CN112402381B - Clindamycin palmitate hydrochloride particle composition and preparation method thereof - Google Patents
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Abstract
The invention relates to a clindamycin palmitate hydrochloride particle composition. It is characterized by comprising: 1) 1-10% clindamycin palmitate hydrochloride; 2) 70-95% of sucrose, wherein the granularity of the sucrose is as follows: not more than 20% of more than 600 μm and not more than 20% of less than 180 μm. According to the invention, through a large number of researches, sucrose with a certain particle size range is used as a filler, and the problem of content uniformity of clindamycin palmitate hydrochloride particles is solved unexpectedly. However, the use of ground sucrose having a particle size close to that of the drug as a filler is disadvantageous in terms of uniformity.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and relates to a clindamycin palmitate hydrochloride particle composition and a preparation method thereof.
Background
The clindamycin palmitate hydrochloride is a prodrug of clindamycin, after the clindamycin palmitate hydrochloride is orally taken, free clindamycin can be quickly hydrolyzed to take effect and be completely absorbed, and clindamycin has higher antibacterial effect which is 2~8 times of the lincomycin. Clindamycin has antibacterial activity against many gram-positive aerobic bacteria (excluding enterococci), streptococcus, bacillus, staphylococcus, and also against many anaerobic bacilli, chlamydia, mycoplasma, plasmodium, and equine protozoa. As a bactericidal drug, the product mainly inhibits the synthesis of bacterial protein, and has the inhibiting effect on the amino activation, transfer and combination sites, the action point is at the ribosome 50s subunit, and the action mechanism is the same as that of erythromycin. The product is mainly used for treating septicemia caused by sensitive bacteria, bacterial endocarditis, pneumonia, respiratory tract infection, soft tissue infection, bone joint infection, ear infection and urogenital system infection in clinic, and especially bacterial infection which is resistant to penicillin and erythromycin and sensitive to the medicine; vulvovaginitis, salpingitis, pelvic peritonitis, endometritis and pelvic postoperative infection caused by anaerobic bacteria.
The content of active ingredients in the clindamycin palmitate hydrochloride granules is low, about 1-10%, so that the content uniformity of the clindamycin palmitate hydrochloride granules is a challenge for a preparation formula and a preparation process for low-dose medicines.
The general method for solving the problem of uniform drug content comprises the following steps: 1) The mixing time is prolonged as much as possible; 2) Wet mixing granulation is adopted, and the mixing granulation time is prolonged as much as possible; 3) Preparing a solid dispersion; 4) Adopts a co-crushing and co-grinding method. 5) The particle size difference of the auxiliary materials and the raw material medicines is reduced, and the mixing and granulating uniformity is improved. However, these methods do not solve the problem of uniform content for the clindamycin palmitate hydrochloride particles.
Disclosure of Invention
The invention aims to provide a stable and uniform-content clindamycin palmitate hydrochloride particle composition.
In order to solve the technical problems, the invention discloses a stable and uniform clindamycin palmitate hydrochloride particle composition, which is characterized by comprising the following components: 1) 1 to 10% clindamycin palmitate hydrochloride; 2) 70 to 95 percent of sucrose, wherein the sucrose with the granularity of more than 600 mu m is not more than 20 percent, and the sucrose with the granularity of less than 180 mu m is not more than 20 percent. Preferably, the sucrose particle size ranges from no more than 10% greater than 600 μm to no more than 20% less than 180 μm.
Further the sucrose particle size ranges are not more than 10% above 600 μm and not more than 10% below 180 μm.
Further said sucrose particle size range is no more than 10% greater than the sum of the particle size ranges of greater than 600 μm and less than 180 μm. .
The sucrose of less than 600 μm and more than 180 μm of the present invention can be obtained by sieving through 24 mesh and 80 mesh sieves, respectively.
The sucrose used in the present invention can be selected from fine granulated sugar (not less than 75% with a particle size of less than 600 μm and not more than 20% with a particle size of less than 300 μm), fine granulated sugar (not more than 10% with a particle size of more than 500 μm and not more than 10% with a particle size of less than 180 μm), and sucrose granules obtained by sieving with a 30-mesh or 80-mesh sieve if necessary.
The clindamycin palmitate hydrochloride particle composition disclosed by the invention also can contain a pharmaceutically acceptable surfactant, a preservative, defoaming agent simethicone and essence. Preferably, the surfactant is poloxamer in an amount of 0.5-2% and the preservative is ethylparaben in an amount of 0.02% -1% of the preservative.
The clindamycin palmitate hydrochloride granular composition disclosed by the invention can be prepared by adopting a wet granulation process, wherein a wetting agent is selected from ethanol and water, the using amount is 1-5%, the drying temperature is 40-60 ℃, and the water content is not more than 0.5%. Preferably, the wetting agent is used in an amount of 1~3%.
