CN100339081C - Oral loratadine disintegrating tablet and its prepn - Google Patents
Oral loratadine disintegrating tablet and its prepn Download PDFInfo
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- CN100339081C CN100339081C CNB2004100679894A CN200410067989A CN100339081C CN 100339081 C CN100339081 C CN 100339081C CN B2004100679894 A CNB2004100679894 A CN B2004100679894A CN 200410067989 A CN200410067989 A CN 200410067989A CN 100339081 C CN100339081 C CN 100339081C
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- loratadine
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- disintegrating tablet
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Abstract
The present invention belongs to the field of medicine. The present invention particularly relates to an oral loratadine disintegrating tablet for treating anaphylactic diseases and a preparation method thereof. The oral loratadine disintegrating tablet comprises loratadine which is medical active ingredients and a mixture of excipient. The oral loratadine disintegrating tablet is characterized in that the excipient comprises a disintegrating agent, a filling agent, soluble polyol and a penetrating agent; the tablet comprises the following ingredients according to the proportion by weight: 20% to 50% of loratadine, 5% to 15% of disintegrating agent, 10% to 30% of soluble polyol and 1% to 5% of penetrating agent. Compared with an ordinary oral preparation, because the mucosa of gstrointestinal tracts is widely covered by medicine which is quickly disintegrated, the effect of the present invention is rapid. The medicine is absorbed by the oral mucosa, the first pass effect is cancelled, the biological availability is enhanced, and the stimulation for gstrointestinal tracts is reduced. The oral disintegrating tablet can be taken from the mouth without water, which provides convenience for people to take the medicine in an oral taking mode when water is inconveniently drunk.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of preparation method for the treatment of the oral loratadine disintegrating tablet of anaphylactic disease.
Background technology
Anaphylaxis be a kind of acute, general, seriously arrive even life-threatening allergy, take place when before the patient, being contacted same allergen once more after certain allergen sensitization.Anaphylactoid symptom can occur behind the contact allergen immediately or in 2 hours.The patient does not feel like oneself, agitation, cardiopalmus, tremble, erubescence is itched, tinnitus, cough, sneeze, urticaria, edema or because of asthma and airway obstruction cause dyspnea, and cardiovascular system depletion can take place under the situation that Respiratory symptoms do not occur.The symptom that when anaphylaxis takes place, may occur cardiovascular or respiratory system usually, but anaphylactoid people repeatedly takes place in the appearance simultaneously of the symptom of two kinds of systems, and the symptom when at every turn showing effect is usually similar.Anaphylactoid process is very fast, can cause collapse, tic, urinary incontinence, loss of consciousness very soon, apoplexy occurs in 1～2 minute.Unless carry out emergency treatment immediately, otherwise anaphylaxis usually causes death.
Anaphylaxis can be caused by various allergens.Anaphylaxis can not take place when contacting allergen for the first time, contact then may take place once more.But when for the first time most of people also do not know contacted certain allergen.
Loratadine is the of new generation long-acting three ring antihistaminics of a kind of long-acting, no sedation, no anticholinergic effect, has the effect of selectivity antagonism periphery H1-receptor.In the therapeutic dose scope, do not have drowsiness effect, be applicable to shed tears, sneeze, allergic rhinitis, acute or chronic urticaria disease and other anaphylaxis dermatosis.Ethanol there is not invigoration effect.Effect rapidly, taking medicine begins onset in back 30 minutes, can not pass through blood brain barrier.
Loratadine is white or off-white color crystalline powder; Almost odorless is tasteless.Atomic molten in water or ethanol, insoluble in ether or chloroform; In alkaline solution, dissolve.Present loratadine generally all is oral gastric solubility preparation, and medicine can not be absorbed rapidly, and onset is slower, and takes inconvenience, especially for because of the bad patient of anaphylactic disease function of deglutition.
Summary of the invention
The objective of the invention is to overcome the defective that exists in the background technology, provide a kind of rapid-action, bioavailability is high, the preparation method of the oral loratadine disintegrating tablet of taking convenience.
