CN1268337C - Desloratadine dry-mixed suspensoid and preparing method thereof - Google Patents
Desloratadine dry-mixed suspensoid and preparing method thereof Download PDFInfo
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- CN1268337C CN1268337C CN 02148577 CN02148577A CN1268337C CN 1268337 C CN1268337 C CN 1268337C CN 02148577 CN02148577 CN 02148577 CN 02148577 A CN02148577 A CN 02148577A CN 1268337 C CN1268337 C CN 1268337C
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- desloratadine
- essence
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Abstract
The present invention discloses a novel preparation of deloratadine, which comprises 0.01 to 1% of deloratadine for coating. Coating materials comprise E type and II type acrylic resin of methacrylic acid amino alkyl ester copolymers. Deloratadine as raw materials is sensitive to light, heat and humidity, so the raw materials are coated for ensuring the stability of deloratadine; furthermore, the instability is improved. Meanwhile, the bad taste and odor of deloratadine can be masked.
Description
Technical field
The invention discloses a kind of novel form of Desloratadine and preparation method thereof.
Background technology
C
19H
19ClN
2 310.82
Desloratadine is the long-acting tricyclic antidepressants antihistaminic of non-sedating, is the active metabolite of loratadine, can be by optionally blocking periphery H
1Receptor suppresses the release that various anaphylaxis cause scorching chemical mediator, as: suppress mastocyte and basophilic leukocyte and discharge histamine, prostaglandin, interleukin etc., alleviate allergic rhinitis or the urticarial related symptoms of chronic idiopathic.
Desloratadine has tablet, dispersible tablet, syrup for the dosage form of selection of clinical, tablet is a kind of general formulation, absorb in vivo and must could pass through gastrointestinal tract arrival blood circulation through processes such as disintegrate, strippings, and tablet in process of production, often, reasons such as adjuvant, technology are difficult to disintegrate because of causing tablet, medicine is difficult to stripping, thereby makes medicine not reach due therapeutical effect.In addition, for the disease of child and dysphagia, tablet is difficult to accept.Though syrup has overcome the above-mentioned shortcoming of tablet, but its production and transportation are inconvenient, and in syrup, must add antiseptic, to prevent the growth of antibacterial, could guarantee its biological stability, syrup itself is a kind of thermodynamic unstable system in addition, and is perishable in the process of storage, the careless slightly curative effect that will influence medicine.Dispersible tablet is owing to be tablet also, in process of production, often, reasons such as adjuvant, technology are difficult to disintegrate (particularly pressure) because of causing tablet, medicine is difficult to stripping, thereby make medicine not reach due therapeutical effect, real technical process repeatability is very poor, and the volume of dispersible tablet tablet can not be too big, otherwise dysphagia.Dry suspension because of taking convenience, absorb special performances such as fast, that bioavailability is high and untoward reaction is little, it both can overcome tablets inconvenience, can solve syrupy unstability and transportation, storage inconvenience again.
Summary of the invention
The objective of the invention is: the Desloratadine raw material is very sensitive to light, heat, humidity, thereby event is carried out coating with raw material and is improved its unstability for guaranteeing its stability, it is not good simultaneously can to cover its taste yet, it is the Desloratadine suspending agent that the present invention adopts new adjuvant, and the present invention intends adopting novel form to be convenient to production and transport, storage and clinical use in addition.
Be the technical measures that realize that the object of the invention is taked:
The Desloratadine dry suspension, it comprises the Desloratadine of coating, and content 0.01-1%, the material of coating are methacrylic acid aminoalkyl ester copolymer E type or II acrylic resin, and the coating weightening finish is 5% to 20%; Suspending agent content is 1% to 5%; Correctives content is 5-50%; Filler or excipient, content 5-60%; The bonding agent of convention amount and coloring agent.
Suspending agent can be that in xanthan gum, sodium carboxymethyl cellulose, hypromellose, gelatin and the tragacanth one or more use simultaneously, and the content of suspending agent is 1% to 5%.
Correctives comprises polyhydric alcohol and essence; Polyhydric alcohol can adopt in sucrose, glucose, saccharin sodium and the stevioside one or more to use simultaneously, and the content of polyhydric alcohol is 5% to 50%; Essence comprises orange flavor, flavoring banana essence, apple essence, Fructus Citri tangerinae essence or strawberry essence, and essence content is 0.01% to 10.0%; Excipient can be mannitol, sucrose, maltodextrin or microcrystalline Cellulose, and excipient content 〉=5% is to 60%; Bonding agent comprises one or more in starch slurry, hydroxypropyl methyl fiber, hydroxypropyl methyl fiber sodium, distilled water and the ethanol; Coloring agent comprises sunset yellow, lemon yellow, pink, red scarlet, rose-red or amaranth, and content is 0.0001% to 0.001%.
