CN116459225B - Alagox sodium tablet and preparation process thereof - Google Patents

Alagox sodium tablet and preparation process thereof Download PDF

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CN116459225B
CN116459225B CN202310462234.7A CN202310462234A CN116459225B CN 116459225 B CN116459225 B CN 116459225B CN 202310462234 A CN202310462234 A CN 202310462234A CN 116459225 B CN116459225 B CN 116459225B
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sodium
alagolide
tablet
butyrate
antigelling agent
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CN116459225A (en
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杨小兵
陈田娥
朱艳飞
陈庆堂
梁富延
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Dongguan Jinmeiji Pharma Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an Alagox sodium tablet and a preparation process thereof. The sodium esagole tablet comprises sodium esagole and an antigelling agent which is sodium 4- (2-oxo-pyrrolidin-1-yl) butyrate. The inventors have surprisingly found that sodium 4- (2-oxo-pyrrolidin-1-yl) butyrate can act as a gelling agent in the sodium alagolide tablet, not only can effectively reduce the formation of alagolide gel, can enable the drug to be released rapidly, smoothly and uniformly, but also can improve the stability of the sodium alagolide, in particular inhibit the generation of lactam impurities, thereby prolonging the storage time of the sodium alagolide tablet and improving the medication safety.

Description

Alagox sodium tablet and preparation process thereof
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to an Alagox sodium tablet and a preparation process thereof.
Background
Sodium elagogram (elagoix, CAS No. 832720-36-2) is a gonadotropin releasing hormone (GnRH) antagonist developed by Abbvie corporation (Abbvie) and is used clinically to relieve moderate to severe pain symptoms caused by uterine fibroids, endometriosis, etc. in adult females.
In developing oral tablets of elagoke sodium, ibovi corporation found at least two difficulties (CN 111698992A, CN111246850 a): 1. the tendency of sodium alagolide to form gels when applied orally in solid dosage forms, particularly when the solid formulation does not contain suitable antigelling agents, is even greater, the gel formed limiting the dissolution of sodium alagolide, which may ultimately lead to a great variation in bioavailability between and among patients; 2. the sodium elagose may degrade to form compounds with lactam structures. By adopting the pharmaceutical composition of 'Igacross sodium+sodium carbonate', the gelation of Igacross sodium can be reduced and/or the generation of lactam degradation products can be reduced, so that the safety and efficacy of the product can be maintained. However, although the use of sodium carbonate improved the dissolution rate of the alagolic tablet to some extent, the dissolution rate was still slow for the first 30 minutes, indicating that the anti-gelling effect was still limited and that sodium carbonate had a weaker efficacy in inhibiting the production of lactam impurity, the tablet comprising sodium carbonate only reduced the content of lactam impurity by about 50% compared to the tablet without the anti-gelling agent.
Accordingly, there remains an unmet need for developing oral sodium argan tablets with improved dissolution rate and storage stability.
Disclosure of Invention
In order to solve the above problems, the present invention provides an alagolica sodium tablet comprising alagolica sodium and an antigelling agent which is sodium 4- (2-oxopyrrolidin-1-yl) butyrate.
The chemical structural formula of the Alagox sodium is shown as follows:
the chemical structural formula of the sodium 4- (2-oxo-pyrrolidin-1-yl) butyrate is shown as follows:
sodium 4- (2-oxopyrrolidin-1-yl) butyrate is readily available from the acid-base reaction of commercially available 4- (2-oxopyrrolidin-1-yl) butyric acid with a base such as sodium hydroxide.
Further, the weight ratio of the sodium elagose to the antigelling agent is 1:1 to 20:1. For example, the weight ratio of the sodium elagogram to the antigelling agent is 1:1, 2:1, 3:1, 4:1, 5:1, 6:1, 7:1, 8:1, 9:1, 10:1, 11:1, 12:1, 13:1, 14:1, 15:1, 16:1, 17:1, 18:1, 19:1, or 20:1.
Still further, the weight ratio of the sodium elagose to the antigelling agent is 4:1.
