CN115400136A - Clarithromycin solid preparation and preparation method thereof - Google Patents
Clarithromycin solid preparation and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a clarithromycin solid preparation and a preparation method thereof, wherein the solid preparation comprises clarithromycin with the particle size distribution within the range of 80-120 meshes, an adsorbent, a diluent, a disintegrant and a lubricant. The adsorbent is PROSOLV, the porosity of the PROSOLV has high load capacity and can adsorb clarithromycin, the diluent is one or more of microcrystalline cellulose, pre-crosslinked starch, lactose and sorbitol, and the clarithromycin and the PROSOLV (SMCC 90 LM) are mixed according to a ratio of 2. Meanwhile, the porosity of the PROSOLV has high loading capacity, so that the clarithromycin can be completely adsorbed in the gaps of the PROSOLV, the PROSOLV has good moisture absorption resistance, and the 90LM is a low-moisture model, so that the condition that the impurity I grows due to the increase of moisture in a sample is reduced.
Description
Technical Field
The invention relates to the technical field of medicines, in particular to a clarithromycin solid preparation and a preparation method thereof.
Background
Clarithromycin is a derivative of erythromycin, also called 6-O-methylerythromycin, belongs to 14-membered macrolide antibiotics, has a molecular formula of C38H69NO13, and has a structural formula shown in the specification. The character is white or white-like crystalline powder, which is dissolved in acetone or ethyl acetate, slightly soluble in methanol or ethanol, insoluble in water, BCS is classified as IV.
Clarithromycin belongs to the second generation macrolide antibiotics, and has wide antibacterial spectrum and strong antibacterial activity. At present, the clarithromycin oral solid preparation on the domestic market mainly comprises five dosage forms of a clarithromycin tablet, a dispersible tablet, a capsule, a dry suspension and a sustained release tablet, but only three dosage forms of the clarithromycin tablet, the sustained release tablet and the dry suspension exist in a reference preparation catalogue published by the state.
The national pushes forward the evaluation work of the consistency of the imitation drugs, and guarantees the safety and the effectiveness of the drugs, and the key of the quality evaluation of the solid oral imitation preparation lies in two major aspects, namely consistent quality and consistent curative effect. In the aspect of quality consistency evaluation, the most concerned about measuring whether the imitation drugs are consistent with the reference preparation is the consistency of dosage forms, the consistency of dissolution curves and the scientific and reasonable impurity control.
The inventor researches on clarithromycin to find that the main degradation impurity of the clarithromycin oral solid preparation is impurity I, the impurity I is 3-O-descladinosyl-6-O-methylerythromycin A, the impurity I is a hydrolysis product of clarithromycin, the solid condition is mainly influenced by temperature and is related to the moisture of a sample, the addition of an acidic auxiliary material in the preparation process also causes the increase of the impurity I, and the dissolution curve is related to the particle size distribution of API.
CN101002790B discloses a clarithromycin sustained release tablet and a preparation method thereof, wherein citric acid is added in a formula as a pH regulator, which is more beneficial to the absorption of drugs by human intestines and stomach, but the impurity condition of the preparation is not explained, and the addition of an acidic auxiliary material is very unfavorable for controlling the impurities of the product.
CN101502492B, CN101912613B and CN103315964B all disclose a taste masking preparation and a preparation method thereof, the taste problem which is difficult to tolerate in the process of oral administration is solved by adopting acrylic resin, but the acrylic resin is an acidic adjuvant which can cause the increase of impurity I in the process of placing the product, and the stability condition of the product is not studied in the patent.
CN102178659B and CN103239406B both disclose a clarithromycin enteric-coated preparation and a preparation method thereof, and dosage forms are inconsistent with reference preparations, and biological equivalence conditions are not described, so that the consistency of curative effects and the reference preparations cannot be ensured.
Therefore, there is an urgent need to provide a clarithromycin preparation with the advantages of good stability, controllable impurities, high safety, high bioavailability, etc.
Therefore, a solid preparation of clarithromycin and a method for preparing the same have been proposed to solve the above problems.
Disclosure of Invention
In order to overcome the above-mentioned drawbacks of the prior art, embodiments of the present invention provide a clarithromycin solid preparation and a method for preparing the same, which solve the above-mentioned problems of the prior art.