The preparation method of Desloratadine dry suspension may further comprise the steps: (1) methacrylic acid aminoalkyl ester copolymer E type is dissolved in the ethanol, is transparent coating solution; The Desloratadine raw material that (2) will sieve is put in the boiling granulating machine, carries out the raw material coating with above-mentioned coating solution; (3) each composition of suspending agent, correctives, filler, excipient and bonding agent is crossed 100 mesh sieves, mix homogeneously, spray painted, drying, packing promptly.
Desloratadine dry suspension of the present invention, its principal agent is a Desloratadine, Desloratadine is insoluble in water, is soluble in methanol, ethanol, slightly is dissolved in dilute hydrochloric acid, shows alkalescence, thus can not with the basic auxiliary compatibility.Methacrylic acid aminoalkyl ester copolymer E type (EUDRAGIT
E100) characteristic finds that it is the best coating material of taste masking coating, because of it is a cation type polymer, contains amino so EUDRAGIT in the structure
The formed film of E100 does not dissolve in neutral medium such as oral cavity, and can the salify dissolving in gastric acid environment.
The specific embodiment
Below by embodiment technical scheme of the present invention is further elaborated.
Embodiment 1: use hydroxypropyl emthylcellulose (HPMC), ethyl cellulose (EC), methacrylic acid aminoalkyl ester copolymer E type (EUDRAGIT respectively
E100) carry out the coating solution screening, finally determine coating material.Coating weightening finish 10%.The screening of raw material coating
Test 1:HPMC 25g
Propylene glycol 10ml
Oleum Ricini 10ml
Polyoxyethylene sorbitan monoleate 10ml
Ethanol 500ml
Water 500ml technology: take by weighing 25gHPMC, use the 500ml hot water dissolving, cold to room temperature becomes viscous solution, adds 500ml ethanol, stirs, and adds Oleum Ricini, polyoxyethylene sorbitan monoleate, propylene glycol, stirs;
Test 2:EC 25g
Isopropyl alcohol 150ml
Ethanol 850ml technology: take by weighing 25g EC, be dissolved in 150ml isopropyl alcohol, the 850ml ethanol, dissolving.
Test 3:EUDRAGITE100 25g
Ethanol 1000ml technology: take by weighing 25g EUDRAGIT
E100 is dissolved in 1000ml
In the ethanol, be clear solution.
Operation: will be through the Desloratadine raw material of 100 mesh sieves; put in the boiling granulating machine; coating solution is placed peristaltic pump; regulating each parameter of boiling granulating machine is: 60～80 ℃ of inlet temperature; 30～35 ℃ of leaving air temps; pressure 0.2Pa, flow velocity are 10～15ml/min, carry out the raw material coating with above-mentioned coating solution respectively.
Raw material coating The selection result
| The investigation project | The result | |||||
| Test 1 | Test 2 | Test 3 | ||||
| 0 day | 5 days | 0 day | 5 days | 0 day | 5 days | |
| Mouthfeel | Generally | Generally | Generally | Generally | Good | Good |
| The settling volume ratio | 0.67 | 0.66 | 0.84 | 0.81 | 0.96 | 0.97 |
The result is as seen in the table: test 3 film coating prescription taste masking better performances, so writing out a prescription of selecting for use as the raw material coating.
Embodiment 2:
Prescription
Coating Desloratadine 2.5 does not restrain
Sucrose 212 grams
Mannitol 270 grams
Sodium carboxymethyl cellulose 10 grams
Orange flavor 0.5 gram
Xanthan gum 5 grams
Sunset yellow 0.001 gram is made 1000 bags of technologies altogether: above-mentioned each composition is crossed 100 mesh sieves, mix homogeneously.Spray painted, drying, packing promptly.
Embodiment 3:
Prescription
Desloratadine raw material 2.5 grams of coating
(by Desloratadine)
Sucrose 212 grams
Mannitol 270 grams
Sodium carboxymethyl cellulose 10 grams
Orange flavor 0.5 gram
Xanthan gum 5 grams
Sunset yellow 0.001 gram is made 1000 bags altogether
Technology: it is granulating coated to carry out raw material with coating solution; Above-mentioned each composition is crossed 100 mesh sieves, mix homogeneously.Spray painted, drying, packing promptly.
| The settling volume ratio | Related substance (%) | Content (%) | |||
| Embodiment 2 | 0 day | 0.88 | 2.35％ | 97.21％ | |
| 10 days | Illumination | 0.87 | 4.55％ | 95.23％ | |
| 60℃ | 0.88 | 4.63％ | 95.01％ | ||
| RH92.5％ | 0.22 | 4.82％ | 95.11％ | ||
| Embodiment 3 | 0 day | 0.99 | 0.11％ | 99.75％ | |
| 10 days | Illumination | 0.98 | 0.10％ | 99.88％ | |
| 60℃ | 0.99 | 0.09％ | 99.90％ | ||
| RH92.5％ | 0.97 | 0.10％ | 99.89％ | ||
Above-mentioned experiment show manufactured place of the present invention loratadine taste be improved significantly, raw material is coated also extremely stable.