Preferably, the preparation method is a one-step granulation method, the clindamycin palmitate hydrochloride is dissolved in ethanol, the temperature of the materials in a fluidized bed is 40 to 60 ℃, the materials are sprayed on the sucrose granules, and the sucrose granules are dried until the moisture is less than 0.5 percent.
The wet granulation method of the invention is a method for preparing granules by adding an adhesive or a wetting agent into the powder of the medicine and the auxiliary material and agglomerating the powder together by the bridge frame or the bonding action of the adhesive.
The one-step granulation, also called fluidized bed granulation, is a method for agglomerating powder into granules by spraying a solution containing a binder while keeping the powder of a material in a fluidized state under the action of hot air passing from bottom to top. The three steps of mixing, granulating and drying of the conventional wet granulation are completed in a closed container at one time.
The wet granulation process of the present invention may be: adding sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate hydrochloride into a wet mixing granulator, premixing, starting a stirring paddle and a shearing knife, adding ethanol for granulation, transferring the granulated wet material into a fluidized bed for drying at 40-60 ℃, controlling the water content to be below 1%, sieving or granulating the dry granules, mixing the granules and cherry essence in a mixer until the granules are uniform, and subpackaging to obtain the finished product.
Sucrose is used as a bulking agent in pharmaceutical applications and is typically sieved through an 80 mesh sieve. It is generally believed that the size of the filler is similar to the size of the drug, which is beneficial for uniformity of the blended granulation. The granularity of the clindamycin palmitate hydrochloride raw material medicine is D 90 About 200 μm, so that it should be easier to mix uniformly by using sucrose (less than 180 μm) which is crushed and then passed through 80 mesh.
According to the invention, through a large number of researches, sucrose with a certain particle size range (the particle size is larger than 600 mu m and is not more than 25%, and the particle size is smaller than 180 mu m and is not more than 20%) is used as a filler, so that the problem of content uniformity of clindamycin palmitate hydrochloride particles is solved unexpectedly. However, the use of ground sucrose having a particle size close to that of the drug as a filler is disadvantageous in terms of uniformity.
At the same time, it was found that the moisture in the composition is also important, directly affecting the physical stability of the combination.
Detailed Description
The above-mentioned aspects of the present invention will be further described in detail with reference to the following specific examples. It should not be understood that the scope of the above-described subject matter of the present invention is limited to the following examples. Various substitutions and alterations according to the general knowledge and the conventional means in the art are included in the scope of the present invention without departing from the technical idea of the present invention.
Example 1:
1) Prescription: the clindamycin palmitate hydrochloride granules are formulated as follows, in 1kg of formulation, containing:
clindamycin palmitate hydrochloride 37.5g (calculated as clindamycin)
Sucrose (920 g)
Poloxamer 13g
0.3g of ethylparaben
Simethicone 0.06g
Cherry essence 5g
20ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose, and selecting sucrose with particle size of more than 600 μm and less than 25% and less than 180 μm and less than 20% for use; crushing and sieving ethylparaben, and selecting the particle size range not more than 300 mu m for later use;
(b) Weighing clindamycin palmitate hydrochloride and auxiliary materials according to the prescription amount;
(c) Sequentially adding the weighed sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate hydrochloride into a wet granulator for premixing for 180S; adding ethanol with the formula amount into a wet granulating machine, simultaneously starting stirring and shearing for granulating for 180S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 30min at 40-60 ℃ to obtain dry granules with the water content of 0.5%;
(d) And (4) granulating the dry particles, mixing the granules with the cherry essence in a mixer until the granules are uniform, and subpackaging to obtain the finished product.
Example 2:
1) Prescription: the clindamycin palmitate hydrochloride granules are formulated as follows, in 5kg of formulation, containing:
clindamycin palmitate hydrochloride 0.5kg (calculated as clindamycin)
4kg of sucrose (fine granulated sugar)
Poloxamer 150g
Ethylparaben 5g
Simethicone 2g
Cherry essence 20g
150ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose (fine granulated sugar), and selecting sucrose with particle size of more than 600 μm and not more than 25%, and less than 300 μm and not more than 20%; crushing and sieving ethylparaben, and selecting the particle size range not more than 300 mu m for later use;
(b) Weighing clindamycin palmitate hydrochloride and auxiliary materials according to the prescription amount;
(c) Sequentially adding the weighed sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate hydrochloride into a wet granulator for premixing for 120S; adding ethanol with the formula amount into a wet granulating machine, simultaneously starting stirring and shearing for granulating for 240S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 40min at 40-60 ℃ to obtain dry granules;
(d) And (4) granulating the dry particles, mixing the granules with the cherry essence in a mixer until the granules are uniform, and subpackaging to obtain the finished product.
