scholarly journals High-Amylose Sodium Carboxymethyl Starch Matrices: Development and Characterization of Tramadol Hydrochloride Sustained-Release Tablets for Oral Administration

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Teresa Nabais ◽  
Grégoire Leclair

Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.

Author(s):  
Ganesh Basarkar ◽  
Vijay Suryawanshi ◽  
Dinesh Hire

The objective of the present study was to control the release of freely water soluble Tramadol hydrochloride over a prolonged period of time by embedding the drug into novel wax matrix system. The matrix granules were prepared by melt granulation technique. The need for the administration two to four times a day when larger dose are required can decrease patient compliance. Sustained release formulation that would maintain plasma levels for 24 hrs for once daily dosing of Tramadol hydrochloride was prepared. The compatibility of the drug and wax examined using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectrophotometer (FTIR). The effect of wax concentration (5 to 35%) and channeling agents (Avicel PH-101 and Di-calcium phosphate) on the in vitro drug release at 24 hrs. was studied.  Results of DSC confirmed drug-wax compatibility. Increasing the wax concentration resulted in a significant retardation of drug release. The drug release study revealed that the optimized formulation (F6) 30% novel wax sustained drug release for 24hrs. At the same wax concentration, drug release from tablets decreased with Di-calcium phosphate and increased with Avicel PH 101. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. A hydrophobic matrix system is thus useful technique for prolonging the drug release of freely water soluble drugs such as Tramadol hydrochloride


2016 ◽  
Vol 4 (4) ◽  
pp. 760-767 ◽  
Author(s):  
Liping wu ◽  
Liyan Qiu

CA4P-loaded microspheres (CA4P-MS) composed of PELA reverse micelles (CA4P-RM) and PLGA with a sea-island structure were prepared. This unique type of construction can greatly improve the encapsulation efficiency of water-soluble CA4P and provide sustained drug release and action for cancer therapy.


2007 ◽  
Vol 65 (3) ◽  
pp. 371-378 ◽  
Author(s):  
T. Nabais ◽  
F. Brouillet ◽  
S. Kyriacos ◽  
M. Mroueh ◽  
P. Amores da Silva ◽  
...  

Author(s):  
Kamble Ravindra K. ◽  
Chauhan Chetan S. ◽  
Kamble Priyadarshani R. ◽  
Naruka Pushpendra S.

The main aim of the present work was to develop the microcapsules of tramadol hydrochloride for the oral sustained release drug delivery. Tramadol hydrochloride a BCS class I drug a centrally acting synthetic analgesic was complexed with Indion 254 ion exchange resin. The microcapsules were prepared by encapsulating the prepared resinates by o/o solvent evaporation technique. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of eudragit RS 100 and plasticized PEG 400. The results of multiple linear regression analysis indicated that for obtaining a sustained release drug delivery the optimum concentrations of both the plasticizer and coating solution to be used. The factorial models were used to prepare optimized microcapsules and optimized formulations showed sustained release profiles for the extended period of more than 12 hrs. From the present investigations concluded that resinate microcapsules of highly water soluble drug can provide controlled release of drug for extended period.Key Words: Tramadol hydrochloride, ion exchange resinate, microcapsules, sustained release


2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.


2016 ◽  
Vol 4 (14) ◽  
pp. 2477-2485 ◽  
Author(s):  
Jing Chen ◽  
Juan Ge ◽  
Baolin Guo ◽  
Kun Gao ◽  
Peter X. Ma

A conveniently fabricated electroactive nanofibrous composite scaffold serves as a sustained drug release system and promotes myoblast differentiation.


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