Solid dispersion containing ridecevir, solid dosage form and preparation method
A solid dispersion and solid dosage form technology, which is applied in the field of pharmaceutical preparations, can solve problems such as easy adverse reactions, difficulty in forming oral tablets, and overdose of drugs, and achieve high bioavailability for in vivo absorption, stable and reliable product quality, and excellent preparation technology. The effect of simple process
Inactive Publication Date: 2021-11-12
QILU PHARMA CO LTD
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Problems solved by technology
[0008] Remdesivir for injection currently in clinical use has the following disadvantages: 1. Improper handling is prone to systemic or local infection; 2. Overdose or infusion of drugs is too fast, which is prone to adverse reactions and even life-threatening; 3. Persistence Excessive infusion of gastrointestinal fluids can easily cause circulatory overload or electrolyte imbalance; 4. The increase of iatrogenic diseases
[0010] The micronization treatment of the raw material medicine of this product will lead to the loss of raw materials and the phenomenon of easy agglomeration
The saturated solubility of remdesivir in different cyclodextrin concentrations was investigated, and it was found that to dissolve 100mg of remdesivir, the required amount of sulfobutyl beta-cyclodextrin was 1.3g, and the cyclodextrin was sticky, making it difficult to prepare oral tablets forming
Method used
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Comparison scheme
Effect test
Embodiment 1
[0057]
[0058] Preparation:
[0059] (1) Mix remdesivir and copovidone VA64 uniformly according to the prescription amount to make a physical mixture;
[0060] (2) Set the extrusion temperature of the twin-screw hot-melt extruder to 140-220°C, start the screw when the preset temperature is reached, control the screw speed at 20rpm-400rpm, and add the physical mixture in step (1) to In the extruder, the solid is extruded through the screw and cooled;
[0061] (3) Pulverizing the solid obtained in step (2), passing through a 60-mesh sieve to obtain a solid dispersion with uniform particle size distribution;
[0062] (4) Mix the solid dispersion obtained in step (3) with filler, disintegrating agent, glidant and lubricant according to the recipe quantity to obtain the total mixture;
[0063] (5) Compressing the total mixture obtained in step (4) into tablets, controlling the average weight difference ± 3%, and tableting hardness 8-18kg.
Embodiment 2
[0065]
[0066] Preparation method: same as Example 1.
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Abstract
The invention provides a solid dispersion containing ridecevir and a solid dosage form containing the solid dispersion, and belongs to the technical field of pharmaceutical preparations. The invention also provides a preparation method of the solid dispersion and the solid dosage form. According to the solid dosage form containing the ridecevir, firstly, the solid dispersion containing the ridecevir and copovidone is prepared by adopting a hot melt extrusion technology, then the solid dispersion, a filling agent, a disintegrating agent, a flow aid and a lubricating agent are prepared into a mixture, and finally the mixture is prepared into the solid dosage form, such as tablets. The ridecevir solid dosage form, provided by the invention, improves the dissolution rate and the bioavailability of medicines in an oral solid preparation, and has a relatively high clinical application value; and in addition, the ridecevir solid dosage form prepared by the invention is stable and controllable in quality, and is convenient for industrial production.
Description
technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid dispersion containing remdesivir, a method for preparing the solid dispersion, a solid dosage form containing the solid dispersion, and a method for preparing the solid dosage form. Background technique [0002] Remdesivir, or Remdesivir, is a broad-spectrum antiviral drug developed by the American pharmaceutical company Gilead. It was originally planned to treat Ebola virus. Preliminary cell experiments and animal experiments have shown that it can inhibit RNA polymerase. Good antiviral activity against SARS coronavirus and MERS coronavirus. In November 2018, in response to the Ebola epidemic, Congo (Kinshasa) launched a controlled clinical trial under the initiative of the WHO to test the efficacy of four new drugs including Remdesivir, MAb114, REGN-EB3 and Zmapp. It took just nine months for the contest to be decided. Due to the obviou...
Claims
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IPC IPC(8): A61K9/14A61K47/32A61K9/20A61K31/685A61P31/14
CPCA61K9/146A61K9/2095A61K9/2027A61K31/685A61P31/14
Inventor 张春霞郑晓清杨清敏程丽珍
Owner QILU PHARMA CO LTD