Claims (4)
1. Desloratadine dry suspension, it comprises the Desloratadine of coating, and content 0.01-1%, the material of coating are methacrylic acid aminoalkyl ester copolymer E types, and the coating weightening finish is 5% to 20%; Suspending agent content is 1% to 5%; Correctives content is 5-50%; Filler or excipient, content 5-60%; The bonding agent of convention amount and coloring agent.
2. by the described Desloratadine dry suspension of claim 1, it is characterized in that: suspending agent can be that in xanthan gum, sodium carboxymethyl cellulose, hypromellose, gelatin and the tragacanth one or more use simultaneously, and the content of suspending agent is 1% to 5%.
3. by claim 1 or 2 described dry suspension, it is characterized in that: correctives comprises polyhydric alcohol and essence; Polyhydric alcohol can adopt in sucrose, glucose, saccharin sodium and the stevioside one or more to use simultaneously, and the content of polyhydric alcohol is 5% to 50%; Essence comprises orange flavor, flavoring banana essence, apple essence, Fructus Citri tangerinae essence or strawberry essence, and essence content is 0.01% to 10.0%; Excipient can be mannitol, sucrose, maltodextrin or microcrystalline Cellulose, and excipient content 〉=5% is to 60%; Bonding agent comprises one or more in starch slurry, hydroxypropyl methyl fiber, hydroxypropyl methyl fiber sodium, distilled water and the ethanol; Coloring agent comprises sunset yellow, lemon yellow, pink, red scarlet, rose-red or amaranth, and content is 0.0001% to 0.001%.
4. the preparation method of Desloratadine dry suspension, may further comprise the steps: (1) methacrylic acid aminoalkyl ester copolymer E type is dissolved in the ethanol, is transparent coating solution; The Desloratadine raw material that (2) will sieve is put in the boiling granulating machine, carries out the raw material coating with above-mentioned coating solution; (3) each composition of suspending agent, correctives, filler, excipient and bonding agent is crossed 100 mesh sieves, mix homogeneously, spray painted, drying, packing promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02148577 CN1268337C (en) | 2002-12-19 | 2002-12-19 | Desloratadine dry-mixed suspensoid and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02148577 CN1268337C (en) | 2002-12-19 | 2002-12-19 | Desloratadine dry-mixed suspensoid and preparing method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1507868A CN1507868A (en) | 2004-06-30 |
| CN1268337C true CN1268337C (en) | 2006-08-09 |
Family
ID=34233212
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02148577 Expired - Lifetime CN1268337C (en) | 2002-12-19 | 2002-12-19 | Desloratadine dry-mixed suspensoid and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1268337C (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3881640B2 (en) * | 2003-08-08 | 2007-02-14 | 塩野義製薬株式会社 | Dry syrup containing loratadine |
| CN101455643B (en) * | 2009-01-08 | 2012-05-30 | 杭州高成生物营养技术有限公司 | Dry suspension and preparation method thereof |
| CN102038645B (en) * | 2009-10-12 | 2013-11-27 | 杭州赛利药物研究所有限公司 | Desloratadine grain and preparation method thereof |
| CN102475689B (en) * | 2010-11-30 | 2015-04-01 | 杭州赛利药物研究所有限公司 | Suspension dispersible tablets and preparation method |
| CN104306338A (en) * | 2014-09-24 | 2015-01-28 | 万特制药(海南)有限公司 | Granule containing acrylic acid resin and desloratadine, and preparation method thereof |
| CN104337774A (en) * | 2014-11-04 | 2015-02-11 | 万全万特制药江苏有限公司 | Preparation method of desloratadine granules |
| CN109875966B (en) * | 2019-04-09 | 2021-03-26 | 海南普利制药股份有限公司 | Dry suspension of desloratadine |
| CN110638785B (en) * | 2019-09-29 | 2021-09-24 | 黄山中皇制药有限公司 | Andrographolide dry suspension |
-
2002
- 2002-12-19 CN CN 02148577 patent/CN1268337C/en not_active Expired - Lifetime
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| Publication number | Publication date |
|---|---|
| CN1507868A (en) | 2004-06-30 |
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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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| CP01 | Change in the name or title of a patent holder |
Address after: Hangzhou City, Zhejiang province 310009 Qingchun Road No. 11 Triumphal Arch commercial center 18 floor, room D C Patentee after: HAINAN POLY PHARM. Co.,Ltd. Patentee after: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Address before: Hangzhou City, Zhejiang province 310009 Qingchun Road No. 11 Triumphal Arch commercial center 18 floor, room D C Patentee before: Hainan Poly Pharm Co.,Ltd. Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. |
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Granted publication date: 20060809 |