In order to achieve the purpose, the invention provides the following technical scheme: a clarithromycin solid preparation and a preparation method thereof comprise a solid preparation, wherein the solid preparation comprises clarithromycin with the particle size distribution within the range of 80-120 meshes, an adsorbent, a diluent, a disintegrant and a lubricant.
In the invention, clarithromycin and PROSOLV (SMCC 90 LM) are mixed according to the proportion of 2. Meanwhile, the porosity of the PROSOLV has high load capacity, so that the clarithromycin can be completely adsorbed in the gaps of the PROSOLV, the PROSOLV has good moisture resistance and absorption performance, and the 90LM is a low-moisture model, so that the condition that the impurity I is increased due to the increase of moisture in a sample is reduced.
In a preferred embodiment, the adsorbent is prosollv (SMCC 90 LM), the porosity of which has a high loading capacity and can adsorb clarithromycin, wherein prosollv is silicified microcrystalline cellulose.
In a preferred embodiment, the diluent is one or more of microcrystalline cellulose, pregelatinized starch, lactose, and sorbitol.
In a preferred embodiment, the disintegrant is one or more of croscarmellose sodium, sodium carboxymethyl starch, low substituted hydroxypropyl cellulose, and crospovidone.
In a preferred embodiment, the lubricant is one or more of stearic acid, magnesium stearate and talcum powder.
In a preferred embodiment, the solid preparation can be prepared by a powder direct compression process and a dry granulation and tabletting process.
In a preferred embodiment, the solid preparation is prepared by a powder direct compression process, and the preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM), grinding, and sieving with 80-120 mesh sieve;
s2: sieving the rest adjuvants with 60 mesh sieve;
s3: weighing a dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the formula amount 1 and a diluent and a disintegrant in the formula amount 2, and uniformly mixing;
s4: weighing the lubricant in the formula amount 2, and totally mixing the lubricant with the material obtained in the step S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
The invention has the technical effects and advantages that:
the clarithromycin and the PROSOLV (SMCC 90 LM) are mixed according to the proportion of 2. Meanwhile, the porosity of the PROSOLV has high loading capacity, so that the clarithromycin can be completely adsorbed in the gaps of the PROSOLV, the PROSOLV has good moisture absorption resistance, and the 90LM is a low-moisture model, so that the condition that the impurity I grows due to the increase of moisture in a sample is reduced.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all embodiments. All other embodiments, which can be obtained by a person skilled in the art without making any creative effort based on the embodiments in the present invention, belong to the protection scope of the present invention.
Example 1: a clarithromycin solid preparation and a preparation method thereof, S1: mixing clarithromycin and PROSOLV (SMCC 90 LM), wherein PROSOLV is silicified microcrystalline cellulose, grinding, and sieving with 80-120 mesh sieve;
s2: sieving the rest adjuvants with 60 mesh sieve;
s3: weighing a dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the formula amount 1 and a diluent and a disintegrant in the formula amount 2, and uniformly mixing;
s4: weighing the lubricant in the formula amount 2, and totally mixing the lubricant with the material obtained in the step S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
The second embodiment:
preparation of Clarithromycin tablets by powder direct compression process:
the prescription composition is as follows (made into 1000 pieces in total):
the preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the ratio of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve for later use;
s3: weighing 375g of dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the S1 step, 92.5g of pre-crosslinked starch in the S2 step and 25g of croscarmellose sodium, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2 and the material obtained in the step S3, and mixing for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (5) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
Example three:
preparing a Clarithromycin tablet by a powder direct pressing process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weight (g) |
| Clarithromycin | 250 |
| PROSOLV(SMCC 90LM) | 125 |
| Pre-crosslinked starch | 92.5 |
| Croscarmellose sodium | 25 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the proportion of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve for later use;
s3: weighing 375g of dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the S1 step, 92.5g of pre-crosslinked starch in the S2 step and 25g of croscarmellose sodium, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2, and totally mixing the magnesium stearate with the material obtained in the step of S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
Example four:
preparing a Clarithromycin tablet by a powder direct pressing process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weights (g) |
| Clarithromycin | 250 |
| PROSOLV(SMCC 90LM) | 125 |
| Pre-crosslinked starch | 92.5 |
| Croscarmellose sodium | 25 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the ratio of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve for later use;
