scholarly journals Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

2015 ◽  
Vol 51 (2) ◽  
pp. 383-392
Author(s):  
Cristina Helena dos Reis Serra ◽  
Kyung Hee Chang ◽  
Thaisa Marinho Dezani ◽  
Valentina Porta ◽  
Sílvia Storpirtis
Keyword(s):  
Urinary Excretion ◽  
Healthy Volunteers ◽  
High Performance ◽  
Bioequivalence Study ◽  
Immediate Release ◽  
International Standards ◽  
Pharmacokinetic Parameters ◽  
Tablet Formulations ◽  
Dissolution Efficiency

<p>The aim of the present study was to assess the bioequivalence of two cephalexin tablet formulations available in the Brazilian market (product A as reference formulation and product B as test formulation). Dissolution efficiency (DE%) was calculated for both formulations to evaluate their <italic>in vitro</italic>biopharmaceutical features. The oral bioequivalence study was performed in twenty-four healthy volunteers in a crossover design. Single oral dose (tablet containing 500 mg of cephalexin) of each product was administered with two weeks of washout period. Urinary concentrations of cephalexin were measured by high-performance liquid chromatography (HPLC) method and pharmacokinetics parameters were estimated by urinary excretion data. The bioequivalence was determined by the following parameters: the cumulative amount of cephalexin excreted in the urine, the total amount of cephalexin excreted in the urine and the maximum urinary excretion rate of cephalexin. DE values of immediate-release cephalexin tablets (500 mg) were 68.69±4.18% for product A and 71.03±6.63% for product B. Regarding the dissolution test of the two brands (A and B) analysed, both were in compliance with the official pharmacopeial specifications, since the dissolution of both formulations was superior to 80% of the amount declared in the label after 45 minutes of test (A=92.09%±1.84; B=92.84%±1.08). The results obtained indicated that the products A and B are pharmaceutical equivalents. Confidence intervals for the pharmacokinetic parameters were in compliance with the international standards, indicating that products A and B can be considered bioequivalents and, therefore, interchangeable.</p>

scholarly journals Bioequivalence Study of Pantoprazole Sodium-HPBCD and Conventional Pantoprazole Sodium Enteric-Coated Tablet Formulations

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Sandesh P. Kamdi ◽  
Prashant J. Palkar
Keyword(s):  
High Performance ◽  
Bioequivalence Study ◽  
Pharmacokinetic Parameters ◽  
Two Phase ◽  
Enteric Coated Tablet ◽  
Coated Tablet ◽  
Bioequivalence Range ◽  
The Mean ◽  
Tablet Formulations ◽  
Enteric Coated

The objective of this study was to investigate the bioequivalence of two formulations of 40 mg pantoprazole sodium enteric-coated tablets: Tripepsa as the test and Pantocid as the reference. The two products were administered as a single oral dose according to a randomized two-phase crossover with a 1-month washout period in 25 healthy Indian volunteers. After drug administration, serial blood samples were collected over a period of 30 hours. Plasma pantoprazole concentrations were measured by high-performance liquid chromatography with UV detection. Pharmacokinetic parameters were analyzed based on noncompartmental analysis. The logarithmically transformed data of and were analyzed for 90% confidence intervals (CI) using ANOVA. The mean (90% CI) values for the ratio of and values of the test product over those of the reference product were 90.21 (83.69–97.24) and 108.68 (100.21–117.86), respectively (within the bioequivalence range of 80–125%). On the basis of pharmacokinetic parameters including , , and values, both the formulations were bioequivalent.

scholarly journals In Vivo Predictive Dissolution (IPD) for Carbamazepine Formulations: Additional Evidence Regarding a Biopredictive Dissolution Medium

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 558 ◽  
Author(s):  
Marival Bermejo ◽  
Jessica Meulman ◽  
Marcelo Gomes Davanço ◽  
Patricia de Oliveira Carvalho ◽  
Isabel Gonzalez-Alvarez ◽  
...  
Keyword(s):  
Latin American ◽  
Bioequivalence Study ◽  
Immediate Release ◽  
Dissolution Medium ◽  
Time Scaling ◽  
Health Authorities ◽  
Medium Level ◽  
One Step

