Iloperidone crystal and preparation method and medicinal composition thereof
A technology of iloperidone and its composition, applied in the field of iloperidone crystals, can solve problems such as inability to obtain stable and definite crystal forms, and no mention of iloperidone crystal forms
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Embodiment 1
[0032] Example 1 : Preparation method of iloperidone crystal
[0033] The present embodiment is the preparation method of iloperidone crystal, specifically comprises the following steps:
[0034] First, according to the method described in EP402644A1, iloperidone is prepared, and its nuclear magnetic spectrum is as follows figure 1 shown.
[0035] Next, heat 1g of iloperidone in a vacuum drying oven at 125-130°C, while evacuating (30mmHg) until the solid is completely melted, then naturally cool to 80°C, crystallization is formed, and continue to naturally cool to room temperature (25°C). Grinding to prepare iloperidone crystals.
[0036] The prepared iloperidone crystals are characterized by the following powder X-ray diffraction patterns. The Japanese Rigaku D / Max-2500 X-ray diffractometer was used for the measurement, and the specific experimental parameters were set as follows: CuKα radiation, tube voltage: 40KV, tube current: 100mA, 2θ angle scanning range of 2 to 4...
Embodiment 2
[0038] Example 2 : Detection of physical properties of iloperidone crystals
[0039] In this example, the iloperidone prepared in Example 1 was used as a reference substance, and the physical properties of the iloperidone crystals prepared in Example 1 were tested, including solubility, hygroscopicity and stability.
[0040] 1. Solubility
[0041] According to the Chinese Pharmacopoeia 2005 edition, the dissolubility of the iloperidone crystals prepared in 0.1M hydrochloric acid is detected by the method XIII of the second part of the Chinese Pharmacopoeia, and compared with the iloperidone prepared in embodiment 1, the results are shown in Table 2 shown.
[0042] Table 2 Solubility comparison in 0.1M hydrochloric acid
[0043] sample name
[0044] From the results in Table 2, it can be seen that the solubility of iloperidone crystals in 0.1M hydrochloric acid is better than that of the reference substance.
[0045] 2. Hygroscopicity
[0046] According to " Chi...
Embodiment 3
[0057] Example 3 : Tablets of pharmaceutical composition comprising crystals of iloperidone
[0058] This embodiment is a pharmaceutical composition comprising iloperidone crystals prepared in embodiment 1.
[0059] The pharmaceutical composition is prepared into tablets, and the specific prescription is as follows (1000 tablets, each containing 1 mg, 4 mg or 6 mg of active ingredient iloperidone crystal):
[0060]
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