scholarly journals FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF TRANSDERMAL DRUG DELIVERY SYSTEMS CONTAINING EPLERENONE

2022 ◽  
pp. 198-207
Author(s):  
RAMESH SHINDE ◽  
MALARKODI VELRAJ
Keyword(s):  
Skin Irritation ◽  
In Vitro Dissolution ◽  
Log P ◽  
P Value ◽  
Dissolution Profile ◽  
After Effects ◽  
Transdermal Drug Delivery Systems

Objective: The proposed work was aimed at optimization, formulation, and characterization of transdermal patches of eplerenone for efficient transdermal delivery of the drug. Methods: The log p estimation of eplerenone is 1.34, it was closer to standard worth. Log P value in a range of 1 to 4 indicates higher permeation through the skin. FTIIR study was carried out individually for drug, each polymer, and finished product (Patches) compared eplerenone and FTIR spectra of pure drug and polymer. The calibration curve of eplerenone in Phosphate buffer pH 6.8 was analyzed. Results: The selected range of eplerenone was found to be linear. A regression coefficient (R2) at 245 nm was found to be 0.994. Drug content outcomes additionally discovered uniform in all clusters in a range of 97 % to 98 %, that batches arranged with ERS 100 show great mechanical properties contrast with different polymers however helpless glue properties. The flatness of 4 cm2 patches ranges from 348±0.087 mg to 387±0.527 mg. skin irritation it was produced irritation with negligible erythema following 10 d and unequivocal erythema, promptly obvious edema was produced following 12 d. Conclusion: These after-effects of the in vivo skin irritation study recommended that advanced batch S9 doesn't show any kind of significant disturbance on rodent skin for as long as 14 d and it was securely utilized around 24 h. the optimized batch S9 drug was constantly discharged through the Wistar rodent skin up to 16 hr and the delivery design was like an in vitro dissolution profile of the market product.

scholarly journals FORMULATION OF ATOVAQUONE TABLET USING BIOSURFACTANT IN A TERNARY SOLID DISPERSION SYSTEM: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 44-49
Author(s):  
UDAYKUMAR B. BOLMAL ◽  
PRAMOD H. J.
Keyword(s):  
Ternary System ◽  
Solid Dispersion ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Enhanced Dissolution ◽  
Bioavailability Study

Objective: The goal of the present investigation was to improve the solubility and bioavailability of atovaquone tablet, using in-house biosynthesized biosurfactant in the ternary system of solid dispersion containing hydrophilic polymers with varying concentrations of biosurfactant. Atovaquone is an anti-malarial agent and belongs to biopharmaceutical classification system class IV. Methods: The solid dispersion of binary and ternary mixture was prepared using hydroxyl propyl methyl cellulose (HPMC) and biosurfactant respectively by a solvent evaporation method. All the atovaquone tablet formulations were prepared by incorporation of physical mixture, binary and ternary solid dispersed products with excipients by direct compression method. Pre-compression and post-compression parameters of atovaquone tablets were evaluated. In vivo bioavailability study was performed using female albino rabbits. Results: In vitro dissolution profile of binary and ternary system of solid dispersion products showed 8.65% and 34.64% respectively. Precompression and post-compression values of all atovaquone tablets formulations were within the specified limits. In vitro dissolution efficiency of F2 and F5 were 1.44 fold and 6.62 fold respectively, in accordance to the F1. In vivo study revealed that bioavailability of optimized formulation F5 was increased by 2.5 times and time to reach peak concentration was reduced to 1.4 h, in accordance to pure atovaquone suspension. Conclusion: Potential application of biosurfactant in the solid dosage form of atovaquone tablet was proved for enhanced dissolution rate and bioavailability of atovaquone for malaria treatment.

Preclinical evaluation of 99mtechnetium-HYNIC(tricine/TPPTS)-aca-bombesin(7–14) as a targeted imaging agent in prostate cancer.

