Solid dose nanoparticulate compositions comprising a...

Details Solid dose nanoparticulate compositions comprising a... Solid dose nanoparticulate compositions comprising a...

2000-09-21

2002-04-23

Dudash, Diana (Department: 1619)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

C424S466000, C424S464000, C424S434000, C424S044000, C424S043000, C514S535000

Reexamination Certificate

active

06375986

ABSTRACT:

FIELD OF THE INVENTION
The present invention is directed to solid dose nanoparticulate compositions having a synergistic combination of at least one polymeric surface stabilizer and dioctyl sodium sulfosuccinate (DOSS). The solid dose compositions exhibit superior redispersion of the nanoparticulate composition either upon administration to a mammal, such as a human or animal, or reconstitution in an aqueous electrolyte solution.
BACKGROUND OF THE INVENTION
A. Background Regarding Nanoparticulate Compositions
Nanoparticulate compositions, first described in U.S. Pat. No. 5,145,684 (“the '684 patent”), are particles consisting of a poorly soluble therapeutic or diagnostic agent having adsorbed onto the surface thereof a non-crosslinked surface stabilizer. This invention is an improvement over that disclosed in the '684 patent, as the '684 patent does not describe the use of synergistic combinations of polymeric surface stabilizers and DOSS in solid dose compositions.
Prior U.S. patents teach the use of DOSS as a primary or secondary surface stabilizer for nanoparticulate compositions. See e.g., U.S. Pat. No. 5,145,684, for “Surface Modified Drug Nanoparticles;” U.S. Pat. No. 5,302,401, for “Method to Reduce Particle Size Growth During Lyophilization;” U.S. Pat. No. 5,318,767, for “X-Ray Contrast Compositions Useful in Medical Imaging;” U.S. Pat. No. 5,336,507, for “Use of Charged Phospholipids to Reduce Nanoparticle Aggregation;” U.S. Pat. No. 5,346,702, for “Use of Non-Ionic Cloud Point Modifiers to Minimize Nanoparticulate Aggregation During Sterilization;” U.S. Pat. No. 5,399,363, for “Surface Modified Anticancer Nanoparticles;” U.S. Pat. No. 5,401,492, for “Water-Insoluble Non-Magnetic Manganese Particles as Magnetic Resonance Enhancement Agents;” U.S. Pat. No. 5,429,824, for “Use of Tyloxapol as a Nanoparticulate Stabilizer;” U.S. Pat. No. 5,451,393, for “X-Ray Contrast Compositions Useful in Medical Imaging;” U.S. Pat. No. 5,466,440, for “Formulations of Oral Gastrointestinal Diagnostic X-Ray Contrast Agents in Combination with Pharmaceutically Acceptable Clays;” U.S. Pat. No. 5,470,583, for “Method of Preparing Nanoparticle Compositions Containing Charged Phospholipids to Reduce Aggregation;” U.S. Pat. No. 5,494,683, for “Surface Modified Anticancer Nanoparticles;” U.S. Pat. No. 5,503,723, for “Isolation of Ultra Small Particles;” U.S. Pat. No. 5,510,118, for “Process for Preparing Therapeutic Compositions Containing Nanoparticles;” U.S. Pat. No. 5,543,133, for “Process of Preparing X-Ray Contrast Compositions Containing Nanoparticles;” U.S. Pat. No. 5,552,160, for “Surface Modified NSAID Nanoparticles;” U.S. Pat. No. 5,560,931, for “Formulations of Compounds as Nanoparticulate Dispersions in Digestible Oils or Fatty Acids;” U.S. Pat. No. 5,560,932, for “Microprecipitation of Nanoparticulate Pharmaceutical Agents;” U.S. Pat. No. 5,571,536, for “Formulations of Compounds as Nanoparticulate Dispersions in Digestible Oils or Fatty Acids;” U.S. Pat. No. 5,580,579, for “Site-Specific Adhesion Within the GI Tract Using Nanoparticles Stabilized by High Molecular Weight, Linear Poly(ethylene Oxide) Polymers;” U.S. Pat. No. 5,587,143, for “Butylene Oxide-Ethylene Oxide Block Copolymer Surfactants as Stabilizer Coatings for Nanoparticulate Compositions;” U.S. Pat. No. 5,593,657, for “Novel Barium Salt Formulations Stabilized by Non-Ionic and Anionic Stabilizers;” U.S. Pat. No. 5,628,981, for “Improved Formulations of Oral Gastrointestinal Diagnostic X-Ray Contrast Agents and Oral Gastrointestinal Therapeutic Agents;” U.S. Pat. No. 5,665,331, for “Co-Microprecipitation of Nanoparticulate Pharmaceutical Agents with Crystal Growth Modifiers;” U.S. Pat. No. 5,716,642, for “Microprecipitation of Nanoparticulate Pharmaceutical Agents Using Surface Active Material Derived from Similar Pharmaceutical