CN101897681A - Method for preparing rifampicin oral preparation - Google Patents
Method for preparing rifampicin oral preparation Download PDFInfo
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- CN101897681A CN101897681A CN200910074499XA CN200910074499A CN101897681A CN 101897681 A CN101897681 A CN 101897681A CN 200910074499X A CN200910074499X A CN 200910074499XA CN 200910074499 A CN200910074499 A CN 200910074499A CN 101897681 A CN101897681 A CN 101897681A
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- rifampicin
- preparation
- chloroform
- oral preparation
- polyethylene glycol
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Abstract
The invention discloses a method for preparing a new rifampicin oral preparation. The method comprises the following steps of: a, dissolving rifampicin serving as a raw material of which the amount is 1/4 to 1/6 that of chloroform with the chloroform, and adding polyethylene glycol, wherein the mass ratio of the polyethylene glycol to the rifampicin is 4-8:1; b, heating the mixture in water bath, and preparing solid dispersions after the chloroform finishes volatilizing; c, preparing the remaining rifampicin serving as the raw material into a soft material; d, pelletizing the soft material by using a 14 to 20-mesh screen, drying the particles, granulating the dried particles, adding an auxiliary material into the particles, and mixing the particles and the auxiliary material to obtain dry particles; and e, filling the solid dispersions and the dry particles into capsules or stamping the solid dispersions and the dry particles into tablets. The dissolution and quality stability of the rifampicin oral preparation are improved effectively.
Description
Technical field
The present invention relates to the preparation method of medicine, specifically a kind of medicament preparation method that can effectively improve the rifampicin oral preparation dissolution.
Background technology
Rifampicin is a kind of oral antibiotic preparation of high-efficiency low-toxicity broad-spectrum antiseptic, is mainly used in treatment lungy.Rifampicin oral preparation mainly includes rifampicin capsules, rifampicin tablet.
Usually the method for preparing rifampicin capsules is to be raw material with the rifampicin, is adjuvant with magnesium stearate, Pulvis Talci, crosses 20 mesh sieves, mix homogeneously, and packing is promptly.The method for preparing the rifampicin tablet is to take by weighing mixing by recipe quantity after supplementary material is sieved respectively, adds 10% starch slurry and makes soft material.Granulate with 14 eye mesh screens, wet grain is in 65 ℃ of left and right sides aeration-dryings.Dried granule adds dried starch, micropowder silica gel, the magnesium stearate of recipe quantity with 16 eye mesh screen granulate, fully mix homogeneously.After mensuration content is qualified, tabletting, packing.These these method technologies are simple, adopt adjuvant few, but the medication medication dissolution are not only low, and unstable.Very easily occur dissolution phenomenon fluctuated during batch process, drug quality is difficult to control.，
Summary of the invention
Purpose of the present invention is exactly the preparation method that a kind of new rifampicin oral preparation will be provided, and in the hope of improving and stable rifampicin oral preparation dissolution, effectively ensures drug quality.
The object of the present invention is achieved like this:
The preparation method of rifampicin oral preparation provided by the present invention, it may further comprise the steps:
A, with the rifampicin material dissolution of chloroform with 1/4-1/6 amount, according to quality than Polyethylene Glycol: rifampicin is 4-8: 1, the adding Polyethylene Glycol;
B, with the heating in water bath of said mixture at 45 ℃-75 ℃, constantly be stirred to simultaneously chloroform volatilization to the greatest extent after, make solid dispersion;
C, remaining rifampicin raw material is crossed the 60-80 order pulverize,, use the 8%-15% gelatinized corn starch, make soft material with the carboxymethyl starch sodium mix homogeneously;
D, soft material is granulated with the 14-20 mesh sieve, after 50 ℃ of-65 ℃ of dryings, 14-20 mesh sieve granulate adds the magnesium stearate adjuvant, always mixes 8-30 minute, makes dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, be filled into capsule or strike out tablet.
