CN103054857A - Solid preparation taking ramatroban as active ingredient - Google Patents
Solid preparation taking ramatroban as active ingredient Download PDFInfo
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- CN103054857A CN103054857A CN2012105929142A CN201210592914A CN103054857A CN 103054857 A CN103054857 A CN 103054857A CN 2012105929142 A CN2012105929142 A CN 2012105929142A CN 201210592914 A CN201210592914 A CN 201210592914A CN 103054857 A CN103054857 A CN 103054857A
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Abstract
A solid preparation taking ramatroban as an active ingredient is an oral solid preparation which is prepared from ramatroban and pharmaceutically acceptable auxiliary materials through a preparation technology. The solid preparation taking ramatroban as the active ingredient, provided by the invention, has the advantages of stable process quality, controllability, safety and effectiveness. The preparation is mainly used for treating allergic rhinitis clinically.
Description
Technical field
The present invention relates to a kind of solid preparation technique take Leimaquban as active component, belong to medical technical field.
Background technology
Thromboxane (Tx) A2 and precursor thereof---prostaglandin endoperoxide H 2(PGH2) all acts on same receptor, have extremely strong blood vessel, bronchial smooth muscle contraction and platelet activation effect.TxA2 mainly forms in platelet, but also can be produced such as lung, polymorphonuclear leukocyte and people's blood vessel by other cell and tissue.It is believed that TxA2 is thrombotic disease, the important pathophysiological medium of the heart, cerebrovascular and bronchial asthma.Visible TxA2 discharges and increases in cardiovascular disease.The stable catabolite of the TxB2(TxA2 that its bronchoalveolar lavage fluid of patient of asthma of bringing out anaphylactogen contains), prostatosis (PG) D2, PG2 α F and 9 α, 11 β PGF concentration significantly raise.The a large amount of prostanoid of people pulmonary release under the exciting of anaphylactogen of passive sensitization, and then activate a large amount of PGD of people's mastocyte release.
Leimaquban is efficient selectivity TxA2/PGH2 receptor antagonist, can be combined with smooth muscle and hematoblastic TxA2 receptor-specific.The antianaphylaxis of this product is based on suppressing vascular permeability and nasal mucosa hyperreaction and preventing that other inflammatory reaction from occuring.
Summary of the invention
The purpose of this invention is to provide a kind of prolongation and discharge, bioavailability and the blood drug level of energy Effective Raise medicine, simultaneously the Leimaquban solid preparation of taking convenience, few side effects.
The Leimaquban solid preparation, its preparation process is to carry out wet granulation behind the Leimaquban micronization, it is characterized in that the particle diameter of Leimaquban is less than 150um, the particle diameter of preferred Leimaquban is less than 75um, more preferably the particle diameter of Leimaquban is less than 57um, and most preferably the particle diameter of Leimaquban is less than 20um.
Leimaquban solid preparation provided by the invention contains Leimaquban active ingredient and the excipient substance that is fit to make solid preparation, and wherein the percentage by weight of Leimaquban is 25-40%, and the percentage by weight of adjuvant is 60-75%.Every of described Leimaquban solid preparation preferably contains Leimaquban 20-100mg.
Described oral administration solid preparation is oral ordinary tablet, freeze-dried instant sheet, Film coated tablets, enteric coatel tablets, hard capsule, granule, oral cavity disintegration tablet, the effervescent tablet of making by preparation technique with Leimaquban and pharmaceutically acceptable adjuvant.
The oral solid formulation of Leimaquban and pharmaceutically acceptable adjuvant can be filler, binding agent, disintegrating agent, lubricant and coating materials.
The oral solid formulation of Leimaquban and pharmaceutically acceptable adjuvant can be filleies, include but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch or microcrystalline Cellulose;
The oral solid formulation of Leimaquban and pharmaceutically acceptable adjuvant can be binding agents, include but not limited to starch, gelatin dextrin, maltodextrin, sucrose, arabic gum, polyvinylpyrrolidone, various viscosity methylcellulose, low viscosity carboxymethyl cellulose, various viscosity ethyl cellulose, various viscosity polyvinyl alcohol, polyethylene glycol 6000 or the following hyprolose of 50mpaS.
