Dr. Yogesh Baburao Raut¹, Kalyan Chakravarthy Janjanam², Dr. Trinayan Deka³, Vijay Gajananrao Thakare⁴, Dr. Pramod Khobragade⁵, Dr. Arul Prakasam K C⁶, Dr. Ravindra Chandrakant Sutar⁷, Dr. Rahul L. Shirole^8*

¹Associate Professor, Fabtech College of Pharmacy, Sangola, India

²Director R&D, Epic Pharma LLC, 227-15N Conduit Ave, Laurelton, New York, USA

³Assistant Professor, Faculty of Pharmaceutical Science, University details: Assam down town University, Panikhaiti, Guwahati, 781026-Assam, India 

⁴Assistant Professor, Yeshwantrao Chavan College of Engineering Hingna road, Wanadongri Nagpur, 441110, India

⁵Professor, Datta Meghe Ayurvedic Medical College, Hospital and Research Centre, Nagpur, India

⁶Professor, JKKMMRF ANNAI JKK Sampoorani Ammal College Of Pharmacy, Komarapalayam Po 638183, Affiliate By The Tamil Nadu Dr Mgr Medical University, Chennai, India

⁷Associate Professor.& HOD, Department of Pharmacology SRES'S Sanjivani College of Pharmaceutical Education and Research, Kopargaon (Autonomous) At. Sahajanandnagar, Post. Shingnapur, Tal. Kopargaon, Dist. Ahmednagar 423603, India

⁸Associate Professor, Department of Pharmacology, DCS’s A.R.A. College of Pharmacy, Nagaon, Dhule (MS) India

* Address    for  Correspondence:

Dr. Rahul L. Shirole

Associate Professor, Department of Pharmacology, DCS’s A.R.A. College of Pharmacy, Nagaon, Dhule (MS) India

Orcid ID: https://orcid.org/0000-0002-9410-6097

Abstract

Objective: This work is aimed to Formulate, Optimize and Evaluate Gastro-Retentive Microspheres of Antidiabetic Agent by Full Factorial Design.

Methods: Microspheres were prepared using Emulsification-cross linking technique. To this HPMC-K4M and Carbopol was dissolved in 250 ml of water and allowed to swell for 24 hr at room temperature. And separately chitosan was dissolved in 3% (v/v) glacial acetic acid and this also kept for 24 h to swell or dissolve properly. After 24hr this swelled mixture was mixed under magnetic stirrer (Remi, India) at specific stirring rate for 1hr in order to find homogeneous mass of both the gum. Then slurry of chitosan also was homogenized for half an hour. The drug, Glipizide (1g) was then added to the chitosan solution and mixed homogenesously. 

Results: The aim of the study was to formulate and evaluate microspheres, for Gastro-Retentive Microspheres of the chosen drug. The EE of microspheres was found to be 91.52%, maximum . Buoyancy property observed was 93.82% for Optimized formulation F-9, Drug release 57.34% till 8 h. The work also aims to study various parameters affecting the behaviour of microspheres in oral dosage form.

Conclusion: Drugs with short half-life that are absorbed from the gastrointestinal tract (GIT) are eliminated rapidly from the blood flow. To avoid this, the oral SR Gastro-retentive was developed as this formulation released the drug slowly into the GIT and maintained a stable drug concentration in the serum for a longer duration of time.

Keywords  Glipizide, KPMC-K4M, Carbopol, Chitosan, Sustained release microspheres, In-vitro activity

PDF Development, Optimization and Evaluation of Gastro-Retentive Microspheres of Antidiabetic Agent by Full Factorial Design.pdf