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Medicine preparation containing 5-fluorouracil drug eutectic with nicotinamide as precursor and preparation method of medicine preparation

A technology for fluorouracil and pharmaceutical preparations, which can be used in medical preparations containing active ingredients, drug combinations, drug delivery, etc., and can solve the problems of bone marrow suppression, patient inconvenience, and short half-life in vivo.

Active Publication Date: 2016-07-06
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 5-Fluorouracil is poorly soluble, slightly soluble in water, slightly soluble in ethanol, and almost insoluble in chloroform; it dissolves in dilute hydrochloric acid or sodium hydroxide solution, so it is difficult to formulate it into a form suitable for administration
However, this method of administration also has many disadvantages, such as bone marrow suppression, short half-life in vivo, nausea and vomiting and other adverse gastrointestinal reactions.
In addition, the clinical intravenous injection time is prolonged, which brings inconvenience and pain to the patient

Method used

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  • Medicine preparation containing 5-fluorouracil drug eutectic with nicotinamide as precursor and preparation method of medicine preparation
  • Medicine preparation containing 5-fluorouracil drug eutectic with nicotinamide as precursor and preparation method of medicine preparation
  • Medicine preparation containing 5-fluorouracil drug eutectic with nicotinamide as precursor and preparation method of medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] 1. Synthesis of 5-fluorouracil drug co-crystal with nicotinamide as precursor by liquid phase assisted grinding method:

[0116] Accurately weigh 3mmol (390.0mg) of 5-fluorouracil and 1mmol (122.0mg) of nicotinamide with an analytical balance, put them into an agate mortar with a diameter of 8-15cm, carefully grind the reactants evenly and finely grind the reactants to a powder of 100-300 mesh. Use a micropipette to transfer 20 μL of deionized water into the above powder, and grind it uniformly for 10 minutes quickly to obtain a 5-fluorouracil drug cocrystal with nicotinamide as the precursor.

[0117] The 5-fluorouracil pharmaceutical co-crystal prepared above was subjected to structural characterization and performance testing through the above-mentioned equipment:

[0118] like figure 1 As shown, three 5-fluorouracil molecules, one nicotinamide molecule and one water molecule jointly constitute the basic structural unit of the 5-fluorouracil co-crystal through hydro...

Embodiment 25

[0128] Wet granulation tableting:

[0129] 1. Prescription:

[0130] 5-fluorouracil drug co-crystal with nicotinamide as precursor 15g 15% starch slurry Appropriate amount Tween starch 6％ Magnesium stearate 1％ production 40 pieces

[0131] 2. Preparation:

[0132] 1) Weigh 0.5g of polysorbate-80, dissolve in 15ml of ethanol, add 15g of starch, stir evenly, dry at 70°C, pass through a 100-mesh sieve to obtain Tween starch, and set aside;

[0133] 2) Preparation of dry starch: dry the starch at 105°C for about 2 hours to make the water content 8%-10%;

[0134] 3) Weigh 6g of dry starch, dissolve it in 40ml of distilled water and disperse evenly, heat and gelatinize at 80°C to obtain starch slurry;

[0135] 4) Preparation of wet granules: Take 15 g of 5-fluorouracil pharmaceutical eutectic with nicotinamide as the precursor, add appropriate amount of starch slurry to prepare soft materials, pass through a 16-mesh sieve to granulate, dry...

Embodiment 3

[0150] 1. Preparation of erosion matrix tablets

[0151] 1. Prescription:

[0152] 5-fluorouracil drug co-crystal with nicotinamide as precursor 10g stearyl alcohol 1g HPMC K10M 0.1g Magnesium stearate 1.2％

[0153] A total of 50 tablets were produced

[0154] 2. Preparation:

[0155] 1) Grind the 5-fluorouracil drug eutectic with nicotinamide as the precursor and pass it through a 100-mesh sieve, and put stearyl alcohol in an evaporating dish, heat and melt it on a water bath at 80°C, add the drug eutectic, stir well, cool, Grind in a mortar.

[0156] 2) According to the ratio of 1 gram of hypromellose to 7ml of 80% ethanol, soak the hypromellose in 80% ethanol to make hypromellose mucilage;

[0157] 3) Add hypromellose mucilage to the drug eutectic obtained in step 1) to make a soft material (if the mucilage is insufficient, an appropriate amount of 80% ethanol can be added), and granulate with a 40-mesh sieve;

[0158] 4) Dry at 50°C, w...

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Abstract

The invention discloses a medicine preparation containing 5-fluorouracil drug eutectic with nicotinamide as a precursor and a preparation method of the medicine preparation.5-fluorouracil raw material medicine is selected as medicine API, nicotinamide serves as the medicine precursor, a liquid-phase assisted grinding method is adopted, the high-purity 5-fluorouracil drug eutectic is obtained, and the effect that the medicine can be more stable can be achieved; in addition, the invention further provides the medicine preparation containing the 5-fluorouracil drug eutectic, the medicine preparation comprises tablets, slow-release tablets, microspheres, micro-capsules, suppository, emulsion, a film agent and an injection agent so that stability and the curative effect of the 5-fluorouracil drug eutectic with the nicotinamide as the precursor can be better improved, different medicine application modes are utilized, and possibility of fully playing the treatment function of medicine and lowering or avoiding adverse reactions is provided.Auxiliaries applied to the preparation method of the preparation are easy to buy in the market and low in price, therefore cost is quite low, and the medicine application burden of patients can be remarkably lowered.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a pharmaceutical preparation of 5-fluorouracil drug co-crystal containing nicotinamide as a precursor and a preparation method thereof, and belongs to the technical field of preparation of pharmaceutical preparations. Background technique [0002] 5-Fluorouracil, synthesized by Heidelberger in 1957, has lethality to proliferating cells. It is a classic antineoplastic drug collected in Pharmacopoeia. 5-Fluorouracil is the first anti-metabolite drug synthesized according to a certain assumption and is currently the most widely used anti-pyrimidine drug in clinical practice. In recent decades, 5-fluorouracil has always played an important role in medical oncology treatment. It is effective in the treatment of a variety of tumors such as digestive tract cancer, breast cancer, ovarian cancer, choriocarcinoma, cervical cancer, bladder cancer, liver cancer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/553C07D213/82A61K31/513A61K31/455A61P35/00
CPCA61K9/0002A61K9/0019A61K9/02A61K9/06A61K9/08A61K9/1658A61K9/2054A61K9/2059A61K9/50A61K9/7007A61K31/455A61K31/513A61K47/14A61K47/38A61K47/42A61K47/44C07D213/82C07D239/553A61K2300/00
Inventor 于楠韩思莹张良栓张竹艳李海波王健鑫
Owner HARBIN MEDICAL UNIVERSITY
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