{
  "patent_number": "US 4727064",
  "country": "US",
  "title": "How Special Sugars Make Medicines Dissolve Better",
  "original_title": "Pharmaceutical preparations containing cyclodextrin derivatives",
  "summary": "This patent describes how to make poorly water-soluble drugs dissolve and absorb better by mixing them with specially modified, non-crystalline sugar molecules called cyclodextrin derivatives.",
  "what_it_does": "The patent describes a way to create a stable drug mixture that helps medicines dissolve in the body. It starts with a special type of sugar molecule, called a cyclodextrin derivative, which has been chemically changed to be water-soluble and non-crystalline (amorphous). These modified cyclodextrins are dissolved in water (Claim 1, step 1). Then, a drug that doesn't dissolve well in water, like a hormone such as testosterone (Claim 5), is added to this solution. The cyclodextrins wrap around the drug molecules, forming a \"solubilized drug/cyclodextrin complex\" (Claim 1, step 2) that dissolves much better. This improved dissolution helps the body absorb the medicine more effectively. The resulting complex can be dried into a powder (Claim 2) or used in liquid form (Claim 11).",
  "what_it_does_not_cover": [
    "Does not cover using cyclodextrins that are not chemically modified derivatives (e.g., plain alpha, beta, or gamma cyclodextrins).",
    "Does not cover drug-cyclodextrin complexes that are crystalline rather than amorphous.",
    "Does not cover drugs that are already highly water-soluble.",
    "Does not cover methods where the cyclodextrin mixture is not intrinsically amorphous before complexing with the drug.",
    "Does not cover cyclodextrin derivatives made using alkylation agents other than those exemplified (e.g., propylene oxide, glycidol, iodoacetamide, chloroacetate, 2-diethylaminoethylchloride) or similar non-selective alkylation processes."
  ],
  "filed": "1985-05-29",
  "granted": "1988-02-23",
  "expires": null,
  "status": "active",
  "holder": "US Department of Health and Human Services",
  "holder_url": "https://patentbrief.org/company/us-department-of-health-and-human-services",
  "inventors": [
    {
      "name": "Josef Pitha",
      "url": "https://patentbrief.org/inventor/josef-pitha"
    }
  ],
  "times_cited": 341,
  "tags": [
    "pharmaceutical",
    "biotech",
    "materials",
    "chemistry"
  ],
  "abstract": "The invention comprises pharmaceutical preparations consisting generally of a drug with a substantially low water solubility and an amorphous, water-soluble cyclodextrin-based mixtures. In these preparations a stable amorphous state can be achieved. This improves the dissolution properties of the drug and hence its absorption by the body. The required cyclodextrin-based mixtures were prepared from alpha -, beta -, or gamma -cyclodextrin which were rendered amorphous through non-selective alkylation. The alkylation agents suitable for that purposes are exemplified by propylene oxide, glycidol, iodoacetamide, chloroacetate, or 2-diethylaminoethylchloride; their reactions with cyclodextrins were performed in a manner to yield mixtures containing many components, a circumstance which effectively prevents crystallization processes within the above pharmaceutical preparation.",
  "url": "https://patentbrief.org/patent/us/4727064/azt-zidovudine",
  "markdown_url": "https://patentbrief.org/patent/us/4727064/azt-zidovudine/md",
  "google_patents_url": "https://patents.google.com/patent/US4727064",
  "relatedPatents": []
}