A kind of preparation method of oral loratadine disintegrating tablet, oral loratadine disintegrating tablet comprise the mixture of active constituents of medicine loratadine and excipient, and described excipient comprises disintegrating agent, filler, solubility polyhydric alcohol and penetrating agent; The weight ratio of each component is in this tablet: loratadine 20%～50%, disintegrating agent 5%～15%, filler 10%～30%, solubility polyhydric alcohol 30%～60%, penetrating agent 1%～5%; Described disintegrating agent is a crospovidone, one or more mixing in cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, the carboxymethyl starch sodium; Described filler is one or more mixing in pregelatinized Starch, amylum pregelatinisatum, lactose, sucrose and glucose, cellulose and microcrystalline Cellulose, the gelatin; Described solubility polyhydric alcohol is one or more mixing in mannitol, xylitol, Sorbitol and the maltose alcohol; Described penetrating agent is for having the silicon dioxide of high-affinity, one or more mixing in the maltodextrin to water; The main processing step of this method is as follows: mix by the component prescription, prepare tablet with powder pressing method or freeze-drying.
Above-mentioned tablet can also comprise one or more in the lubricant of 0.5%～3% essence, 0.5%～3% sweeting agent and 0.5%～1.5%.
In the above-mentioned method, use loratadine 250g, mannitol 420g, microcrystalline Cellulose 150g, crospovidone 70g and an amount of essence, sweeting agent and lubricant when preparing 1000 tablets of tablets.
In the above-mentioned method, use loratadine 250g, sorbitol 400g, glucose 80g, sucrose 70g, cross-linking sodium carboxymethyl cellulose 60g, silicon dioxide 20g and an amount of essence, sweeting agent and lubricant when preparing 1000 tablets of tablets.
In the above-mentioned method, use loratadine 250g, mannitol 200g, sucrose 220g gelatin 50g, hydroxyethyl-cellulose 40g and an amount of essence when preparing 1000 tablets of tablets.
The oral cavity disintegration tablet of method preparation of the present invention is compared with common oral preparation, is extensively covered by the medicine after fast the collapsing because of gastrointestinal tract mucous, and onset is rapid.And medicine can the through port transmucosal absorbs, and removed first pass effect from, improved bioavailability, and having reduced stimulates gastrointestinal.For the anaphylactic disease patient provides a kind of new dosage form that makes things convenient for.Because oral cavity disintegration tablet does not need in mouth under water can obey, for people's oral medication of the inconvenience of drinking water provides convenience.
This tablet is to produce disintegrate, generally disintegrate in less than 40 seconds, or even disintegrate in less than 30 seconds when contacting with saliva in the oral cavity.The oral cavity disintegration tablet that provides among the present invention has better hardness, both can be convenient to packing and transportation, is convenient to suitability for industrialized production again.
The specific embodiment
We never are limited to this from the further illustrated in greater detail the present invention of the following example but should understand scope of the present invention.
Embodiment 1: 1000 oral loratadine disintegrating tablets of present embodiment preparation (specification: 0.25g), use following compositions:
The name of material inventory
Loratadine 250g
Mannitol 420g
Microcrystalline Cellulose 150g
Crospovidone 70g
Aspartame 20g
Herba Menthae essence 10g
Silicon dioxide 20g
Magnesium stearate 5g
Processing step: raw material, granules of accessories add aspartame, Herba Menthae essence and silicon dioxide, magnesium stearate, mix homogeneously, tabletting, packing.
Sample to above-mentioned prescription carries out mouthfeel, Orally disintegrating time, disintegration, friability mensuration.
Test item
Mouthfeel is good
28 seconds Orally disintegrating time limits
19 seconds disintegrations
Friability 0.5%
Embodiment 2: 1000 oral loratadine disintegrating tablets of present embodiment preparation (specification: 0.25g), use following compositions:
The name of material inventory
Loratadine 250g
Sorbitol 400g
Glucose 80
Sucrose 70g
Cross-linking sodium carboxymethyl cellulose 60g
Stevioside 25g
Orange flavor 10g
Titanium dioxide 20g
Sodium stearyl fumarate 5g
Processing step: raw material, granules of accessories add stevioside, orange flavor and silicon dioxide, sodium stearyl fumarate, mix homogeneously, tabletting, packing.
