needing after gastrointestinal absorption enters blood can onset, onset time is slower, and the patient who occurs nauseating symptom during for migraine is difficult to take, and this has affected curative effect of medication and the clinical use of this medicine to a certain extent.
Summary of the invention
The Almogran medicine of absorbed through oral mucosa of the present invention, take Almogran or its pharmaceutically acceptable salt as the active drug composition, wherein preferably apple acid Almogran, form jointly with acceptable auxiliary element in oral mucosa medicament.
Acceptable auxiliary element in said oral mucosa medicament can be selected the common multiple auxiliary materials composition that needs and/or use in the oral mucosa medicament preparation at present, comprising:
Disintegrating agent: as one or more in polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, microcrystalline Cellulose-micropowder silica gel, amylum pregelatinisatum, dried starch, starch, sodium alginate, alginic acid, hydroxypropyl starch, carboxymethylcellulose calcium;
Filler: as one or more in microcrystalline Cellulose, lactose, lactose complex, amylum pregelatinisatum, starch, Icing Sugar, glucose, calcium sulfate, dextrin, mannitol, erythritol, maltose, maltose alcohol, maltodextrin, sorbitol, xylitol;
binding agent: as polyvidone constituents commonly used (as Kollidon VA 64, Kollidon VA 64 Fine, Plasdone S-630), starch slurry, hydroxypropyl emthylcellulose, methylcellulose, carrageenin, carbomer, guar gum, gelatin, arabic gum, xanthan gum, alginic acid or as sodium alginate, potassium alginate, the its esters compositions such as calcium alginate, one or more in the various compositions such as propylene glycol alginate, sodium starch phosphate, chitosan, one or more in dextrin and syrup,
Wetting agent: as one or more in the alcoholic solution of commonly used water, ethanol, dehydrated alcohol and variable concentrations;
Taste masking (taste masking) agent: as glycyrrhizin commonly used, aspartame, crystalline maltose, the sweeting agent of processing the permission uses such as agar (TAG), stevioside, sucralose, xanthan gum, glucide, vitamin C, fructose, glucosan, cyclamate, Talin, glucide, menthol and/or one or more in the edible essence composition;
Lubricant: as one or more in the compositions such as magnesium stearate commonly used, stearic acid, sodium stearyl fumarate, sodium lauryl sulphate, Macrogol 4000 (or polyethylene glycol 6000), micropowder silica gel, Pulvis Talci.
Malic acid Almogran in the above-mentioned absorbed through oral mucosa medicine of the present invention, containing in oral cavity (mainly in Sublingual or mouthful buccal), all or basically be by comprising that the intraoral mucosal tissue such as buccal mucosa and hypoglossis mucous membrane absorbs onset, its concrete dosage form can comprise existing mouth buccal tablet, buccal tablet, oral cavity disintegration tablet, Sublingual tablet, oral cavity adhesion tablet and the mouth paster etc. that use at present.
In Almogran oral mucosa medicament of the present invention, said active drug composition Almogran or the content of its pharmaceutically acceptable salt in pharmaceutical preparation, generally can be 1%～70% of medicine gross weight, the consumption of above-mentioned auxiliary element can be respectively uses by the usual manner of each corresponding preparations at present, the content specification of pharmaceutical preparation unit take Almogran as 6.25mg, 12.5mg etc.
The preparation of Almogran oral mucosa medicament of the present invention can adopt the usual manner of present similar drugs preparation to prepare.Take Sublingual tablet as example, its typical preparation method can have:
(1) wet granulation mode: active drug composition Almogran or its pharmaceutically acceptable salt are carried out pretreatment (adopting suitable size reduction machinery that Almogran is pulverized) or do not carry out pretreatment, with selected auxiliary element mix homogeneously, after adding binding agent granulation and dry (or adopting the fluidized bed granulation drying), add again and add disintegrating agent and the abundant mixing of lubricant, tabletting makes the Sublingual tablet preparation.
(2) direct compression mode: active drug composition Almogran or its pharmaceutically acceptable salt are carried out pretreatment (adopting suitable size reduction machinery that Almogran is pulverized) or do not carry out pretreatment, with selected auxiliary element mix homogeneously, direct compression makes the Sublingual tablet preparation.
The Almogran medicine of absorbed through oral mucosa of the present invention, taking convenience, do not need water when taking, be placed in the positions such as the Sublingual in oral cavity or mouthful cheek, containing in oral cavity (mainly in Sublingual and/or mouthful buccal), all or basically be by comprising that the intraoral mucosal tissue such as hypoglossis mucous membrane and buccal mucosa absorbs, and directly enters blood circulation and onset through jugular vein and superior vena cava.Can avoid the first pass effect of medicine, and after administration, drug effect is fast, headache symptom in the time of alleviating migraine rapidly, easy to use, be particularly suitable for the patient of the dysphagias such as old man, and under the special environment such as field, hydropenia, the patient takes, patient compliance is better.
