CN114209807A - Goserelin implant preparation and preparation method thereof - Google Patents
Goserelin implant preparation and preparation method thereof Download PDFInfo
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- CN114209807A CN114209807A CN202210037428.8A CN202210037428A CN114209807A CN 114209807 A CN114209807 A CN 114209807A CN 202210037428 A CN202210037428 A CN 202210037428A CN 114209807 A CN114209807 A CN 114209807A
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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
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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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
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Immunology (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a goserelin implant preparation and a preparation method thereof, wherein the implant preparation comprises 3-8 parts of dimethylformamide, 0.8-1.5 parts of oxidized proline, 2-4 parts of dimethyl sulfoxide, 3-7 parts of dioxane solution, 10-30 parts of lactic acid, 20-40 parts of glycolic acid and 3-12 parts of dimeticone.
Description
Technical Field
The invention relates to the technical field of pharmacy, in particular to a goserelin implant preparation and a preparation method thereof.
Background
The implant is a sterile solid preparation prepared from medicines and auxiliary materials and used for being implanted into a body. The implant is generally implanted in the body by a special syringe or can be implanted by incision operation. The released medicine directly enters the blood circulation to act through subcutaneous absorption or cavity absorption, so the first-pass effect is avoided, the bioavailability is high, the acting time is long, even for years, and goserelin is the gonadotropin releasing hormone analogue which is widely researched at present and is used for treating the premenopausal hormone receptor positive breast cancer patients. The composition has the effect of relieving symptoms of menopause, and can reduce estrogen level of patients. Goserelin is indicated in a number of conditions, including post-prostate cancer monotherapy, as an alternative to orchiectomy or estrogen administration, which is not suitable or acceptable for patients. Goserelin is also used for control, pain relief and relief of endometriosis, and to reduce endometriosis damage during treatment. The medicine is effective in relieving clinical symptoms (dysmenorrhea, sexual intercourse pain and pelvic pain) and signs of endometriosis and reducing damage of endometrium after administration, and can be used for treating advanced breast cancer.
However, the existing goserelin implant has the defects of complex manufacturing process, high production cost, easy occurrence of the phenomenon of drug burst release at the end of the release period and high defect.
Disclosure of Invention
1. Technical problem to be solved
The invention aims to solve the problems that the preparation process of a goserelin implant in the prior art is complex, the production cost is high, and the phenomenon of sudden drug release is easy to occur at the end of a release period, and provides a goserelin implant preparation and a preparation method thereof.
2. Technical scheme
In order to achieve the purpose, the goserelin implant preparation provided by the invention comprises 3-8 parts of dimethylformamide, 0.8-1.5 parts of oxidized proline, 2-4 parts of dimethyl sulfoxide, 3-7 parts of dioxane solution, 10-30 parts of lactic acid, 20-40 parts of glycolic acid and 3-12 parts of simethicone.
Preferably, the implant preparation comprises 8 parts of dimethylformamide, 1.5 parts of oxidized proline, 4 parts of dimethyl sulfoxide, 7 parts of dioxane solution, 30 parts of lactic acid, 40 parts of glycolic acid and 10 parts of simethicone.
Preferably, the implant preparation comprises 3 parts of dimethylformamide, 0.8 part of oxidized proline, 2 parts of dimethyl sulfoxide, 3 parts of dioxane solution, 10 parts of lactic acid, 20 parts of glycolic acid and 3 parts of simethicone.
Preferably, the implant preparation comprises 7 parts of dimethylformamide, 0.8 part of oxidized proline, 3 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 11 parts of lactic acid, 24 parts of glycolic acid and 7 parts of simethicone.
Preferably, the implant preparation comprises 8 parts of dimethylformamide, 0.9 part of oxidized proline, 2.7 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 15 parts of lactic acid, 22 parts of glycolic acid and 4 parts of simethicone.