s3: weighing 375g of the clarithromycin and PROSOLV (SMCC 90 LM) dry mixture obtained in the S1 step, 92.5g of the pre-crosslinked starch in the S2 step and 25g of croscarmellose sodium, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2, and totally mixing the magnesium stearate with the material obtained in the step of S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (5) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
Example five:
preparing a Clarithromycin tablet by a dry granulation process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weights (g) |
| Clarithromycin | 250 |
| PROSOLV(SMCC 90LM) | 125 |
| Pre-crosslinked starch | 82.5 |
| Croscarmellose sodium | 30 |
| Stearic acid | 5 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the proportion of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve, and sieving the stearic acid with a 20-mesh sieve for later use;
s3: weighing 375g of dry mixture of clarithromycin obtained in the S1 step and PROSOLV (SMCC 90 LM), 82.5g of pre-crosslinked starch in 2) and 15g of croscarmellose sodium, and uniformly mixing;
s4: weighing 5g of stearic acid in the step S2 and uniformly mixing the stearic acid with the material obtained in the step 3);
s5: carrying out dry pressing and crushing on the material obtained in the step S4 by using a dry granulating machine, sieving the material by using a 20-mesh sieve, and then mixing the material with 7.5g of magnesium stearate in the step 2) for 10 minutes to obtain uniformly mixed intermediate granules;
s6: and (3) tabletting the intermediate granules obtained in the step (S5) by using a tabletting machine according to the weight of 500mg tablets to obtain the dry-granulated Clarithromycin tablets.
Comparative example one:
preparing a Clarithromycin tablet by a powder direct pressing process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weight (g) |
| Clarithromycin | 250 |
| Microcrystalline cellulose | 125 |
| Pre-crosslinked starch | 92.5 |
| Croscarmellose sodium | 25 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: sieving clarithromycin with 80-120 mesh sieve;
s2: sieving microcrystalline cellulose, pre-crosslinked starch, croscarmellose sodium and magnesium stearate with a 80-mesh sieve for later use;
s3: weighing 250g of clarithromycin obtained in the S1 step, 125g of microcrystalline cellulose, 92.5g of pre-crosslinked starch and 25g of croscarmellose sodium in the S2 step, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2 and the material obtained in the step S3, and mixing for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (5) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the Clarithromycin tablets.
Comparative example two:
preparation of Clarithromycin tablets by powder direct compression process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weight (g) |
| Clarithromycin | 250 |
| PROSOLV(SMCC 90LM) | 125 |
| Pre-crosslinked starch | 92.5 |
| Croscarmellose sodium | 25 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the proportion of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve for later use;
s3: weighing 375g of dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the S1 step, 92.5g of pre-crosslinked starch in the S2 step and 25g of croscarmellose sodium, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2, and totally mixing the magnesium stearate with the material obtained in the step of S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the Clarithromycin tablets.
Comparative example three:
preparation of Clarithromycin tablets by powder direct compression process:
the prescription composition is as follows (made into 1000 pieces in total):
| raw and auxiliary materials | Weight (g) |
| Clarithromycin | 250 |
| PROSOLV(SMCC 90LM) | 125 |
| Pre-crosslinked starch | 92.5 |
| Croscarmellose sodium | 25 |
| Magnesium stearate | 7.5 |
The preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV (SMCC 90 LM) according to the ratio of 2;
s2: sieving the pre-crosslinked starch, the croscarmellose sodium and the magnesium stearate with a 60-mesh sieve for later use;
s3: weighing 375g of dry mixture of clarithromycin and PROSOLV (SMCC 90 LM) obtained in the S1 step, 92.5g of pre-crosslinked starch in the S2 step and 25g of croscarmellose sodium, and uniformly mixing;
s4: weighing magnesium stearate in the step of 7.5gS2 and the material obtained in the step S3, and mixing for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the Clarithromycin tablets.
Test example 1
Stability survey
Taking a reference preparation
The samples prepared in examples 1-2 and comparative example 1 were continuously stored for 6 months in an environment of 40 ℃. + -. 2 ℃,75% RH. + -.5% RH, and the impurity I contents (%) of the Clarithromycin tablets were measured for 0 day and 6 months by HPLC, and the results were as follows:
from the above data, it can be seen that the samples prepared in examples 1-2 of the present invention all contain the adsorbent (prosoll), and the measured impurity I increases slowly at the accelerated 6 months, even better than the reference formulation; whereas comparative example 1, which contains no adsorbent, showed a significant increase in impurity I at 6 months of acceleration. Indicating that the porosity of prosollv has high loading capacity, allowing clarithromycin to be completely adsorbed in the voids of prosollv, having good anti-hygroscopicity, and 90LM is a low-moisture type, thereby reducing the increase of impurity I caused by the increase of moisture in the sample.
