scholarly journals Evaluation of Dissolution Behavior of Paracetamol Suspensions

1970 ◽  
Vol 7 (1) ◽  
pp. 53-58 ◽  
Author(s):  
Md Golam Azam ◽  
Syed Shabbir Haider
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
First Order ◽  
Key Words Paracetamol ◽  
Suspending Agents ◽  
Initial Drug

Ten brands of commercial paracetamol suspensions were investigated for their dissolution characteristics in 0.1 N HCl at a speed of 25 rpm using USP dissolution test apparatus II (Paddle method). It was observed that differences exist among the rate of paracetamol dissolution from the samples, particularly at the early stages. For nine of the brands, paracetamol dissolution varied between 72% and 100% at 15 minutes. One of the samples showed a very unsatisfactory rate and extent of drug dissolution as only 39% and 52% paracetamol was released after 15 and 30 minutes respectively. The effect of two commonly used suspending agents, CMC-Na and Avicel, on the release of paracetamol was studied using four laboratory-made suspensions. Retarded drug dissolution was observed which was related to the concentration of the suspending agents. Drug release kinetics followed first order as well Higuchi models. Viscosity of the samples and initial drug release was found to be inversely correlated (R2=0.9081 at 3 minutes) which faded away with the lapse of time. Key words: Paracetamol suspension, in vitro dissolution, suspending agents   DOI = 10.3329/dujps.v7i1.1218 Dhaka Univ. J. Pharm. Sci. 7(1): 53-58, 2008 (June)

scholarly journals In Vitro Release Kinetics Study of Different Brands of Esomeprazole Sustained Release Tablets Available in Bangladesh

1970 ◽  
Vol 2 (1) ◽  
pp. 27-31 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Tasbira Jesmeen ◽  
Md Mesbah Uddin Talukder ◽  
Abu Taher Md Rajib ◽  
DM Mizanur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
National Brand ◽  
First Order ◽  
Time Period ◽  
Esomeprazole Magnesium

Commercially available four national and four international brands of esomeprazole magnesium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours and simulated intestinal medium (pH 6.8) for 8 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specifications for drug release in simulated gastric medium. However, one of the national brands (Code: MP-1) and one of the international brands (MP-7) failed to fulfill the official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of that national and international brand were 70.49% and 67.05% respectively within the specified time period, however one national brand (Code: MP-4) released 103.46 % drug within 8th hour in intestinal medium. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of esomeprazole magnesium sustained release matrix tablets. It was found that zero order release kinetics was the predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: MP-2, MP-3, MP-4, MP-5, MP-6 and MP-8) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for one national and also one international non compliant brands (Code: MP-1 and MP-6). Key Words: In vitro dissolution; Sustained release; Market preparations; Kinetic analysis; Esomeprazole; National brand; International brand. DOI: 10.3329/sjps.v2i1.5812Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 27-31

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 In vitro Release Kinetics Study of Ambroxol Hydrochloride Pellets Developed by Extrusion Spheronization Technique Followed by Acrylic Polymer Coating

1970 ◽  
Vol 7 (1) ◽  
pp. 75-81 ◽  
Author(s):  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Golam Kibria ◽  
Muhammad Rashedul Islam ◽  
Reza-ul Jalil
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Acrylic Polymer ◽  
Eudragit Rs ◽  
Methacrylate Copolymer ◽  
Ambroxol Hydrochloride ◽  
Eudragit Rl ◽  
Extrusion Spheronization

