CN101502515A - Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same - Google Patents
Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same Download PDFInfo
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- CN101502515A CN101502515A CNA2008102155181A CN200810215518A CN101502515A CN 101502515 A CN101502515 A CN 101502515A CN A2008102155181 A CNA2008102155181 A CN A2008102155181A CN 200810215518 A CN200810215518 A CN 200810215518A CN 101502515 A CN101502515 A CN 101502515A
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- enteric
- loratadine
- preparation
- coated
- hydrochloric acid
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Abstract
The invention discloses a lorapadine hydrochloride enteric preparation combination and a preparation method thereof. The lorapadine hydrochloride enteric preparation combination is mainly prepared from lorapadine hydrochloride bulk drugs and appropriate auxiliary materials. Compared with the common lorapadine hydrochloride preparations, the lorapadine hydrochloride enteric preparation provided by the invention has the advantages that the lorapadine hydrochloride enteric preparation is less irritant to the stomach, thereby reducing the adverse reactions. The lorapadine hydrochloride enteric preparation combination is particularly suitable for patients with stomach-upset diseases. The invention provides a novel form of drug featuring higher safety and better curative effect and having the advantages of high quality controllability and stability of the preparation process.
Description
Technical field
The invention belongs to medical technical field, relate to a kind of hydrochloric acid loratadine enteric-coated formulation composition and preparation method thereof.
Background technology
The hydrochloric acid loratadine is long-acting tricyclic antidepressants antihistaminic, can pass through optionally antagonism peripheral H1-receptor, alleviates the nose or the non-sniffle of seasonal allergic rhinitis, belongs to the nonprescription drugs management area at present.According to reports, hydrochloric acid loratadine oral absorption is rapid, and onset in 45 minutes is the fastest antihistaminic of present onset, reaches 18～24 hours action time.Protein binding rate is 97～99%.Be potent, long lasting novel antihistaminic,, be difficult for seeing through blood brain barrier, so no central inhibitory action to periphery H1 receptor affinity height.
This product is used to alleviate the relevant symptom of allergic rhinitis, itches and burn feeling as sneeze, watery nasal discharge and rhinocnesmus, nasal obstruction and eye.Nose and eye symptom and sign are able to rapid alleviation behind the oral drugs, also are applicable to the symptom and the sign of relieve chronic urticaria, itching skin disease and other anaphylaxis dermatosis.
The hydrochloric acid loratadine, its chemistry 4-(8-chloro-5,6-dihydro-11H-benzo [5,6] suberyl [1,2-b] pyridine-11-alkene) by name-1-piperidine carboxylate hydrochlorate.As prolonged application nonprescription drugs widely, the hydrochloric acid loratadine has been obtained good clinical therapeutic efficacy on treatment market, but untoward reaction such as the gastrointestinal system that causes because of the medicine self-characteristic such as dyspepsia, flatulence, the sense of taste changes, appetite decline, constipation, diarrhoea, singultus, appetite increase, nauseating, gastritis, toothache, vomiting.These problems make doctor and patient not satisfied to this medicine safety in utilization.
At present, the hydrochloric acid loratadine oral formulations of having developed on the market has tablet, capsule, granule etc., these dosage forms are because dosage form itself is, exist easily to make the release under one's belt of hydrochloric acid loratadine, esterlysis and increase the defective that the acid of stomach is stimulated and causes the pepsic secretion minimizing of stomach.Untoward reaction such as above-mentioned gastrointestinal system symptom can appear in long-term prescription, especially the patient that stomach upset diseases is arranged are had certain use limitation.Therefore, searching out the preparation that a kind of existing common hydrochloric acid loratadine oral formulations more can satisfy the more reasonable safe clinical instructions for use of doctor and patient, is the essential problem that solves.
To this, we explore repeatedly and study, developed a kind of preparation of hydrochloric acid loratadine enteric-coated formulation composition, the advantage of said preparation is that medicine does not discharge under one's belt and dissolves, therefore do not exist and destroy the possibility that chemical compound produces the untoward reaction triggering factor in the acid, do not stimulate and cause a series of side effect thereby can not cause stomach, to have activeness digestive tract hemorrhage, digestive tract ulcer active stage etc. patient's particularly suitable of stomach upset diseases.