2011 ◽  
Vol 29 (7_suppl) ◽  
pp. 122-122
Author(s):  
H. J. Ananias ◽  
Z. Yu ◽  
P. H. Elsinga ◽  
I. J. de Jong
Keyword(s):  
Prostate Cancer ◽  
Specific Activity ◽  
Human Prostate ◽  
Log P ◽  
P Value ◽  
Targeted Imaging ◽  
Human Prostate Cancer ◽  
Athymic Mice

122 Background: The peptide bombesin (BN) and derivates thereof show high binding affinity for the gastrin-releasing peptide receptor (GRPR), which is highly expressed in primary and metastasized prostate cancer. We have synthesized a new BN-based radiopharmaceutical 99mTechnetium-HYNIC(tricine/TPPTS)-Aca-BN(7–14) (99mTc-HABN) and evaluated its GRPR targeting properties in vitro and in a xenograft tumor model for human prostate cancer in athymic mice. Methods: 99mTc- HABN was synthesized and its lipophilicity and stability were investigated. The IC50, internalization and efflux properties were determined in vitro using the GRPR expressing human prostate cancer cell line PC-3. 99mTc-HABN biodistribution and microSPECT imaging were performed in PC-3 tumor-bearing athymic mice. Results: 99mTc-HABN was prepared with high labeling yield (>90%), high radiochemical purity (>95%) and a specific activity of ∼19.8 MBq/nmol. The partition coefficient log P value was −1.60±0.06. 99mTc-HABN proved to be stable in human serum for 6 hours. The IC50 of HABN was 12.81±0.14 nM. Incubation of PC-3 cells with 99mTc-HABN demonstrated rapid cellular internalization and a long intracellular retention time. When mice were injected with 99mTc-HABN the activity was predominantly cleared via the kidneys. Uptake in the tumor was 2.24±0.64 %ID/g after 30 minutes, with a steady decrease during the 4 hours study period. In vivo experiments with a blocking agent showed GRPR mediated uptake. 99mTc-HABN microSPECT imaging resulted in clear delineation of the tumor. Conclusions: 99mTc-HABN is a novel BN-based radiopharmaceutical that appears to be suitable for targeted imaging of prostate cancer. No significant financial relationships to disclose.

Comparative study of different meloxicam generic products with the brand product

2019 ◽  
pp. 116-124
Keyword(s):  
Immediate Release ◽  
Generic Product ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Innovator Product ◽  
Similarity Factor ◽  
Generic Products ◽  
Brand Product

This study aims to evaluate different products of meloxicam Table; Five meloxicam immediate-release generic products (15 mg Tables) were compared with the innovator, reference product, (Mobic®, Boehringer) to find the interchangeable product with the innovator product. Different physical tests were conducted including weight uniformity, thickness, diameter, hardness, friability and disintegration test. In addition, prediction of in-vivo behavior was assessed by measuring the dissolution profile of meloxicam for all the products. Similarity factor (f2) was calculated to compare between the dissolution profile of the generic products with the dissolution profile of innovator product. The results revealed that all the studied products are complied with the British Pharmacopoeia requirements. However, not all of them showed similar in-vitro profile to the brand product. Four out of five generic products, included in this study, showed similarity in dissolution profile to the brand one, which indicates possible bio-equivalency, with the advantages of money saving of using such generic products. One generic product showed similarity factor less than 50, which might give an indication that this generic product is not capable to be bioequivalent with the brand (innovator) product. Overall, this study can be considered an important applicable study that gives an indication about the in-vivo performance of different products. In addition, the study demonstrates the applicability of a simple in-vitro dissolution study as a surrogate way of assessing product bioavailability instead of an expensive and complicated in-vivo bioequivalent study.

scholarly journals Characterization of Hepatitis B Surface Antigen Loaded Polylactic Acid-Based Microneedle and Its Dermal Safety Profile

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 531 ◽  
Author(s):  
Young-Guk Na ◽  
Minki Kim ◽  
Mingu Han ◽  
Hyun Wook Huh ◽  
Ji-Seok Kim ◽  
...  
Keyword(s):  
Hepatitis B ◽  
Surface Antigen ◽  
Hepatitis B Surface Antigen ◽  
Skin Irritation ◽  
Hepatitis B Vaccination ◽  
Histological Changes ◽  
Release Testing

A surge of interest in microneedle (MN) vaccines as a novel vaccination system has emerged. Before the clinical application of MN vaccine, an assessment of potential biological risks to skin and quality control of MN must be performed. Therefore, the present study aims to evaluate the physicochemical properties of MN and to evaluate the histological changes and inflammatory cell infiltrations after the application of MN with hepatitis B surface antigen (HBsAg). During in vitro and in vivo release testing, HBsAg MN released over 70% of HBsAg at 30 min. During the pyrogen test of HBsAg MN in rabbit, no rabbit showed an individual rise in temperature of 0.5 °C or more. MN with HBsAg produced the moderate immunization in mice. MN application did not alter the thickness of dermal and epidermal layers in mice. In addition, the topical applications of MN and MN for hepatitis B vaccine did not acutely induce the inflammation, allergic reaction, dermal toxicity and skin irritation. Thus, the MN system for the delivery of HBsAg could be the promising technology in the hepatitis B vaccination.

