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Pharmaceutical formulation of clavulanic acid

A technology of clavulanic acid and clavulanic acid potassium, applied in the field of depression, immediate release composition and sustained release composition, sexual dysfunction and neurological disorders, and treatment of anxiety, which can solve problems such as no CNS effect

Inactive Publication Date: 2010-12-15
REXAHN PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

β-lactam antibiotics have become the most widely used antibiotics since the first discovery of penicillin in 1928, but have not shown significant toxic CNS effects at standard antimicrobial doses

Method used

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  • Pharmaceutical formulation of clavulanic acid
  • Pharmaceutical formulation of clavulanic acid
  • Pharmaceutical formulation of clavulanic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: the preparation of clavulanic acid substance tablet

[0065] Example 1A - Preparation of Immediate Release Clavulanic Acid Using Potassium Clavulanate Powder Qualitative tablet

[0066] Illustrative description of tablet manufacturing process: A wet granulation tablet formulation process has been found in which water is included in the granulation step followed by drying to obtain granules with low moisture content (<3%). The dry formulations are non-hygroscopic compared to prior art formulations, but maintain equivalent physical properties (eg, solubility, disintegration, bioavailability, and other physical properties) of tablets made from them. Tablet preparation is carried out by granulating the clavulanic acid with water in the presence of a binder / diluent.

[0067] For the preparation of sample C, Maltrin M150 (130 g) was dissolved in purified water and potassium clavulanate (API; 59.5 g) was added. Prosolve SMCC-50 (490.5g), Pharmaburst (130.0g...

Embodiment 1D

[0072] Example 1D - Preparation of slow-release clavulanates using potassium clavulanate powder Qualitative tablet

[0073] For the preparation of sample G for extended release tablets using potassium clavulanate, potassium clavulanate (API; 20.69g) was sieved through a #60 mesh sieve, while other excipients, Methocel K100LVPrem CR (90.02g), Isomalt (83.56g), Avicel PH-112 (100.41g), Cabosil (1.52g), talc (2.4g) and magnesium stearate (1.5g) were sieved through a #40 mesh sieve. Each component was collected in a separate bag. The API and Methocel K100LV Prem CR were loaded into a V-type mixer and mixed for 5 minutes. The mixture was sieved and mixed for an additional 5 min. Avicel PH-112 and Isomalt were added to the mixture and mixed in a V-blender for 5 minutes. The resulting mixture was sieved and mixed for an additional 5 min. Cabosil and talc were mixed and added to the mixture and the resulting mixture was then mixed for 2 min. Finally, magnesium stearate was bl...

Embodiment 2

[0074] Example 2: Clavulanates thing qualitative analysis

[0075] Clavulanates of the prepared pharmaceutical composition thing The content of the substance was passed through the Waters HPLC (high performance liquid chromatography) system (column: μ Bondapack-NH 2 (10μm)300mm×3.9mm, mobile phase: CH 3 CN: pH 5.2KH 2 PO 4 =65:35, flow rate: 1.0ml / min) The following steps were used for the determination: about 10 tablets were accurately weighed and crushed, 100 mL of water was added and the mixture was sonicated for 20 min. After dilution with water, a portion of the solution was filtered and injected into HPLC. The main peak is determined by the retention time of the sample corresponding to the chromatogram of the HPLC standard preparation. Clavulanates thing The mass % is calculated based on the response factor of the analyte relative to the response factor of the reference standard.

[0076] Clavulanates thing The linearity of the quality standard curve was tes...

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Abstract

The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as potassium clavulanate or ClavitesseTM, preferably in an immediate-release solid dosage form or an extended-release solid dosage form. Also provided are methods for making and using such immediate-release and stabilized compositions or extended-release and stabilized compositions.

Description

technical field [0001] The present invention relates to solid oral dosage forms containing clavulanic acid, pharmaceutically acceptable clavulanate salts, salt compositions and derivatives. In particular, the present invention provides immediate release and sustained release compositions of potassium clavulanate suitable for daily use and achieving therapeutic levels of clavulanate. The invention also relates to a process for its preparation and to its use as a medicament, for example, for the treatment of anxiety, depression, sexual dysfunction and neurological disorders. Background technique [0002] Clavulanic acid gets its name from the microorganism Streptomyces clavuligerus that produces it. Clavulanic acid is produced biosynthetically from the amino acid arginine and the sugar glyceraldehyde 3-phosphate. [0003] Clavulanic acid has negligible intrinsic antimicrobial activity despite the β-lactam ring characteristic of β-lactam antibiotics. However, similarities in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/70
CPCA61K9/1694A61K9/2054A61K9/205A61K31/70A61K31/424A61K9/2027
Inventor 李永福金德中安昌浩爱德华·卡尔·朔尔茨
Owner REXAHN PHARMA INC
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