The invention also provides a preparation method of the goserelin implant preparation, which comprises the following steps:
s1, placing dimethyl formamide and dimethyl sulfoxide in the raw materials into a stirrer, and preparing a mixed solvent under the condition of neutralization and stirring at the temperature of 0 ℃;
s2, suspending the oxidized proline in the mixed solvent, adding the dioxane solution, and stirring for 5min to obtain a clear goserelin solution;
s3, mixing and stirring lactic acid 1 and glycolic acid in the raw materials to obtain a mixed solution;
s4, injecting the dimeticone into the mixture, and condensing to form a microsphere blank;
s5, transferring the formed microsphere embryo into a quenching liquid, stirring, quenching and hardening, washing the hardened microsphere with a washing liquid, collecting, drying and freeze-drying to obtain microsphere powder;
s6, adding the microsphere powder into the goserelin solution, uniformly stirring at a high speed, and cooling to prepare the goserelin implant solution;
s7, the goserelin implant solution is filled into the reagent bottles by a filling machine.
3. Advantageous effects
Compared with the prior art, the invention has the advantages that: the goserelin sustained-release microsphere has the advantages of simple process, low solvent residue and long-acting sustained-release effect, and has the effects of small burst release effect, mild release curve, long release period and the like by fusing the goserelin sustained-release microsphere and the goserelin solution.
Detailed Description
The present invention will be further illustrated with reference to the following specific examples.
Example 1:
the goserelin implant preparation provided by the invention comprises 8 parts of dimethylformamide, 1.5 parts of oxidized proline, 4 parts of dimethyl sulfoxide, 7 parts of dioxane solution, 30 parts of lactic acid, 40 parts of glycolic acid and 10 parts of simethicone.
A method of preparing a goserelin implant formulation, the method comprising the steps of:
s1, placing dimethyl formamide and dimethyl sulfoxide in the raw materials into a stirrer, and preparing a mixed solvent under the condition of neutralization and stirring at the temperature of 0 ℃;
s2, suspending the oxidized proline in the mixed solvent, adding the dioxane solution, and stirring for 5min to obtain a clear goserelin solution;
s3, mixing and stirring lactic acid 1 and glycolic acid in the raw materials to obtain a mixed solution;
s4, injecting the dimeticone into the mixture, and condensing to form a microsphere blank;
s5, transferring the formed microsphere embryo into a quenching liquid, stirring, quenching and hardening, washing the hardened microsphere with a washing liquid, collecting, drying and freeze-drying to obtain microsphere powder;
s6, adding the microsphere powder into the goserelin solution, uniformly stirring at a high speed, and cooling to prepare the goserelin implant solution;
s7, the goserelin implant solution is filled into the reagent bottles by a filling machine.
Example 2
The goserelin implant preparation provided by the invention comprises 7 parts of dimethylformamide, 0.8 part of oxidized proline, 3 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 11 parts of lactic acid, 24 parts of glycolic acid and 7 parts of simethicone.
The preparation method of goserelin implant preparation is the same as that of example 1.
Example 3
The goserelin implant preparation provided by the invention comprises 8 parts of dimethylformamide, 0.9 part of oxidized proline, 2.7 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 15 parts of lactic acid, 22 parts of glycolic acid and 4 parts of simethicone.
The preparation method of goserelin implant preparation is the same as that of example 1.
Example 4
The goserelin implant preparation provided by the invention comprises 3 parts of dimethylformamide, 0.8 part of oxidized proline, 2 parts of dimethyl sulfoxide, 3 parts of dioxane solution, 10 parts of lactic acid, 20 parts of glycolic acid and 3 parts of simethicone.
The preparation method of goserelin implant preparation is the same as that of example 1.
The above description is only for the preferred embodiment of the present invention, but the scope of the present invention is not limited thereto, and any person skilled in the art should be considered to be within the technical scope of the present invention, and the technical solutions and the inventive concepts thereof according to the present invention should be equivalent or changed within the scope of the present invention.
Claims (6)
1. The goserelin implant preparation is characterized by comprising 3-8 parts of dimethylformamide, 0.8-1.5 parts of oxidized proline, 2-4 parts of dimethyl sulfoxide, 3-7 parts of dioxane solution, 10-30 parts of lactic acid, 20-40 parts of glycolic acid and 3-12 parts of simethicone.
