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New self emulsifying drug delivery system

A drug release technology, applied in the field of new self-emulsifying drug release system, can solve problems such as poor long-term storage stability, unpleasant bitter or soapy taste, thermodynamic instability, etc.

Inactive Publication Date: 2003-05-07
NICOX SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the problem with emulsions is that they are thermodynamically unstable and have poor long-term storage stability as they often tend to coalesce, emulsion stratification / precipitation or phase separation
Furthermore, they do not represent a convenient oral dosage form, as large volumes are required to incorporate a dose, and an unpleasant bitter or soapy taste can also be a major problem

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] amount [g]

[0087] (i) compound of formula (Ia) 1000

[0088] (ii) Pluronic F127  1000

[0089] Melt 1kg of Pluronic F127 by heating to 62°C  (poloxamer 407) to obtain a semi-solid preparation. The melt was stirred thoroughly to ensure that no solid particles were present.

[0090] 1kg formula (Ia) compound is added to the Pluronic F127 of melting  medium and bring the mixture to 62 °C. The liquid formulation was mixed until homogeneous (visual inspection). The resulting liquid formulation is then filled into hard gelatin capsules. Upon cooling, the formulation becomes semi-solid (in the capsule). Characteristic analysis

[0091] 150 mg of the formulation was placed in 12.5 mL of SGF (without enzyme) and magnetically stirred. The following results are obtained:

[0092] Emulsification time: 13 minutes

[0093] Average particle size: 2-3μm

[0094] Viscosity was determined in a Stress Tech cone and plate viscometer with a C 40 4 PC meas...

Embodiment 2

[0095] amount [g]

[0096] (i) compound of formula (Ia) 1000

[0097] (ii) Pluronic L121  1000

[0098] A liquid formulation was prepared by mixing 1 kg of the liquid surfactant Poloxamer 401 with 1 kg of the compound of formula (Ia) at room temperature. The liquid formulation was mixed until homogeneous (visual inspection). The resulting liquid formulation is then filled into hard gelatin capsules. Characteristic Analysis

[0099] 150 mg of the formulation was placed in 12.5 mL of SGF (without enzyme) and magnetically stirred. The following results are obtained:

[0100] Emulsification time: 20 seconds

Embodiment 3

[0102] amount [g]

[0103] (i) compound of formula (Ia) 1000

[0104] (ii) Polyglycol BM 45  1000

[0105] (iii) Sodium lauryl sulfate 40

[0106] Mix 1kg Polyglycol BM 45  (Poloxamine 1107), 40 g of sodium lauryl sulfate as cosurfactant and 1 kg of compound of formula (Ia) to obtain a formulation. The liquid formulations were mixed until homogeneous (by visual inspection). The resulting liquid formulation is then filled into hard gelatin capsules. Characteristic Analysis

[0107] 150 mg of the formulation was placed in 12.5 mL of SGF (without enzyme) and magnetically stirred. The following results are obtained:

[0108] Emulsification time: 15 minutes

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PUM

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Abstract

The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) one or more NO-releasing NSAID(s); (ii) one or more surfactants; (iii) optionally an additional oil or semi-solid fat; said composition forming an in-situ oil-in-water emulsion upon contact with gastrointestinal fluids. The composition may optionally also comprise one or more short-chain alcohols. Also within the scope of the invention is a combination with a proton pump inhibitor. The pharmaceutical composition is useful in the treatment of pain and inflammation. Further within the scope of the invention is kit comprising a pharmaceutical composition according to the invention in a unit dosage form, in combination with a proton pump inhibitor, and said proton pump inhibitor is enteric coated

Description

field of invention [0001] The present invention relates to novel pharmaceutical compositions in the form of emulsion preconcentrates, unit dosage forms comprising said compositions, their use in therapy and processes for their preparation. Background technique [0002] Non-steroidal anti-inflammatory drugs, often abbreviated NSAIDs, are well-known drugs used to treat pain and inflammation. One of the major disadvantages of NSAIDs is that they have serious gastrointestinal side effects. Patients on long-term treatment with NSAIDs, such as naproxen, often suffer from problems with gastrointestinal side effects. [0003] It has recently been found that nitric oxide releasing NSAID compounds (hereinafter referred to as NO-releasing NSAIDs) have reduced side effects, see eg WO 94 / 04484, WO 94 / 12463, WO 95 / 09831 and WO 95 / 30641. [0004] NO-releasing NSAIDs are lipophilic compounds with poor water solubility. According to the biopharmaceutical classification system (Biopharmace...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/08A61K9/113A61K9/20A61K9/48A61K9/50A61K9/68A61K31/21A61K31/215A61K31/216A61K31/407A61K31/4439A61K45/06A61K47/10A61K47/14A61K47/34A61K47/44A61P25/02A61P29/00
CPCA61K45/06A61K31/216A61K9/5084A61K9/107A61K31/407A61K31/21A61K9/4858A61K9/4866A61P25/00A61P25/02A61P29/00
Inventor C·霍姆贝里B·西克曼
Owner NICOX SA