Development and evaluation of orodispersible sustained release formulation of amisulpride–οcyclodextrin inclusion complex

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• 作者：Shivpal Singh (1)
  Jeetendra Singh Negi (1)
  Rohit Bisht (1)
  Vandana Negi (1)
  Nikhil Kasliwal (2)
  Vinay Thakur (3)
  Aadesh Upadhyay (4)
  
• 关键词：Amisulpride ; Gamma cyclodextrin ; CDSR ; OD ; CDSR ; Orodispersion
• 刊名：Journal of Inclusion Phenomena and Macrocyclic Chemistry
• 出版年：2014
• 出版时间：April 2014
• 年：2014
• 卷：78
• 期：1-4
• 页码：239-247
• 全文大小：622 KB
• 作者单位：Shivpal Singh (1)
  Jeetendra Singh Negi (1)
  Rohit Bisht (1)
  Vandana Negi (1)
  Nikhil Kasliwal (2)
  Vinay Thakur (3)
  Aadesh Upadhyay (4)
  
  1. Department of Pharmaceutical Sciences, S. Bhagwan Singh PG Institute of Bio-medical Sciences and Research, Balawala, Dehradun, Uttarakhand, 248161, India
  2. Formulation and Development Division, Glenmark Pharmaceuticals Ltd., Mumbai, 400099, Maharashtra, India
  3. Government College of Pharmacy, Rohru, Shimla, 171207, Himanchal Pradesh, India
  4. Division of Pharmaceutical Technology, Defence Research Laboratory, Tezpur, 784001, Assam, India
  
• ISSN：1573-1111

文摘

Amisulpride (AMI) is an atypical antipsychotic having poor aqueous solubility and poor oral bioavailability. Inclusion complex between AMI and gamma cyclodextrin (γ-CD) was prepared by kneading method using 1:1 stoichiometry. Solubility of AMI was enhanced by 3.74 times after inclusion complex formation. Amisulpride–οcyclodextrin inclusion complex was characterized by FTIR, DSC and XRD techniques. Further sustained release granules of Amisulpride–οcyclodextrin inclusion complex (CDSR) were prepared by treating complex with molten stearic acid. Drug release from CDSR granules was sustained up to 12?h with 100?% stearic acid proportion. The integrity of AMI–οCD inclusion complex in lipid phase was assessed by XRD study. Finally orodispersible tablets of CDSR granules (OD-CDSR) were prepared using Ac-Di-Sol and microcrystalline cellulose. Disintegration time was assessed by both pharmacopoeial and modified method. Optimized formulation was rapidly disintegrated within 25?s. Thus solubility enhancement and sustained release of AMI was achieved by orodispersion of CDSR granules for improvement of patient compliance.