The aim of the present study was to bring additional evidence regarding a biopredictive dissolution medium containing 1% sodium lauryl sulphate (SLS) to predict the in vivo behavior of carbamazepine (CBZ) products. Twelve healthy volunteers took one immediate release (IR) dose of either test and reference formulations in a bioequivalence study (BE). Dissolution profiles were carried-out using the medium. Level A in vitro–in vivo correlations (IVIVC) were established using both one-step and two-step approaches as well as exploring the time-scaling approach to account for the differences in dissolution rate in vitro versus in vivo. A detailed step by step calculation was provided to clearly illustrate all the procedures. The results show additional evidence that the medium containing 1% SLS can be classified as a universal biopredictive dissolution tool, and that both of the approaches used to develop the IVIVC (one and two-steps) provide good in vivo predictability. Therefore, this biopredictive medium could be a highly relevant tool in Latin-American countries to ensure and check the quality of their CBZ marketed products for which BE studies were not requested by their regulatory health authorities.

scholarly journals COMPARATIVE IN VITRO DISSOLUTION STUDY ON METFORMIN MARKET PRODUCTS USING DIFFERENT DISSOLUTION APPARATUSES

2019 ◽  
pp. 65-72
Author(s):  
HANAN M. HASHEM ◽  
AYA R. ABDOU ◽  
NADIA M. MURSI ◽  
LAILA H. EMARA
Keyword(s):  
Reference Product ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Metformin Hydrochloride ◽  
Innovator Product ◽  
Similarity Factor ◽  
Generic Products ◽  
Dissolution Efficiency ◽  
Usp Apparatus

Objective: This study was proposed to evaluate and compare the in vitro dissolution profiles of six Metformin Hydrochloride (MH) market products. Methods: Different dissolution apparatuses (USP apparatus II, IV and beaker method) were used to evaluate the dissolution profiles (in phosphate buffer, pH 6.8) of two immediate release (IR) generic products of Metformin Hydrochloride (MH): Cidophage® 1000 mg (G1, Egyptian market) and Metformin arrow® 1000 mg (G2, French market) with respect to the reference products named Glucophage® 850 mg (R1, Egyptian market and R2, French market). In addition to a generic controlled-release (CR) product; Cidophage Retard® 850 mg (G3) versus the reference product; Glucophage XR® 1000 mg (R3) (both from Egyptian market). Dissolution efficiency (D. E.) and the similarity factor (f2) were calculated. Weight uniformity, hardness, tablet dimensions and MH content were measured. Results: Results of the three apparatuses showed that MH IR products studied (reference and generics) did not meet the 75% USP 30 specifications for MH dissolved at 30 min. For MH CR products, Glucophage XR® did not fulfill the USP release criteria, while Cidophage Retard® did. USP apparatus IV revealed the highest sensitivity and discriminative capability. Conclusion: Generally, MH IR generics (G1 and G2) might be interchangeable with the innovator product (Glucophage®). However, Cidophage Retard® might not be interchangeable with Glucophage XR®.

Bioequivalence study of two perindopril erbumine tablet formulations in healthy volunteers

2011 ◽  
Vol 61 (04) ◽  
pp. 234-238 ◽  
Author(s):  
Effi Setiawati ◽  
Siti Deniati ◽  
Danang Yunaidi ◽  
Lucia Handayani ◽  
Iwan Santoso ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Bioequivalence Study ◽  
Perindopril Erbumine ◽  
Tablet Formulations

Application of hot-melt extrusion technology in immediate-release abuse-deterrent formulations

2017 ◽  
Vol 13 (6) ◽  
pp. 473 ◽  
Author(s):  
Klaus Wening, PhD ◽  
Sebastian Schwier, PhD ◽  
Hans-J. Stahlberg, MD ◽  
Eric Galia, PhD
Keyword(s):  
Phase 1 ◽  
White Male ◽  
Immediate Release ◽  
Hot Melt Extrusion ◽  
Pharmacokinetic Parameters ◽  
Mechanical Resistance ◽  
In Vitro Test ◽  
Melt Extrusion ◽  
Hot Melt

Objective: Hot-melt extrusion (HME) technology has been used for manufacturing extended-release abuse-deterrent formulations (ADFs) of opioid-type analgesics with improved tamper-resistant properties. Our objective was to describe application of this technology to immediate-release (IR) ADFs.Design: For development of a sample IR ADF (hydrocodone 10 mg/acetaminophen 325 mg) based on HME, feasibility studies were performed using different excipients. The formulation selected for further development was evaluated via in vitro test battery. Moreover, in vivo performance of IR ADF technologies was investigated in an open-label, randomized, cross-over, phase 1, relative oral bioavailability study with another opioid (model compound).Setting: Single-center bioavailability trial.Participants: Twenty-four healthy white male subjects.Interventions: ADF IR formulation of an opioid and marketed IR formulation.Main Outcome Measure(s): For feasibility and in vitro studies, dissolution profiles, syringeability, particle size distribution after physical manipulation, and extractability were evaluated. For the phase 1 study, pharmacokinetic parameters were evaluated and compared for ADF IR and a marketed IR formulation.Results: After manipulation, the majority of particles from the ADF IR formulation were >500 μm and, thus, not considered suitable for intranasal abuse, while the majority of particles for the reference marketed IR formulation were <500 μm. The ADF IR formulation was resistant to syringing and preparation for potential intravenous injection. In healthy subjects, pharmacokinetics of an ADF and marketed IR formulation of an opioid were nearly identical.Conclusions: Application of HME to IR formulations led to development of products with improved mechanical resistance to manipulation for intranasal or intravenous preparation, but similar bioavailability.