Further, the sodium argatrovix tablet comprises 10-40wt% of sodium argatrovix. For example, the sodium argyi tablet comprises 10wt%, 11wt%, 12wt%, 13wt%, 14wt%, 15wt%, 16wt%, 17wt%, 18wt%, 19wt%, 20wt%, 21wt%, 22wt%, 23wt%, 24wt%, 25wt%, 26wt%, 27wt%, 28wt%, 29wt%, 30wt%, 31wt%, 32wt%, 33wt%, 34wt%, 35wt%, 36wt%, 37wt%, 38wt%, 39wt%, or 40wt% sodium argyi. Still further, the sodium argatrovix tablet comprises 50mg, 100mg, 150mg, 200mg, 250mg or 300mg of sodium argatrovix.
Further, the sodium alagolicum tablet also comprises a pharmaceutically acceptable excipient.
Further, the pharmaceutically acceptable excipients include one or more of fillers, binders, lubricants, disintegrants, glidants, and surfactants.
Further, the filler includes one or more of starch, pregelatinized starch, mannitol, sorbitol, lactose, sucrose, microcrystalline cellulose, and calcium phosphate. Still further, the filler comprises mannitol or pregelatinized starch or a combination thereof.
Further, the filler is contained in the sodium argag tablet in an amount of 5 to 65wt%, or 10 to 60wt%, or 15 to 55wt%, or 10 to 50wt%, or 15 to 45wt%, or 20 to 40wt%, or 25 to 40wt%, or 30 to 40wt%.
Further, the sodium alagolicum tablet comprises 20wt% to 50wt% of the first filler and 1wt% to 20wt% of the second filler. Further, the sodium alagolicum tablet comprises 25wt% to 40wt% of the first filler and 5wt% to 15wt% of the second filler. Further, the sodium alagolicum tablet comprises 38wt% of the first filler and 12wt% of the second filler. Further, the first filler is mannitol and the second filler is pregelatinized starch.
Further, the binder includes one or more of povidone, copovidone, polyacrylate, polymethacrylate, polyacrylamide, polyvinyl alcohol, vinyl acetate polymer, hydroxypropyl cellulose, hydroxypropyl methylcellulose, ethyl cellulose, oligosaccharides, and polysaccharides. Still further, the binder comprises povidone or hydroxypropyl cellulose.
Further, the binder is present in the sodium alagogram tablet in an amount of 0.1 to 20wt%, or 0.5 to 15wt%, or 1 to 10wt%, or 1.5 to 18wt%, or 2 to 16wt%, or 2.5 to 14wt%, or 3 to 12wt%, or 3.5 to 10wt%, or 4 to 8wt%, or 3 to 7wt%, or 2 to 9wt%, or 2 to 6wt%, or 1 to 5wt%, or 1.5 to 5wt%, or 2 to 5wt%, or 2.5 to 5wt%, or 3 to 5wt%.
Further, the lubricant includes one or more of magnesium stearate, calcium stearate, aluminum stearate, glyceryl monostearate, stearic acid and talc, preferably one or more of magnesium stearate, calcium stearate and talc. Still further, the lubricant comprises magnesium stearate.
Further, the lubricant is contained in the sodium argag tablet in an amount of 0.1 to 10wt%, or 0.5 to 8wt%, or 1 to 5wt%, or 1.5 to 9wt%, or 1.7 to 8wt%, or 1.6 to 7wt%, or 1.7 to 6wt%, or 1.8 to 5wt%, or 1.9 to 4wt%, or 2 to 3wt%, or 1.5 to 6wt%, or 1.5 to 5wt%, or 1.5 to 4wt%, or 1.5 to 3wt%, or 1 to 2wt%.
Further, the disintegrant comprises one or more of crospovidone, croscarmellose sodium, sodium carboxymethylcellulose, calcium carboxymethylcellulose, low substituted hydroxypropyl cellulose and sodium starch glycolate. Further, the content of the disintegrating agent in the sodium argyi-goke tablet is 0-20wt%.
Further, the glidant includes one or more of colloidal silicon dioxide and talc. Further, the content of the disintegrating agent in the sodium argyi-goke tablet is 0-5wt%.
Further, the surfactant comprises one or more of polysorbate, sorbitan fatty acid, glyceride fatty acid, sucrose fatty acid ester, polyoxyethylene fatty alcohol ether, poloxamer, sodium dodecyl sulfate and sodium docusate. Further, the content of the disintegrating agent in the sodium argyi-goke tablet is 0-3wt%.
Further, the sodium alagolicum tablet further comprises a coating.
