CN1935123A - Carvedilo oral disintegrating tablet - Google Patents
Carvedilo oral disintegrating tablet Download PDFInfo
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- CN1935123A CN1935123A CN 200610096694 CN200610096694A CN1935123A CN 1935123 A CN1935123 A CN 1935123A CN 200610096694 CN200610096694 CN 200610096694 CN 200610096694 A CN200610096694 A CN 200610096694A CN 1935123 A CN1935123 A CN 1935123A
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- China
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- carvedilol
- oral cavity
- silica gel
- correctives
- filler
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Abstract
The present invention relates to a carvedilol oral disintegrant preparation. It contains 5-20% of carvedilol, and the rest is auxiliary material, including mannitol, lactose, avicel, low-substituted hydroxypropyl cellulose, cross-linked carboxymethylcellulose sodium, citric acid, micropowder silica gel, magnesium stearate and essence, etc. Said invention adopts powder direct tabletting process to make preparation.
Description
One, technical field
The present invention relates to a kind of medicine, specifically a kind of carvedilol oral cavity disintegration tablet.
Two, background technology
Carvedilol (Carvedilol), chemistry is by name: (±)-1-(Bian azoles base-4-oxygen base)-3-[2-(neighbour-methoxyl group phenoxy group) ethylamine]-the 2-propanol, molecular formula: C
24H
26N
2O
4, molecular weight: 406.48, structural formula is:
Carvedilol is novel α, beta-blocker, is the antiadrenergic drug medicine with treatment hypertension and chronic heart failure dual function.Known carvedilol is emulative non-selective beta-adrenoceptor antagonists and vasodilation simultaneously.When being used for the treatment of hypertension, the vasodilative effect of carvedilol mainly is by blocking-up α
1-adrenoceptor causes that the receptor, blocking-up activity of carvedilol then can stop reflex tachycardia.This multiple activity of carvedilol is that medicine has the reason that resisting hypertension is renderd a service.In addition, because its antioxidant action in the lipid peroxidation that weakens the oxygen-derived free radicals initiation, carvedilol also can be used for Organoprotective, particularly Cardioprotective.In addition, carvedilol also can be used for treating congestive heart failure.
Because treatment hypertension need be taken medicine for a long time, and medication crowd major part is the old people, the carvedilol formulations that is gone on the market at present is conventional oral formulations, concerning the old man that swallows certain difficulty and child, use but very inconvenient as tablet and capsule, often have gerontal patient or child patient to be unwilling to take these conventional solid preparations, and the complaint medicine is difficult to swallow or block esophagus.When taking above-mentioned conventional oral formulations, also need drink water simultaneously, under the occasion of many hydropenias or inconvenience drinking-water medication just very inconvenient, thereby bring adverse effect to disease treatment.
Three, summary of the invention
The object of the present invention is to provide a kind ofly can not need under the conditions of water drinking disintegrate in the oral cavity rapidly, discharging and have oral solid formulation of good taste and preparation method thereof, and technical problem to be solved is to select adjuvant to make oral cavity disintegration tablet disintegrate rapidly in the oral cavity.
Technical scheme of the present invention is as follows:
This carvedilol oral cavity disintegration tablet comprises principal agent and adjuvant, and described adjuvant comprises filler, disintegrating agent, lubricant and correctives, and the each component percentage by weight is as follows:
Carvedilol 5～20%
Filler 20～80%
Disintegrating agent 10～60%
Micropowder silica gel 0.5～2%
Magnesium stearate 0.1～1%
Correctives 0.01～0.1%.
Preferably:
Carvedilol 8～18%
Filler 40～75%
Disintegrating agent 15～45%
Micropowder silica gel 0.8～1.5%
Magnesium stearate 0.2～1.0%
Correctives 0.01～0.05%.
Further preferred:
Carvedilol 10～15%
Filler 45～65%
Disintegrating agent 20～40%
Micropowder silica gel 1.0～1.5%
Magnesium stearate 0.2～1.0%
Correctives 0.01～0.05%.
Described filler be selected from mannitol or/and lactose or/and microcrystalline Cellulose.Wherein microcrystalline Cellulose also has good mobility and disintegration.
