CN-122005476-A - Dexketoprofen tromethamine sustained release tablet and preparation method thereof

Abstract

The invention discloses a dexketoprofen tromethamine sustained release tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The invention relates to a dexketoprofen tromethamine sustained release tablet which is prepared from dexketoprofen tromethamine, sustained release framework material, stabilizing agent, filling agent, adhesive and lubricant, wherein the sustained release framework material is selected from the combination of hypromellose, polyethylene glycol 6000, tragacanth and shellac, the stabilizing agent is a compound system of meglumine, vitamin E and proline, and the sustained release tablet is prepared by adopting a wet granulation process. The sustained release tablet can show stable release trend in different pH environments, has no release stagnation or abrupt release phenomenon, has excellent storage stability, can meet clinical medication requirements, and improves medication compliance and safety of patients.

Inventors

• XUE LEI

Assignees

• 常州市武进人民医院(常州市第八人民医院)

Dates

Publication Date

20260512

Application Date

20260304

Claims (10)

1. 1. The sustained release tablet is characterized by comprising, by weight, 8-15 parts of dexketoprofen tromethamine, 20-35 parts of sustained release framework materials, 1-3 parts of stabilizers, 30-50 parts of fillers, 2-5 parts of adhesives and 0.3-1.5 parts of lubricants.
2. 2. The sustained release tablet of dexketoprofen tromethamine according to claim 1, wherein the filler is at least one of lactose, microcrystalline cellulose, mannitol.
3. 3. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the binder is one of povidone K30 and hydroxypropyl cellulose.
4. 4. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the lubricant is at least one of micro powder silica gel, talcum powder and magnesium stearate.
5. 5. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the sustained release matrix material is at least one of hypromellose, polyethylene glycol 6000, tragacanth, shellac.
6. 6. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the stabilizer is selected from the group consisting of meglumine, vitamin E and proline.
7. 7. The sustained release tablet of dexketoprofen tromethamine according to claim 6, wherein the stabilizer comprises 0.25-0.5 parts of meglumine, 0.5-1.5 parts of vitamin E and 0.25-1 part of proline.
8. 8. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the sustained release matrix material is: the combination comprises polyethylene glycol 6000, tragacanth gum and shellac; the combination of the two components is hydroxypropyl methylcellulose, tragacanth gum and shellac.
9. 9. The dexketoprofen tromethamine sustained release tablet according to claim 8, wherein the sustained release matrix material is: The combination comprises polyethylene glycol 6000 10-20 parts, tragacanth gum 4-6 parts and shellac 6-9 parts; 10-20 parts of hydroxypropyl methylcellulose, 4-6 parts of tragacanth and 6-9 parts of shellac.
10. 10. The dexketoprofen tromethamine sustained release tablet according to claim 1, wherein the preparation method of the dexketoprofen tromethamine sustained release tablet is wet granulation.

Description

Dexketoprofen tromethamine sustained release tablet and preparation method thereof Technical Field The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a dexketoprofen tromethamine sustained release tablet and a preparation method thereof. Background Dexketoprofen tromethamine is a non-steroidal anti-inflammatory drug, and plays remarkable anti-inflammatory, analgesic and antipyretic roles by selectively inhibiting the activity of cyclooxygenase-2 (COX-2), and meanwhile, has weaker inhibition effect on cyclooxygenase-1 (COX-1) for maintaining normal physiological functions of gastrointestinal tract and kidney, so that compared with traditional non-selective NSAIDs, the incidence rate of adverse reactions of the gastrointestinal tract is remarkably reduced by 30% -40%, and the safety is higher. The composition is mainly used for treating joint pain caused by rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gouty arthritis and the like, and various acute and chronic pains such as dysmenorrhea, toothache, postoperative pain, cancer pain, acute sprain or soft tissue contusion pain, general pain caused by cold fever and the like, and can also be used as an auxiliary opioid analgesic for acute moderate to severe postoperative pain which is not suitable for oral administration for adults. Currently, the marketed dosage forms of dexketoprofen tromethamine mainly comprise ordinary tablets, capsules and injections. The common tablet and capsule are rapidly absorbed after oral administration, and the peak concentration of the blood can be reached after the healthy subjects take 12.5mg or 25mg for a single time, but the half-life period is shorter and is about 1.6-1.9 hours, so that the patients need frequent administration (usually 3-4 times per day), the medication compliance of the patients is reduced, the severe fluctuation of the blood concentration can be caused, the adverse reaction risk can be increased in the peak concentration, and the pain symptoms can not be effectively controlled in the valley concentration. The injection has quick response, needs to be operated by a professional medical staff, is only used for a short period, is not suitable for long-term treatment of chronic pain, and has adverse reactions such as pain and inflammation at an injection part. In order to solve the problems, the development of a sustained release preparation becomes an important direction for improving the formulation of the dexketoprofen tromethamine. In the prior art, chinese patent publication No. CN106137997A discloses a sustained release tablet of dexketoprofen tromethamine, which is prepared by directly tabletting a composition of a framework material, a lubricant, a glidant, PC-10 and Equid EPO. The Chinese patent with publication number CN108542889A discloses a dextro-ketoprofen tromethamine gastric-retention slow-release tablet, which consists of dextro-ketoprofen tromethamine, hydrophilic gel auxiliary materials, microcrystalline cellulose and magnesium stearate, and can fully absorb gastric juice after oral administration, expand to form hydrogel, control drug release speed and gastric-retention effect, and achieve slow-release effect. But has the following problems that (1) the release behavior difference is large in different pH value environments, particularly, the release of the drug is stagnated in an acidic medium and the drug is suddenly released after entering a neutral or alkaline medium, and (2) the existing slow release preparation is not subjected to targeted formula design aiming at the instability characteristic of dexketoprofen tromethamine, and lacks effective stabilization means, so that the preparation has a short effective period and is difficult to adapt to the requirements of large-scale production, long-term storage and clinical long-term medication. Therefore, the development of the dexketoprofen tromethamine sustained release tablet which can be stably released in different pH environments and has excellent stability has important significance for meeting clinical requirements and improving the medication safety and compliance of patients, and is also a technical problem to be solved in the field. Disclosure of Invention The invention overcomes the technical defects that the release behavior of a dexketoprofen tromethamine sustained release preparation in the prior art is greatly influenced by pH and the stability of the preparation is insufficient, and provides a dexketoprofen tromethamine sustained release tablet which can be stably released in different pH environments and has excellent storage stability and a preparation method thereof, so as to meet clinical medication requirements and improve medication compliance and safety of patients. In order to achieve the aim of the invention, the invention adopts the following technical scheme: Prescription composition of dexketoprofen tromethamine sustained release tablet The d