Wherein preferred technological parameter is:
In a procedure with chloroform with 1/6 the amount the rifampicin material dissolution;
Polyethylene Glycol: rifampicin is 6: 1;
Bath temperature is 55 ℃-65 ℃ in the b procedure;
Adjuvant in the d procedure also has sodium lauryl sulphate.
Innovation part of the present invention is: utilize solid dispersion technology, make rifampicin be scattered in the macromolecule carrier skeleton of water-soluble material with amorphous state or molecularity, form the amorphous substance of non-crystalline state, effectively improved the dissolution and the quality stability of rifampicin oral preparation.
The consumption proportion of the inventive method Central Plains, adjuvant can be with reference to existing drug standard, and the conventional amount used in the pharmaceutical preparation.
Beneficial effect of the present invention has obtained checking by following contrast test.
Test method:
Adopt four samples of the inventive method preparation and four samples of existing method preparation, respectively 10,20,30, the dissolution of its medicine of 45min sampling and measuring (according to Pharmacopoeia of People's Republic of China 2005 editions (two ones) appendix 73-74 page or leaf), it the results are shown in Table 1.
Table 1:
| 1 | 2 | 3 | 4 | On average | |
| Embodiment 1 | 92.45 | 93.26 | 94.08 | 94.65 | 93.61 |
| Embodiment 2 | 94.25 | 94.50 | 94.48 | 94.59 | 94.54 |
| Embodiment 3 | 91.43 | 92.08 | 92.66 | 92.53 | 92.17 |
| Embodiment 4 | 90.55 | 91.15 | 91.32 | 91.61 | 91.14 |
| Comparative Examples 1 | 79.57 | 80.20 | 80.62 | 81.07 | 80.37 |
| Comparative Examples 2 | 73.10 | 73.21 | 74.22 | 74.53. | 73.77 |
| Comparative Examples 3 | 69.88 | 70.05 | 70.34 | 72.13 | 70.58 |
| Comparative Examples 4 | 72.20 | 72.29 | 72.38 | 72.86 | 72.43 |
By detecting data as can be known: its dissolution of the oral formulations that the inventive method is made is high and stable.
Following examples are used to be described in further detail the inventive method, but it is not to be limitation of the present invention.
The specific embodiment:
Embodiment 1: rifampin (RFP) capsules
Technology preparation:
Rifampicin raw material 150g, Polyethylene Glycol 80g, carboxymethyl starch sodium 20g, magnesium stearate 3g, 10% gelatinized corn starch is an amount of.Make 1000.
Processing step:
A, an amount of with chloroform, with the rifampicin material dissolution of 20g, taking polyethylene glycol 80g is put in the beaker again, and constantly heating in water bath makes its fusing, pours dissolved rifampicin chloroformic solution then into;
B is with the heating in water bath of said mixture at 50 ℃, and the while with the fast cooling of mixture, makes it become solid after constantly being stirred to chloroform volatilization to the greatest extent, in the storing and drying device, crosses the granulation of 40 mesh sieves, makes solid dispersion, and is standby;
C, remaining 130g rifampicin raw material is crossed 80 mesh sieves, with the carboxymethyl starch sodium mix homogeneously, add 10% gelatinized corn starch for preparing in advance, make soft material, 14 orders are granulated;
D, soft material is granulated with the 14-20 mesh sieve, after 55 ℃ of dryings, 14 mesh sieve granulate add the adjuvant magnesium stearate, always mix 30 minutes, make dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, be filled into capsule, make 0.3g/ seed lac wafer.
Embodiment 2: rifampin (RFP) capsules
Technology preparation:
Rifampicin raw material 150g, Polyethylene Glycol 150g, carboxymethyl starch sodium 15g, magnesium stearate 2g, sodium lauryl sulphate 2g, 8% gelatinized corn starch is an amount of.Make 1000.
