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Naproxcinod self-emulsifying dripping pills and preparation method thereof

A naprocino and self-emulsifying technology, applied in the field of naprocino self-emulsifying dropping pills and preparation thereof, can solve the problems of low oral bioavailability of prototype drugs, difficulty in production and storage, unstable storage and the like, and achieve self-emulsion. The effect of shortening the emulsification time, high safety, and improving the oral absorption effect

Inactive Publication Date: 2012-07-11
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, according to Fagerholm's literature (Journal of Pharmacy and Pharmacology, 2005, 57: 1539-1554) and the clinical pharmacokinetic data of naproxil self-emulsifying preparations provided by the FDA, the clinical use dose of naproxil is as high as 375-500 mg. 750mg, the complete dissolution rate of SEDDS in vitro self-emulsification is slow (about 100 minutes), the particle size is larger after self-emulsification, the oral bioavailability of the original drug is low (about 20%), and it is a semi-solid emulsion pre-concentration There are certain difficulties in production and storage
Therefore the naproxino SEDDS that above-mentioned patent relates to still needs to be improved
In addition, FDA data shows that since the self-emulsifying prescription is poured into the capsule, the storage is unstable (it should be caused by the gelatin crosslinking of the capsule shell, which is caused by the inherent nature of the prescription itself after the self-emulsifying prescription is poured into the capsule), so PABA must be added as a Stabilizers, which also complicate the preparation of the formulation and drive up the cost

Method used

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  • Naproxcinod self-emulsifying dripping pills and preparation method thereof
  • Naproxcinod self-emulsifying dripping pills and preparation method thereof
  • Naproxcinod self-emulsifying dripping pills and preparation method thereof

Examples

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Embodiment 1

[0038]

[0039]

[0040] Preparation method: Heat polyethylene glycol 4000 and polyethylene glycol 6000 to about 80°C, add poloxamer 407 and naproxino, stir continuously to melt them all, put them in a storage bottle, and keep warm at 80°C. Drop into liquid paraffin at 2°C by drop method, and condense into pellets. Use filter paper to suck off the adhering liquid paraffin to obtain naproxil self-emulsifying dropping pill 1 of the present invention.

Embodiment 2

[0042]

[0043] Preparation method: Heat polyethylene glycol 6000 to about 80°C, add poloxamer 407, polyoxyethylene sorbitan monooleate and naproxino, stir continuously to melt all, and place in a storage bottle , 80 ℃ insulation. Drop into liquid paraffin at 2°C by drop method, and condense into pellets. Use filter paper to suck off the adhering liquid paraffin to obtain naproxil self-emulsifying dropping pill 2 of the present invention.

Embodiment 3

[0045]

[0046] Preparation method: heat polyethylene glycol 4000 to about 80°C, add poloxamer 188, polyoxyethylene hydrogenated castor oil and naprocinov, stir continuously to melt all, put in a storage bottle, and keep warm at 80°C . Drop into liquid paraffin at 5°C by drop method, and condense into pellets. Use filter paper to suck off the adhering liquid paraffin to obtain naproxil self-emulsifying dropping pill 3 of the present invention.

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Abstract

The invention relates to naproxcinod self-emulsifying dripping pills and a preparation method of the naproxcinod self-emulsifying dripping pills. The naproxcinod self-emulsifying dripping pills comprise an active substance naproxcinod, an emulsifier and a dripping pill matrix. The self-emulsifying dripping pills rapidly self-emulsify to form an oil-in-water emulsion when contacting with an aqueous medium. The preparation method of the naproxcinod self-emulsifying dripping pills comprises the steps of adding naproxcinod and the emulsifier into the melting matrix, dripping and carrying out condensation in a coolant to obtain the dripping pills. The self-emulsifying dripping pills provided by the invention can improve bioavailability, are convenient in storage and transportation, and have good control for production process.

Description

technical field [0001] The invention relates to a naproxino self-emulsifying dropping pill and a preparation method thereof. Background technique [0002] Naproxcinod (I) is a well-known non-steroidal anti-inflammatory drug for the treatment of pain and inflammation, and is widely used due to its mild gastrointestinal side effects. It is a lipophilic oily compound with poor water solubility and fairly good penetration. Its absorption in the gastrointestinal tract after oral administration may be limited by the dissolution rate, resulting in poor bioavailability. [0003] [0004] For high doses of naproxil, such as when the dose exceeds about 350 mg, it is somewhat challenging to formulate such a large amount of oily or semi-solid material into a suitable formulation. WO2001 / 066087 applied by NicOx Company discloses a self-emulsifying drug delivery system (SEDDS) emulsion pre-concentrate of naproxino, which includes at least an active compound and a surfactant. The com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/216A61P29/00
Inventor 孙飘扬卢韵韩晓王菊陈永江
Owner JIANGSU HENGRUI MEDICINE CO LTD