scholarly journals Release Modification of Indomethacin Controlled Release Press Coated Tablets

2016 ◽  
Vol 19 (2) ◽  
pp. 219-225 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Md Elias Al Mamun ◽  
Md Mizanur Rahman Moghal

The study was carried out to evaluate the release modification of indomethacin press coated tablets through different polymers. Several batches of press coated tablets were prepared with indomethacin and Avicel PH 102. The core tablet was compression coated with minimal compression pressure. Formulation IX was modified by incorporating PEG 6000, sodium chloride and sodium lauryl sulphate (SLS). In vitro dissolution studies of the formulations of different excipients were done at pH 7.2 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm and 37 ± 0.5 °C temperature. The drug release data was treated in different mathematical fashion to identify the kinetic behaviour. It was found that, drug release which was inversely proportional to the amount of xanthan gum in the coating formulations was significantly changed by the polymers used in the study. Incorporation of SLS caused the drug to be released in near zero order fashion. Drug release was found to follow Higuchi mechanism for all the formulations. The study reveals that the polymers used may be a significant factor for the discrepancy in release rate of indomethacin.Bangladesh Pharmaceutical Journal 19(2): 219-225, 2016

2017 ◽  
Vol 15 (2) ◽  
pp. 203-208
Author(s):  
Md Haider Ali ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Selim Reza ◽  
Samira Karim

The aim of this research was to develop and evaluate gastric floating tablets of salbutamol sulphate. The oral delivery of anti-asthmatic salbutamol sulphate tablets were facilitated by preparing floating dosage form which could increase its absorption in the stomach by increasing the gastric residence time of the drug. Floating tablets were formulated by using different polymers like carbopol, xanthan gum, HPMC-K4 MCR and HPMC- K100 MCR with different proportions. A comparative study of normal effervescent tablets of salbutamol sulphate had also been done. The prepared tablets were evaluated for all their physicochemical properties and in vitro buoyancy study. In vitro dissolution studies of the formulations were done in pH 6.8 phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. Percent drug release of the formulations (F-1 to F-11) was from 87.34%- 99.12% after 12 hours. From the results, F-11 was selected as an optimized formulation based on 12 h drug release which showed minimal floating lag time and maximum floating time. On the other hand, 100% drug was released within 2 hours from the F-12 of effervescent salbutamol sulphate tablets in which polymer was absent while gas generating sodium bicarbonate and citric acid were present. The results of the study were consistent and may encourage formulating similar dosage form with other drugs.Dhaka Univ. J. Pharm. Sci. 15(2): 203-208, 2016 (December)


2019 ◽  
Vol 3 (2) ◽  
pp. 18-22
Author(s):  
Letícia Lenz Sfair ◽  
Caren Gobetti ◽  
Martin Steppe ◽  
Elfrides Schapoval

A dissolution test for mianserin hydrochloride in coated tablets containing 30 mg was developed and validated using a fast ultraviolet spectrophotometric method. The appropriate conditions were determinate after testing sink conditions, agitation spped and dissolution medium. The sink conditions tested showed that mianserin hydrochloride was soluble in 0.01 and 0.1 M hydrochloric acid (HCl), acetate buffer pH 4.1 and 5.0 and phosphate buffer pH 6.8. Then, dissolution tests were performed to investigate the drug release in each medium. Optimal conditions to carry out the dissolution test were 900 mL 0.1 M HCl and USP apparatus 2 (paddle) at 50 rpm stirring speed. The quantification method was also adapted and validated. The UV method showed specificity, linearity, precision and accuracy. The in vitro dissolution test can be used to evaluate the drug release profile and the data was used as an aid to establish a possible correlation with in vivo data.


2013 ◽  
Vol 16 (1) ◽  
pp. 1-9
Author(s):  
Shahriar Ahmed ◽  
Mehrina Nazmi ◽  
Ikramul Hasan ◽  
Sabiha Sultana ◽  
Shimul Haldar ◽  
...  

Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37°C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14483 Bangladesh Pharmaceutical Journal 16(1): 1-9, 2013


2015 ◽  
Vol 18 (1) ◽  
pp. 66-71 ◽  
Author(s):  
Sumaiya Mehjabin Tosha ◽  
Ashima Aziz ◽  
Sharmin Jahan Chisty ◽  
Md Asaduzzaman ◽  
Mohiuddin Ahmed Bhuiyan

Pulsatile drug delivery of enalapril maleate is one such system that, by delivering drug at the right time, right place and in right amounts, holds good promises of benefit to the patients suffering from hypertension. The basic design involves the preparation of cross linked hard gelatin capsules using formaldehyde. Then the drug diluent mixtures were prepared and loaded which was separated by using hydrogel plug of polymers of different grades such as HPMC 50 cps, HPMC 100 cps, HPMC K4M, HPMC K15M, HPMC K100M, xanthan gum, carbopol 971 and sodium CMC at different amount (100 and 120 mg). Prepared formulations were subjected to evaluation of various physical parameters and in vitro drug release studies. Dissolution tests were performed using the USP type I basket method at 50 rpm in 6.8 phosphate buffer. From the in vitro dissolution studies it was found that by increasing the amount of polymers, release rate was decreased. Here, 100 mg of HPMC K100M showed 80% drug release in 8 hours whereas 120 mg showed 78.87% drug release in 10 hours. Similar decrease in the release rates were found with the increase of other polymers used in this study. The release data was fitted to various mathematical models such as zero order, first order, Higuchi, Korsmeyer Peppas and Hixson Crowell cube root law. The drug release follows mixed order kinetics and mechanism was found to be non-Fickian diffusion.Bangladesh Pharmaceutical Journal 18(1): 66-71, 2015


2015 ◽  
Vol 4 (10) ◽  
pp. 447-452
Author(s):  
S. Dineshmohan ◽  
V R M Gupta ◽  
A. Ramesh ◽  
V. Harika ◽  
T. Sravani

The main objective of the present exploration was to formulate and evaluate chronomodulated press-coated tablets to deliver the NSAID lornoxicam, when a pain in the joints, functional disability persist in the early morning time is typically observed in most Rheumatoid arthritis (RA) patients. Pre formulation studies and drug excipient compatibility studies were carried out for lornoxicam and excipients. Core tablets containing lornoxicam was prepared by direct compression method and the tablets were subjected to various pre-compression and post-compression parameters (C1-C4 formula) based on the above result best core tablet batch was selected and used for press coating processes. HPMC and EC granules were used as controlled release polymers in the outer layer. These tablets were subjected to pre and post compression parameters, finally the tablets were evaluated for lag time and in vitro dissolution. Results of preformulation studies were acceptable limits. No interaction was observed between lornoxicam and excipients by FTIR. The results of pre and post compression studies were within limits. Formulation code CC3 was identified as best formulation that extends a release profile with 6 h lag time followed by complete lornoxicam release after 8 h. From the graphical representation it can be well perceive that this is perfectly fit in to Korsemeyer which had a Regression coefficient (R2) of 0.9431. The results of the in-vitro release data of this layer were fitted to the Korsemeyer-Peppas equation to examine the release pattern of the drug from the polymeric system. The drug release was identified as super case II transport as the “n” value found to be more than 0.89.Dineshmohan et al., International Current Pharmaceutical Journal, September 2015, 4(10): 447-452


2019 ◽  
Vol 22 (2) ◽  
pp. 135-145
Author(s):  
Aditi Bhowmick ◽  
Tushar Saha ◽  
James Regun Karmoker ◽  
Md Selim Reza

In this present investigation, gastroretentive mucoadhesive microspheres of Repaglinide was formulated, characterized and optimized by applying the design of experiment (DoE) for better release profile and sustain action of the drug. Solvent evaporation technique was used to prepare microspheres, where Methocel K15M CR (X1), Eudragit L 100 (X2) and rpm (X3) were used as independent variables whereas percent cumulative drug release at 8 hours (Y1), bond strength (Y2) and swelling at 8 hours (Y3) were used as dependent variables. Particle size, surface morphology, mucoadhesive bond strength, swelling study, and drug entrapment efficiency were determined to characterize the prepared microspheres. In vitro dissolution study was performed in 0.1N HCl (pH 1.2) media for 8 hours. Response surface of dependent variables was calculated by design expert software and it was found that most of the responses were fitted to the quadratic model. Percent cumulative drug release at 8 hours was found minimum 61.34% and maximum 87.29%, the minimum and maximum range of mucoadhesive bond strength was found 426.02 to 13335.74 N/m2 and in case of swelling at 8 hours, it was found 157.43 and 230.22%. After analyzing the responses, proposed formula was obtained from which minimization of percent cumulative drug release at 8 hours as well as swelling and maximization of bond strength was obtained. Thermal behavior was investigated by DSC study and no interaction was found between drug and excipients from FTIR study. Bangladesh Pharmaceutical Journal 22(2): 135-145, 2019