Example 3:
1) Prescription: the prescription of the clindamycin palmitate hydrochloride particles comprises the following components in 10kg of preparation, wherein the components comprise:
clindamycin palmitate hydrochloride 0.75kg (in clindamycin)
8.6kg of sucrose (Young granulated sugar)
Poloxamer 130g
8g of ethylparaben
Simethicone 2g
Cherry essence 25g
200ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose (young granulated sugar), and selecting sucrose with particle size of more than 500 μm and less than 10% and less than 180 μm and less than 10%; crushing and sieving ethylparaben, and selecting the particle size range not more than 250 μm for later use; (b) Weighing sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate according to the prescription amount, adding into a wet granulator, and premixing for 180S; adding ethanol with the formula amount into a wet granulating machine, simultaneously starting stirring and shearing for granulating for 120S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 35min at the temperature of 40-60 ℃ to obtain dry granules;
(c) And (4) granulating the dry particles, mixing the granules with the cherry essence in a mixer, and subpackaging to obtain a finished product.
Example 4:
1) Prescription: the clindamycin palmitate hydrochloride granules are formulated as follows, in 20kg of formulation, containing:
clindamycin palmitate hydrochloride 0.75kg (in clindamycin)
18.4kg of sucrose (fine granulated sugar)
Poloxamer 0.26g
Ethyl hydroxybenzene 6g
Simethicone 1.2g
Cherry essence 0.1kg
40ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose, and selecting sucrose with particle size of more than 600 μm and less than 300 μm and not more than 10%; crushing and sieving ethylparaben, and selecting the particle size range not more than 300 mu m for later use;
(c) Sequentially adding sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate hydrochloride into a wet granulator for premixing for 240S; adding ethanol with a formula amount into a wet granulator, simultaneously starting stirring and shearing for granulation, wherein the granulation time is 240S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 50min at the temperature of 40-60 ℃ to obtain dry granules;
(d) And (4) granulating the dry particles, mixing the granules with cherry essence in a mixer, and subpackaging to obtain a finished product.
Example 5:
1) Prescription: the prescription of the clindamycin palmitate hydrochloride granules comprises the following components in 100kg of preparation, wherein the components comprise:
clindamycin palmitate hydrochloride 7.5kg (calculated as clindamycin)
86kg of cane sugar
Poloxamer 1.3kg
Hydroxyphenyl Ethyl ester 30g
Simethicone 6g
Cherry essence 0.35kg
200ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose, and selecting sucrose with particle size of more than 600 μm and less than 180 μm and not more than 10%; crushing and sieving ethylparaben, and selecting the particle size range not more than 300 mu m for later use;
(b) Weighing clindamycin palmitate hydrochloride and auxiliary materials according to the prescription amount;
(c) Sequentially adding the weighed sucrose, ethylparaben, simethicone, poloxamer and clindamycin palmitate hydrochloride into a wet granulator for premixing for 180S; adding ethanol with the formula amount into a wet granulating machine, simultaneously starting stirring and shearing for granulating for 150S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 30min at the temperature of 40-60 ℃ to obtain dry granules.
(d) And (4) granulating the dry particles, mixing the granules with the cherry essence in a mixer, and subpackaging to obtain a finished product.
Comparative example 1:
1) Prescription: the prescription of the clindamycin palmitate hydrochloride particles comprises the following components in 1kg of preparation, wherein the components comprise:
clindamycin palmitate hydrochloride 37.5g (calculated as clindamycin)
Sucrose 910g
Poloxamer 13g
Saccharin sodium 10g
0.3g of ethylparaben
Simethicone 0.06g
Cherry essence 5g
20ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Pulverizing sucrose, and sieving with 80 mesh sieve (not more than 180 μm sucrose);
(b) Weighing sucrose, ethylparaben, simethicone, poloxamer, saccharin sodium and clindamycin palmitate hydrochloride according to the prescription amount, and adding the weighed materials into a wet granulator for premixing for 240S; adding ethanol with the formula amount into a wet granulator, simultaneously starting stirring and shearing for granulation, wherein the granulation time is 240S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 1h at the temperature of 40-60 ℃ to obtain dry granules;
(d) And (4) granulating the dry particles, mixing the granules with the cherry essence in a mixer, and subpackaging to obtain a finished product.