Further, the coating may be used, for example, to facilitate easy swallowing of the tablet. The coating may also be used to improve taste and provide a beautiful appearance. The coating may comprise one or a mixture or copolymer of at least two of hypromellose, hydroxypropyl cellulose, methylcellulose, hydroxyethyl cellulose, polyethylene glycol, polyvinyl alcohol, povidone, etc., such as polyvinyl alcohol-polyethylene glycol graft copolymer, for exampleII or->IR. The coating may also include talc as an anti-adherent. The coating may comprise less than about 5% by weight of the tablet.
The invention also provides a method for preparing the sodium Igurative tablet, which comprises the steps of uniformly mixing sodium Igurative, an antigelling agent and a pharmaceutically acceptable excipient, granulating, mixing, tabletting and coating to obtain the sodium Igurative tablet.
Further, the method comprises pulverizing the antigelling agent and sieving with an 80 mesh sieve; weighing the raw materials and pharmaceutically acceptable excipients according to the prescription, mixing, granulating, weighing the antigelling agent and pharmaceutically acceptable excipients according to the prescription, mixing, tabletting and coating to obtain the Igacross sodium tablets. Further, the granulating includes dry granulating or wet granulating.
Advantageous effects of the invention
The inventors have unexpectedly found that sodium 4- (2-oxopyrrolidin-1-yl) butyrate can act as an antigelling agent in the sodium alagolide tablet, not only can effectively reduce the formation of alagolide gel, can enable the drug to be released rapidly, smoothly and uniformly, but also can improve the stability of the alagolide sodium, in particular, inhibit the generation of lactam impurities, thereby prolonging the storage time of the sodium alagolide tablet and improving the medication safety. In contrast, sodium (2S) -2- (2-oxopyrrolidin-1-yl) butyrate, which is a structural analogue of sodium 4- (2-oxopyrrolidin-1-yl) butyrate, does not possess this feature (its structure is described in the examples). Without being bound by theory, it is believed that this is probably due to the lower pKa of sodium (2S) -2- (2-oxopyrrolidin-1-yl) butyrate compared to sodium 4- (2-oxopyrrolidin-1-yl) butyrate.
On one hand, the sodium esagole tablet has excellent dissolution characteristics, and the problem that esagole sodium is easy to gel is successfully solved by using the sodium esagole 4- (2-oxo-pyrrolidine-1-yl) butyrate, so that quick dissolution in the first 30min is realized, the dissolution performance of the medicine is improved, and the good release and absorption of the medicine in a body are facilitated. The sodium argatrovix tablet of the invention shows excellent dissolution rate in the medium simulating the conditions of pre-meal (pH 1.2) and post-meal (pH 4.5), especially the dissolution rate of the first 30min is obviously improved, which shows the rapidity of the anti-gelling agent effect and the durability of the anti-gelling effect.
On the other hand, the sodium esagole tablet has excellent stability and can remarkably inhibit the generation of lactam impurities. The examples demonstrate that the lactam impurity content is almost unchanged after 10 days of storage and less than about 0.3wt% after 20 days of storage when accelerated stability studies are carried out at 60 ℃ and 40% relative humidity.
Drawings
Fig. 1 shows the dissolution profile of the sodium alagolide tablets of examples 1-4 at pH 1.2.
Fig. 2 shows the dissolution profile of the sodium alagolide tablets of examples 1-4 at pH 4.5.
Detailed Description
The present invention is further illustrated below with reference to specific examples, which are not intended to limit the invention in any way. Unless specifically stated otherwise, the reagents, methods and apparatus employed in the present invention are those conventional in the art.