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1394
Author(s):  
Tobias Auel ◽  
Linus Großmann ◽  
Lukas Schulig ◽  
Werner Weitschies ◽  
Anne Seidlitz

An in vitro dissolution model, the so-called EyeFlowCell (EFC), was developed to test intravitreal dosage forms, simulating parameters such as the gel-like consistency of the vitreous body. The developed model consists of a stereolithography 3D-printed flow-through cell with a polyacrylamide (PAA) gel as its core. This gel needed to be coated with an agarose sheath because of its low viscosity. Drug release from hydroxypropyl methylcellulose-based implants containing either triamcinolone acetonide or fluorescein sodium was studied in the EFC using a schematic eye movement by the EyeMovementSystem (EyeMoS). For comparison, studies were performed in USP apparatus 4 and USP apparatus 7. Significantly slower drug release was observed in the PAA gel for both model drugs compared with the compendial methods. Drug release from fluorescein sodium-containing model implants was completed after 40 min in USP apparatus 4, whereas drug release in the gel-based EFC lasted 72 h. Drug release from triamcinolone acetonide-containing model implants was completed after 35 min in USP apparatus 4 and after 150 min in USP apparatus 7, whereas this was delayed until 96 h in the EFC. These results suggest that compendial release methods may overestimate the drug release rate in the human vitreous body. Using a gel-based in vitro release system such as the EFC may better predict drug release.


2021 ◽  
Vol 12 (2) ◽  
pp. 1063-1073
Author(s):  
Medina-López J R ◽  
Sánchez-Badajos S ◽  
Carreto-Jiménez R M ◽  
García-Hernández P ◽  
Contreras-Jiménez J M

A simple and rapid UV derivative method with zero-crossing determinations was developed for estimation of acetaminophen (ACE) and caffeine (CAF) in fixed-dose combination formulations. The first-derivative of standard solutions of both drugs were used and ACE and CAF were quantified at 273.0 and 216.5 nm, respectively. The method was validated, and it was applied to dissolution studies with the USP Apparatus 2 and flow-through cell (USP Apparatus 4). Dissolution profiles comparisons (generic vs reference) were carried out with model-independent and model-dependent approaches. Mean dissolution time and dissolution efficiency were calculated and significant differences, in almost all calculated parameters, were found (p<0.05). Weibull, logistic, Gompertz, and Probit models were used to fit dissolution data and Probit was the best-fit model that describes the in vitro dissolution performance of ACE and CAF. Using t50% data, derived from this fit, dissolution profiles of ACE in USP Apparatus 2 were significant different (p<0.05). The proposed UV derivative method generates reliable information that can be compared with published results. Dissolution studies of fixed-dose combination formulations are important because quality of generic drug products depends on quality of references. It is essential to maintain a post-marketing evaluation of formulations with analgesic drugs mixed with CAF to offer the population high quality medicines.


Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.


2019 ◽  
Vol 9 (2) ◽  
pp. 89-96
Author(s):  
Abbaraju Krishna Sailaja ◽  
Juveria Banu

Aim: The aim of this investigation was to develop and characterize naproxen loaded chitosan nanoparticles by emulsion interfacial reaction method. Methodology: For emulsion interfacial reaction method chitosan was used as a polymer. In this method, eight formulations were prepared by varying drug to polymer concentration. Discussion: Out of eight formulations prepared using emulsion interfacial reaction method EI8 formulation was found to be the best formulation. The drug content was observed as 94.4%, entrapment efficiency and loading capacity were found to be 87.5% and 75%, respectively. The mean particle diameter was measured as 324.6nm and the Zeta potential value was found to be -42.4mv. In vitro drug release data showed 97.2% of drug release rate sustained up to 12hrs. Conclusion: The results clearly reveal that EI8 formulation having the highest amount of drug was considered as the best formulation because of its small mean particle diameter, good entrapment efficiency, and stability.


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