Almogran oral mucosa medicament preparation of the present invention is simple, need not special installation, is easy to industrialization, and production efficiency is high, and cost is low, has both satisfied clinical needs, has filled up again blank both domestic and external, has the wide market space.
The specific embodiment by the following examples is described in further detail foregoing of the present invention again.But this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following example.Do not breaking away from the above-mentioned technological thought situation of the present invention, various replacements or change according to ordinary skill knowledge and customary means are made all should comprise within the scope of the invention.
The specific embodiment
Embodiment 1 Sublingual tablet
Form:
Preparation method: the auxiliary elements such as Almogran raw material and lactose, microcrystalline Cellulose are crossed 100 mesh sieves, after mix homogeneously, direct compression and get final product.
Embodiment 2 oral cavity disintegration tablets
Form:
Preparation method: Almogran and the auxiliary element mix homogeneously such as pregelatinized Starch and microcrystalline Cellulose with recipe quantity add 0.4% xanthan gum solution, mix homogeneously, soft material processed, granulate, drying, granulate, add to add polyvinylpolypyrrolidone and Pulvis Talci mixing, tabletting and get final product.
Embodiment 3 Sublingual tablets
Form:
Preparation method: Almogran and the auxiliary element mix homogeneously such as pregelatinized Starch and erythritol with recipe quantity add 10% starch slurry, mix homogeneously, soft material processed, granulate, drying, granulate, add to add cross-linking sodium carboxymethyl cellulose and Pulvis Talci mixing, tabletting and get final product.
4 mouthfuls of buccal tablets of embodiment
Form:
Preparation method: Almogran and the auxiliary element mix homogeneously such as starch and xylitol with recipe quantity, add the 2%HPMC aqueous solution, fluidized bed granulation, drying, granulate adds to add polyethylene glycol 6000, mixing, tabletting, and get final product.
Embodiment 5 Sublingual tablets
Form:
Preparation method: the auxiliary elements such as recipe quantity Almogran and lactose, microcrystalline Cellulose were pulverized 100 mesh sieves, after mix homogeneously, direct compression and get final product.
Embodiment 6 buccal tablets
Form:
Preparation method: Almogran and the auxiliary element mix homogeneously such as microcrystalline Cellulose and erythritol with recipe quantity, add 5% starch slurry, mix homogeneously, soft material processed is granulated, drying, granulate adds Pulvis Talci, mixing, tabletting, and get final product.
Embodiment 7 oral cavity adhesion tablets or mouth paster
Form:
Preparation method: the auxiliary elements such as the Almogran of recipe quantity and starch, pregelatinized Starch are pulverized, crossed 100 mesh sieves, after mix homogeneously, direct compression and get final product.
8 mouthfuls of buccal tablets of embodiment
Form:
Preparation method: Almogran and the auxiliary element mix homogeneously such as microcrystalline Cellulose and lactose with recipe quantity, add the 4%PVP aqueous solution, mix homogeneously, soft material processed is granulated, drying, granulate adds to add carboxymethyl starch sodium and stearic acid, mixing, tabletting and get final product.
Below result of the test will help to prove the remarkable result of the Almogran medicine of the above-mentioned absorbed through oral mucosa of the present invention.
1. disintegration, dissolution
The sample of each embodiment preparation carries out disintegration, dissolution test by 2010 editions two appendix related requests of Chinese Pharmacopoeia, the results are shown in Table 1, and result shows that medicine can be in the in setting time disintegrate, and dissolution reaches more than 95%, substantially meets designing requirement.
Table 1 disintegration and dissolution result
| Embodiment | Disintegration | Dissolution (%) |
| Embodiment 1 | 55 seconds | 96 |
| Embodiment 2 | 49 seconds | 97 |
| Embodiment 3 | 46 seconds | 98 |
| Embodiment 4 | 12 minutes | 98 |
| Embodiment 5 | 50 seconds | 99 |
| Embodiment 6 | 12 minutes | 97 |
| Embodiment 7 | 18 minutes | 95 |
| Embodiment 8 | 11 minutes | 100 |
2. oral mucosa irritation test
Test method: 16 of healthy Golden Hamster, respectively the Sublingual tablet (embodiment 3) of preparation and mouthful buccal tablet (embodiment 6) are placed in the utmost point lower of central buccal mucosa on the left of animal (embodiment 3 and embodiment 6 each with 8 animals) after anesthesia, right side not administration of buccal mucosa in contrast.All dissolve rear perusal and make tissue slice until Sublingual tablet and mouthful buccal tablet.