Comparative example 2:
1) Prescription: the prescription of the clindamycin palmitate hydrochloride granules comprises the following components in 100kg of preparation, wherein the components comprise:
clindamycin palmitate hydrochloride 7.5kg (calculated as clindamycin)
Sucrose 85kg
Poloxamer 1.3kg
Saccharin sodium 1kg
Hydroxyphenyl Ethyl ester 30g
Simethicone 6g
Cherry essence 0.35kg
200ml of medicinal ethanol
2) The preparation method comprises the following steps:
(a) Sieving sucrose, and selecting sucrose with particle size larger than 600 μm;
(b) Crushing ethylparaben, and sieving with 80-mesh sieve for later use;
(c) Weighing clindamycin palmitate hydrochloride and other auxiliary materials according to the prescription amount;
(d) Sequentially adding the weighed sucrose, ethylparaben, simethicone, poloxamer, saccharin sodium and clindamycin palmitate hydrochloride into a wet granulator for premixing for 240S; adding ethanol with the formula amount into a wet granulating machine, simultaneously starting stirring and shearing for granulating for 240S, and after the granulation is finished, transferring the wet granules into a fluidized bed to dry for 15min at the temperature of 40-60 ℃ to obtain dry granules;
(d) And (4) granulating the dry particles, mixing the granules with cherry essence in a mixer, and subpackaging to obtain a finished product.
The detection results of the embodiment and the comparative example disclosed by the invention are as follows:
examples 1-5 and comparative examples 1-2, 10 samples of each example, about 2g each, were taken and content uniformity was determined by HPLC, the HPLC conditions were as follows: detection method high performance liquid chromatography (refer to the general rules of the four parts 0512 of the 2015 year edition of Chinese pharmacopoeia) specifically as follows:
a chromatographic column: octadecylsilane chemically bonded silica gel as filler
Mobile phase: methanol-water-triethylamine (95
Detection wavelength: flow rate at 210 nm: column temperature 0.8 ml/min: 30 deg.C
Sample introduction volume: 20 μ l of solvent: water (W)
System applicability requirements: the separation between the clindamycin palmitate peak and the clindamycin B palmitate peak (relative retention time is about 0.90) in the chromatogram of the control solution should be no less than 2.0.
Test solution: precisely measuring 10ml of test solution under the item of ethylparaben examination, placing the test solution into a 100ml measuring flask, diluting the test solution to a scale with water, shaking up, and preparing a solution containing about 1.5mg of clindamycin in each 1 ml.
Control solution: taking a proper amount of clindamycin palmitate reference substance, precisely weighing, adding water to dissolve, and quantitatively diluting to prepare a solution containing about 1.5mg of clindamycin in each 1 ml.
The moisture is measured by Karl Fischer according to Chinese pharmacopoeia.
Stability examination was performed (temperature and humidity of 40 ℃ C., RH 75%).
* Content uniformity: a + 2.2S <15, the content uniformity of the sample meets the specification. RSD is less than or equal to 5 percent, and the sample uniformity is good.
The experimental results show that: the uniformity of the content of the clindamycin palmitate hydrochloride particles prepared by the embodiment of the invention by controlling the size range of the sucrose is obviously higher than that of the comparative embodiment. Meanwhile, the lower the moisture, the better the stability of the formulation.
Claims (5)
1. The clindamycin palmitate hydrochloride particle composition is characterized by comprising the following components: 1) 1 to 10% clindamycin palmitate hydrochloride; 2) 70 to 95 percent of sucrose, wherein the granularity is more than 25 percent when being more than 600 mu m, and the granularity is less than 20 percent when being less than 180 mu m; the moisture of the composition is less than 0.5%;
the composition also contains pharmaceutically acceptable surfactant, preservative, defoamer simethicone and essence; the surfactant is 0.5-2% of poloxamer, and the preservative is 0.02% -1% of ethylparaben; the composition is prepared by a wet granulation process, wherein a wetting agent is selected from ethanol and water, the using amount is 1-5%, the drying temperature is 40-60 ℃, and the water content is not more than 0.5%; the dosage of the wetting agent is 1~3%; dissolving clindamycin palmitate hydrochloride and other components in ethanol by adopting a one-step granulation method, spraying the materials into the sucrose granules at the temperature of 40-60 ℃ in a fluidized bed, and drying until the water content is less than 0.5%.
2. The composition of claim 1, wherein said sucrose has a particle size of no more than 10% greater than 600 μm and a particle size of no more than 10% less than 300 μm.
3. The composition of claim 2, wherein the sucrose has a particle size greater than 600 μm and less than 180 μm that does not add up to 10%.
4. The composition according to claim 1, wherein the sucrose is fine granulated sugar having a particle size of not more than 20% less than 300 μm.
5. The composition according to claim 1, wherein the sucrose is young granulated sugar, wherein the particle size is not more than 10% of the particle size greater than 500 μm and not more than 10% of the particle size less than 180 μm.
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| CN1726009A (en) * | 2002-12-19 | 2006-01-25 | 阿库斯菲尔公司 | Methods for making pharmaceutical formulations comprising deagglomerated microparticles |
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| CN112402381A (en) | 2021-02-26 |
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