Sample to above-mentioned prescription carries out mouthfeel, Orally disintegrating time, disintegration, friability mensuration.
Test item
Mouthfeel is good
25 seconds Orally disintegrating time limits
16 seconds disintegrations
Friability 0.6%
Embodiment 3: 1000 oral loratadine disintegrating tablets of present embodiment preparation (specification: 0.25g), use following compositions:
The name of material inventory
Loratadine 250g
Mannitol 200g
Sucrose 220g
Gelatin 50g
Hydroxyethyl-cellulose 40g
Herba Menthae essence 10g
Processing step: raw material, adjuvant water dissolution, fully mixing joins and is positioned over sharp freezing in the freeze dryer in the mould, is evacuated to dry materials, packs.
Sample to above-mentioned prescription carries out mouthfeel, Orally disintegrating time, disintegration time mensuration.
Test item
Mouthfeel is good
19 seconds Orally disintegrating time limits
14 seconds disintegrations
Claims (5)
1. the preparation method of an oral loratadine disintegrating tablet, oral loratadine disintegrating tablet comprises the mixture of active constituents of medicine loratadine and excipient, it is characterized in that described excipient comprises disintegrating agent, filler, solubility polyhydric alcohol and penetrating agent; The weight ratio of each component is in this tablet: loratadine 20%～50%, disintegrating agent 5%～15%, filler 10%～30%, solubility polyhydric alcohol 30%～60%, penetrating agent 1%～5%; Described disintegrating agent is a crospovidone, one or more mixing in cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, the carboxymethyl starch sodium; Described filler is one or more mixing in pregelatinized Starch, amylum pregelatinisatum, lactose, sucrose and glucose, cellulose and microcrystalline Cellulose, the gelatin; Described solubility polyhydric alcohol is one or more mixing in mannitol, xylitol, Sorbitol and the maltose alcohol; Described penetrating agent is for having the silicon dioxide of high-affinity, one or more mixing in the maltodextrin to water; The main processing step of this method is as follows: mix by the component prescription, prepare tablet with powder pressing method or freeze-drying.
2. the preparation method of a kind of oral loratadine disintegrating tablet according to claim 1 is characterized in that also comprising in the lubricant of 0.5%～3% essence, 0.5%～3% sweeting agent and 0.5%～1.5% one or more.
3. the preparation method of a kind of oral loratadine disintegrating tablet according to claim 2 is used loratadine 250g, mannitol 420g, microcrystalline Cellulose 150g, crospovidone 70g and an amount of essence, sweeting agent and lubricant when it is characterized in that preparing 1000 tablets of tablets.
4. the preparation method of a kind of oral loratadine disintegrating tablet according to claim 2 is used loratadine 250g, sorbitol 400g, glucose 80g, sucrose 70g, cross-linking sodium carboxymethyl cellulose 60g, silicon dioxide 20g and an amount of essence, sweeting agent and lubricant when it is characterized in that preparing 1000 tablets of tablets.
