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Anti-inflammatory composition and preparation method thereof

A technology of composition and crystallization inhibitor, which is applied in anti-inflammatory agents, drug combinations, pharmaceutical formulas, etc., can solve problems affecting patient compliance, capsules cannot be filled, and tablet weight is too large, so as to improve the stability of the dissolution platform , Improve bioavailability, reduce the effect of carrier usage

Pending Publication Date: 2021-11-23
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the amount of carrier used in this scheme is large, and the technical effect of reducing the amount of carrier while increasing solubility cannot be achieved, that is, the technical effect of improving the solubility of insoluble drugs, increasing drug loading, and reducing the amount of carrier
[0005] The existing technology of celecoxib preparations has problems such as large size, low solubility, low bioavailability, slow onset of action, low drug loading in solid dispersion, and large amount of carrier
In solid dispersion technology, the level of drug loading has a great influence on the preparation of the final preparation. When the carrier ratio is too high, that is, the drug loading is low, the weight ratio of the prepared solid dispersion particles in the final preparation If the weight of the tablet is too large, it will lead to problems such as the weight of the single-dose tablet is too large or the capsule cannot be filled; and if the prepared tablet is too heavy, it is not conducive to the patient's swallowing and affects the patient's compliance

Method used

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  • Anti-inflammatory composition and preparation method thereof
  • Anti-inflammatory composition and preparation method thereof
  • Anti-inflammatory composition and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment 1: HPMCAS single carrier prescription

[0075] Solid dispersion preparation: adopt the hot melt extrusion process to prepare the solid dispersion according to the following formula:

[0076]

[0077] Dissolution results: Take the solid dispersions of the above prescriptions 1-8, place them in dissolution cups containing 1000mL of pH 6.8 buffer salt dissolution medium, rotate at 50rpm, and temperature 37°C, respectively for 10min, 20min, 30min, Sampling 2mL at 60min, and supplementing 2mL of dissolution medium respectively at the same time, the sampled 2mL was filtered through a 0.45μm microporous membrane, and the filtrate was then used to measure the content of celecoxib by high performance liquid chromatography, and calculate the dissolution percentage. The dissolution results are shown in the following table shown.

[0078]

[0079] in conclusion:

[0080] (1) For prescriptions 1-3, when the drug loading ratio is fixed at 1:1, appropriately increas...

Embodiment 2

[0083] Embodiment 2: PVPVA64 single carrier prescription

[0084] Solid dispersion preparation: adopt the hot melt extrusion process to prepare the solid dispersion according to the following formula:

[0085]

[0086] Dissolution result: get the solid dispersion of above-mentioned prescription 9-18, carry out dissolution in the phosphate buffer solution of pH6.8 (dissolution condition is the same as embodiment 1), its dissolution result is shown in the following table.

[0087]

[0088] in conclusion:

[0089] (1) The prescription of PVPVA64 single carrier can achieve better dissolution results only when the drug-loading ratio (1:5) is below and the prescription (prescription 17) with TPGS is added; the high drug-loading ratio (1:1-1 :4), especially the formulations with a drug-loading ratio of 1:1-1:3 have poor dissolution results.

[0090] (2) In PVPVA64 single-vehicle formulations (prescriptions 9-12) with a drug-loading ratio of 1:1-1:2, the addition of TPGS had n...

Embodiment 3

[0091] Embodiment 3: Dissolution and stability results of tablets prepared by prescription 15

[0092] Preparation of tablets: Take the solid dispersion described in prescription 15, microcrystalline cellulose, sodium chloride, croscarmellose sodium and magnesium stearate, and press the following prescription to prepare celecoxib piece:

[0093] Tablet components Prescription ratio (%) Solid dispersion as described in prescription 15 62.50 microcrystalline cellulose 22.00 Sodium chloride 10.00 Croscarmellose Sodium 5.00 Magnesium stearate 0.50 total 100.00

[0094] Stability results: the above tablets were placed in accelerated conditions (40°C, 75%RH) for 1, 2, 3, and 6 months, and placed in long-term conditions (25°C, 60%RH) for 3, 6 months, and samples were taken Carry out content, related substance and dissolution detection (dissolution condition is the same as embodiment 1), and its result is as shown in table 1-table 4...

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Abstract

The invention relates to an anti-inflammatory composition and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The composition comprises a pharmaceutical active ingredient, a surfactant, a crystallization inhibitor and optional other pharmaceutically acceptable auxiliary materials. The invention also discloses a preparation method of the composition. The composition disclosed by the invention has the advantages of high solubility, high dissolution speed, high dissolution platform, high bioavailability, good stability, high disintegration speed, capability of improving the drug loading capacity while keeping high bioavailability, and the like.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an anti-inflammatory composition and a preparation method thereof. Background technique [0002] Celecoxib is a specific non-steroidal anti-inflammatory analgesic commonly used in clinical practice. Compared with traditional non-steroidal anti-inflammatory drugs, celecoxib specifically inhibits cyclooxygenase-2 (COX -2) Blocking the synthesis of prostaglandins from arachidonic acid to exert an anti-inflammatory effect, it does not act on COX-1, does not affect the synthesis of PGI2, which has a protective effect on the gastrointestinal tract and kidneys, and can effectively reduce the side effects of the gastrointestinal tract. It is commonly used clinically to treat acute pain in adults, relieve symptoms and signs of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis; it was launched in the United States in 1999 and is approved for sale in my country. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/635A61K47/22A61K47/32A61K47/38A61P29/00
CPCA61K31/635A61K47/32A61K47/38A61K47/22A61P29/00
Inventor 于丽萍汪志辉黄心石添香游劲松黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD
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