scholarly journals Optimization of the Factors Affecting the Absorption of Vardenafil from Oral Disintegrating Tablets: A Clinical Pharmacokinetic Investigation

2018 ◽  
Author(s):  
Hytham Al-Gethmy ◽  
Usama Fahmy ◽  
Nabil Alhakamy ◽  
Osama Ahmed ◽  
Khalid El-Say
Keyword(s):  
Oral Absorption ◽  
Taste Masking ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Factors Affecting ◽  
Lower Solubility

Because of lower solubility and considerable metabolism, vardenafil (VRD) bioavailability is 15 %. To get over this obstacle, this study aimed to increase the solubility, hasten the onset of action, and mask the unpleasant taste of VRD utilizing β-cyclodextrin (β-CD) and formulation of the inclusion complex as oral disintegrating tablets (ODTs). The solubility of the obtained complexes in various ratios has been studied. A Box-Behnken design (BBD) was utilized to investigate the influence of excipients on the quality of ODTs. The solubility of VRD was improved at 1:2 drug: β-CD ratio. The formulated VRD-ODTs exhibited satisfying results regarding the hardness and disintegration time. In addition, in vivo taste masking and disintegration time showed improved results, after placing the tablets in the oral cavity of the healthy volunteers. The pharmacokinetic parameters for the optimized VRD–ODTs exhibited a significant improvement with P < 0.05 in the maximum plasma concentration and reduction in the time needed to reach this concentration when compared with the marketed tablets. Finally, the optimized VRD-ODTs exhibited increased oral absorption of VRD and subsequent decreasing the time of onset of clinical effect and masking the unpleasant taste, which is favored for patients with erectile dysfunction.

scholarly journals Optimization of the Factors Affecting the Absorption of Vardenafil from Oral Disintegrating Tablets: A Clinical Pharmacokinetic Investigation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 11 ◽  
Author(s):  
Hytham A. Al-Gethmy ◽  
Usama A. Fahmy ◽  
Nabil A. Alhakamy ◽  
Osama A. A. Ahmed ◽  
Khalid M. El-Say
Keyword(s):  
Oral Absorption ◽  
Taste Masking ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Factors Affecting ◽  
Subsequent Decrease

Because of poor solubility and considerable metabolism, vardenafil (VRD) bioavailability is 15%. To overcome this obstacle, this study aimed to increase the solubility, hasten the onset of action, and mask the unpleasant taste of VRD utilizing β-cyclodextrin (β-CD) and formulation of the inclusion complex as oral disintegrating tablets (ODTs). The solubility of the obtained complexes in various ratios has been studied. A Box–Behnken design (BBD) was utilized to investigate the influence of excipients on the quality of ODTs. The solubility of VRD was improved at 1:2 drug:β-CD ratio. The formulated VRD-ODTs exhibited satisfying results regarding the hardness and disintegration time. In addition, in vivo taste masking and disintegration time showed improved results, after placing the tablets in the oral cavity of the healthy volunteers. When compared with the marketed tablets, the pharmacokinetic parameters for the optimized VRD-ODTs exhibited a significant improvement with p < 0.05 in the maximum plasma concentration and reduction in the time needed to reach this concentration. Finally, the optimized VRD-ODTs exhibited increased oral absorption of VRD and subsequent decrease in the time of onset of clinical effect and masking the unpleasant taste.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

scholarly journals Between biology and medicine: perspectives on the use of dendritic cells in anticancer therapy

2017 ◽  
Vol 71 (0) ◽  
pp. 0-0
Author(s):  
Agnieszka Szczygieł ◽  
Elżbieta Pajtasz-Piasecka
Keyword(s):  
Dendritic Cells ◽  
Ex Vivo ◽  
Anticancer Therapy ◽  
Point Of View ◽  
Proper Function ◽  
Innate And Adaptive Immunity ◽  
Factors Affecting ◽  
Antigen Presenting

Dendritic cells (DCs), as a link between innate and adaptive immunity, play a pivotal role in maintaining homeostasis of the immune system. The DC population is characterized by heterogeneity; it consists of many subpopulations which, despite their phenotypic and localization differences, play an essential function – they are professional antigen presenting cells. Due to their role, DCs can be utilized in a new cancer treatment strategy. Their main purpose is to generate an anticancer response leading to the elimination of cancer cells. The tumor microenvironment, abundant in immunosuppressive factors (e.g. IL-10, TGF-β, Arg1, IDO), impairs the proper function of DCs. For this reason, various strategies are necessary for ex vivo preparation of DC-based vaccines and for the support of in vivo DCs to fight against tumors. DC-based vaccines are combined with other forms of immunotherapy (e.g. blockade of immune checkpoint molecules, e.g. PD-1 or CTLA-4) or conventional types of therapies (e.g. chemotherapy). Despite the enormous progress that has been made in anticancer therapy in the past two decades, there are still many unresolved issues regarding the effectiveness of the DCs usage. In this paper we described, in both a mouse and a human subject, a series of DC subpopulations, differentiating in normal conditions or under the influence of cancer microenvironment. We listed factors affecting the quality of the in vivo and ex vivo generations of antitumoral responses, significant from a therapeutic point of view. Moreover, the most important strategies for the use of DCs in anticancer therapies, as well as further developments on this field, have been discussed.

