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Method for preparing stable amorphous drug preparation
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A technology of pharmaceutical preparations and amorphous state, which is applied in the field of preparation of amorphous pharmaceutical preparations, and can solve problems such as complex processes and unsatisfactory stability of amorphous pharmaceutical preparations
Active Publication Date: 2013-12-11
SHANGHAI AUCTA PHARMA CO LTD
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But handle like this, the stability of amorphous drug preparation is still not ideal enough, and, technology is also more complicated
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Embodiment 1
[0026] Example 1: Urea (urea) amorphous preparation
[0027] The molecules of urea are small and crystallize easily. Amorphous urea has not been reported so far. Using the technology of this patent, the amorphous preparation of urea is successfully prepared, and has good stability.
[0028] Prescription Screening:
[0029] 1. Dissolve urea, citric acid (citric acid) and hydroxypropyl methylcellulose (HPMC) in methanol, wherein the amount of citric acid added is 10% to 30% of the total weight, hydroxypropylmethylcellulose The addition amount of element is 60%~80% of total weight;
[0030] 2. The solvent methanol is volatilized at room temperature to obtain an amorphous urea preparation;
[0031] 3. The urea amorphous preparation is stored in a vacuum desiccator; the temperature is 24 ℃ ~ 28 ℃, preferably 25 ℃;
[0032] Microscopy and powder X-ray diffraction were used to check whether a pure amorphous preparation was obtained. figure 1 is the screening phase diagram for...
[0035] Lapatinib is an oral small molecule epidermal growth factor (EGFR: ErbB-1, ErbB-2) tyrosine kinase inhibitor for the treatment of advanced or metastatic breast cancer. Lapatinib is a poorly soluble drug with a solubility of <0.030 mg / mL in water at 25°C. Therefore, the bioavailability of lapatinib is relatively low (<25%). Preparation into an amorphous preparation can increase the solubility of lapatinib, thereby increasing its bioavailability.
[0036] The prescription of lapatinib amorphous preparation is shown in Table 1:
[0040] 1. Dissolve lapatinib, PVPK30 and citric acid monohydrate in a...
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Abstract
The invention belongs to the technical field of drug preparation, in particular to a method for preparing a stable amorphous drug preparation. According to the method, a small quantity of micromolecule auxiliary materials are added to an amorphous pharmaceutical preparation, such as citric acid, succinic acid, sorbitol and the like, which can be used for effectively stabilizing the amorphous pharmaceutical preparation. Compared with macromolecule auxiliary materials, the micromolecule auxiliary materials can have better interaction and compatibility with drug molecules, so that the micromolecule auxiliary materials can be used for better stabilizing the amorphous drug preparation. The invention also provides an optimization method of an amorphous drug preparation prescription, and the optimization process comprises the following steps of: screening proper micromolecule auxiliary materials according to different drugs, and determining an optimal dosage of the screened micromolecule auxiliary materials.
Description
technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a preparation method of an amorphous medicine preparation. Background technique [0002] In recent years, with the emergence of more poorly soluble drugs, amorphous pharmaceutical preparations have received more and more attention. Amorphous pharmaceutical preparations can improve the solubility of poorly soluble drugs, thereby increasing drug absorption and bioavailability. Amorphous pharmaceutical preparations have a wide range of applications and are suitable for the development of new drugs in the early stage and the improvement of preparations in the later stage. [0003] To prepare amorphous drug preparations, the usual method is to dissolve the drug and auxiliary materials in a solvent, then spray dry, and then freeze-dry or rotary evaporate to remove the solvent. Another commonly used method is the melt extrusion method, in which the drug and ex...
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