Examples 1 to 4: preparation of sodium Igacross tablets of different formulations
The sodium alagolide tablets were prepared according to the following formulation of table 1:
table 1: formula (mass percent) of different Alagox sodium tablets
Wherein sodium (2S) -2- (2-oxopyrrolidin-1-yl) butyrate is compared as a structural analogue of sodium 4- (2-oxopyrrolidin-1-yl) butyrate in the examples of the present invention, the chemical structural formula is shown below:
the preparation method of the sodium Igacross tablet by dry granulation comprises the following steps:
step (1) pretreatment: crushing sodium 4- (2-oxo-pyrrolidin-1-yl) butyrate (or sodium (2S) -2- (2-oxo-pyrrolidin-1-yl) butyrate or sodium carbonate), and sieving with a 80-mesh sieve;
and (2) weighing: respectively weighing raw materials and auxiliary materials according to the prescription amount;
and (3) granulating: mixing sodium alagolicum, mannitol, pregelatinized starch, magnesium stearate and povidone in a mixer, and performing dry granulation by using a dry granulator with the following parameters: rotation speed of the press roller: 6rpm, feed rate: 32rpm, nip: 1.0mm, pressure of the press roll: 80-90 bar, finishing speed of 100rpm, finishing screen 14 mesh;
step (4) total mixing: mixing the granules obtained in the step (3) with magnesium stearate, sodium 4- (2-oxo-pyrrolidin-1-yl) butyrate (or sodium (2S) -2- (2-oxo-pyrrolidin-1-yl) butyrate or sodium carbonate) and mannitol;
and (5) tabletting: adding the total mixed materials into a rotary tablet press, and adjusting the loading (the loading is 450 mg) and tabletting (the hardness is 8-10 kg);
coating in the step (6): adopts a high-efficiency coating machineAnd II, coating, wherein the weight of the coating is increased by 3%, and the Alagox sodium tablet is prepared.
Example 5: dissolution characteristics of the sodium Igacross tablets of examples 1-4
Dissolution rate measurement method: according to the general oral solid preparation dissolution test technical guidelines and dissolution and release rate measurement methods (four general regulations of Chinese pharmacopoeia 2020 edition), a hydrochloric acid solution with a pH of 1.2 and a citrate buffer solution with a pH of 4.5 are respectively used as dissolution media, the volume of the dissolution media is 900ml, the rotating speed is 50rpm, the dissolution media are respectively sampled at 5, 10, 15, 20, 25, 30, 45 and 60min, the absorbance (n=6) is measured at the wavelength of ultraviolet 274nm, and the dissolution curves are shown in figures 1 and 2.
As can be seen from the results of fig. 1 and 2, the dissolution profile of the alagolica sodium tablet is slightly better using sodium 4- (2-oxopyrrolidin-1-yl) butyrate as an antigelling agent (example 1) than using sodium carbonate as an antigelling agent. Instead of using an antigelling agent or using sodium (2S) -2- (2-oxopyrrolidin-1-yl) butyrate as an antigelling agent, the dissolution characteristics of the alagolica sodium tablet are significantly deteriorated.
Example 6: stability characteristics of the Alagox sodium tablets of examples 1-4
The chemical structural formula of the lactam impurity of the sodium elagose is shown as follows:
the lactam impurity content was determined using reverse phase High Performance Liquid Chromatography (HPLC) and detection with ultraviolet light (UV) at 275nm as described in CN 111698992. The HPLC system consisted of a C8 column with a flow rate of 1.1mL/min. Throughout the analysis, the column temperature was maintained at 50 ℃. Both mobile phases a and B were used, wherein mobile phase a was a triethylamine/acetic acid buffer solution at ph5.3 and the ratio of water to triethylamine to acetic acid was 100:0.1:0.06 (v/v) and mobile phase B was acetonitrile. The diluent is a 50:50 (v/v) ratio of triethylamine/acetic acid buffer and acetonitrile. The detection limit standard is prepared in a diluent having a known concentration of about 0.06 μg of alagolica sodium per ml.
The sodium esagole tablets of examples 1-4 were subjected to accelerated stability studies at 60 ℃ and 40% relative humidity, sampled over a defined period of time and analyzed using HPLC, and the results are shown in table 2.
Table 2: results of lactam impurity content test of the Alagox sodium tablets of examples 1 to 4
From the results of table 2, it is seen that the use of sodium 4- (2-oxopyrrolidin-1-yl) butyrate as an antigelling agent (example 1) resulted in a slow increase in lactam impurity after storage of the drug for a certain period of time, and that the effect of inhibiting the production of lactam impurity was significantly better than that of sodium carbonate (antigelling agent used in CN111698992, example 3) or sodium (2S) -2- (2-oxopyrrolidin-1-yl) butyrate (example 2).