Processing step:
A, an amount of with chloroform, with the rifampicin material dissolution of 25g, taking polyethylene glycol 150g is put in the beaker again, and constantly heating in water bath makes its fusing, pours dissolved rifampicin chloroformic solution then into;
B, with the heating in water bath of said mixture at 65 ℃, constantly be stirred to simultaneously chloroform volatilization to the greatest extent after, with the fast cooling of mixture, make it become solid, in the storing and drying device, cross 40 mesh sieves and granulate, make solid dispersion, standby;
C, remaining 125g rifampicin raw material is crossed 80 mesh sieves, with the carboxymethyl starch sodium mix homogeneously, add 8% gelatinized corn starch for preparing in advance, make soft material, 14 orders are granulated;
D, with soft material 14 mesh sieves, granulate, after 55 ℃ of dryings, 14 mesh sieve granulate add adjuvant magnesium stearate, sodium lauryl sulphate, always mix 15 minutes, make dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, be filled into capsule, make 0.15g/ seed lac wafer.
Embodiment 3: the rifampicin tablet
Technology preparation:
Rifampicin 150g, Polyethylene Glycol 105g, carboxymethyl starch sodium 10g, magnesium stearate 5g, 15% gelatinized corn starch is an amount of.Make 10000.
Processing step:
A, an amount of with chloroform, with the rifampicin material dissolution of 21g, taking polyethylene glycol 105g is put in the beaker again, and constantly heating in water bath makes its fusing, pours dissolved rifampicin chloroformic solution then into;
B, with the heating in water bath of said mixture at 55 ℃, constantly be stirred to simultaneously chloroform volatilization to the greatest extent after, with the fast cooling of mixture, make it become solid, in the storing and drying device, cross 60 mesh sieves and granulate, make solid dispersion, standby;
C, remaining 129g rifampicin raw material is crossed 100 mesh sieves,, add 12% gelatinized corn starch for preparing in advance, make soft material with the carboxymethyl starch sodium mix homogeneously;
D, with soft material 18 mesh sieves, granulate, after 55 ℃ of dryings, 16 mesh sieve granulate add the adjuvant magnesium stearate, always mix 15 minutes, make dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, make the tablet of 0.1g/ sheet with tablet machine.
Embodiment 4: the rifampicin tablet
Technology preparation:
Rifampicin 150g, Polyethylene Glycol 80g, carboxymethyl starch sodium 15g, magnesium stearate 2g, 15% gelatinized corn starch is an amount of.Make 10000.
Processing step:
A, an amount of with chloroform, with the rifampicin material dissolution of 25g, taking polyethylene glycol 105g is put in the beaker again, and constantly heating in water bath makes its fusing, pours dissolved rifampicin chloroformic solution then into;
B, with the heating in water bath of said mixture at 60 ℃, constantly be stirred to simultaneously chloroform volatilization to the greatest extent after, with the fast cooling of mixture, make it become solid, in the storing and drying device, cross 60 mesh sieves and granulate, make solid dispersion, standby;
C, remaining 125g rifampicin raw material is crossed 100 mesh sieves,, add 10% gelatinized corn starch for preparing in advance, make soft material with the carboxymethyl starch sodium mix homogeneously;
D, with soft material 18 mesh sieves, granulate, after 55 ℃ of dryings, 16 mesh sieve granulate add the adjuvant magnesium stearate, always mix 15 minutes, make dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, make the tablet of 0.1g/ sheet with tablet machine.
Comparative Examples 1: rifampicin capsules
Technology preparation:
Rifampicin 150g, magnesium stearate 4.5g, Pulvis Talci 7g.
Rifampicin, magnesium stearate, Pulvis Talci are crossed 60 mesh sieves, mix homogeneously, and packing is promptly.
Comparative Examples 2: rifampicin capsules
Technology preparation:
Rifampicin 150g, magnesium stearate 3g, sodium lauryl sulphate 3g.
Rifampicin, magnesium stearate, sodium lauryl sulphate are crossed 60 mesh sieves, and mix homogeneously is filled into capsule.
Make 0.3g/ seed lac wafer
Comparative Examples 3 rifampicin tablets
Technology preparation:
Rifampicin 150g, crosslinked carboxymethylstach sodium 23g, magnesium stearate 3g, starch slurry is an amount of.