scholarly journals IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF METRONIDAZOLE, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

2020 ◽  
Author(s):  
EM Ahmed ◽  
ME Ibrahim ◽  
FF Magbool
Keyword(s):  
Peer Review ◽  
Immediate Release ◽  
Correlation Study ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Gastric Emptying Rate ◽  
E Mail ◽  
Release Tablet

Objective: The aim of present study is to examine the in-vitro in-vivo correlation (IVIVC) of immediate release product. Metronidazole 500mg and its brands of immediate release dosage forms. Metronidazole is clearly classified into BCS class I, and could be evaluated under bio waiver conditions. Methods: The in vitro parameters employed were hardness, weight uniformity, friability, disintegration time, absolute drug content, dissolution rate (in 0.1 N Hydrochloric acid, phosphate buffer and acetate buffer at 37ºC), and dissolution efficiencies were also analyzed. The in-vitro dissolution study was performed on the brands, according to FDA,USP dissolution profile in three different PH (1.2), (4.5), and (6.8) at37ºC, using the USP apparatus II, then f1, f2 were determined for the time intervals of 10, 15, 30, 45 and 60 minutes, and dissolution efficiencies were calculated. MINITAB 14 statistical program used for in vitro in vivo correlation, level A was done for reference product. Results: A non linear relation was established which is typical for immediate release formulation, of class 1. There was significant relationship between in vitro and in vivo data of reference metronidazole product, Correlation and distribution of data with correlation coefficient (r=0.724, 0.837, 0.707), nonlinear relationship with p-value (>0.05) =(0.167, 0.098, 0.182), there is no out lines, no lake of fits at P-Values=0.0040, 006, 0.026.Conclusion: Study concluded that there is no linear correlation between percent of drug released and percent of drug absorbed ,this may be due to uncontrollable gastric emptying rate for class one Metronidazole. Peer Review History: Received 2 January 2020;   Revised 1 February; Accepted 3 March, Available online 15 March 2020 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Name: Dr. Hayriye Eda Şatana Kara Affiliation: Gazi University, Turkey E-mail: [email protected]   Name: Dr. Mohamed Ismail Nounou Affiliation: Appalachian College of Pharmacy, Oakwood, Virginia, USA E-mail: [email protected] Comments of reviewer(s): Similar Articles: IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

scholarly journals IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

2020 ◽  
Author(s):  
Ahmed EM ◽  
Ibrahim ME ◽  
Magbool FF
Keyword(s):  
Drug Delivery ◽  
Peer Review ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Class Iii ◽  
Release Formulation ◽  
E Mail

The aim of present study is to examine the in-vitro-in-vivo correlation (IVIVC) of immediate release product. Atenolol 100mg and its brands of immediate release dosage forms. Atenolol is clearly classified into BCS class III, and could be evaluated under bio waiver conditions. The in vitro parameters employed were hardness, weight uniformity, friability, disintegration time, absolute drug content, dissolution rate (in 0.1 N Hydrochloric acid, phosphate buffer and acetate buffer at 37ºC), and dissolution efficiencies were also analyzed. The in-vitro dissolution study was performed on the brands, according to FDA,USP  dissolution profile in three different PH (1.2),(4.5), and (6.8) at 37ºC, using the USP apparatus II,  then f1, f2 were determined for the time intervals of 10, 15, 30, 45 and 60 minutes, and dissolution efficiencies were calculated.  MINITAB 14 statistical program used for in vitro-in vivo correlation, level A was done for reference product. A non linear relation was established which is typical for immediate release formulation, of class III. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 3.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Name: Dr. Hayriye Eda Şatana Kara   Affiliation: Gazi University, Turkey E-mail: [email protected]   Name: Dr. Nicola Micale   Affiliation: University of Messina, Italy E-mail: [email protected]   Comments of reviewer(s): Similar Articles: FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION FAST DISSOLVING TABLETS: A PROMISING APPROACH FOR DRUG DELIVERY DEVELOPMENT AND EVALUATION OF FAST DISSOLVING THIN FILMS OF ARIPIPRAZOLE TABLET GRANULATION: CURRENT SCENARIO AND RECENT ADVANCES  

scholarly journals Development, Characterization, and Pharmacodynamic Evaluation of Hydrochlorothiazide Loaded Self-Nanoemulsifying Drug Delivery Systems