5. the preparation method of a kind of oral loratadine disintegrating tablet according to claim 2 is used loratadine 250g, mannitol 200g, sucrose 220g gelatin 50g, hydroxyethyl-cellulose 40g and an amount of essence when it is characterized in that preparing 1000 tablets of tablets.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100679894A CN100339081C (en) | 2004-11-10 | 2004-11-10 | Oral loratadine disintegrating tablet and its prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100679894A CN100339081C (en) | 2004-11-10 | 2004-11-10 | Oral loratadine disintegrating tablet and its prepn |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1739513A CN1739513A (en) | 2006-03-01 |
| CN100339081C true CN100339081C (en) | 2007-09-26 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB2004100679894A Active CN100339081C (en) | 2004-11-10 | 2004-11-10 | Oral loratadine disintegrating tablet and its prepn |
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Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100463674C (en) * | 2006-12-22 | 2009-02-25 | 江苏奥赛康药业有限公司 | Oral cavity quick dissolved film containing civeran, and method for preparing the same |
| US20100286045A1 (en) | 2008-05-21 | 2010-11-11 | Bjarke Mirner Klein | Methods comprising desmopressin |
| LT2712622T (en) | 2008-05-21 | 2016-09-26 | Ferring B.V. | Orodispersible desmopressin for increasing initial period of sleep undisturbed by nocturia |
| US11963995B2 (en) | 2008-05-21 | 2024-04-23 | Ferring B.V. | Methods comprising desmopressin |
| 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 |
| JO3112B1 (en) * | 2010-03-29 | 2017-09-20 | Ferring Bv | A fast dissolving pharmaceutical composition |
| CA2793485A1 (en) * | 2010-03-29 | 2011-10-06 | Ferring B.V. | A fast dissolving pharmaceutical composition |
| CN107648191B (en) * | 2017-09-27 | 2018-08-17 | 扬子江药业集团上海海尼药业有限公司 | A kind of loratadine tablet and its preparation process |
| CN111249239B (en) * | 2020-01-17 | 2022-02-11 | 中国药科大学 | Loratadine nanocrystal and preparation method thereof |
-
2004
- 2004-11-10 CN CNB2004100679894A patent/CN100339081C/en active Active
Non-Patent Citations (3)
| Title |
|---|
| 口腔崩释片研制简介 李先何等，实用中西医结合临床，第3卷第2期 2003 * |
| 口腔速崩片拓的研究进展 马萍，中国药师，第7卷第3期 2004 * |
| 口腔速释片的进展及前景 刘梅等，中国药学杂志，第36卷第9期 2001 * |
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| Publication number | Publication date |
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| CN1739513A (en) | 2006-03-01 |
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Owner name: HAINAN POLY PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: FAN MINHUA Effective date: 20100707 Owner name: ZHEJIANG RUIDA PHARMACEUTICAL CO., LTD. HANGZHOU S |
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Free format text: CORRECT: ADDRESS; FROM: 310004 HOUSE 5, BUILDING 9, NO.167, HUANCHENG NORTH ROAD, HANGZHOU CITY, ZHEJIANG PROVINCE TO: 571127 GUILINYANG ECONOMIC AND TECHNOLOGICAL DEVELOPMENT ZONE, MEILAN DISTRICT, HAIKOU CITY, HAINAN PROVINCE |
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Effective date of registration: 20100707 Address after: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Co-patentee after: Zhejiang Ruida Pharmaceutical Co.,Ltd. Patentee after: Hainan Poly Pharm Co.,Ltd. Co-patentee after: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Address before: 5, No. 9, building 167, building 310004, Ring North Road, Hangzhou, Zhejiang Patentee before: Fan Minhua |
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Correction item: Patentee Correct: Zhejiang Ruida Pharm Co.,Ltd. False: Zhejiang Ruida Pharmaceutical Co.,Ltd. Number: 33 Volume: 26 |
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Correction item: Patentee Correct: Zhejiang Ruida Pharm Co.,Ltd. False: Zhejiang Ruida Pharmaceutical Co.,Ltd. Number: 33 Page: The title page Volume: 26 |
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Owner name: HAINAN PLOY PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME: HAINAN PULIN PHARMACEUTICAL CO., LTD. |
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Address after: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Patentee after: HAINAN POLY PHARM. Co.,Ltd. Patentee after: ZHEJIANG POLY PHARMACEUTICAL Co.,Ltd. Patentee after: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Address before: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Patentee before: Hainan Poly Pharm Co.,Ltd. Patentee before: Zhejiang Ruida Pharm Co.,Ltd. Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. |
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Effective date of registration: 20221012 Address after: 571127 Guilin Ocean Economic Development Zone, Meilan District, Haikou City, Hainan Province Patentee after: HAINAN POLY PHARM. Co.,Ltd. Patentee after: ZHEJIANG POLY PHARMACEUTICAL Co.,Ltd. Address before: 571127 Guilin Ocean Economic and Technological Development Zone, Meilan District, Haikou City, Hainan Province Patentee before: HAINAN POLY PHARM. Co.,Ltd. Patentee before: ZHEJIANG POLY PHARMACEUTICAL Co.,Ltd. Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. |