Show through relevant patent and prior art literature search result, there is no the relevant report of hydrochloric acid loratadine enteric-coated formulation composition.
Summary of the invention
In order to overcome the hydrochloric acid loratadine to the stimulation of stomach and the untoward reaction that causes, and make the hydrochloric acid loratadine in gastric acid, be difficult for destroyed and affect the treatment, the invention provides hydrochloric acid loratadine enteric-coated formulation composition.
The object of the present invention is to provide hydrochloric acid loratadine enteric-coated formulation composition and preparation method thereof.
Technical scheme of the present invention is: hydrochloric acid loratadine enteric-coated formulation composition and preparation method thereof, it is characterized in that: said composition is counted 1:0.1～500 by weight and is formed by hydrochloric acid loratadine crude drug and one or more pharmaceutically acceptable pharmaceutical carrier and/or adjuvants; Specification is 1～100mg.This hydrochloric acid loratadine enteric-coated formulation composition preparation method is to wrap enteric material to make enteric coated tablet and enteric coated granule on the plain sheet of molding or crude granule, and the shaped granule enteric coated capsule of packing into is made enteric coated capsule and maybe will be made the enteric coated micropill common hard capsule of packing into and make enteric-coated pellet capsule.
Described hydrochloric acid loratadine enteric-coated formulation composition, also can further contain carrier and/or adjuvant commonly used in the pharmaceuticals industry, for example enteric material, binding agent, filler, disintegrating agent, lubricant, wetting agent, solubilizing agent, emulsifying agent, plasticizer, fluidizer etc.
Described enteric material is selected from one or more of copolymer, hydroxypropyl CAP, CAP, hypromellose phthalate ester, hydroxypropylmethyl cellulose phthalate, polyvinyl acetate phthalate of acrylate copolymer, methacrylic acid and acrylate or methacrylate etc.
Described binding agent is selected from one or more in the following material: starch, gelatin, sugar (as xylose, lactose etc.), rubber polymer, sodium alginate, hydroxy methocel, methylcellulose, polyvinylpyrrolidone, Polyethylene Glycol, ethyl cellulose, water, wax, alcohol etc.
Described filler can be selected from one or more in the following material: dicalcium phosphate, calcium sulfate, cellulose, microcrystalline Cellulose, hydroxypropyl emthylcellulose, xylose, lactose, Kaolin, mannitol, sodium chloride, dried starch etc.
Described disintegrating agent can be selected from one or more in the following material: low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, its derivant of starch etc.
Described lubricant can be selected from one or more in the following material: Pulvis Talci, magnesium stearate, calcium stearate, stearic acid, hydrogenated vegetable oil, Polyethylene Glycol etc.
Described solubilizing agent can be selected one or more of tartaric acid, citric acid, Polyethylene Glycol etc. for use; Described emulsifying agent can be selected one or more of span80, span85 etc. for use; Described plasticizer can be selected from least a in propylene glycol, glycerol, Polyethylene Glycol, triacetin, acetyl list monoglyceride, phthalic acid ester, the Semen Ricini wet goods.
Oral enteric preparation involved in the present invention can pass through the moulding process of corresponding preparations, the oral enteric preparation that gets final product correspondingly then by existing granulating process preparation such as dry method, wet method, spray drying, centrifugal granulating.
Hydrochloric acid loratadine enteric coated preparation provided by the invention makes and the not disintegrate under one's belt of hydrochloric acid loratadine gastric mucosa do not caused stimulation, untoward reaction such as can avoid takes medicine feeling sick of causing, stomachache, diarrhoea.
Provided by the invention group of hydrochloric acid loratadine enteric-coated formulation composition preparation technology's quality controllability and good stability.
