scholarly journals In vivo Evaluation of Theophylline Sustained Release Matrix Tablets Containing Low Viscosity Guar Gum

Author(s):  
Rama Rao Tadikonda ◽  
Satyanarayana Sreemantula

The present investigation was carried out to evaluate the utility of guar gum as a hydrophilic matrix carrier in the design of oral controlled drug delivery. Based on the earlier reports, the low viscosity guar gum appears to be superior to medium and high viscosity grades of guar gum in providing a sustained delivery of theophylline along the GI tract. Conducting in vivo studies on theophylline matrix tablets containing 10% of low viscosity guar gum as a representative formulation assessed the in vivo performance of the guar gum matrix tablets. The in vivo studies were carried out in dogs. The effective concentration of theophylline was sustained for a period of 16 hours. The extended tmax, reduced absorption rate constant, prolonged MRT, unchanged Cmax and unchanged bioavailability indicate a controlled release of theophylline from the guar gum matrix tablets resulting in a sustained absorption and prolonged blood levels of theophylline. The theophylline matrix tablets showed blood levels well below 15 ?g/mL indicating freedom from adverse effects. Based on the studies, guar gum appears to be a potential carrier in the design of oral controlled drug delivery systems.

2005 ◽  
Vol 2 (2) ◽  
pp. 155-163 ◽  
Author(s):  
S. Al-Saidan ◽  
Y. Krishnaiah ◽  
V. Satyanarayana ◽  
G. Rao

Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release


2005 ◽  
Vol 6 (1) ◽  
pp. E14-E21 ◽  
Author(s):  
Saleh M. Al-Saidan ◽  
Yellela S. R. Krishnaiah ◽  
S. Patro ◽  
Vemulapalli Satyanaryana

Author(s):  
Bhikshapathi D. V. R. N. ◽  
Chenna Madipalli Shalina ◽  
Vishnu Pulavarthy ◽  
Viswaja Medipally

The aim of this study was to explore the application of Gelucire 43/01 for the design of sustained release gastro retentive drug delivery system of Amlodipine besylate. Gelucire 43/01 has been used in floating sustained release formulations to prolong gastric residence time and increase its bioavailability. Gelucire 43/01 in combination with HPMC and Polyox was used as a release retarding polymer. HPMC of various viscosity grades HPMC K4M, HPMC K15M and HPMC K100M in combination of Gelucire were tested to obtain optimal total floating time as well as controlled drug release for prolonged period. Melt granulation technique has been used to prepare gastro retentive Amlodipine besylate formulations. All the formulations were evaluated in vitro for their floating ability and drug release. The floating times of all tablet formulations were greater than 12h. HPMC K4M in combination with Gelucire as polymeric matrix enhanced the drug release due to addition of hydrophilic polymer facilitated the swelling and erosion of the tablets. Incorporation of low viscosity polymer HPMC K100 M resulted in optimal floating as well as drug release for longer time. In vivo studies of optimized formulation show floating ability for 6 h in stomach. The results indicate that Gelucire 43/01 in combination with dissolution enhancers HPMC increase the permeability of the wax matrix, which provides improved dissolution thereby bioavailability of Amlodipine besylate and can be considered as a carrier for the development of sustained release floating drug delivery systems.  


Author(s):  
Ravi Shekhar ◽  
P. Sharma

A new approach to zero- order drug delivery that includes geometric factors is described. Systems such as multilayered tablets and other geometrically altered devices have been created to perform this function. The multi-layered matrix system overcomes inherent disadvantages of non-linearity associated with diffusion controlled matrix devices by providing additional release surface with time to compensate for the decreasing release rate. These formulations designed to deliver the drug at predetermined rate, maintain therapeutically effective concentrations in systemic circulation for prolonged period of time. Recently, pharmaceutical research has focused on controlled drug delivery offer definite advantages over conventional release formulation of the same drug. Controlled delivery systems that can provide zero-order drug delivery have the potential for maximizing efficacy while minimizing dose frequency and toxicity. In the present study, guar gum was used as hydrophilic matrix carrier for designing oral controlled drug delivery systems of highly soluble drug lamivudine. Three layered matrix tablets of lamivudine prepared by wet granulation technique were subjected for various evaluating parameters and optimized.


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