scholarly journals Pharmacokinetics of a 1,000 mg Disintegrating Aspirin Tablet Formulation

2018 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
Forder S ◽  
Voelker M
Keyword(s):  
Early Onset ◽  
Migraine Headache ◽  
Bioequivalence Study ◽  
Maximum Plasma ◽  
Onset Of Action ◽  
Tablet Strength ◽  
Tablet Disintegration ◽  
Inflammatory Drugs ◽  
New Formulation

Migraine is a global disorder and considerably affecting people`s quality of life. Treatments include nonsteroidal anti-inflammatory drugs-containing medicinal products among whom acetylsalicylic acid-containing Aspirin® has been proven effectively to relief migraine headache. Early treatment is recommended for patients with migraine attacks. A requirement for early onset of action includes tablet disintegration and consequent active ingredient dissolution and absorption. The bioavailability of a new quickly disintegrating 1,000 mg aspirin formulation has been investigated in a bioequivalence study versus a marketed Aspirin® formulation with clinically demonstrated early onset of action. The new formulation has a tablet strength (1,000 mg) and time to maximum plasma concentration (mean 21.6 minutes) providing upside for people requiring treatment of migraine headache

scholarly journals FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

2021 ◽  
pp. 99-108
Author(s):  
NAGADANI SWARNALATHA ◽  
VIDYAVATHI MARAVAJHALA
Keyword(s):  
Desirability Function ◽  
Research Work ◽  
In Vivo Studies ◽  
Taste Masking ◽  
Wet Granulation ◽  
Maximum Plasma ◽  
In Vivo Evaluation ◽  
Eudragit Epo

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak
Keyword(s):  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Geriatric Population ◽  
Orodispersible Tablets ◽  
Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

scholarly journals Pharmacokinetic Profile of μSMIN Plus™, a new Micronized Diosmin Formulation, after Oral Administration in Rats

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Rosario Russo ◽  
Angelo Mancinelli ◽  
Michele Ciccone ◽  
Fabio Terruzzi ◽  
Claudio Pisano ◽  
...  
Keyword(s):  
Oral Administration ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Sprague Dawley ◽  
Time Curve ◽  
Maximum Plasma Drug Concentration

Diosmin is a naturally occurring flavonoid present in citrus fruits and other plants belonging to the Rutaceae family. It is used for the treatment of chronic venous insufficiency (CVI) for its pheblotonic and vaso-active properties, safety and tolerability as well. The aim of the current in vivo study was to investigate the pharmacokinetic profile of a branded micronized diosmin (μSMIN Plus™) compared with plain micronized diosmin in male Sprague-Dawley rats. After oral administration by gastric gavage, blood samples were collected via jugular vein catheters at regular time intervals from baseline up to 24 hours. Plasma concentrations were assessed by LC/MS. For each animal, the following pharmacokinetic parameters were calculated using a non-compartmental analysis: maximum plasma drug concentration (Cmax), time to reach Cmax (Tmax), area under the plasma concentration-time curve (AUC0-last), elimination half-life (t1/2), and relative oral bioavailability (%F). The results of the current study clearly showed an improvement in the pharmacokinetic parameters in animals treated with μSMIN Plus™ compared with animals treated with micronized diosmin. In particular, μSMIN Plus™ showed a 4-fold increased bioavailability compared with micronized diosmin. In conclusion, the results from the current study provided a preliminary pharmacokinetic profile for μSMIN Plus™, which may represent a new tool for CVI management.

scholarly journals Pharmacokinetics of Stereoisomeric Dipeptide Prodrugs of Acyclovir following Intravenous and Oral Administrations in Rats: A study Involving in vivo corneal Uptake of Acyclovir following Oral Dosing

2009 ◽  
Vol 1 ◽  
pp. OED.S2857 ◽  
Author(s):  
Ravi S. Talluri ◽  
Ripal Gaudana ◽  
Sudharshan Hariharan ◽  
Ashim K. Mitra
Keyword(s):  
Oral Administration ◽  
Oral Absorption ◽  
Area Under The Curve ◽  
Systemic Circulation ◽  
Precipitation Method ◽  
Drug Candidate ◽  
Pharmacokinetic Parameters ◽  
Sprague Dawley ◽  
Uptake Studies