The specific embodiment
Embodiment 1
Enteric coatel tablets
Prescription:
Preparation technology:
With the hydrochloric acid loratadine; lactose; carboxymethyl starch sodium; microcrystalline Cellulose; magnesium stearate is crossed behind 80 mesh sieves standby respectively; take by weighing lactose by recipe quantity; carboxymethyl starch sodium; microcrystalline Cellulose is put in the mixer behind the mixing and hydrochloric acid loratadine equivalent incremental method mixing again; it is an amount of to add 5% polyvinylpyrrolidone aqueous solution; granulate; granulate; 50 ℃ of dry 30min; dried granule adds the magnesium stearate mixing of recipe quantity; cross 16 eye mesh screen granulate with oscillating granulator; granule is carried out assay; and the heavy scope of definite sheet; tabletting; the coating powder that contains the enteric material polyvinyl acetate phthalate with the allotment of 65% ethanol acetone soln is equipped with enteric coating liquid; on the plain sheet of gained, wrap enteric coating again, pack after the passed examination.
Zhi Bei hydrochloric acid loratadine enteric coatel tablets as stated above meet the requirement of coherent detection project of regulation in " Chinese Pharmacopoeia 2005 version two ones " ' rules of preparations '.
Embodiment 2
Enteric coated capsule
Prescription:
Preparation technology:
Hydrochloric acid loratadine, microcrystalline Cellulose, starch are crossed 80 mesh sieves respectively; take by weighing microcrystalline Cellulose, starch by recipe quantity; put in the mixer mix after again with hydrochloric acid loratadine equivalent incremental method mixing; add 50% alcoholic solution and make soft material in right amount; in granulation machine, granulate; granule in 45 ℃ of dry 30min, is passed through oscillating granulator, again with 20 eye mesh screen granulate.Hybrid particles is carried out assay, and definite enteric capsule shell range of capacity is filled.After the passed examination, packing.
Zhi Bei hydrochloric acid loratadine enteric coated capsule as stated above meets the requirement of coherent detection project of regulation in " Chinese Pharmacopoeia 2005 version two ones " ' rules of preparations '.
Embodiment 3
Enteric-coated pellet capsule
Prescription: plain micropill
Prescription: enteric coating liquid
4 parts of Pulvis Talci
6 parts of titanium dioxides
20 parts of polyacrylic resin II
10 parts of polyacrylic resin III
1.5 parts of Tween 80s
3 parts of propylene glycol
50% alcoholic solution is an amount of
Preparation technology:
Hydrochloric acid loratadine, lactose, microcrystalline Cellulose, magnesium stearate are crossed 120 mesh sieves respectively; by plain micropill recipe quantity take by weighing lactose, microcrystalline Cellulose, magnesium stearate put mix in the mixer after again with hydrochloric acid loratadine equivalent incremental method mixing; place the centrifugal granulator machine; spray into the plain micropill of 50% an amount of alcoholic solution system; be equipped with coating solution by the enteric coating liquid prescription plain micropill is carried out coating; coated micropill is carried out assay, determine common hard capsule case range of capacity filling.After the passed examination, packing.
Zhi Bei hydrochloric acid loratadine enteric-coated pellet capsule as stated above meets the requirement of coherent detection project of regulation in " Chinese Pharmacopoeia 2005 version two ones " ' rules of preparations '.
Embodiment 4
Enteric coated granule
Prescription: crude granule
Prescription: enteric coating liquid
4 parts of Pulvis Talci
6 parts of titanium dioxides
35 parts of hypromellose phthalate esters
1 part of Tween 80
3 parts of propylene glycol
50% alcoholic solution is an amount of
Preparation technology:
Hydrochloric acid loratadine, polyvinylpyrrolidone, microcrystalline Cellulose, magnesium stearate are crossed 120 mesh sieves respectively; by the crude granule recipe quantity take by weighing polyvinylpyrrolidone, microcrystalline Cellulose, magnesium stearate put mix in the mixer after again with hydrochloric acid loratadine equivalent incremental method mixing; place the centrifugal granulator machine; spray into an amount of 50% alcoholic solution system crude granule; be equipped with coating solution by the enteric coating liquid prescription crude granule is carried out coating, coated granule is carried out assay.After the passed examination, packing.
Zhi Bei hydrochloric acid loratadine enteric coated particles as stated above meets the requirement of coherent detection project of regulation in " Chinese Pharmacopoeia 2005 version two ones " ' rules of preparations '.