Described disintegrating agent be selected from low-substituted hydroxypropyl cellulose (L-HPC) or/and cross-linking sodium carboxymethyl cellulose (CCNa) or/and crospolyvinylpyrrolidone (CPVP).
Micropowder silica gel and magnesium stearate are lubricant, and wherein the micropowder silica gel good fluidity has the fluidizer effect.
Described correctives is essence or sweeting agent,, cyclamate sweet as Fructus Citri sinensis solid essence, Herba Menthae solid essence, stevioside, A Siba etc.
In above-mentioned composition, also can add 1～3% gas-producing disintegrant citric acid and sodium bicarbonate, meet water generates CO
2Bubble makes the rapid disintegrate of tablet.Citric acid and sodium bicarbonate are equivalent, and total amount satisfies 1～3%.
This carvedilol oral cavity disintegration tablet adopts the preparation method of known direct powder compression, comprises pulverizing, mixing and tabletting, and detailed process is as follows:
Step 1: carvedilol and each adjuvant are crossed 50～100 mesh sieves, standby.
Step 2: take by weighing carvedilol by recipe quantity, take by weighing various adjuvants by accessory formula, and with its abundant mix homogeneously.
Step 3: mixed powder is delivered to tablet machine, carry out tabletting.Relative air humidity control is lower than 40% in the tabletting process.
This carvedilol oral cavity disintegration tablet hardness is 20～40N.In purified water disintegrate become particle diameter less than the particulate time of 710 μ m less than 60 seconds.
The invention has the advantages that:
1, the present invention fills a prescription rationally, disintegrating property is good, enter the mouth no sand type and uncomfortable taste, and sweet, the tool fruit aroma of distinguishing the flavor of.Compliance when having improved patient's medication.
2, preparation technology of the present invention adopts direct powder compression, and process is simple, be easy to control, is fit to industrial scale production.
Four, the specific embodiment
The invention is further illustrated by the following examples:
Example 1
The carvedilol oral cavity disintegration tablet is made up of principal agent and adjuvant, and proportioning is: principal agent 12.5%, adjuvant 87.5%.The each component proportioning is as follows:
| Carvedilol 10.0g |
| Mannitol 40.0g |
| Microcrystalline Cellulose 20.0g |
| Cross-linking sodium carboxymethyl cellulose 5.0g |
| Low-substituted hydroxypropyl cellulose 4.0g |
| Micropowder silica gel 1.0g |
| Magnesium stearate 0.4g |
| Fructus Citri sinensis solid essence 0.01g |
| Make 1000 altogether |
Concrete preparation process is as follows:
Step 1: carvedilol and each adjuvant are crossed 80 mesh sieves, standby.
Step 2: take by weighing carvedilol and various adjuvant by proportional quantity, and with its abundant mix homogeneously.
Step 3: mixed powder is delivered to tablet machine, carry out tabletting, make sheet and heavily be the tablet of 80mg.Relative air humidity control is lower than 40% in the tabletting process.
Manufacture test result: tablet hardness: 30N;
Disintegration in the purified water: 8 seconds;
The intraoral disintegration time limit: disintegrate in 10 seconds;
Mouthfeel: no sand type, it is sweet to distinguish the flavor of, and faint refrigerant sense is arranged, and Fructus Citri sinensis fragrance is arranged.
Example 2:
The carvedilol oral cavity disintegration tablet is made up of principal agent and adjuvant, and proportioning is: principal agent 11.1%, adjuvant 88.9%.The each component proportioning is as follows:
| Carvedilol 10.0g |
| Mannitol 35.0g |
| Lactose 20.0g |
| Microcrystalline Cellulose 15.0g |
| Crospolyvinylpyrrolidone 6.0g |
| Low-substituted hydroxypropyl cellulose 3.0g |
| Micropowder silica gel 1.0g |
| Magnesium stearate 0.25g |
| Fructus Citri sinensis solid essence 0.01g |
| Make 1000 altogether |
The preparation method of this example carvedilol disintegrating tablet is with example 1, and the finished product sheet weighs 90mg.
