CN111388435A - Preparation method and pharmaceutical composition of silodosin compound - Google Patents
Preparation method and pharmaceutical composition of silodosin compound Download PDFInfo
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- CN111388435A CN111388435A CN202010285484.4A CN202010285484A CN111388435A CN 111388435 A CN111388435 A CN 111388435A CN 202010285484 A CN202010285484 A CN 202010285484A CN 111388435 A CN111388435 A CN 111388435A
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- silodosin
- fully mixing
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a preparation method and a pharmaceutical composition of silodosin compound, comprising the following steps: dissolving the antioxidant in distilled water, and uniformly stirring for later use; step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use; step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use; step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use; step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding silodosin and a binder, stirring and fully mixing, and then granulating by a wet method; step f: and e, tabletting and forming the granules obtained in the step e. The preparation method of the silodosin compound and the pharmaceutical composition have the advantages of simple production process, high production efficiency and fewer produced impurities, improve the yield of the silodosin compound and the pharmaceutical composition, and further reduce the production cost.
Description
Technical Field
The invention relates to a preparation method of a silodosin compound and a pharmaceutical composition, belonging to the technical field of medicines.
Background
The sirodoxine capsule is used for treating symptoms and signs caused by Benign Prostatic Hyperplasia (BPH) by dry treatment, the sirodoxine is used as a brand-new generation high-selectivity adrenoceptor α A receptor blocker, on one hand, the sirodoxine can effectively block the adrenoceptors α A on smooth muscles of prostate, urethra and trigonal area, so that bladder and prostate smooth muscle tissues become loose, thereby increasing urine flow and reducing the probability of urine reflux in prostate, on the other hand, the affinity of the sirodoxine to the adrenoceptors α A, which is present in peripheral vasculature and plays an important role in blood pressure regulation, is low, the side effects (headache, dizziness and the like) caused by the sirodoxine are far less than that of the same drugs (terazosin, tamsulosin and the like), therefore, the sirodoxine and levofloxacin are the best choices for all prostatitis patients needing to prevent cardiovascular related adverse events, the combined use of the sirodoxine and levofloxacin achieves good treatment effect, and the effects of the chronic bacterial prostatitis are mainly achieved by the following two aspects of (1) preparing the sirodoxine capsule, selectively reducing the symptoms and the prostatic pain caused by the prostatic hyperplasia, the urinary tract pain of the prostatic urethra, the urinary tract obstruction of the prostatic urethra, the urinary tract pain of the urinary tract of the prostate by the conventional creative technology, the intraurethral pain of the urinary tract pain of the cystofloxacin, the urinary tract pain of the urinary tract is improved, the urinary tract pain of the prostanoid, the urinary tract is improved, the urinary tract pain of the urinary tract pain of the prostanoid is improved, the urinary tract.
Disclosure of Invention
The invention aims to provide a preparation method of a silodosin compound and a pharmaceutical composition, and aims to solve the problems that the existing preparation method of the silodosin compound is complicated and time-consuming, high in solvent toxicity, low in production efficiency and high in production cost in the background art.
In order to achieve the purpose, the invention provides the following technical scheme: a preparation method of silodosin compound comprises the following steps:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
Preferably, the antioxidant in step a is sodium hydroxide solution, and the concentration of the sodium hydroxide solution is 1.8 × 10- 4mg·ml-1。
Preferably, sorbitol is selected as the filling agent in the step c, and one or more of methanol, ethanol and water is adopted as the lubricating agent.
Preferably, the adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
Preferably, the time for stirring the mixed solution of the filling agent and the lubricant in the step e is 10-25min, and the stirring temperature is 30-45 ℃.
The silodosin pharmaceutical composition comprises the following components in parts by weight:
preferably, the weight parts of each component are as follows:
preferably, the weight parts of each component are as follows:
preferably, the weight parts of each component are as follows:
compared with the prior art, the invention has the following beneficial effects: the preparation method of the silodosin compound and the pharmaceutical composition have simple production process, can be used for large-scale production and preparation, have high production efficiency, produce fewer impurities, improve the yield of the silodosin compound and the pharmaceutical composition, and further reduce the production cost.
Detailed Description
In order to make the technical solutions of the present invention more clear and definite for those skilled in the art, the present invention is further described in detail with reference to the following examples, but the embodiments of the present invention are not limited thereto.
The preparation method of silodosin compound provided by this embodiment includes the following steps:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
The antioxidant in the step a is sodium hydroxide solution, and the concentration of the sodium hydroxide solution is 1.8 × 10-4mg·ml-1。
Sorbitol is selected as a filling agent in the step c, and one or more of methanol, ethanol and water is adopted as a lubricating agent.
The adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
And e, stirring the mixed solution of the filling agent and the lubricant for 10-25min at the stirring temperature of 30-45 ℃.
