scholarly journals FORMULATION AND IN-VITRO-IN-VIVO EVALUATION OF ALGINATE-CHITOSAN MICROSPHERES OF GLIPIZIDE BY IONIC GELATION METHOD

Author(s):  
Maya Sharma ◽  
Choudhury Pk ◽  
Suresh Kumar Dev

Objective: The present work is aimed to formulate and evaluate alginate-chitosan microspheres of glipizide for the effective use in the treatment of diabetes.Methods: Sustained release microspheres were prepared by gentle mixing of polymers in water phase with drug by agitation. The polymers used for preparation were sodium alginate and chitosan, which was extruded into 5% calcium chloride solution to produce microspheres by ionic gelation method.Results: Single unit dosage form of Glipizide causes gastric irritation. To convert it in to the multiple unit dosage form will release the drug evenly throughout the stomach which suppresses the irritation. The aim of study towards formulation and evaluation of alginate-chitosan microspheres, which can provide sustained release of the model drug. It shows better in-vitro and in-vivo activity than conventional dosage forms. The work also aims to study various parameters affecting the behavior of microspheres in oral dosage form. Conclusion:  Drugs that are simply absorbed from the gastrointestinal tract (GIT) and having a short half life are eliminated rapidly from the blood flow. To avoid this trouble, the oral sustained release (SR) has been developed as these will release the drug slowly in to the GIT and maintain a stable drug concentration in the serum for a longer period of time.

Author(s):  
Akhilesh Kumar Singh ◽  
Neeraj Sharma

Over the last few years, therapeutic efficacy of drugs that have poor bioavailability or narrow absorption window have challenged the pharmaceutical industry. In this framework, many Hydrodynamic Balance System (HBS) also known as Gastro retentive dosage forms (GRDFs) have been used to enhance the therapeutic efficacy of drugs. Such drug have a narrow absorption window, are unstable at higher pH, are soluble in acidic conditions, and are local effect in the gastric-part. The drug development with recent technology of various novel polymeric-based gastroretentive drug delivery technologies that may regulate the bioavailability and extend time of therapeutic efficacy of such drugs. Our focus on the significance of in vitro study and in vivo evaluation parameters of various HBS drugs along with their applications.  This study provides a promising platform for advantages and guide formulation of HBS dosage form were covered in detail.


2011 ◽  
Vol 22 (4) ◽  
pp. 865-878 ◽  
Author(s):  
Gopal V. Shavi ◽  
Usha Y. Nayak ◽  
M. Sreenivasa Reddy ◽  
A. Karthik ◽  
Praful B. Deshpande ◽  
...  

2019 ◽  
Vol 52 ◽  
pp. 177-188 ◽  
Author(s):  
Ehsan Kaffash ◽  
Farinaz Saremnejad ◽  
Mohammadreza Abbaspour ◽  
Seyed Ahmad Mohajeri ◽  
Hadi Afrasiabi Garekani ◽  
...  

2021 ◽  
Vol 26 (3) ◽  
pp. 349-361
Author(s):  
Napoleon-Nikolaos Vrettos ◽  
Peng Wang ◽  
Yan Zhou ◽  
Clive J. Roberts ◽  
Jinyi Xu ◽  
...  

2021 ◽  
Vol 11 ◽  
Author(s):  
Hardik Rana ◽  
Rushikesh Chaudhari ◽  
Vaishali Thakkar ◽  
Tejal Gandhi

Background: The better control of the drug release with immediate effect is the major concern to achieve better therapeutic action and patient compliance. The failure of the solid dispersion complex during storage as well as in-vivo is another concern for the oral solid dosage form. Objective: The prime objective of the present study was to optimize the biphasic minitablet incorporating quality by design approach using the combination of waxy erodible and water-impermeable excipients. Exploration of Soluplus as a precipitation inhibitor and Dexolve as a solubility enhancer in oral solid dosage form was the secondary objective. Methods: The drug-Excipient compatibility study was assessed by FTIR. Clozapine was chosen as a model drug that has poor aqueous solubility. The complex was formulated using B-cyclodextrin or HP B-CD or Dexolve by kneading method. The screening of solubility enhancers and their amount were performed based on phase solubility study. The precipitation inhibitor was screened as per the parachute effect study. Immediate release minitablets were formulated using a direct compression method using different disintegrating agents. The IR minitablets were evaluated for different evaluation parameters. The sustained release minitablets was formulated by hot-melt granulation technique incorporating the Precirol ATO 5 as a waxy excipient and ethyl cellulose as water impermeable excipient. The SR minitablet was optimized using a central composite design. The amount of Precirol ATO 5 and ethyl cellulose were chosen as independent variables and % drug release at 1, 6, and 10 h was selected as responses. The designed batches were evaluated for different pre and post compressional parameters. The IR and SR minitablets were filled in a capsule as per dose requirement and evaluated for in-vitro drug release. The in-vivo plasma concentration was predicted using the Back calculation of the Wagner – Nelson approach. Results: Drug – Excipient study revealed that no significant interaction was observed. Dexolve was screened as a solubility enhancer for the improvement of the solubility of clozapine. The Soluplus was chosen as a precipitation inhibitor from the parachute effect study. The immediate-release tablet was formulated using Prosolv EASYtab SP yield less disintegration time with better flowability. The sustained release mini-tablet was formulated using Precirol ATO 5 and ethyl cellulose. Two-dimensional and three-dimensional plots were revealed the significant effect of the amount of Precirol ATO 5 and ethyl cellulose. The overlay plot locates the optimized region. The in-vitro drug release study revealed the desired drug release of the final combined formulation. The in-vivo plasma concentration-time confirms the drug release up to 12h. Conclusion: The biphasic mini-tablets were formulated successfully for better control of drug release leads to high patient compliance. The use of soluplus as a precipitation inhibitor is explored in the oral solid dosage form for a poorly aqueous drug. Prosolv EASYtab SP was incorporated in the formulation as super disintegrant. The amount of Precirol ATO 5 and ethyl cellulose had a significant effect on drug release in sustained-release minitablet. The approach can be useful in the industry.


2010 ◽  
Vol 2 ◽  
pp. 89-103
Author(s):  
Muhammad Sajid Hamid Akash . ◽  
Ikram Ullah Khan . ◽  
Syed Nisar Hussain Shah . ◽  
Sajid Asghar . ◽  
Asif massud . ◽  
...  

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