Example 7: reproductive toxicity characteristics of the sodium Igacross tablet of example 1
Reproduction toxicity was tested in a repeat dose toxicity study in combination with reproduction/developmental toxicity screening test (Guideline for the testing of chemicals, combined Repeated Dose Toxicity Study with the Reproduction/Development Toxicity Screening Test) similar to the OECD422 method "chemical test guidelines. According to this test, the method comprises administering (preferably orally) test substances in graded doses to groups of male and female rats allowed to mate. The males under test will be dosed for a minimum of four weeks up to and including the day prior to the scheduled kill, including: a minimum of two weeks before mating, during the mating period, and about two weeks after mating. A combination of two weeks of pre-mating dosing period, followed by observation of mating and fertility during at least four weeks of total dosing, and then detailed histopathology of the male gonads is considered sufficient to be able to detect major effects on male fertility and spermatogenesis. Female rats were dosed throughout the study.
The sodium alagolide tablets according to the invention show no evidence of any reproductive toxicity when tested in Han Wistar rats according to OECD422 guidelines.
In the description of the specification, reference to the term "one embodiment," "a particular embodiment," "an example," etc., means that a particular feature, structure, material, or characteristic described in connection with the embodiment or example is included in at least one embodiment or example of the invention. In this specification, schematic representations of the above terms do not necessarily refer to the same embodiments or examples. Furthermore, the particular features, structures, materials, or characteristics described may be combined in any suitable manner in any one or more embodiments or examples.
The foregoing is merely illustrative and explanatory of the invention, as various modifications and additions may be made to the particular embodiments described, or by similar arrangements, by those skilled in the art, without departing from the scope of the invention or beyond the scope of the appended claims.

Claims (10)

1. An elargogue sodium tablet comprising elargogue sodium and an antigelling agent which is sodium 4- (2-oxopyrrolidin-1-yl) butyrate.
2. The sodium alagolide tablet of claim 1, wherein the weight ratio of the sodium alagolide to the antigelling agent is 1:1 to 20:1.
3. The sodium alagolide tablet of claim 1, wherein the weight ratio of the sodium alagolide to the antigelling agent is 4:1.
4. The sodium alagolide tablet of claim 1, wherein the sodium alagolide tablet comprises 10-40wt% of sodium alagolide.
5. The sodium alagolide tablet of claim 1, wherein the sodium alagolide tablet further comprises a pharmaceutically acceptable excipient.
6. The sodium alagolide tablet of claim 5, wherein the pharmaceutically acceptable excipients comprise one or more of fillers, binders, lubricants, disintegrants, glidants and surfactants.
7. The sodium alagolide tablet of claim 6, wherein the filler comprises one or more of starch, pregelatinized starch, mannitol, sorbitol, lactose, sucrose, microcrystalline cellulose, and calcium phosphate;
the adhesive comprises one or more of povidone, copovidone, polyacrylate, polymethacrylate, polyacrylamide, polyvinyl alcohol, vinyl acetate polymer, hydroxypropyl cellulose, hydroxypropyl methylcellulose, ethyl cellulose, oligosaccharides and polysaccharides;
the lubricant comprises one or more of magnesium stearate, calcium stearate, aluminum stearate, glyceryl monostearate, stearic acid and talcum powder;
the disintegrating agent comprises one or more of crospovidone, croscarmellose sodium, sodium carboxymethylcellulose, calcium carboxymethylcellulose, low-substituted hydroxypropyl cellulose and sodium starch glycolate;
the glidant comprises one or more of colloidal silicon dioxide and talcum powder;
the surfactant comprises one or more of polysorbate, sorbitan fatty acid, glyceride fatty acid, sucrose fatty acid ester, polyoxyethylene fatty alcohol ether, poloxamer, sodium dodecyl sulfate and sodium docusate.
8. The sodium alagolide tablet of claim 1, wherein the sodium alagolide tablet further comprises a coating.
9. The sodium alagolide tablet of claim 8, wherein the coating comprises one or a mixture of at least two of hypromellose, hydroxypropyl cellulose, methylcellulose, hydroxyethyl cellulose, polyethylene glycol, polyvinyl alcohol, and povidone.
10. A process for preparing the sodium alagolide tablet according to any one of claims 8 to 9, comprising the steps of mixing the sodium alagolide and the antigelling agent uniformly, granulating, mixing, tabletting and coating to obtain the sodium alagolide tablet.
CN202310462234.7A 2023-04-26 2023-04-26 Alagox sodium tablet and preparation process thereof Active CN116459225B (en)

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