Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

Author(s):  
R. Nagaraju ◽  
Rajesh Kaza

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

Author(s):  
RASHMITHA V ◽  
MADHUSUDAN RAO Y ◽  
PAVANI S

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile. Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations. Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism. Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.


2018 ◽  
Vol 8 (1) ◽  
pp. 88-103 ◽  
Author(s):  
Mahmoud A. Mohamed ◽  
Amr H. Ali ◽  
Abdelfatah M. Abdelfatah ◽  
Mahmoud O. Ahmed

2010 ◽  
Vol 46 (4) ◽  
pp. 761-768 ◽  
Author(s):  
Mustafa Çelebier ◽  
Mustafa Sinan Kaynak ◽  
Sacide Altınöz ◽  
Selma Sahin

A simple, rapid and reproducible HPLC method was developed for the simultaneous determination of amlodipine and valsartan in their combined dosage forms, and for drug dissolution studies. A C18 column (ODS 2, 10 μm, 200 x 4.6 mm) and a mobile phase of phosphate buffer (pH 3.6 , 0.01 mol L-1):acetonitrile: methanol (46:44:10 v/v/v) mixture were used for separation and quantification. Analyses were run at a flow-rate of 1 mL min-1 and at ambient temperature. The injection volume was 20 μL and the ultraviolet detector was set at 240 nm. Under these conditions, amlodipine and valsartan were eluted at 7.1 min and 3.4 min, respectively. Total run time was shorter than 9 min. The developed method was validated according to the literature and found to be linear within the range 0.1 - 50 μg mL-1 for amlodipine, and 0.05 - 50 μg mL-1 for valsartan. The developed method was applied successfully for quality control assay of amlodipine and valsartan in their combination drug product and in vitro dissolution studies.


Author(s):  
A. Y. Kanugo ◽  
N. I. Kochar ◽  
A. V. Chandewar

The goal of present work was to investigate the effects of rupturable material ethyl cellulose combines with erodible material Klucel EXF on the pulsatile release pattern of Candesartan cilexetil in order to prevent morning rise in blood pressure. A tablet prepared by compression coating method contains core and coat components. Core consists of active ingredients with its various superdisintegrants where as coat contains different grades of ethyl cellulose and Klucel HXF in various combinations. All these tablets were evaluated for its micromeritics, weight variations, hardness, friability and in vitro dissolution testing. Drug-excipients interactions were carried out by FTIR. Dissolution studies were carried out in simulated gastric fluid followed by phosphate buffer of pH 6.5. The optimized formulation PT6 which give lag time of 6 hrs and released 99.10 % within 7 hr, as well as found to be stable in ICH stability testing guidelines.


Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 507
Author(s):  
Isabel Gonzalez-Alvarez ◽  
Marival Bermejo ◽  
Yasuhiro Tsume ◽  
Alejandro Ruiz-Picazo ◽  
Marta Gonzalez-Alvarez ◽  
...  

The purpose of this study was to predict in vivo performance of three oral products of Etoricoxib (Arcoxia® as reference and two generic formulations in development) by conducting in vivo predictive dissolution with GIS (Gastro Intestinal Simulator) and computational analysis. Those predictions were compared with the results from previous bioequivalence (BE) human studies. Product dissolution studies were performed using a computer-controlled multicompartmental dissolution device (GIS) equipped with three dissolution chambers, representing stomach, duodenum, and jejunum, with integrated transit times and secretion rates. The measured dissolved amounts were modelled in each compartment with a set of differential equations representing transit, dissolution, and precipitation processes. The observed drug concentration by in vitro dissolution studies were directly convoluted with permeability and disposition parameters from literature to generate the predicted plasma concentrations. The GIS was able to detect the dissolution differences among reference and generic formulations in the gastric chamber where the drug solubility is high (pH 2) while the USP 2 standard dissolution test at pH 2 did not show any difference. Therefore, the current study confirms the importance of multicompartmental dissolution testing for weak bases as observed for other case examples but also the impact of excipients on duodenal and jejunal in vivo behavior.


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