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盐酸乐卡地平Ⅰ、Ⅱ晶型及无定型对制剂制备的影响
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| 篇名： | 盐酸乐卡地平Ⅰ、Ⅱ晶型及无定型对制剂制备的影响 |
| TITLE： | |
| 摘要： | 目的：研究盐酸乐卡地平Ⅰ、Ⅱ晶型及无定型对制剂制备的影响，为其制剂开发及一致性评价提供理论基础。方法：采用X-射线粉末衍射（XRD）、红外分光光度（IR）和差式扫描量热（DSC）法鉴定盐酸乐卡地平的3种晶型；采用XRD法比较粉粹、研磨、加压工艺，湿法制粒中黏合剂溶剂（水、乙醇）和干燥温度（50、60、70 ℃）对盐酸乐卡地平3种晶型稳定性的影响；比较3种晶型盐酸乐卡地平片在水、盐酸、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液4种介质中的体外溶出度。结果：XRD显示，Ⅰ、Ⅱ晶型均有特征衍射峰，且2 θ值不一致，无定型无特征衍射峰；IR显示，3种晶型具有不同的吸收强度和吸收峰数目；DSC显示，Ⅰ、Ⅱ晶型分别在194.6、207.3 ℃有明显吸热峰，无定型在86.1 ℃有明显吸热峰、 299.8 ℃有放热峰。粉粹、研磨、加压及干燥温度对3种晶型转变均无影响；湿法制粒时水对晶型转变无影响，乙醇会引起Ⅰ晶型的晶型转变。除在盐酸中Ⅰ晶型与Ⅱ晶型片比较f2＝68外，4种介质中3种晶型盐酸乐卡地平片溶出度两两比较的f2均小于50。结论：XRD、IR、DSC法均能鉴定盐酸乐卡地平的3种晶型。用Ⅰ晶型制备盐酸乐卡地平片时，湿法制粒应避免使用乙醇作为黏合剂溶剂，建议使用水。不同晶型会影响所制盐酸乐卡地平片的体外溶出度。 |
| ABSTRACT： | OBJECTIVE： To study the effects of Ⅰ， Ⅱ crystal and amorphous forms of lercanidipine hydrochloride on the preparation， and provide theoretical basis for its development and consistency evaluation. METHODS： X-ray powder diffraction （XRD）， infrared spectrophotometry （IR） and differential scanning calorimetry （DSC） were adopted to identify the 3 crystal forms of lercanidipine hydrochloride. XRD was used to compare the effects of crushing， grinding， pressing technology， wetting granulation， adhesive solvents （water， ethanol） and drying temperature （50， 60， 70 ℃） on stability of 3 crystal forms of lercanidipine hydrochloride； the dissolution in vitro in water， hydrochloride， pH 4.5 acetate buffer， pH 6.8 phosphate buffer were compared among 3 crystal forms of Lercanidipine hydrochloride tablet. RESULTS： XRD showed both Ⅰ， Ⅱ crystal forms had characteristic diffraction peak with inconsistent 2 θ values， amorphous had no characteristic diffraction peak； IR showed 3 crystal forms had different absorption intensity and absorption peak number； DSC showed Ⅰ， Ⅱ crystal forms had obvious endothermic peak in 194.6 ℃， 207.3 ℃， respectively， amorphous had obvious endothermic peak in 86.1 ℃ and exothermic peak in 299.8 ℃. Crushing， grinding， pressing and drying temperature had no effects on the stability of 3 crystal forms； water had no effect on the stability of crystal in wetting granulation， ethanol may cause the change of Ⅰcrystal form. Except for the comparison between Ⅰ， Ⅱ crystal forms in hydrochloride （f2＝68）， the dissolution f2 of 3 crystal forms in 4 kinds of medium were lower than 50. CONCLUSIONS： XRD， IR， DSC methods can identify the 3 crystal forms of Lercanidipine hydrochloride tablet. When preparing lercanidipine hydrochloride by Ⅰcrystal form， wetting granulation should avoid using ethanol as a adhesive solvent， instead of water. Different crystal forms can affect the dissolution in vitro of prepared Lercanidipine hydrochloride tablet. |
| 期刊： | 2017年第28卷第10期 |
| 作者： | 卜鑫珏，张涛，王驰，夏喜坚，陈国松 |
| AUTHORS： | BU Xinjue，ZHANG Tao，WANG Chi，XIA Xijian，CHEN Guosong |
| 关键字： | 盐酸乐卡地平；Ⅰ晶型；Ⅱ晶型；无定型；鉴定；稳定性；体外溶出 |
| KEYWORDS： | Lercanidipine hydrochloride； Ⅰcrystal form； Ⅱ crystal form； Amorphous； Identification； Stability； Dissolution in vitro |
| 阅读数： | 367 次 |
| 本月下载数： | 9 次 |
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