# How Special Sugars Make Medicines Dissolve Better > 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. - **Patent:** US 4727064 - **Original title:** Pharmaceutical preparations containing cyclodextrin derivatives - **Owner:** US Department of Health and Human Services - **Granted:** 1988 - **Status:** Public domain (expired) - **Times cited:** 341 - **Field:** pharmaceutical, biotech, materials, chemistry ## 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. ## The clever bit The novelty lies in using an amorphous mixture of cyclodextrin derivatives. By ensuring the cyclodextrins themselves are non-crystalline and a mixture of many components, they prevent the drug-cyclodextrin complex from crystallizing. This stable, non-crystalline state is key to improving the drug's dissolution and absorption. ## Real-world examples 1. Testosterone formulations 2. Estrogen and progesterone therapies 3. Antiviral drug formulations (e.g., acyclovir) 4. Anti-inflammatory drug formulations 5. Oral drug delivery systems for poorly soluble compounds 6. Buccal administration of hormones ## Why it matters Many effective drugs don't dissolve well in water, making it hard for the body to absorb them. This patent offers a method to overcome this challenge, potentially making such drugs more effective or allowing for lower doses. This technology is fundamental to improving the "bioavailability" of medicines, ensuring that a larger portion of the drug reaches its target in the body. It has implications for a wide range of pharmaceutical products, from hormones to antiviral agents. ## Frequently asked questions ### What does How Special Sugars Make Medicines Dissolve Better cover? 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. ### Who owns patent US 4727064? US Department of Health and Human Services owns this patent, granted in 1988. ### When does this patent expire? This patent has expired and is now in the public domain — anyone can use the invention freely. ### What is patent US 4727064 cited by? This patent has been cited by 341 later patents that build on its ideas. ### What problem does this patent solve? Many effective drugs don't dissolve well in water, making it hard for the body to absorb them. This patent offers a method to overcome this challenge, potentially making such drugs more effective or allowing for lower doses. This technology is fundamental to improving the "bioavailability" of medicines, ensuring that a larger portion of the drug reaches its target in the body. It has implications for a wide range of pharmaceutical products, from hormones to antiviral agents. ### What does this patent NOT cover? Does not cover using cyclodextrins that are not chemically modified derivatives (e.g., plain alpha, beta, or gamma cyclodextrins). **Full plain-English explainer:** https://patentbrief.org/patent/us/4727064/azt-zidovudine **Original patent:** https://patents.google.com/patent/US4727064 --- _Source: PatentBrief — https://patentbrief.org. Patent facts are from public records; the plain-English explanation is PatentBrief's._ ## Related patents Semantically similar inventions in the PatentBrief corpus: - [How to Make Hard-to-Absorb Medicines Easier for the Body to Use](https://patentbrief.org/patent/us/5002952/duragesic-fentanyl-patch) — A method for mixing specific chemical compounds with surfactants to help the body absorb them more effectively. - [Making Ivacaftor Easier for the Body to Absorb](https://patentbrief.org/patent/us/8410274/kalydeco-ivacaftor) — A patent describing a specific way to turn a drug molecule into an amorphous solid to help the body absorb it more effectively. - [Using Vitamin B12 to Help Proteins Survive the Human Digestive System](https://patentbrief.org/patent/us/5574018/herceptin-trastuzumab) — A method for attaching therapeutic proteins to Vitamin B12 so they can be absorbed through the gut instead of being injected. - [How to Store Fragile Biological Materials Without Refrigeration](https://patentbrief.org/patent/us/RE39497/epogen-epoetin-alfa) — A method for preserving unstable biological materials like proteins by trapping them in a solid, glass-like sugar or polymer matrix that prevents decay at room temperature. - [A Gel That Helps Nicotine Absorb Through Your Skin](https://patentbrief.org/patent/us/7387788/soliris-eculizumab) — A specialized gel formula designed to help nicotine pass through the skin or mouth lining without crystallizing or rubbing off on clothes.