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Insoluble medicine solid dispersoid and preparation method thereof
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A technology for solid dispersions and insoluble drugs, applied in pharmaceutical formulations, drug delivery, organic active ingredients, etc., can solve problems such as solubility, low bioavailability, and low encapsulation efficiency, and achieve improved dissolution performance and solubility. rate, the effect of increasing solubility
Inactive Publication Date: 2012-07-04
DONGHUA UNIV
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Problems solved by technology
Those drugs with high pharmacological activity in vitro often cannot fully exert their clinical application value due to solubility problems
The problems that plague poorly soluble pharmaceutical preparations include: ①Due to poor solubility, the absorption of oral administration is incomplete and the bioavailability is low; ②Even if a solubilizer is used, the drug cannot be administered by injection to achieve good curative effect; ③ For those drugs with poor water solubility but certain fat solubility, mixed solvent or microencapsulation technology can be used
However, it also brings problems such as low drug loading, low encapsulation efficiency, and the need to use a large amount of carrier materials, resulting in the failure to obtain the desired therapeutic effect, or increasing the difficulty of drug approval.
④ For drugs with poor water solubility and fat solubility, there is still a lack of effective methods to solve the problem
[0005] Therefore, so far, there is no relevant report on the preparation process and method for this type of drug solid dispersion.
Method used
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Embodiment 1
[0027] (1) Preparation of acyclovir-polyvinylpyrrolidone heating eutectic solution
[0028] Under measuring different temperatures (25,40,60,80 ℃), the saturation solubility of acyclovir in the polyvinylpyrrolidone aqueous solution (0%, 50%, 10%, 15%, 20%w / v) of different contents . The sample was shaken at a fixed temperature for 48 hours, then the sample was filtered with a 0.22 μm filter membrane, diluted about 400 times with 0.1N NaOH aqueous solution, and the UV absorbance was measured at 252nm to calculate the saturation solubility. The results are as follows figure 1 shown;
[0029] according to figure 1 As a result, 25 grams of acyclovir and 50 grams of polyvinylpyrrolidone were put into 1000 grams of water to form a suspension of acyclovir at room temperature. Unsaturated eutectic solution of vinylpyrrolidone, keep the solution at this temperature for 24h.
[0030] (2) Acyclovir solid dispersion preparation
[0031] according to figure 2 As shown, the thermal e...
Embodiment 2
[0038] Preparation of Ferulic Acid-Polyvinylpyrrolidone Solid Dispersion
[0039] Put 20 grams of ferulic acid and 50 grams of polyvinylpyrrolidone into 1000 grams of water to form a suspension of ferulic acid at room temperature, and continuously increase the temperature to 70 ° C to make the suspension become an unsaturated mixture of ferulic acid and polyvinylpyrrolidone. eutectic solution, will the solution be constant at this temperature? ? time. Then the hot eutectic solution is rapidly cooled into a solid with liquid nitrogen, and then transferred to a vacuum freeze dryer for drying (vacuum degree 500Pa, temperature is minus 46°C, take it out after 24 hours to obtain ferulic acid-polyvinylpyrrolidone solid dispersion body.
Embodiment 3
[0041] Preparation of paracetamol-eudragit solid dispersion
[0042]Put 40 grams of acetaminophen and 50 grams of Eudragit into 1000 grams of water to form an acetaminophen suspension at room temperature, and keep raising the temperature to 70°C to make the suspension into acetaminophen and Udraqi Special unsaturated eutectic solution, the solution is kept at this temperature for 24h; then the hot eutectic solution is rapidly cooled into a solid with liquid nitrogen, and then transferred to a vacuum freeze dryer for drying (vacuum degree 500Pa, temperature below zero 46°C), take it out after 24 hours to obtain the paracetamol-Udragit solid dispersion.
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Abstract
The invention relates to an insoluble medicine solid dispersoid comprising an insoluble medicine and a water-soluble polymer, wherein the mass ratio of the insoluble medicine to the water-soluble polymer is 1-80 : 20-99. A preparation method of the insoluble medicine solid dispersoid comprises the following steps: the insoluble medicine and the water-soluble polymer are together dissolved into water according to the mass ratio of 1-80: 20-99 so as to obtain a suspending solution, and then the temperature of the suspending solution is increased to 70-90 DEG C to form an unsaturated consolute solution; the consolute solution is fast cooled into a solid by liquid nitrogen while the consolute solution is hot and then transferred into a vacuum freezing drier with the vacuum degree of 500 Pa and the temperature of -46 DEG C, and the solid consolute solution is dried for 20-24 hours so as to obtain the insoluble medicine solid dispersoid. The insoluble medicine solid dispersoid utilizes the characteristic of the insoluble medicine, i.e. the dissolubility of the insoluble medicine has temperature dependence in water, to enhance the dissolubility of the medicine and the soluble speed of the medicine and improve the dissolving out property of the medicine by increasing the temperature. The preparation method has easy operation and low cost and is environmentally-friendly, thereby being suitable for industrialized production.
Description
technical field [0001] The invention belongs to the field of solid dispersion and its preparation, in particular to a kind of insoluble drug solid dispersion and its preparation method. Background technique [0002] Due to the application of high-throughput screening and combinatorial chemistry and the rapid development of bioengineering technology, more and more active substances can be used in the treatment and protection of diseases, but about 40% of them have solubility problems. Those drugs with high pharmacological activity in vitro often cannot fully exert their clinical application value due to solubility problems. The problems that plague poorly soluble pharmaceutical preparations include: ①Due to poor solubility, the absorption of oral administration is incomplete and the bioavailability is low; ②Even if a solubilizer is used, the drug cannot be administered by injection to achieve good curative effect; ③ For those drugs with poor water solubility but certain fat ...
Claims
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Application Information
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