The silodosin pharmaceutical composition comprises the following components in parts by weight:
in this embodiment, a preparation method of silodosin compound includes the following specific steps:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
The antioxidant in the step a is sodium hydroxide solution, and the concentration of the sodium hydroxide solution is 1.8 × 10-4mg·ml-1。
Sorbitol is selected as a filling agent in the step c, and one or more of methanol, ethanol and water is adopted as a lubricating agent.
The adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
And e, stirring the mixed solution of the filling agent and the lubricant for 10-25min at the stirring temperature of 30-45 ℃.
The silodosin pharmaceutical composition comprises the following components in parts by weight:
in this embodiment, a preparation method of silodosin compound includes the following specific steps:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
The antioxidant in the step a is sodium hydroxide solution, and the concentration of the sodium hydroxide solution is 1.8 × 10-4mg·ml-1。
Sorbitol is selected as a filling agent in the step c, and one or more of methanol, ethanol and water is adopted as a lubricating agent.
The adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
And e, stirring the mixed solution of the filling agent and the lubricant for 10-25min at the stirring temperature of 30-45 ℃.
The silodosin pharmaceutical composition comprises the following components in parts by weight:
in this embodiment, a preparation method of silodosin compound includes the following specific steps:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
The antioxidant in step a isSodium hydroxide solution with concentration of 1.8 × 10-4mg·ml-1。
Sorbitol is selected as a filling agent in the step c, and one or more of methanol, ethanol and water is adopted as a lubricating agent.
The adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
And e, stirring the mixed solution of the filling agent and the lubricant for 10-25min at the stirring temperature of 30-45 ℃.
The silodosin pharmaceutical composition comprises the following components in parts by weight:
the above description is only for the purpose of illustrating the present invention and is not intended to limit the scope of the present invention, and any person skilled in the art can substitute or change the technical solution of the present invention and its conception within the scope of the present invention.
Claims (9)
1. A preparation method of silodosin compounds is characterized by comprising the following steps of:
step a: dissolving the antioxidant in distilled water, and uniformly stirring for later use;
step b: crushing and grinding the silodosin raw material in a grinder, and screening to 80-140 meshes by using a sieve for later use;
step c: weighing the filler and the lubricant according to the weight ratio, and fully mixing for later use;
step d: weighing silodosin and the adhesive according to the weight ratio, and fully mixing for later use;
step e: weighing pregelatinized starch according to the weight ratio, fully mixing, adding the mixed solution of the filler and the lubricant in the step c, stirring and fully mixing, adding silodosin and the adhesive, stirring and fully mixing, and performing wet granulation;
step f: and e, drying the granules obtained in the step e, adding starch, uniformly mixing, and tabletting for forming.
2. The method of claim 1, wherein the antioxidant in step a is NaOH solution, and the concentration of NaOH solution is 1.8 × 10-4mg·ml-1。
3. The process for preparing silodosin compound according to claim 1, wherein: sorbitol is selected as a filling agent in the step c, and one or more of methanol, ethanol and water is adopted as a lubricating agent.
4. The process for preparing silodosin compound according to claim 1, wherein: the adhesive is one or more of starch, hydroxypropyl methylcellulose and mannitol.
5. The process for preparing silodosin compound according to claim 1, wherein: and e, stirring the mixed solution of the filling agent and the lubricant in the step e for 10-25min at the stirring temperature of 30-45 ℃.
6. A silodosin pharmaceutical composition according to claims 1 to 5, wherein the weight parts of the components are as follows:
7. the silodosin pharmaceutical composition according to claim 6, wherein the weight parts of the components are as follows:
8. the silodosin pharmaceutical composition according to claim 6, wherein the weight parts of the components are as follows:
9. the silodosin pharmaceutical composition according to claim 6, wherein the weight parts of the components are as follows:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010285484.4A CN111388435A (en) | 2020-04-13 | 2020-04-13 | Preparation method and pharmaceutical composition of silodosin compound |
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| Application Number | Priority Date | Filing Date | Title |
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| CN202010285484.4A CN111388435A (en) | 2020-04-13 | 2020-04-13 | Preparation method and pharmaceutical composition of silodosin compound |
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| Publication Number | Publication Date |
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| CN111388435A true CN111388435A (en) | 2020-07-10 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN202010285484.4A Pending CN111388435A (en) | 2020-04-13 | 2020-04-13 | Preparation method and pharmaceutical composition of silodosin compound |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103933001A (en) * | 2014-05-09 | 2014-07-23 | 浙江华海药业股份有限公司 | Stable silodosin oral solid pharmaceutical composition and preparation method thereof |
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- 2020-04-13 CN CN202010285484.4A patent/CN111388435A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103933001A (en) * | 2014-05-09 | 2014-07-23 | 浙江华海药业股份有限公司 | Stable silodosin oral solid pharmaceutical composition and preparation method thereof |
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Application publication date: 20200710 |