The oral solid formulation of Leimaquban and pharmaceutically acceptable adjuvant can not contain or contain one or more disintegrating agents, include but not limited to pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure wood fiber element, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, methylcellulose or cross-linking sodium carboxymethyl cellulose.
The oral solid formulation of Leimaquban and pharmaceutically acceptable adjuvant can be lubricants, include but not limited to magnesium stearate, calcium stearate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, PEG 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate.
Pharmaceutical preparation of the present invention also comprises wetting agent, is purified water or ethanol etc.The used coating material of the present invention includes but not limited to cellulose and derivant thereof, crylic acid resin, ethene polymers etc.
The specific embodiment:
Following case study on implementation is used for explaining the present invention, but is not limited to this.
Embodiment 1
Make 1000 Leimaquban sheets with the raw material of following weight proportion.
Preparation technology:
1. Leimaquban crude drug micronization, particle diameter is controlled at D90 ≈ 15um, and is for subsequent use;
2. get Leimaquban and lactose, the abundant mix homogeneously of hyprolose.
3. with 50% ethanol water soft material processed, 24 mesh sieves are granulated, 60 ℃ of dryings, 40 mesh sieve granulate.
4. add the abundant mix homogeneously of magnesium stearate, tabletting, and get final product.
Embodiment 2
1. prepare the water-soluble coating materials alcoholic solution of 6% Opadry;
2. get embodiment 1 gained element sheet, pour in the coating pan, start coating pan, and blowing hot-air, at 30-40 ℃ of preheating 10min, and blow plain sheet off adhere on the label medicated powder, evenly spray into coating solution, medicinal liquid is evenly coated on the label, namely get the Leimaquban coated tablet.
Embodiment 3:
Make 1000 Leimaquban sheets with the raw material of following weight ratio.
Preparation technology:
1. Leimaquban crude drug micronization, particle diameter is controlled at D90 ≈ 15um, and is for subsequent use;
2. get Leimaquban and lactose, the abundant mix homogeneously of hyprolose.
3. with 50% ethanol water soft material processed, 24 mesh sieves are granulated, 60 ℃ of dryings, 40 mesh sieve granulate.
4. add the abundant mix homogeneously of magnesium stearate, tabletting, and get final product.
Embodiment 4:
3. prepare the water-soluble coating materials alcoholic solution of 6% Opadry;
4. get embodiment 1 gained element sheet, pour in the coating pan, start coating pan, and blowing hot-air, at 30-40 ℃ of preheating 10min, and blow plain sheet off adhere on the label medicated powder, evenly spray into coating solution, medicinal liquid is evenly coated on the label, namely get the Leimaquban coated tablet.
Embodiment 5: the Leimaquban sheet is alleviated the pharmacological evaluation of sniffle
30 of Cavia porcelluss make sensitinogen with the 10%TDI olive oil solution, the slow collunarium of micro sample adding appliance.Modeling process is divided into sensitization and excited for two phases.The sensitization phase: model group collunarium every day 1 time, continuously 7d.Stimulating phase: since 9d, collunarium is 1 time next day of changing into, excites 4 times, altogether 8d.The modeling time is 15d altogether.
The Cavia porcellus of modeling success is divided into three groups at random, is respectively the blank matched group of model, Chlorate group, Leimaquban sheet group (embodiment 1), each organizes equal gastric infusion, and blank group gavage gives the normal saline of equivalent.More than each treated animal excite rear 1h to give the corresponding treatment medicine at every turn, observe 30min after the administration behind the 2h.Observation item comprises: the number of times that scratches, and the sneeze number of times, the thin nasal discharge degree, each treated animal becomes mold process and typical case's performance.The symptom and sign standards of grading: number of times scratches: gently scratch nose several times, remember 1 minute; Scratching nasal surface section is more than, and scouring everywhere, remembers 2 minutes.Sneeze: l～3 note 1 minute is remembered 2 minutes for 410, and note is 3 minutes more than 11.Thin nasal discharge: flow to prenaris note 1 minute, flow between prenaris and the lower lip and remember 2 minutes, thin nasal discharge is had one's face covered with and is remembered 3 minutes.Between 2 standards, use 0.5 minute mark.More than every stack scoring method that all adopts, it is invalid that total points surpasses 5 minutes and then is considered as Drug therapy.
