CN105617352A - Stable telavancin pharmaceutical composition - Google Patents
Stable telavancin pharmaceutical composition Download PDFInfo
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- CN105617352A CN105617352A CN201410632975.6A CN201410632975A CN105617352A CN 105617352 A CN105617352 A CN 105617352A CN 201410632975 A CN201410632975 A CN 201410632975A CN 105617352 A CN105617352 A CN 105617352A
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- lawan star
- cross
- lawan
- star
- sodium carboxymethyl
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/14—Peptides containing saccharide radicals; Derivatives thereof, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin
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- Gastroenterology & Hepatology (AREA)
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Abstract
The present invention discloses a stable telavancin pharmaceutical composition, which is characterized in that the components in the formula for preparing 1000 tablets of the stable telavancin pharmaceutical composition comprise 375-750 g of telavancin, 70-140 g of microcrystalline cellulose, 0.5-1 g of micro-powder silica gel, 50-100 g of cross-linked sodium carboxymethyl cellulose, and a proper amount of a 10% pre-gelatinized starch solution. The present invention further relates to a preparation method of the telavancin tablets. According to the present invention, the stable telavancin pharmaceutical composition prepared by using the prescription and the preparation method has characteristics of good dissolution, high bioavailability, and good treatment effect.
Description
Technical field
The present invention relates to a kind of stable Te Lawan star pharmaceutical composition and preparation method thereof.
Background technology
Te Lawan star (telavancin) is a kind of LG antibiotic, within 2009, it is used for treating the microbial complexity skin of Grain-positive and skin structure infection by FDA approval, this time expands indication and be used for the Nosocomial bacterial pneumonia that staphylococcus aureus causes.
By the research to prior art, Te Lawan star bioavailability in human body is low is still puzzlement people's urgent problem. It addition, suitable preparation method and process conditions, the kind of filler and consumption are most important to the result of extraction of tablet, mobility. Conventional filler lactose, microcrystalline Cellulose, starch etc., conventional disintegrating agent has microcrystalline Cellulose, carboxymethyl starch sodium etc. But, how obtaining more excellent dissolution rate by dissolution adjustment formula and the technique adjustment of described Te Lawan star, prior art does not provide further prompting, in view of this, this invention of special proposition.
Summary of the invention
It is contemplated that overcome the problems such as the mobility of existing Te Lawan star pharmaceutical composition is bad, dissolution is low, change the dissolution of Te Lawan star and the shortcoming that bioavailability is low, improve curative effect. According to existing adjuvant and working condition, ensureing that there is relatively low production cost and simple preparation technology, have been adapted under the premise of large-scale industrial production, it is necessary to work out a kind of suitable prescription composition and preparation technology, make Te Lawan star have good bioavailability.
Therefore, it is an object of the invention to provide a kind of Te Lawan star sheet, it is characterised in that the formula making 1000 is composed as follows:
Te Lawan star 375-750g
Cross-linking sodium carboxymethyl cellulose 50-100g
Microcrystalline Cellulose 70-140g
Micropowder silica gel 0.5-1g
10% pregelatinized Starch solution is appropriate.
Preferably, to make the formula of 1000 composed as follows for the Te Lawan star of the present invention:
Te Lawan star 375g
Cross-linking sodium carboxymethyl cellulose 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate.
In the present invention, microcrystalline Cellulose does filler, and pregelatinized Starch plays dual parts bonding and disintegrate, promotes disintegration of tablet.
By prescription screening, the present invention determines that the group of microcrystalline Cellulose and pregelatinized Starch joins application, prepared Te Lawan star Dissolution of Tablet is better, and determines the optimizing prescriptions of the present invention through adjuvant screening test. Under prescription screening test and result are shown in:
From above result of the test: prescription 1 dissolution trend is better than other prescription.
Another object of the present invention is to the preparation method that Te Lawan star pharmaceutical composition of the present invention is provided, it is characterised in that the method comprises the steps:
1) respectively Te Lawan star, cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose are dried, pulverize, sieve, respectively obtain Te Lawan star powder, cross-linking sodium carboxymethyl cellulose powder and microcrystalline Cellulose powder;
2) take the Te Lawan star of recipe quantity, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose, mix homogeneously, be subsequently adding 10% pregelatinized Starch solution and make soft material in right amount, cross 40 eye mesh screens and granulate, obtain Te Lawan star wet granular;
3) above-mentioned Te Lawan star wet granular is dried to moisture less than 5% under 60 DEG C of conditions, obtains the dry granule of Te Lawan star;
4) the above-mentioned dry granule of Te Lawan star is crossed 40 eye mesh screen granulate, be subsequently adding lubricant, mix homogeneously, after quality examination is qualified, tabletting, i.e. get Te Lawan star tablet.
In above-mentioned preparation method, sieving of step 1) was 100 mesh sieves.
Preferably, screening in order that obtain and have the material of more uniform granularity. This is smoothed out important meaning to what drug quality and preparation produced. The operation of the unit such as mixing, granulation, tabletting is sieved on degree of mixing, particle mobility, etc. have obvious impact. Remix after former, adjuvant is pulverized, sieved by the present invention, former, adjuvant can be made to be evenly distributed, what mix is more uniform, and in the present invention, employing microcrystalline Cellulose and major ingredient remix after pulverizing respectively, can make degree of mixing, the mobility of particle is significantly improved so that medicine better plays drug effect.
