Oral curcumin nano-granule and preparation method thereof
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A technology of curcumin and nanoparticles, which is applied in the direction of medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low bioavailability and unsuitable self-administration of drugs, etc., to increase drug Absorption, overcoming low bioavailability, and convenient use
Inactive Publication Date: 2014-12-31
THE FIRST PEOPLES HOSPITAL OF CHANGZHOU +1
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Common routes of administration for these preparations include oral administration, intramuscular injection, and intravenous injection. Among them, intramuscular injection and intravenous injection need to be completed by professionals and are not suitable for self-medication. Although traditional oral administration is convenient to use, it often has low bioavailability
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[0011] Preparation steps:
[0012] 1. Activation of taurocholic acid and connection with heparin
[0013] (1) Dissolve 1 mol of TCA sodium salt in 5 ml of DMF at 0°C, then add 5 mol of TEA and 4 mol of 4-NPC, react under these conditions for 1 h, then stir at room temperature for 5 h. The reaction solution was extracted by centrifugation and a separatory funnel (ethanol 20ml, deionized water 20ml), repeated three times. The separated solution was placed in a rotary evaporator to evaporate the organic solvent, and finally freeze-dried for 24 hours to obtain TCA-NPC powder. Dissolve 1mol of TCA-NPC in 5ml of DMF, add 3mol of 4-MMP, react at 50°C for 2h, then add 50mol of EDA dropwise, then stir at room temperature for 20h, filter the crystalline part and dry it in a vacuum desiccator to obtain TCA -NH2.
[0014] (2) Dissolve 1mol heparin in distilled water and add hydrochloric acid solution to adjust the pH value within the range of 5.5-6, add 7mol EDC, stir for 10min, then a...
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Abstract
The invention belongs to the technical field of pharmaceutical preparation and particularly relates to an oral curcumin nano-granule and a preparation method thereof. The nano-granule is prepared by self-assembling a ternary conjugated compound which is obtained by connecting taurocholic acid, heparin and curcumin through amido bonds, the curcumin is a core of the nano-granule, and the hydrophilic taurocholic acid is on the surface of the nano-granule. The oral curcumin nano-granule overcomes the poor water solubility of curcumin, the absorption of the nano-granule can be enhanced by utilizing the interaction of taurocholic acid and bile acid transporter of small intestine, the defect that the bioavailability of the oral curcumin is low can be overcome, and the heparin also has anti-thrombosis and anti-angiogenesis effect.
Description
1. Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a curcumin oral nanoparticle and a preparation method thereof 2. Background technology [0002] Curcumin (curcumin) is a fat-soluble phenolic pigment extracted from the rhizomes of turmeric, zedoary and turmeric, etc., which have anti-inflammatory, anti-oxidation, anti-cancer and other pharmacological effects, and can improve cancer, Diabetes, metabolic disease, autoimmune disease, atherosclerosis, arthritis, stroke, peripheral neuropathy, enteritis, and traumatic brain injury. However, due to the poor water solubility of curcumin, it is easily oxidized in vitro, and there is currently no stable pharmaceutical dosage form, so it is difficult to administer. 目前已上市或报道的姜黄素制剂主要有:乳化剂(200510042547.9,200780008293.6,200910101327.7,201010214085.5)、固体分散剂(200510035060.8)、脂质体(200610026576.0,200810155819.X,200910009097.1,201010561666.6)、纳米微粒(200610125179.9 ,...
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