Manufacture test result: tablet hardness: 35N;
Disintegration in the purified water: 20 seconds;
The intraoral disintegration time limit: disintegrate in 30 seconds;
Mouthfeel: no sand type, it is sweet to distinguish the flavor of, and Fructus Citri sinensis fragrance is arranged.
Example 3:
The carvedilol oral cavity disintegration tablet is made up of principal agent and adjuvant, and proportioning is: principal agent 10%, adjuvant 90%.The each component proportioning is as follows:
| Carvedilol 10.0g |
| Mannitol 20.0g |
| Lactose 40.0g |
| Microcrystalline Cellulose 20.0g |
| Crospolyvinylpyrrolidone 3.0g |
| Low-substituted hydroxypropyl cellulose 4.0g |
| Citric acid 1.0g |
| Sodium bicarbonate 1.0g |
| Micropowder silica gel 1.0g |
| Magnesium stearate 0.25g |
| Fructus Citri sinensis solid essence 0.01g |
| Make 1000 altogether |
The preparation method of this example carvedilol disintegrating tablet is with example 1, and the finished product sheet weighs 100mg.
Manufacture test result: tablet hardness: 35N;
Disintegration in the purified water: 8 seconds;
The intraoral disintegration time limit: disintegrate in 10 seconds;
Mouthfeel: no sand type, little have a numb feeling in the tongue, and it is sweet to distinguish the flavor of, and Fructus Citri sinensis fragrance is arranged.
Claims (5)
1, a kind of carvedilol oral cavity disintegration tablet, it is characterized in that: each component has following percentage by weight:
Carvedilol 5～20%
Filler 20～80%
Disintegrating agent 10～60%
Micropowder silica gel 0.5～2%
Magnesium stearate 0.1～1%
Correctives 0.01～0.1%.
2, carvedilol oral cavity disintegration tablet according to claim 1 is characterized in that:
Carvedilol 8～18%
Filler 40～75%
Disintegrating agent 15～45%
Micropowder silica gel 0.8～1.5%
Magnesium stearate 0.2～1.0%
Correctives 0.01～0.05%.
3, carvedilol oral cavity disintegration tablet according to claim 1 and 2 is characterized in that:
Carvedilol 10～15%
Filler 45～65%
Disintegrating agent 20～40%
Micropowder silica gel 1.0～1.5%
Magnesium stearate 0.2～1.0%
Correctives 0.01～0.05%.
4, carvedilol mouth according to claim 3 collapses card, it is characterized in that: 1～3% citric acid and sodium bicarbonate are arranged in the compositions.
5, according to claim 1 or 2 or 4 described carvedilol oral cavity disintegration tablets, it is characterized in that: filler be selected from mannitol or/and lactose or/and microcrystalline Cellulose; Disintegrating agent be selected from low-substituted hydroxypropyl cellulose or/and cross-linking sodium carboxymethyl cellulose or/and crospolyvinylpyrrolidone; Correctives is that essence is or/and sweeting agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610096694 CN1935123A (en) | 2006-10-18 | 2006-10-18 | Carvedilo oral disintegrating tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610096694 CN1935123A (en) | 2006-10-18 | 2006-10-18 | Carvedilo oral disintegrating tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1935123A true CN1935123A (en) | 2007-03-28 |
Family
ID=37952990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610096694 Pending CN1935123A (en) | 2006-10-18 | 2006-10-18 | Carvedilo oral disintegrating tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1935123A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103845297A (en) * | 2012-11-29 | 2014-06-11 | 倪伟华 | Carvedilol orally disintegrating tablet |
| CN113995728A (en) * | 2020-07-28 | 2022-02-01 | 江苏康缘药业股份有限公司 | Pharmaceutical composition and preparation method thereof |
-
2006
- 2006-10-18 CN CN 200610096694 patent/CN1935123A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103845297A (en) * | 2012-11-29 | 2014-06-11 | 倪伟华 | Carvedilol orally disintegrating tablet |
| CN113995728A (en) * | 2020-07-28 | 2022-02-01 | 江苏康缘药业股份有限公司 | Pharmaceutical composition and preparation method thereof |
| CN113995728B (en) * | 2020-07-28 | 2023-03-14 | 江苏康缘药业股份有限公司 | Medicinal composition and preparation method thereof |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Open date: 20070328 |