Claims (9)
1, a kind of hydrochloric acid loratadine enteric-coated formulation composition and preparation method thereof, it is characterized in that: said composition is counted 1:0.1～500 by weight and is formed by hydrochloric acid loratadine crude drug and one or more pharmaceutically acceptable pharmaceutical carrier and/or adjuvants; Specification is 1～100mg.This hydrochloric acid loratadine enteric-coated formulation composition preparation method is to wrap enteric material to make enteric coated tablet and enteric coated granule on the plain sheet of molding or crude granule, and the shaped granule enteric coated capsule of packing into is made enteric coated capsule and maybe will be made the enteric coated micropill common hard capsule of packing into and make enteric-coated pellet capsule.
2, described according to claim 1, it is characterized in that hydrochloric acid loratadine enteric-coated formulation composition, also can further contain carrier and/or adjuvant commonly used in the pharmaceuticals industry, for example enteric material, binding agent, filler, disintegrating agent, lubricant, wetting agent, solubilizing agent, emulsifying agent, plasticizer, fluidizer etc.
3, described according to claim 1 and 2, it is characterized in that enteric material is selected from one or more of the copolymer of acrylate copolymer, methacrylic acid and acrylate or methacrylate, hydroxypropyl CAP, CAP, hypromellose phthalate ester, hydroxypropylmethyl cellulose phthalate, polyvinyl acetate phthalate etc.
4, pharmaceutical carrier according to claim 2 is characterized in that: described binding agent is selected from one or more in the following material: starch, gelatin, sugar (as xylose, lactose etc.), rubber polymer, sodium alginate, hydroxy methocel, methylcellulose, polyvinylpyrrolidone, Polyethylene Glycol, ethyl cellulose, water, wax, alcohol etc.
5, pharmaceutical carrier according to claim 2 is characterized in that: wherein filler can be selected from one or more in the following material: dicalcium phosphate, calcium sulfate, cellulose, microcrystalline Cellulose, hydroxypropyl emthylcellulose, lactose, Kaolin, mannitol, sodium chloride, dried starch etc.
6, pharmaceutical carrier according to claim 2 is characterized in that: wherein disintegrating agent can be selected from one or more in the following material: low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, its derivant of starch etc.
7, pharmaceutical carrier according to claim 2 is characterized in that: wherein lubricant can be selected from one or more in the following material: Pulvis Talci, magnesium stearate, calcium stearate, stearic acid, hydrogenated vegetable oil, Polyethylene Glycol etc.
8, pharmaceutical carrier according to claim 2 is characterized in that: wherein solubilizing agent can be selected one or more of tartaric acid, citric acid, Polyethylene Glycol for use; Emulsifying agent can select for use span80 one or more of span85; Wherein plasticizer can be selected from least a in propylene glycol, glycerol, Polyethylene Glycol, triacetin, acetyl list monoglyceride, phthalic acid ester, the Semen Ricini wet goods.
9, described according to claim 1, it is characterized in that in the described preparation method, granule/micropill can pass through the moulding process of corresponding preparations, the oral enteric preparation that gets final product correspondingly then by existing granulating process preparation such as dry method, wet method, spray drying, centrifugal granulating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102155181A CN101502515A (en) | 2008-09-04 | 2008-09-04 | Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102155181A CN101502515A (en) | 2008-09-04 | 2008-09-04 | Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same |
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| Publication Number | Publication Date |
|---|---|
| CN101502515A true CN101502515A (en) | 2009-08-12 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNA2008102155181A Pending CN101502515A (en) | 2008-09-04 | 2008-09-04 | Hydrochloride loratadine enteric-coated formulation composition and method for preparing the same |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103399101A (en) * | 2013-08-22 | 2013-11-20 | 山东淄博新达制药有限公司 | Method for detecting content of related substances of loratadine hydrochloride capsules |
-
2008
- 2008-09-04 CN CNA2008102155181A patent/CN101502515A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103399101A (en) * | 2013-08-22 | 2013-11-20 | 山东淄博新达制药有限公司 | Method for detecting content of related substances of loratadine hydrochloride capsules |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20090812 |