Test example 2
Dissolution determination
Taking the product, and performing dissolution determination method (Chinese pharmacopoeia 2020 edition two part appendix X C secondMethod), 900ml of phosphate buffer solution with pH6.8 is used as dissolution medium, the rotating speed is 50 revolutions per minute, the method is operated, a proper amount of dissolution liquid is taken after 5min, 10min, 15min, 30min, 45min, 60min, 90min and 120min, the dissolution medium with the same temperature and volume is supplemented at the same time, and the filtration is carried out, and the subsequent filtrate is taken as the test solution. Determination of samples of examples 1-2 and comparative examples 2-3 and reference formulations
Dissolution (%) of (a), the experimental results are as follows:
from the analysis of the results in the table above, it can be seen that: the particle size of the clarithromycin raw material has a remarkable influence on the dissolution rate of the preparation, and the inventor finds that the dissolution curve of the clarithromycin tablet in the particle size range (80-120 meshes) of the invention is consistent with that of a reference preparation, and the F2 of the samples in examples 1-3 are 71.87, 75.60 and 74.22 respectively, because the particle size of API is closer to that of PROSOLV (SMCC 90 LM) in the particle size range of 80-120 meshes, the API can be completely adsorbed in the gaps of the PROSOLV, the in-vitro dissolution rate can be greatly improved, and the bioavailability can be improved. Comparative example 2 increased the particle size of clarithromycin, slowed the dissolution, and was not similar to the dissolution profile of the reference formulation, with an F2 of 47.92. Comparative example 3 reduced the particle size of clarithromycin, which also slowed the dissolution, which was not similar to the dissolution profile of the reference formulation, with an F2 of 49.86.
The above description is only for the purpose of illustrating the preferred embodiments of the present invention and is not to be construed as limiting the present invention, and any modifications, equivalents, improvements and the like made within the spirit and principle of the present invention should be included in the scope of the present invention.
Claims (7)
1. A clarithromycin solid preparation, characterized in that; comprises a solid preparation, wherein the solid preparation comprises clarithromycin with the particle size distribution within the range of 80-120 meshes, an adsorbent, a diluent, a disintegrant and a lubricant.
2. The solid preparation of clarithromycin according to claim 1, wherein: the adsorbent is PROSOLV, and the porosity of the PROSOLV has high loading capacity and can adsorb clarithromycin.
3. A clarithromycin solid according to claim 1, characterized in that: the diluent is one or more of microcrystalline cellulose, pre-crosslinked starch, lactose and sorbitol.
4. The solid preparation of clarithromycin according to claim 1, wherein: the disintegrating agent is one or more of croscarmellose sodium, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose and crospovidone.
5. The solid preparation of clarithromycin according to claim 1, wherein: the lubricant is one or more of stearic acid, magnesium stearate and talcum powder.
6. The solid preparation of clarithromycin according to claim 1, wherein: the solid preparation can be prepared by a powder direct compression process and a dry granulation and tabletting process.
7. A preparation method of a clarithromycin solid preparation is characterized by comprising the following steps: the solid preparation is prepared by a powder direct-pressing process, and the preparation process comprises the following steps:
s1: mixing clarithromycin and PROSOLV, grinding with 80-120 mesh sieve;
s2: sieving the rest adjuvants with 60 mesh sieve;
s3: weighing the dry mixture of clarithromycin and PROSOLV obtained in the prescription amount 1 and the diluent and the disintegrant in the prescription amount 2, and uniformly mixing;
s4: weighing the lubricant in the formula amount 2, and totally mixing the lubricant with the material obtained in the step S3 for 10 minutes to obtain uniformly mixed intermediate particles;
s5: and (4) tabletting the intermediate granules obtained in the step (S4) by using a tabletting machine according to the weight of 500mg tablets to obtain the powder direct-compression clarithromycin tablets.
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| CN115400136B (en) | 2023-10-03 |
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