Result:
Perusal: normal with buccal mucosa color and luster after medicament contact, have no coarse, red and swollen phenomenon.
Histological observation: complete with the buccal mucosa epithelium of medicament contact, have no pathological change.
Result of the test shows, the said medicine of the present invention is to the effect of oral mucosa nonirritant, can make medicine can have good mouthfeel, make the patient have satisfied compliance, thereby effectively guaranteed the abundant absorbed through oral mucosa onset of medicine, can significantly improve bioavailability and the curative effect of medicine, guarantee therapeutic effect.
Claims (4)
1. the Almogran medicine of absorbed through oral mucosa, it is characterized in that Almogran or its pharmaceutically acceptable salt absorbed through oral mucosa, its concrete medicament forms, can comprise the at present existing Sublingual tablet that uses, mouthful buccal tablet, buccal tablet, oral cavity disintegration tablet, oral cavity adhesion tablet and mouth paster, can be all or mainly by the pharmaceutical preparation of the oral mucosas such as hypoglossis mucous membrane and/or buccal mucosa absorption.
2. the Almogran medicine of absorbed through oral mucosa as claimed in claim 1, take Almogran or its pharmaceutically acceptable salt as the active drug composition, preferably apple hydrochlorate wherein, jointly form with acceptable auxiliary element in oral mucosa medicament, wherein in said auxiliary element, disintegrating agent and filler are arranged, correctives, binding agent, mucosa absorption promoter and lubricant.
3. the Almogran medicine of absorbed through oral mucosa as claimed in claim 1 or 2, is characterized in that Almogran or its pharmaceutically acceptable salt are the active drug composition, can contain disintegrating agent, filler, correctives, binding agent and lubricant; The content of said active drug composition Almogran in pharmaceutical preparation, generally can be 1%～70% of medicine gross weight, the consumption of above-mentioned auxiliary element can be respectively uses by the usual manner of each corresponding preparations at present, the content specification of pharmaceutical preparation unit take Almogran as 6.25mg, 12.5mg etc.
4. as the preparation of the described medicine of claim 1-3, can adopt the usual manner of present similar drugs preparation to prepare.Take malic acid Almogran Sublingual tablet medicine as example, its typical preparation method can have:
(1) wet granulation mode: active drug composition malic acid Almogran is carried out pretreatment (adopting suitable size reduction machinery that Almogran is pulverized) or do not carry out pretreatment, with selected auxiliary element mix homogeneously, after adding binding agent granulation and dry (or adopting the fluidized bed granulation drying), add again and add disintegrating agent and the abundant mixing of lubricant, tabletting makes the Sublingual tablet preparation.
(2) direct compression mode: active drug composition malic acid Almogran is carried out pretreatment (adopting suitable size reduction machinery that Almogran is pulverized) or do not carry out pretreatment, with selected auxiliary element mix homogeneously, direct compression makes the Sublingual tablet preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110427472 CN103156816A (en) | 2011-12-19 | 2011-12-19 | Almotriptan drug absorbed through mouth mucosa |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110427472 CN103156816A (en) | 2011-12-19 | 2011-12-19 | Almotriptan drug absorbed through mouth mucosa |
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| CN103156816A true CN103156816A (en) | 2013-06-19 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN 201110427472 Pending CN103156816A (en) | 2011-12-19 | 2011-12-19 | Almotriptan drug absorbed through mouth mucosa |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103520126A (en) * | 2013-10-11 | 2014-01-22 | 扬子江药业集团四川海蓉药业有限公司 | Almotriptan tablet and preparation method thereof |
| CN115006356A (en) * | 2022-05-09 | 2022-09-06 | 广西纯正堂制药有限公司 | Lumbrukinase oral adhesive tablet and preparation method and application thereof |
-
2011
- 2011-12-19 CN CN 201110427472 patent/CN103156816A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103520126A (en) * | 2013-10-11 | 2014-01-22 | 扬子江药业集团四川海蓉药业有限公司 | Almotriptan tablet and preparation method thereof |
| CN103520126B (en) * | 2013-10-11 | 2016-06-22 | 扬子江药业集团四川海蓉药业有限公司 | A kind of Almotriptan tablet and preparation method thereof |
| CN115006356A (en) * | 2022-05-09 | 2022-09-06 | 广西纯正堂制药有限公司 | Lumbrukinase oral adhesive tablet and preparation method and application thereof |
| CN115006356B (en) * | 2022-05-09 | 2024-02-20 | 九华华源药业(桂林)有限公司 | Lumbrukinase oral cavity adhesive tablet, and preparation method and application thereof |
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Application publication date: 20130619 |