2. The goserelin implant preparation and the preparation method thereof according to claim 1, wherein the implant preparation comprises 8 parts of dimethylformamide, 1.5 parts of oxidized proline, 4 parts of dimethyl sulfoxide, 7 parts of dioxane solution, 30 parts of lactic acid, 40 parts of glycolic acid and 10 parts of simethicone.
3. The goserelin implant preparation and the preparation method thereof according to claim 1, wherein the implant preparation comprises 3 parts of dimethylformamide, 0.8 part of oxidized proline, 2 parts of dimethyl sulfoxide, 3 parts of dioxane solution, 10 parts of lactic acid, 20 parts of glycolic acid and 3 parts of simethicone.
4. The goserelin implant preparation and the preparation method thereof according to claim 1, wherein the implant preparation comprises 7 parts of dimethylformamide, 0.8 part of oxidized proline, 3 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 11 parts of lactic acid, 24 parts of glycolic acid and 7 parts of simethicone.
5. The goserelin implant preparation and the preparation method thereof according to claim 1, wherein the implant preparation comprises 8 parts of dimethylformamide, 0.9 part of oxidized proline, 2.7 parts of dimethyl sulfoxide, 4 parts of dioxane solution, 15 parts of lactic acid, 22 parts of glycolic acid and 4 parts of simethicone.
6. A method of preparing a goserelin implant formulation, the method comprising the steps of:
s1, placing dimethyl formamide and dimethyl sulfoxide in the raw materials into a stirrer, and preparing a mixed solvent under the condition of neutralization and stirring at the temperature of 0 ℃;
s2, suspending the oxidized proline in the mixed solvent, adding the dioxane solution, and stirring for 5min to obtain a clear goserelin solution;
s3, mixing and stirring lactic acid 1 and glycolic acid in the raw materials to obtain a mixed solution;
s4, injecting the dimeticone into the mixture, and condensing to form a microsphere blank;
s5, transferring the formed microsphere embryo into a quenching liquid, stirring, quenching and hardening, washing the hardened microsphere with a washing liquid, collecting, drying and freeze-drying to obtain microsphere powder;
s6, adding the microsphere powder into the goserelin solution, uniformly stirring at a high speed, and cooling to prepare the goserelin implant solution;
s7, the goserelin implant solution is filled into the reagent bottles by a filling machine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210037428.8A CN114209807A (en) | 2022-01-13 | 2022-01-13 | Goserelin implant preparation and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210037428.8A CN114209807A (en) | 2022-01-13 | 2022-01-13 | Goserelin implant preparation and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN114209807A true CN114209807A (en) | 2022-03-22 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210037428.8A Pending CN114209807A (en) | 2022-01-13 | 2022-01-13 | Goserelin implant preparation and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857208A (en) * | 2006-03-17 | 2006-11-08 | 山东蓝金生物工程有限公司 | Slow released anticancer injection with both antimetabolite and its synergist |
| US20150141392A1 (en) * | 2012-06-15 | 2015-05-21 | The Gegents Of The University Of California | Substituted macrocyclic compounds having proteasome inhibitory activity |
| CN104744569A (en) * | 2013-12-26 | 2015-07-01 | 李磊 | Preparation method of goserelin |
| WO2016149561A1 (en) * | 2015-03-17 | 2016-09-22 | Oak Crest Institute Of Science | Subdermal implants for the sustained delivery of water-soluble drugs |
-
2022
- 2022-01-13 CN CN202210037428.8A patent/CN114209807A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857208A (en) * | 2006-03-17 | 2006-11-08 | 山东蓝金生物工程有限公司 | Slow released anticancer injection with both antimetabolite and its synergist |
| US20150141392A1 (en) * | 2012-06-15 | 2015-05-21 | The Gegents Of The University Of California | Substituted macrocyclic compounds having proteasome inhibitory activity |
| CN104744569A (en) * | 2013-12-26 | 2015-07-01 | 李磊 | Preparation method of goserelin |
| WO2016149561A1 (en) * | 2015-03-17 | 2016-09-22 | Oak Crest Institute Of Science | Subdermal implants for the sustained delivery of water-soluble drugs |
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