Taste and dissolution of theophylline extended-release dry syrups

2018 ◽  
Vol 14 (3) ◽  
pp. 117-121
Author(s):  
Sumio Chono ◽  
Akari Ikeda ◽  
Shiori Ishikawa ◽  
Kohei Togami
Keyword(s):  
Controlled Release ◽  
Healthy Volunteers ◽  
Extended Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Sensory Testing ◽  
Dissolution Tests ◽  
Individualized Treatments

Objectives In this study, we examined the taste and dissolution of theophylline extended-release dry syrups using one branded and six generic formulations. Methods Healthy volunteers underwent sensory testing to assess the syrup taste. Drug dissolution was examined using in vitro dissolution tests. Results and discussion: Syrup taste, including sweetness, bitterness, and aftertaste, was different between formulations. These differences can likely be attributed to the presence of different pharmaceutical additives between formulations. Our results indicated that syrup aftertaste was dependent on the level of sweetness and bitterness. In addition, dissolution behaviors were different between formulations, suggesting bio-inequivalence between formulations. These differences likely reflect the use of different controlled-release technologies between formulations. Conclusions This study provides useful information for selecting branded or generic theophylline extended-release dry syrups for individualized treatments.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF SALBUTAMOL SULPHATE AND THEOPHYLLINE EXTENDED-RELEASE TABLETS USING MODIFIED POLYMERS

2018 ◽  
Vol 10 (8) ◽  
pp. 67
Author(s):  
Naveen Goyal ◽  
Anil Kumar
Keyword(s):  
Ethyl Cellulose ◽  
Extended Release ◽  
Research Work ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Salbutamol Sulphate ◽  
Modified Polymers

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).

scholarly journals Synthesis and characterization of molecularly imprinted polymer for controlled release of tramadol

2010 ◽  
Vol 8 (3) ◽  
pp. 687-695 ◽  
Author(s):  
Saman Azodi-Deilamia ◽  
Majid Abdoussa ◽  
S. Rezvaneh Seyedib
Keyword(s):  
Controlled Release ◽  
Bulk Polymerization ◽  
Molecular Structures ◽  
In Vitro Dissolution ◽  
Imprinted Polymer ◽  
Molecularly Imprinted ◽  
Functional Monomers ◽  
Dissolution Tests

AbstractIn this paper, we describe how to prepare a highly selective imprinted polymer by a bulk polymerization technique. We used tramadol as the template, (MAA) as functional monomers, and (EGDMA) as the cross-linker in chloroform as solvent. Results from Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Scanning Electron microscopy (SEM) show that this imprinted sorbent exhibits good recognition and high affinity for tramadol. Selectivity of molecularly imprinted polympers (MIP) was evaluated by comparing several substances with similar molecular structures to that of tramadol. Controlled release of tramadol from MIPs was investigated through in vitro dissolution tests and by measuring the absorbance at λmax of 272 nm by (HPLC-UV). The dissolution media employed were hydrochloric acid pH 3.0 and phosphate buffers, pH 5.0 and 7.4, maintained at 37 and 25 ± 0.5°C. The results show the ability of MIP polymers to control tramadol release. In all cases, the release of MIPs was deferred for a longer time as compared to NMIP. At a pH of 7.4 and 25°C slower release of tramadol imprinted polymer occurred.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

scholarly journals Electrospun Janus Beads-On-A-String Structures for Different Types of Controlled Release Profiles of Double Drugs

Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 635
Author(s):  
Ding Li ◽  
Menglong Wang ◽  
Wen-Liang Song ◽  
Deng-Guang Yu ◽  
Sim Wan Annie Bligh
Keyword(s):  
Controlled Release ◽  
Combined Therapy ◽  
Diffusion Mechanism ◽  
Amorphous State ◽  
Electrospinning Process ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Sem Images ◽  
Release Profiles

A side-by-side electrospinning process characterized by a home-made eccentric spinneret was established to produce the Janus beads-on-a-string products. In this study, ketoprofen (KET) and methylene blue (MB) were used as model drugs, which loaded in Janus beads-on-a-string products, in which polyvinylpyrrolidone K90 (PVP K90) and ethyl cellulose (EC) were exploited as the polymer matrices. From SEM images, distinct nanofibers and microparticles in the Janus beads-on-a-string structures could be observed clearly. X-ray diffraction demonstrated that all crystalline drugs loaded in Janus beads-on-a-string products were transferred into the amorphous state. ATR-FTIR revealed that the components of prepared Janus nanostructures were compatibility. In vitro dissolution tests showed that Janus beads-on-a-string products could provide typical double drugs controlled-release profiles, which provided a faster immediate release of MB and a slower sustained release of KET than the electrospun Janus nanofibers. Drug releases from the Janus beads-on-a-string products were controlled through a combination of erosion mechanism (linear MB-PVP sides) and a typical Fickian diffusion mechanism (bead KET-EC sides). This work developed a brand-new approach for the preparation of the Janus beads-on-a-string nanostructures using side-by-side electrospinning, and also provided a fresh idea for double drugs controlled release and the potential combined therapy.

scholarly journals DESIGN, OPTIMIZATION AND EVALUATION OF CETRIZINE DIHYDROCHLORIDE FAST DISSOLVING FILMS EMPLOYING STARCH TARTRATE–A NOVEL SUPERDISINTEGRANT

