Tanshinol lipidosome bone-targeting pharmaceutical preparation and preparation method thereof
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A technology of pharmaceutical preparations and danshensu, which is applied in liposome delivery, drug combination, pharmaceutical formula, etc.
Inactive Publication Date: 2015-01-14
GUANGDONG MEDICAL UNIV
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[0008] At present, there is no bone-targeted drug delivery preparation of Danshensu liposome in the domestic market, and there are no research reports on this drug preparation. Therefore, the development of this type of drug not only has important clinical significance, but also has broad market prospects.
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[0028] The preparation method for preparing the Danshensu liposome bone-targeted preparation of the present invention comprises the following steps: the first step is to synthesize and prepare the bone-targeted conjugate with bisphosphonate, polyethylene glycol and cholesterol; the second step is to Prepare danshensu liposomes with phospholipids, cholesterol and danshensu as raw materials, and modify the liposomes with bone-targeted conjugates; the third step is to filter and segregate the bone-targeted preparations of danshensu liposomes, and perform column chromatography After separation, a bone-targeted preparation is obtained.
[0029] Bone-targeted conjugates are prepared as follows: dissolve cholesterol in dichloromethane, add triethylamine as an acid-binding agent, cool to -10°C, slowly add methanesulfonyl chloride dropwise and stir for reaction, after the reaction is completed, wash with water and filter A white powdery solid was obtained. After the PEG2000 is fully d...
Embodiment 1
[0031] Weigh 200mg of soybean lecithin, 50mg of cholesterol, and 80mg of bone-targeting guide, put them in a 500ml eggplant-shaped bottle, dissolve them in 15ml of dichloromethane, evaporate at 45°C and 60r / min to form a film, and add an aqueous solution containing 10mg of Danshensu 5ml. Room temperature, 60r / min rotary evaporation to form a suspension, 45 ° C for 2 hours to expand. Sequentially pass through 0.8 μm, 0.45 μm, 0.22 μm microporous membranes to size up the particles, and then separate and remove free danshensu by gel column.
Embodiment 2
[0033] Weigh 200 mg of soybean lecithin, 50 mg of cholesterol, and 80 mg of bone targeting guide, dissolve in 15 ml of dichloromethane, and add 5 ml of an aqueous solution containing 10 mg of danshensu. Stir at 1000rpm for 10min, 45°C, 60r / min rotary evaporation for 60min. Sequentially pass through 0.8 μm, 0.45 μm, 0.22 μm microporous membranes to size up the particles, and then separate and remove free danshensu by gel column.
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Abstract
The invention discloses a tanshinol lipidosome bone-targeting pharmaceutical preparation and a preparation method thereof. The preparation is prepared by jointing and carrying out surface modification on a lipidosome microparticle containing a tanshinol medicine molecule by using a bone-targeting jointer. The preparation method comprises the steps of jointing a bisphosphonate molecule with bone-targeting ability on one end of a polyethylene glycol molecule through synthetic reaction, and jointing a cholesterol molecule serving as a lipidosome raw material on the other end of the polyethylene glycol molecule through synthetic reaction to prepare a jointer with bone-targeting ability, namely bisphosphonate-polyethylene glycol-cholesterol (BP-PEG-CHOL); and then, preparing a lipidosome provided with the bone-targeting jointer on the surface from phospholipid, cholesterol and the bone-targeting jointer which serve as raw materials, adding tanshinol, and containing the tanshinol into the lipidosome to prepare the tanshinol lipidosome bone-targeting preparation. The preparation disclosed by the invention has the bone-targeting ability and can be used for remarkably increasing the concentration of medicines in a bone tissue, improving the curative effect and preventing and treating systemic metabolic bone diseases, osteoporosis and bone fracture.
Description
technical field [0001] The invention relates to a bone-targeted pharmaceutical preparation for bone-targeted treatment and prevention of osteoporosis, fractures and systemic metabolic bone diseases and a preparation method thereof, belonging to the technical field of drug production. Background technique [0002] Osteoporosis is a common degenerative disease in middle-aged and elderly people. Due to the high hardness of bone tissue, poor permeability, and special physiological and biochemical processes, it is difficult for therapeutic drugs to be effectively transported to the site of action according to the general route of administration. Some drugs often need to be administered systemically to reach an effective therapeutic concentration in bone tissue, which not only reduces the therapeutic index of the drug, but also produces toxic side effects on other organs and tissues of the patient. [0003] In 1986, Pierce first proposed the concept of bone targeting: compounds h...
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