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利培酮/随机甲基化β-环糊精包合物-与药用辅料的相容性研究。

Risperidone/Randomly Methylated β-Cyclodextrin Inclusion Complex-Compatibility Study with Pharmaceutical Excipients.

机构信息

Department Pharmacy I, Faculty of Pharmacy, "Victor Babeş" University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania.

Advanced Instrumental Screening Center, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, Romania, 2 Eftimie Murgu Square, 300041 Timisoara, Romania.

出版信息

Molecules. 2021 Mar 17;26(6):1690. doi: 10.3390/molecules26061690.

DOI:10.3390/molecules26061690
PMID:33802960
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8002621/
Abstract

Risperidone (RSP) is an atypical antipsychotic drug used in treating schizophrenia, behavioral, and psychological symptoms of dementia and irritability associated with autism. The drug substance is practically insoluble in water and exhibits high lipophilicity. It also presents incompatibilities with pharmaceutical excipients such as magnesium stearate, lactose, and cellulose microcrystalline. RSP encapsulation by randomly methylated β-cyclodextrin (RM-β-CD) was performed in order to enhance drug solubility and stability and improve its biopharmaceutical profile. The inclusion complex formation was evaluated using thermal methods, powder X-ray diffractometry (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR), UV spectroscopy, and saturation solubility studies. The 1:1 stoichiometry ratio and the apparent stability constant of the inclusion complex were determined by means of the phase solubility method. The compatibility between the supramolecular adduct and pharmaceutical excipients starch, anhydrous lactose, magnesium stearate, and cellulose microcrystalline was studied employing thermoanalytical tools (TG-thermogravimetry/DTG-derivative thermogravimetry/HF-heat flow) and spectroscopic techniques (UATR-FTIR, PXRD). The compatibility study reveals that there are no interactions between the supramolecular adduct with starch, magnesium stearate, and cellulose microcrystalline, while incompatibility with anhydrous lactose is observed even under ambient conditions. The supramolecular adduct of RSP with RM-β-CD represents a valuable candidate for further research in developing new formulations with enhanced bioavailability and stability, and the results of this study allow a pertinent selection of three excipients that can be incorporated in solid dosage forms.

摘要

利培酮（RSP）是一种用于治疗精神分裂症、痴呆和自闭症相关行为和心理症状的非典型抗精神病药物。该药物在水中几乎不溶，表现出高亲脂性。它还与硬脂酸镁、乳糖和微晶纤维素等药物赋形剂不相容。为了提高药物的溶解度和稳定性，改善其生物制药特性，采用随机甲基-β-环糊精（RM-β-CD）对 RSP 进行包封。采用热法、粉末 X 射线衍射（PXRD）、通用衰减全反射傅里叶变换红外（UATR-FTIR）、紫外光谱和饱和溶解度研究对包合物的形成进行了评价。通过相溶解度法确定了包合物的 1:1 化学计量比和表观稳定常数。采用热分析工具（TG-热重/ DTG-导数热重/HF-热流）和光谱技术（UATR-FTIR、PXRD）研究了超分子加合物与药用赋形剂淀粉、无水乳糖、硬脂酸镁和微晶纤维素的相容性。相容性研究表明，超分子加合物与淀粉、硬脂酸镁和微晶纤维素之间没有相互作用，而即使在环境条件下也观察到与无水乳糖不相容。RSP 与 RM-β-CD 的超分子加合物是进一步研究开发具有增强生物利用度和稳定性的新制剂的有价值候选物，本研究的结果允许选择三种赋形剂，可将其纳入固体制剂中。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/4ccc62ee1934/molecules-26-01690-g010a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/0ed2a361c65f/molecules-26-01690-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/33229d21c19d/molecules-26-01690-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/96d2d10a9334/molecules-26-01690-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/a4d4fd7f32ce/molecules-26-01690-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/927f4adac60b/molecules-26-01690-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/4ad5b263fc98/molecules-26-01690-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/c6842b27d20c/molecules-26-01690-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/638c40bff51a/molecules-26-01690-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/8aa131c8c53b/molecules-26-01690-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/4ccc62ee1934/molecules-26-01690-g010a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/0ed2a361c65f/molecules-26-01690-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/33229d21c19d/molecules-26-01690-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/96d2d10a9334/molecules-26-01690-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/a4d4fd7f32ce/molecules-26-01690-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/927f4adac60b/molecules-26-01690-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/4ad5b263fc98/molecules-26-01690-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/c6842b27d20c/molecules-26-01690-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/638c40bff51a/molecules-26-01690-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/8aa131c8c53b/molecules-26-01690-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee40/8002621/4ccc62ee1934/molecules-26-01690-g010a.jpg

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