The aim of the present study was to investigate the effect of Ammonio Methacrylate Copolymer Dispersion Type A (Eudragit RL 30 D) and Ammonio Methacrylate Copolymer Dispersion Type B (Eudragit RS 30 D) combination in different weight ratios on the release kinetics of Ambroxol Hydrochloride from coated pellets. Microcrystalline cellulose, lactose, maize starch, hydroxypropyl methylcellulose and the drug was incorporated in the nuclei prepared by Extrusion-Spheronization technique which was coated with Eudragit RL 30D and Eudragit RS 30D in 1:1,1:1.5,1:2,1:2.5 and 1:3 ratios. The in vitro dissolution studies were carried out in 0.1N HCl for 1 hour followed by phosphate buffer (pH 6.8) for 11 h with USP dissolution apparatus Type-II. Drug release decreased with increasing amount of Eudragit RS 30 D in all cases. The drug release followed first order and Higuchi release kinetics. The Korsmeyer plot revealed n=0.50-0.61 or non-Fickian transport mechanism for drug release. From one way ANOVA it was found that the ratio of binary polymer mixer had significant (p < 0.05) effect on drug release. Key words: Aqueous coating, Eudragit, release kinetics, pellet, extrusion-spheronization  DOI = 10.3329/dujps.v7i1.1222 Dhaka Univ. J. Pharm. Sci. 7(1): 75-81, 2008 (June)

scholarly journals Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?

2014 ◽  
Vol 17 (2) ◽  
pp. 207 ◽  
Author(s):  
Yady Juliana Manrique-Torres ◽  
Danielle J Lee ◽  
Faiza Islam ◽  
Lisa M Nissen ◽  
Julie A.Y. Cichero ◽  
...  
Keyword(s):  
Drug Release ◽  
Orange Juice ◽  
Immediate Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Thickening Agents

Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Statistical assessment of in vitro drug release kinetics and quality evaluation of desloratadine orally disintegrating generic tablets available in Bangladesh

2020 ◽  
pp. 174113432094775
Author(s):  
Madhabi Lata Shuma ◽  
Shimul Halder
Keyword(s):  
Release Kinetics ◽  
The United States ◽  
Quality Parameters ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orally Disintegrating Tablets

The objective of the present study was to compare the in vitro equivalence of different orally disintegrating tablets (ODT) of Desloratadine (DES) available in Bangladesh pharmaceutical market with the reference brand. The in vitro dissolution study was carried out using the United States Pharmacopoeia (USP) paddle method and a comparative study were also carried out with the reference brand. Other pharmacopoeial and non-pharmacopoeial quality assessment parameters including hardness, friability, water absorption ratio, and disintegration time etc. were also evaluated. From the results of the dissolution profile of the commercially available products, it found majority of the products didn’t exhibited compendial requirements in dissolution behavior to the reference brand with model-independent approach ( f2 > 50, f1 < 15) and showed statistically significant differences. Additionally, the data of different physical quality parameters revealed that all commercial products complied with the official specifications. From these findings, it could be suggested that the DES-ODT formulations’ available in the Bangladesh market could be prescribed; however additional experiments might require to clarify the interchangeability among the products.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION

2018 ◽  
Vol 11 (6) ◽  
pp. 148
Author(s):  
Srinivasa Rao Baratam ◽  
Vijayaratna J
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Linear Regression Method ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.

DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE MUCOADHESIVE MICROBEADS CONTAINING SIMVASTATIN WITH DIFFERENT CROSS LINKING AGENTS

2020 ◽  
pp. 118-126
Author(s):  
VENKATA RAMANA REDDY K. ◽  
NAGABHUSHANAM M. V. ◽  
PAMULA REDDY B. ◽  
RAVINDAR NAIK E.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Aluminium Chloride ◽  
In Vitro Dissolution ◽  
Cross Linking ◽  
Stability Studies ◽  
Study Results ◽  
Curing Agents

Objective: The aim of the present work was to prepare and examine drug release of the oral controlled release microbeads using different curing agents by emulsification internal ionic gelation technique. Methods: Cross-linked alginate microbeads were prepared with different cross linking agents by using mucoadhesive properties. The formation and compatibility of microbeads were confirmed by compatibility studies. Prepared microbeads evaluated for encapsulated efficiency, micromeritic properties, drug loading, in vitro wash off studies, in vitro dissolution studies, drug release kinetics and stability studies Results: The in vitro drug release was influenced by both type of curing agents and type of polymers and no significant changes in characterization parameters was observed after 3 mo stability studies. The sustained release profile of optimized batch was found to be 99.66±0.18% in comparison to pure drug profile of 28.64±0.02% at 12 h release study. Results of both wash-off and in vitro studies suggests that batch (SF2) prepared with aluminium chloride has shown better mucoadhesive property. Drug release of optimized batch follows zero order with non fickian mechanism according to Korsmeyer-Peppas equation. Conclusion: The data suggest the use of simvastatin mucoadhesive cross linked microbeads to offer the potential for oral controlled drug delivery with improved gastric retention and capable to provide sustained drug release by using cross linking agents.

Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol

2013 ◽  
Vol 6 (3) ◽  
pp. 2164-2171
Author(s):  
S. B. Shirsand ◽  
G V Wadageri ◽  
S A Raju ◽  
Gopikrishna Kolli
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Hydroxypropyl Methylcellulose ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Stability Studies ◽  
Matrix Layer ◽  
Buccal Tablets ◽  
Carbopol 934P

In present study we studied the feasibility of preparing mucoadhesive buccal delivery systems containing carvedilol to improve drug residence time on buccal mucosa and drug dissolution rate, to circumvent the first-pass metabolism and quick drug entry into the systemic circulation. Bilayer buccal tablets of carvedilol prepared using controlled release and mucoadhesive polymers (hydroxypropyl methylcellulose 15 cps, 50 cps, K4M and Carbopol 934p) along with impermeable backing layer (ethyl cellulose). 15 formulations were developed with varying concentrations of polymers. The designed tablets were evaluated for tablet size, shape, in vitro drug release, stability studies, bioavailability studies and drug-excipients interaction (FTIR). Among the 15 formulations, F151 containing hydroxypropyl methylcellulose 15 cps (48% w/w of matrix layer), Carbopol 934p (2% w/w of matrix layer) and mannitol (channeling agent, 34.5% w/w of matrix layer) was found to be promising. Dissolution tests revealed that 84.73% of carvedilol was dissolved from the formulation F151 in 8 h along with satisfactory bio adhesion strength (5.71 g). Bioavailability studies of the promising formulation were compared with that of the oral solution.  The percentage relative bioavailability of the buccal tablets was found to be 121.27%. Stability studies, on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics (p<0.05). FTIR studies show no evidence of interaction between drug and excipients. It was concluded that mucoadhesive buccal tablets of carvedilol with controlled unidirectional drug release along with satisfactory bioadhesion strength and with sufficient residence time can be successfully developed by direct compression method.

scholarly journals Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 627
Author(s):  
Ahmad A. Shahba ◽  
Ahmad Y. Tashish ◽  
Fars K. Alanazi ◽  
Mohsin Kazi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Negative Impact ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Model ◽  
Dissolution Efficiency ◽  
Drug Free

The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin® US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.

scholarly journals Development of Sustained Release Preparations of Metoclopramide Hydrochloride Based on Fatty Matrix

2013 ◽  
Vol 11 (2) ◽  
pp. 129-136 ◽  
Author(s):  
Monnujan Nargis ◽  
Md Saiful Islam ◽  
Fatima Naushin ◽  
Syed Shabbir Haider
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Solubility Behavior ◽  
Uptake Rates ◽  
S Model

Sustained release formulations of metoclopramide HCl (4-amino-5-chloro-N-(2-diethylaminoethyl)-2- methoxybenzamide hydrochloride) (MH) were prepared using carnauba wax (CW) and stearic acid (SA) as matrix formers. Granules were prepared by melt granulation method while direct compression technique was used to prepare the tablets. The drug release profiles of these products were studied by in-vitro dissolution testing in simulated gastric, gastrointestinal and intestinal media of pH 1.2, 4.5 and 7.5, respectively. The increase in the proportion of SA in the granules produced a concomitant decrease of the initial drug release rate but later on the release rate was enhanced in the intestinal medium. Drug release was found to be affected by compression force and stirring rate but also showed a dependency on pH of the dissolution fluid. The fastest release rate was found at pH 4.5 and the slowest at pH 1.2 which was consistent with the drug’s solubility behavior. Matrix erosion and water uptake rates were highest in the intestinal medium and lowest in the gastric medium. The drug release kinetics followed the Higuchi’s model in all cases. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14563 Dhaka Univ. J. Pharm. Sci. 11(2): 129-136, 2012 (December)

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