Additionally, heating can cause the degraded of Te Lawan star, accordingly, it is determined that the baking temperature being suitable for is critically important. Te Lawan star granule is dried to moisture less than 5% by the present invention under 60 DEG C of conditions, obtains the dry granule of Te Lawan star, not only avoid the heating degraded to Te Lawan star, and drying effect is good.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, it should be understood that the non-scope being only limitted to these embodiments of the scope of the present invention.
Embodiment 1
The formula that Te Lawan star makes 1000 is composed as follows:
Te Lawan star 375g
Cross-linking sodium carboxymethyl cellulose 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate
Preparation method
1) respectively Te Lawan star, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose dried, pulverize, cross 100 mesh sieves, respectively obtain Te Lawan star powder, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose powder;
2) take the Te Lawan star of recipe quantity, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose, mix homogeneously, be subsequently adding 10% pregelatinized Starch solution and make soft material in right amount, cross 40 eye mesh screens and granulate, obtain Te Lawan star wet granular;
3) above-mentioned Te Lawan star wet granular is dried to moisture less than 5% under 60 DEG C of conditions, obtains the dry granule of Te Lawan star
4) the above-mentioned dry granule of Te Lawan star is crossed 40 eye mesh screen granulate, be subsequently adding lubricant, mix homogeneously, after quality examination is qualified, tabletting, i.e. get Te Lawan star tablet.
Embodiment 2
The formula that Te Lawan star makes 1000 is composed as follows:
Te Lawan star 750g
Cross-linking sodium carboxymethyl cellulose 100g
Microcrystalline Cellulose 140g
Micropowder silica gel 1g
10% pregelatinized Starch solution is appropriate
Preparation method
1) respectively Te Lawan star, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose dried, pulverize, cross 100 mesh sieves, respectively obtain Te Lawan star powder and microcrystalline Cellulose powder;
2) take the Te Lawan star of recipe quantity, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose, mix homogeneously, be subsequently adding 10% pregelatinized Starch solution and make soft material in right amount, cross 40 eye mesh screens and granulate, obtain Te Lawan star wet granular;
3) above-mentioned Te Lawan star wet granular is dried to moisture less than 5% under 60 DEG C of conditions, obtains the dry granule of Te Lawan star;
4) the above-mentioned dry granule of Te Lawan star is crossed 40 eye mesh screen granulate, be subsequently adding lubricant, mix homogeneously, after quality examination is qualified, tabletting, i.e. get Te Lawan star tablet.
The beneficial effect of the Te Lawan star tablet of the present invention is described below by way of test example, comparative example.
The study on the stability of [test example 1] product of the present invention
The Te Lawan star tablet adopting prescription 1 of the present invention and preparation method to prepare, tests through study of pharmacy influence factor, under investigation result is shown in:
Conclusion: factors influencing under high temperature, high humidity, illumination condition, product appearance of the present invention observes unchanged, disintegration time and content is all stable.
Claims (5)
1. Te Lawan star pharmaceutical composition one kind stable, it is characterised in that the formula making 1000 is composed as follows:
Te Lawan star 375-750g
Cross-linking sodium carboxymethyl cellulose 50-100g
Microcrystalline Cellulose 70-140g
Micropowder silica gel 0.5-1g
10% pregelatinized Starch solution is appropriate.
2. Te Lawan star pharmaceutical composition according to claim 1, it is characterised in that the formula making 1000 is composed as follows:
Te Lawan star 375g
Cross-linking sodium carboxymethyl cellulose 50g
Microcrystalline Cellulose 70g
Micropowder silica gel 0.5g
10% pregelatinized Starch solution is appropriate.
3. Te Lawan star pharmaceutical composition according to claim 1, it is characterised in that the formula making 1000 is composed as follows:
Te Lawan star 750g
Cross-linking sodium carboxymethyl cellulose 100g
Microcrystalline Cellulose 140g
Micropowder silica gel 1g
10% pregelatinized Starch solution is appropriate.
4. the preparation method of the Te Lawan star described in claim 1 or 2 or 3, it is characterised in that described preparation method comprises the steps:
1) respectively Te Lawan star, cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose are dried, pulverize, sieve, respectively obtain Te Lawan star powder, cross-linking sodium carboxymethyl cellulose powder and microcrystalline Cellulose powder;
2) take the Te Lawan star of recipe quantity, cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose, mix homogeneously, be subsequently adding 10% pregelatinized Starch solution and make soft material in right amount, cross 40 eye mesh screens and granulate, obtain Te Lawan star wet granular;
3) above-mentioned Te Lawan star wet granular is dried to moisture less than 5% under 60 DEG C of conditions, obtains the dry granule of Te Lawan star;
4) the above-mentioned dry granule of Te Lawan star is crossed 40 eye mesh screen granulate, be subsequently adding lubricant, mix homogeneously, after quality examination is qualified, tabletting, i.e. get Te Lawan star sheet.
5. preparation method according to claim 4, it is characterised in that sieving in step 1) referred to 100 mesh sieves.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410632975.6A CN105617352A (en) | 2014-11-12 | 2014-11-12 | Stable telavancin pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410632975.6A CN105617352A (en) | 2014-11-12 | 2014-11-12 | Stable telavancin pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105617352A true CN105617352A (en) | 2016-06-01 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410632975.6A Pending CN105617352A (en) | 2014-11-12 | 2014-11-12 | Stable telavancin pharmaceutical composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105617352A (en) |
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2014
- 2014-11-12 CN CN201410632975.6A patent/CN105617352A/en active Pending
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Application publication date: 20160601 |