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Pankajkumar S. Yadav ◽  
Ekta Yadav ◽  
Amita Verma ◽  
Saima Amin
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Tween 80 ◽  
Delivery Systems ◽  
Dissolution Profile ◽  
Rate Of Dissolution ◽  
Capmul Mcm

The objective of the current work was to develop optimized self-nanoemulsifying drug delivery systems (SNEDDS) and evaluate theirin vitroandin vivoperformance. The research comprised various studies which includes solubility studies in various vehicles, pseudoternary phase diagram construction, and preparation and characterization of SNEDDS along within vitrodissolution andin vivopharmacodynamic profiling. Based on dissolution profile, a remarkable increase in rate of dissolution was observed in comparison with plain drug and marketed formulation. Optimized SNEDDS formulation was composed of Capmul MCM (19.17% w/w), Tween 80 (57.5% w/w), Transcutol P (12.7% w/w), and HCT (4.17% w/w).In vivopharmacodynamic evaluation in Wistar rats showed considerable increase in pharmacological effect of HCT by SNEDDS formulation as compared with plain HCT.

scholarly journals Preliminary Characterization and Comparison of Mucilage from Leaves of Hibiscus Sabdariffa L. as A Tablet Binder

2021 ◽  
Vol 12 (1) ◽  
pp. 487-496
Author(s):  
Gayathri R ◽  
Benedict Jose C ◽  
Ramkanth S ◽  
Pradheesh Mohan S ◽  
Swetha V ◽  
...  
Keyword(s):  
Flow Characteristics ◽  
In Vitro Dissolution ◽  
Binding Property ◽  
Dissolution Profile ◽  
Hibiscus Sabdariffa ◽  
Comparative Binding ◽  
Tablet Formulations ◽  
Granule Properties

The present research dealt with the extraction and characterization of mucilage from the Hibiscus sabdariffa leaves. Compared with normal binding agents such as starch and Poly Vinyl Pyrrolidine (PVP), the mucilage of Hibiscus sabdariffa (HSM) was assessed for its binding properties in tablet formulations. Tablets were formulated using HSM, starch and PVP as binders at a various concentration to evaluate its comparative binding efficiency. The compressed tablets were analyze for their quality control tests as per IP. The extracted HSM showed the characteristics of mucilage and good physicochemical properties. The FTIR and thermal analysis compatibility tests showed that there were no significant reactions between the drug and mucilage. Granule properties of various formulations were found to be comparable and have excellent flow characteristics. Post compression parameters suggested that tablets formulated with mucilage had better hardness and friability as that of the tablets prepared with starch and PVP. The formulations exhibited a better and more consistent release as compared to standard formulations using starch and PVP as a binder. The statistical analysis of in vitro dissolution profile by using DD solver software for difference factor (f1), similarity factor (f2), and Rescigno index (ξ) values also indicated promising results. The results notably indicate that binding property of HSM was at par with starch and PVP.

Performance and paroxetine stability in tablets manufactured by fused deposition modelling-based 3D printing

2021 ◽  
Author(s):  
Sara Figueiredo ◽  
Ana I Fernandes ◽  
Fátima G Carvalho ◽  
João F Pinto
Keyword(s):  
Process Parameters ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Fused Deposition Modelling ◽  
Dissolution Profile ◽  
Fused Deposition ◽  
The Impact ◽  
Hot Melt

Abstract Objectives The objective of this study was to develop a method for the preparation and characterization of paroxetine (PRX) tablets, obtained by coupling hot-melt extrusion and fused deposition modelling (FDM)-based three-dimensional printing (3DP) technology. The impact of the printing process parameters on the drug stability and on the tablets performance was assessed. Methods Tablets were obtained by FDM of hot-melt extruded PRX-loaded filaments. Physicochemical, thermal, spectroscopic, diffractometric analysis and in-vitro dissolution tests of the intermediate products and the finished dosage forms were performed. Key findings The characterization of printed tablets evidenced mass and dimensions uniformity, and consistency of drug content and dissolution profile. The formation of amorphous solid dispersions and interaction of formulation components throughout the manufacturing process were demonstrated. Layer thickness, printing temperature, printing and travelling speeds, and infill were the most impacting process parameters on both the physicochemical properties and the in-vitro performance of the 3D-printed tablets. Conclusions PRX tablets, meeting compendial limits, were manufactured by 3DP, envisaging their clinical use as individually designed dosage forms. The assessment of the impact of processing parameters on the printed tablets provided insights, which will ultimately allow streamlining of the 3D process set-up for quicker and easier production of patient-centric medicines.

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