scholarly journals Determination of Di(2-ethylhexyl phthalate) released in the blood from PVC line during the hemodialysis procedure

2018 ◽  
Vol 23 (1) ◽  
Author(s):  
Beatriz Luci Fernandes ◽  
Fernanda Maria ◽  
Lia Sumie Nakao ◽  
Max Ingberman ◽  
Marcia Regina Cubas
Keyword(s):  
Healthy Volunteers ◽  
Body Mass ◽  
High Performance ◽  
Average Concentration ◽  
International Standards ◽  
Human Beings ◽  
Alternative Materials ◽  
Ethics In Research ◽  
Ethylhexyl Phthalate

ABSTRACT The objective of the work is to demonstrate the applicability of the High-Performance Liquid Chromatography (HPLC) on the quantification of the Di(2-ethylhexyl phthalate) (DEHP) released from the Polyvinyl Chloride (PVC) line into the circulating blood during the hemodialysis procedure. As the proposal is not to validate the method, blood samples from five patients and three healthy volunteers were collected, and the plasmas were isolated, prepared and analyzed. The average concentration of DEHP in the patient's plasma was 0.19±0.12 mg/kg of body mass, while in the plasma of the healthy volunteers was 0.003±0.002 µg/kg of body mass. The results showed that the method presented is an alternative to quantify the DEHP in the blood and could assist in the search for alternative materials to apply to extracorporeal circulation equipment. The study was performed according to the national and international standards of ethics in research involving human beings (CEP PUCPR Prot. n.5802).

scholarly journals Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, andIn VitroandIn VivoEvaluation

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Gagganapalli Santhoshi Reddy ◽  
Usha Yogendra Nayak ◽  
Praful Balavant Deshpande ◽  
Srinivas Mutalik
Keyword(s):  
Blood Pressure ◽  
Drug Release ◽  
Immediate Release ◽  
Lag Time ◽  
Early Morning ◽  
Quadratic Model ◽  
Pharmacokinetic Parameters ◽  
Pulsatile Release

The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat early morning surge in blood pressure. Immediate release core tablets containing lercanidipine HCl were prepared and optimized core tablets were compression-coated using buoyant layer containing polyethylene oxide (PEO) WSR coagulant, sodium bicarbonate, and directly compressible lactose. FPRTs were evaluated for variousin vitrophysicochemical parameters, drug-excipient compatibility, buoyancy, swelling, and release studies. The optimized FPRTs were testedin vivoin New Zealand white rabbits for buoyancy and pharmacokinetics. DoE optimization of data revealed FPRTs containing PEO (20% w/w) with coat weight 480 mg were promising systems exhibiting good floating behavior and lag time in drug release. Abdominal X-ray imaging of rabbits after oral administration of the tablets, confirmed the floating behavior and lag time. A quadratic model was suggested for release at 7th and 12th h and a linear model was suggested for release lag time. The FPRT formulation improved pharmacokinetic parameters compared to immediate release tablet formulation in terms of extent of absorption in rabbits. As the formulation showed delay in drug release bothin vitroandin vivo, nighttime administration could be beneficial to reduce the cardiovascular complications due to early morning surge in blood pressure.

scholarly journals DESIGN, OPTIMIZATION AND EVALUATION OF ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH VALERATE–A NOVEL SUPERDISINTEGRANT

2021 ◽  
pp. 168-176
Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Compression Method ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Dissolution Efficiency

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design. Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min. Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.

scholarly journals Bioequivalence study of two Irbesartan/Hydrochlorothiazide tablet formulations in Mexican healthy volunteers

2017 ◽  
Vol 1 (1) ◽  
Author(s):  
Núñez-Guzmán NA ◽  
Ruíz-Molina D ◽  
Muñoz-Ibarra AI ◽  
Figueroa-Núñez B ◽  
Almada-Alba J
Keyword(s):  
Healthy Volunteers ◽  
Bioequivalence Study ◽  
Tablet Formulations
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