Objective To delineate the plasma pharmacokinetics and determine the corneal uptake of valine based stereoisomeric dipeptide prodrugs of acyclovir (ACV) in rats. Methods Male Sprague-Dawley rats were used for the study. Pharmacokinetics of ACV, L-valine-acyclovir (LACV), L-valine-D-valine-acyclovir (LDACV) and D-valine-L-valine acyclovir (DLACV) prodrugs were delineated. These compounds were administered intravenously as a bolus via jugular vein cannula and orally by gavage. Samples were purified by protein precipitation method and analyzed by LC-MS/MS. Pertinent pharmacokinetic parameters were obtained by using WinNonlin. Corneal uptake studies of LDACV and LACV were studied following oral administration. Results Following i.v. administration, the area under the curve (AUC) in μM*min of generated ACV was in the order of LACV > LDACV > DLACV indicating their rate of metabolism. The AUC values of total drug obtained in the systemic circulation after oral administration LACV and LDACV were 1077.93 ± 236.09 and 1141.76 ± 73.67 μM*min, respectively. DLACV exhibited poor oral absorption. Cmax (μM) and AUC of the intact prodrug obtained in the systemic circulation following oral administration of LDACV were almost 4–5 times higher than LACV. Moreover, concentrations achieved in the cornea after oral administration of LDACV were almost two times of LACV. Conclusions LDACV increased both the oral bioavailability and subsequent in vivo corneal uptake of ACV Hence, LDACV can be considered as the most promising drug candidate for delivery of ACV, in treatment of both genital herpes and ocular herpes keratitis after oral administration.

Formulation and Evaluation of Oro Dispersible Tablets of Ondansetron Hydrochloride by Direct Compression using Superdisintegrants

1970 ◽  
Vol 1 (1) ◽  
pp. 106-111
Author(s):  
Avani R. Gosai ◽  
Sanjay B. Patil ◽  
Krutika K. Sawant
Keyword(s):  
Mechanical Strength ◽  
Direct Compression ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Ondansetron Hydrochloride ◽  
Dispersible Tablets ◽  
In Vitro Disintegration

The objective of the present investigation was to prepare oro dispersible tablets of ondansetron hydrochloride, because of its application in emesis condition, fast onset of action and avoidance of water is highly desirable. Tablets were prepared by direct compression using sodium starch glycolate and croscarmellose as superdisintegrants, as the combination of these two agents gives better disintegration of the tablet. Microcrystalline cellulose was used as diluent and mannitol, mint flavor, sodium saccharine to enhance the organoleptic properties of tablets. The tablets were evaluated for weight variation, mechanical strength, in vitro disintegration time, in vivo disintegration time, wetting time, and drug release characteristics. Hardness and friability data indicated good mechanical strength of tablets.  The results of in vitro disintegration time and in vivo disintegration time indicated that the tablets dispersed rapidly in mouth within 3 to 5 seconds. Dissolution study revealed faster release rate of ondansetron hydrochloride from the tablets as compared to pure drug and marketed conventional tablet formulation of ondansetron hydrochloride. It was concluded that superdisintegrants addition technique is a useful method for preparing oro dispersible tablets by direct compression method

Preparation and Evaluation of Rapidly Disintegrating Glimepiride Tablets

2011 ◽  
Vol 3 (4) ◽  
pp. 1220-1229
Author(s):  
Adel M Aly ◽  
Bassam I Amro ◽  
Feras D El Hajji
Keyword(s):  
Fasting Blood Glucose ◽  
Diabetic Patients ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Glucose Levels ◽  
Orally Disintegrating Tablets ◽  
Accelerated Stability ◽  
The Stability

The objective of this work was to prepare Glimepiride (1 mg) rapidly disintegrating tablets (RDT) by direct compression, and also, to evaluate Pharmaburst™ as a newly introduced diluent for this type of tablets, either alone or in combination with other well known tablet excipients. Another goal was to study the stability, as well as, the in vivo effects of selected formulations. Orange flavor was the most preferred flavor for the prepared rapidly disintegrating tablets containing Pharmaburst™ as a single diluent. Pharmaburst™ alone is sufficient to produce rapidly (orally) disintegrating tablets of Glimepiride with good physical characteristics, better compactability and shorter in-vivo and in-vitro disintegration time. The prepared Glimepiride RDT were found to have faster onset of action than the conventional Glimepiride tablets. Also, they were effective in lowering fasting blood glucose levels (FBG) in rabbits. Glimepiride RDT containing Pharmaburst™ alone were found to be stable when subjected to accelerated stability conditions (40 °C / 75 % relative humidity) for at least 3 months. Packaging the prepared Glimepiride  RDT in 40 CC high density polyethylene (HDPE) bottles with 2 grams silica gel desiccant canisters and rayon had provided sufficient protection for the tablets. The used packaging system is believed to be very practical and convenient for elderly diabetic patients. It is also assumed to be preferred by the manufacturers.

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