2019 ◽  
pp. 75-86
Author(s):  
R. SANTOSH KUMAR ◽  
ANNU KUMARI ◽  
B. KUSUMA LATHA ◽  
PRUDHVI RAJ
Keyword(s):  
Tensile Strength ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Folding Endurance ◽  
Contour Plots ◽  
The Individual

Objective: The aim of the current research is optimization, preparation and evaluation of starch tartrate (novel super disintegrant) and preparation of fast dissolving oral films of cetirizine dihydrochloride by employing starch tartrate. Methods: To check the drug excipient compatibility studies of the selected drug (Cetrizine dihydrochloride) and the prepared excipient i. e starch tartrate, different studies like FTIR (Fourier-transform infrared spectroscopy), DSC (Differential scanning calorimetry) and thin-layer chromatography (TLC) were carried out to find out whether there is any interaction between cetirizine dihydrochloride and starch tartrate. The solvent casting method was used for the preparation of fast dissolving films. The prepared films were then evaluated for thickness, folding endurance, content uniformity, tensile strength, percent elongation, in vitro disintegration time and in-vitro dissolution studies. Response surface plots and contour plots were also plotted to know the individual and combined effect of starch tartrate (A), croscarmellose sodium (B) and crospovidone (C) on disintegration time and drug dissolution efficiency in 10 min (dependent variables). Results: Films of all the formulations are of good quality, smooth and elegant by appearance. Drug content (100±5%), thickness (0.059 mm to 0.061 mm), the weight of films varies from 51.33 to 58.06 mg, folding endurance (52 to 67 times), tensile strength (10.25 to 12.08 N/mm2). Fast dissolving films were found to disintegrate between 34 to 69 sec. Percent dissolved in 5 min were found to be more in F1 formulation which confirms that starch tartrate was effective at 1%. Conclusion: From the research conducted, it was proved that starch tartrate can be used in the formulation of fast dissolving films of cetirizine dihydrochloride. The disintegration time of the films was increased with increase in concentration of super disintegrant.

scholarly journals Automation of dissolution tests

2003 ◽  
Vol 25 (1) ◽  
pp. 7-15 ◽  
Author(s):  
Rolf Rolli
Keyword(s):  
Quality Control ◽  
In Vitro Dissolution ◽  
Pharmaceutical Companies ◽  
Dissolution Testing ◽  
Simultaneous Operation ◽  
Task Forces ◽  
The Core ◽  
Dissolution Tests ◽  
The 1960S

Dissolution testing of drug formulations was introduced in the 1960s and accepted by health regulatory authorities in the 1970s. Since then, the importance of dissolution has grown rapidly as have the number of tests and demands in quality-control laboratories. Recent research works lead to the development of in-vitro dissolution tests as replacements for human and animal bioequivalence studies. For many years, a lot of time and effort has been invested in automation of dissolution tests. There have been a number of in-house solutions from pharmaceutical companies and many have created task forces or even departments to develop automation. Robotic solutions with sequential operation were introduced as well as the simultaneous operation concept developed by SOTAX. Today, pharmaceutical companies focus their resources mainly on the core business and in-house engineering solutions that are very difficult to justify. Therefore, it is important to know the basic considerations in order to plan an automation concept and implement it together with a vendor.

scholarly journals In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 215 ◽  
Author(s):  
Marcelo Dutra Duque ◽  
Daniela Amaral Silva ◽  
Michele Georges Issa ◽  
Valentina Porta ◽  
Raimar Löbenberg ◽  
...  
Keyword(s):  
Reference Product ◽  
Plasma Concentrations ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Time Data ◽  
Simulation Results ◽  
Population Simulation

A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.

scholarly journals Development and Validation of an Eco-friendly HPLC-UV-DAD Method for the Determination of Allopurinol in Pharmaceuticals with Application to In vitro Dissolution Studies

2021 ◽  
Vol 11 (5) ◽  
pp. 13089-13101
Keyword(s):  
Factorial Design ◽  
Matrix Effects ◽  
Dissolution Kinetics ◽  
In Vitro Dissolution ◽  
Dissolution Test ◽  
Dissolution Studies ◽  
Dissolution Tests ◽  
Development And Validation

In this study, a sustainable HPLC-UV-DAD method was developed and validated for the determination of allopurinol in tablets and optimization of the dissolution test using factorial design. The separation of the analyte from the sample matrix was achieved in 3.01 minutes in a C8 column (4.6 mm X 150 mm X 5 μm), using mobile phase 0.1 mol L-1 HCl (25%) + ethanol (50%) + ultrapure water (25%) by UV detection at 249 nm. The method presented satisfactory analytical parameters of validation (specificity, selectivity, linearity, stability, precision, accuracy, and robustness), showing no matrix effects. The dissolution test was optimized by complete factorial design 23 and, the optimal conditions were: HCl 0.001 mol L-1, apparatus II (paddle) and 75 rpm. The analytical procedures and dissolution tests were applied to allopurinol tablets marketed in Bahia, Brazil, to evaluate the dissolution studies. The pharmaceuticals had similar dissolution profiles and first-order dissolution kinetics. This new and sustainable HPLC-UV-DAD method is friendly to the environment and can be used for the routine pharmaceutical analysis of allopurinol in fixed dosage forms.

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