Preparation technology: with rifampicin, crosslinked carboxymethylstach sodium, magnesium stearate sieve respectively the back take by weighing mixing by recipe quantity, add 10% starch slurry and make soft material.Granulate with 14 eye mesh screens, wet grain is in 65 ℃ of left and right sides aeration-dryings.Dried granule adds crosslinked carboxymethylstach sodium with 16 eye mesh screen granulate, and fully behind the mix homogeneously, the tablet machine tabletting is made the tablet of 0.1g/ sheet.
Comparative Examples 4 rifampicin tablets
Technology preparation:
Rifampicin 150g, crosslinked carboxymethylstach sodium 15g, magnesium stearate 6g, micropowder silica gel 5g, starch slurry is an amount of.
Preparation technology: with rifampicin, crosslinked carboxymethylstach sodium, magnesium stearate sieve respectively the back take by weighing mixing by recipe quantity, add 10% starch slurry and make soft material.Granulate with 14 eye mesh screens, wet grain is in 65 ℃ of left and right sides aeration-dryings.Dried granule adds crosslinked carboxymethylstach sodium, micropowder silica gel with 16 eye mesh screen granulate, and fully behind the mix homogeneously, the tablet machine tabletting is made the tablet of 0.1g/ sheet.
Claims (5)
1. the preparation method of a rifampicin oral preparation, its feature and it may further comprise the steps:
A, with the rifampicin material dissolution of chloroform with 1/6-1/8 amount, according to quality than Polyethylene Glycol: rifampicin is 4-8: 1, the adding Polyethylene Glycol;
B, with the heating in water bath of said mixture at 45 ℃-75 ℃, constantly be stirred to simultaneously chloroform volatilization to the greatest extent after, make solid dispersion;
C, remaining rifampicin raw material is crossed the 60-80 mesh sieve,, use the 8%-15% gelatinized corn starch, make soft material with the carboxymethyl starch sodium mix homogeneously;
D, soft material is granulated with the 14-20 mesh sieve, after 50 ℃ of-65 ℃ of dryings, 14-20 mesh sieve granulate adds the magnesium stearate adjuvant, always mixes 8-30 minute, makes dried granule;
E, with above-mentioned solid dispersion and dried granule, always mix after 10-20 minute, be filled into capsule or strike out tablet.
2. the preparation method of rifampicin oral preparation according to claim 1 is characterized in that in a step operation with the rifampicin material dissolution of chloroform with 1/6 amount.
3. the preparation method of rifampicin oral preparation according to claim 1 and 2, it is characterized in that Polyethylene Glycol in a procedure: rifampicin is 6: 1.
4. the preparation method of rifampicin oral preparation according to claim 1 and 2 is characterized in that bath temperature is 55 ℃-65 ℃ in the b procedure.
5. the preparation method of rifampicin oral preparation according to claim 1 and 2 is characterized in that the adjuvant in the d procedure also has sodium lauryl sulphate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910074499XA CN101897681A (en) | 2009-05-27 | 2009-05-27 | Method for preparing rifampicin oral preparation |
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|---|---|---|---|
| CN200910074499XA CN101897681A (en) | 2009-05-27 | 2009-05-27 | Method for preparing rifampicin oral preparation |
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| CN101897681A true CN101897681A (en) | 2010-12-01 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109106693A (en) * | 2017-06-23 | 2019-01-01 | 重庆华邦制药有限公司 | Rifampicin capsules and preparation method thereof |
| CN112472702A (en) * | 2020-12-14 | 2021-03-12 | 卓和药业集团有限公司 | Pharmaceutical composition for treating pulmonary tuberculosis and preparation method thereof |
-
2009
- 2009-05-27 CN CN200910074499XA patent/CN101897681A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109106693A (en) * | 2017-06-23 | 2019-01-01 | 重庆华邦制药有限公司 | Rifampicin capsules and preparation method thereof |
| CN112472702A (en) * | 2020-12-14 | 2021-03-12 | 卓和药业集团有限公司 | Pharmaceutical composition for treating pulmonary tuberculosis and preparation method thereof |
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Application publication date: 20101201 |