Result: see Table the rhinitis classical symptoms such as significantly scratching appears in 1 blank model group, sneeze, nasal discharge increase, nasal obstruction.Leimaquban and chlorphenamine maleate group can significantly reduce these sniffles, but the effect of Leimaquban is better than the chlorphenamine maleate group, and prompting Leimaquban sheet is the treatment rhinitis, effective curative of the relevant sniffle of flu.
Animal dead number after table 1 treatment finishes, symptom and sign scoring, typical case's performance
Claims (9)
1. solid preparation take Leimaquban as active component, it is the solid preparation technique by the Leimaquban micronization is made with single dose Leimaquban and pharmaceutically acceptable adjuvant, includes but not limited to following dosage form ordinary tablet, freeze-dried instant sheet, Film coated tablets, enteric coatel tablets, effervescent tablet, oral cavity disintegration tablet, hard capsule, granule.
2. Leimaquban solid preparation as claimed in claim 1 is characterized in that, the particle diameter of Leimaquban is less than 150um, and the particle diameter of preferred Leimaquban is less than 75um, and more preferably the particle diameter of Leimaquban is less than 57um, and most preferably the particle diameter of Leimaquban is less than 20um.
3. such as the described Leimaquban solid preparation of claim 1-2, it is characterized in that the specification of the Leimaquban in described each prescription is per unit dosage 20-100mg.
4. such as the described Leimaquban solid preparation of claim 1-3, it is characterized in that its pharmaceutically acceptable adjuvant can be filler, binding agent, disintegrating agent, lubricant and coating materials.
5. such as the described Leimaquban solid preparation of claim 1-4, it is characterized in that filler includes but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose, hydroxypropyl cellulose.
6. such as the described Leimaquban solid preparation of claim 1-5, it is characterized in that binding agent includes but not limited to hyprolose, gelatin, dextrin, maltodextrin, sucrose, arabic gum, polyvinylpyrrolidone, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, polyethylene glycols or starch.
7. such as the described Leimaquban solid preparation of claim 1-6, it is characterized in that, do not comprise or comprise one or more disintegrating agents and include but not limited to pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure wood fiber element, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, methylcellulose, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose or gas-producing disintegrant.
8. such as the described Leimaquban solid preparation of claim 1-7, it is characterized in that lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, colloidal silica, sodium stearyl fumarate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, PEG 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, leucine, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate.
9. the described preparation of claim 1-8 is for the preparation of the purposes in the treatment of allergic rhinitis medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105929142A CN103054857A (en) | 2012-12-30 | 2012-12-30 | Solid preparation taking ramatroban as active ingredient |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105929142A CN103054857A (en) | 2012-12-30 | 2012-12-30 | Solid preparation taking ramatroban as active ingredient |
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| CN103054857A true CN103054857A (en) | 2013-04-24 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2012105929142A Pending CN103054857A (en) | 2012-12-30 | 2012-12-30 | Solid preparation taking ramatroban as active ingredient |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH11106337A (en) * | 1997-09-30 | 1999-04-20 | Bayer Yakuhin Ltd | Treating agent for poriasis |
| CN1282320A (en) * | 1997-12-24 | 2001-01-31 | 拜尔药品株式会社 | Thermodynamically stable from of (R)-3-[[(4-fluorophenyl) sulphonyl] amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid (ramatroban) |
| CN1827100A (en) * | 2006-04-14 | 2006-09-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition using ramatroban as active ingredient, its preparation method and use |
-
2012
- 2012-12-30 CN CN2012105929142A patent/CN103054857A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH11106337A (en) * | 1997-09-30 | 1999-04-20 | Bayer Yakuhin Ltd | Treating agent for poriasis |
| CN1282320A (en) * | 1997-12-24 | 2001-01-31 | 拜尔药品株式会社 | Thermodynamically stable from of (R)-3-[[(4-fluorophenyl) sulphonyl] amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid (ramatroban) |
| CN1827100A (en) * | 2006-04-14 | 2006-09-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition using ramatroban as active ingredient, its preparation method and use |
Non-Patent Citations (1)
| Title |
|---|
| 张兆旺主编: "《中药药剂学》", 31 January 2003 * |
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Application publication date: 20130424 |