Agents;” U.S. Pat. No. 5,718,919, for “Nanoparticles Containing the R(−) Enantiomer of Ibuprofen;” U.S. Pat. No. 5,747,001, for “Aerosols Containing Beclomethasone Nanoparticle Dispersions;” U.S. Pat. No. 5,834,025, for “Reduction of Intravenously Administered Nanoparticulate Formulation Induced Adverse Physiological Reactions;” U.S. Pat. No. 6,045,829, for “Nanocrystalline Formulations of Human Immunodeficiency Virus (HIV) Protease Inhibitors Using Cellulosic Surface Stabilizers;” and U.S. Pat. No. 6,068,858, for “Methods of Making Nanocrystalline Formulations of Human Immunodeficiency Virus (HIV) Protease Inhibitors Using Cellulosic Surface Stabilizers.” In addition, several published international applications teach the usefulness of DOSS as a primary or secondary surface stabilizer for nanoparticulate compositions. See e.g., WO 98/35666, for “Formulations of Nanoparticle Naproxen Tablets;” WO 00/18374, for “Controlled Release Nanoparticulate Compositions;” WO 96/25918, for “Aerosols Containing Nanoparticulate Dispersions;” and WO 00/27363, for “Aerosols Comprising Nanoparticle Drugs.”
Prior art patents also teach the use of DOSS as a cloud point modifier for nanoparticulate surface stabilizers. See e.g., U.S. Pat. No. 5,298,262, for “Use of Ionic Cloud Point Modifiers to Prevent Particle Aggregation During Sterilization;” U.S. Pat. No. 5,326,552, for “Novel Formulation for Nanoparticulate X-Ray Blood Pool Contrast Agents Using High Molecular Weigh Non-ionic Surfactants;” U.S. Pat. No. 5,346,702, for “Use of Non-Ionic Cloud Point Modifiers to Minimize Nanoparticulate Aggregation During Sterilization;” U.S. Pat. No. 5,352,459, for “Use of Purified Surface Modifiers to Prevent Particle Aggregation During Sterilization;” U.S. Pat. No. 5,447,710, for “Method for Making Nanoparticulate X-Ray Blood Pool Contrast Agents Using High Molecular Weight Non-Ionic Surfactants;” U.S. Pat. No. 5,565,188, for “Polyalkylene Block Copolymers as Surface Modifiers for Nanoparticles;” U.S. Pat. No. 5,665,330, for “Dual Purpose Diagnostic/Therapeutic Agent Having a Tri-Iodinated Benzoyl Group Linked to a Coumarin.”
And several prior art references teach the use of DOSS in nanoparticulate compositions as both a surface stabilizer and as a cloud point modifier for a primary surface stabilizer. See e.g., U.S. Pat. No. 5,466,433, for “Polyiodinated Aroyloxy Esters;” U.S. Pat. No. 5,472,683, for “Nanoparticle Mixed Carbamic Anhydrides as X-Ray Contrast Agents for Blood Pool and Lymphatic System Imaging;” U.S. Pat. No. 5,500,204, for “Nanoparticulate Diagnostic Dimers as X-Ray Contrast Agents for Blood Pool and Lymphatic System Imaging;” U.S. Pat. No. 5,521,218, for “Nanoparticulate Iododipamide Derivatives for Use as X-Ray Contrast Agents;” U.S. Pat. No. 5,525,328, for “Nanoparticulate Diagnostic Diatrizoxy Ester X-Ray Contrast Agents for Blood Pool and Lymphatic Systems Imaging;” U.S. Pat. No. 5,534,270, for “Method of Preparing X-Ray Contrast Compositions Containing Nanoparticles;” U.S. Pat. No. 5,573,749, for “Nanoparticulate Diagnostic Mixed Carboxylic Anhydrides as X-Ray Contrast Agents for Blood Pool and Lymphatic System Imaging;” U.S. Pat. No. 5,573,750, for “Diagnostic Imaging X-Ray Contrast Agents;” U.S. Pat. No. 5,603,916, for “3,5-Bis-[Alkanoyl Amino]-2,4,6-Triiodobenzyl Esters;” U.S. Pat. No. 5,643,552, for “Nanoparticulate Diagnostic Mixed Carbonic Anhydrides as X-Ray Contrast Agents for Blood Pool and Lymphatic System Imaging;” U.S. Pat. No. 5,668,196, for “3-Amido-Triiodophenyl Esters as X-Ray Contrast Agents;” and U.S. Pat. No. 5,670,136, for “2,4,6-Triiodo-5-Substituted-Amino-Isophthalate Esters Useful as X-Ray Contrast Agents for Medical Diagnostic Imaging.”
U.S. Pat. No 5,585,108, for “Formulations of Oral Gastrointestinal Therapeutic Agents in Combination with Pharmaceutically Acceptable Clays,” claims a nanoparticulate dispersion including, inter alia, a water-insoluble particulate drug, a surfactant which can be a polymeric stabilizer, such as hydroxypropyl methylcellulose, a pharmaceutically acceptable clay, and a secondary stabilizer, such as DOSS or sodium lauryl sulfate. See col. 7 of the patent. This reference differs from the present invention in that it is

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