scholarly journals Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 870
Author(s):  
Amer S. AlAli ◽  
Mohammed F. Aldawsari ◽  
Ahmed Alalaiwe ◽  
Bjad K. Almutairy ◽  
Ramadan Al-Shdefat ◽  
...  
Keyword(s):  
Design Of Experiment ◽  
Rapid Onset ◽  
Sildenafil Citrate ◽  
Onset Of Action ◽  
Fluid Bed ◽  
Fluid Bed Granulation ◽  
New Formulation ◽  
Sublingual Delivery ◽  
Fast Disintegrating Tablets

Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.

scholarly journals Sublingual route for systemic drug delivery

2018 ◽  
Vol 8 (6-s) ◽  
pp. 340-343
Author(s):  
Poonam P Pawar ◽  
Hemant S Ghorpade ◽  
Bhavana A. Kokane
Keyword(s):  
Drug Delivery ◽  
Blood Vessels ◽  
Psychiatric Patients ◽  
Rapid Onset ◽  
Oral Route ◽  
Sublingual Gland ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Systemic Drug Delivery ◽  
Sublingual Delivery

Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a rapid onset of action and better patient compliance than orally ingested tablets. Sublingual literally meaning is “under the tongue”, administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability.  Sublingual technology is convenient for dosing in geriatric, pediatric and psychiatric patients with dysphagia. Sublingual drug delivery shows fast therapeutic action than orally ingested drugs with fewer side effects. This review highlights advantages, disadvantages, different sublingual Gland, sublingual formulation such as tablets, films drops, sprays etc, evaluation parameters. Keywords: Sublingual delivery, dysphagia, sublingual gland, improved bioavailability, evaluations.

An Evaluation of Andursil – A New Antacid

1977 ◽  
Vol 5 (6) ◽  
pp. 99-104 ◽  
Author(s):  
G Beaumont ◽  
G I J Rigby ◽  
J Seldrup
Keyword(s):  
General Practitioner ◽  
Rapid Onset ◽  
Onset Of Action ◽  
Duration Of Effect ◽  
The Ideal

A number of characteristics of an ideal antacid are proposed. A new antacid formulation, Andursil, has been assessed both by in vitro and in vivo methods. Andursil has been found to compare favourably in its properties, with the profile of the ideal antacid. In a multicentre general practitioner trial it was found to be effective in relieving the symptoms of dyspepsia, to have a rapid onset of action and a satisfactory duration of effect, to be palatable and to be relatively free from undesirable effects.

scholarly journals Deimmunized Lysostaphin Synergizes with Small-molecule Chemotherapies and Re-sensitizes MRSA to β-Lactam Antibiotics

2020 ◽  
pp. AAC.01707-20
Author(s):  
Yongliang Fang ◽  
Jack R. Kirsch ◽  
Liang Li ◽  
Seth A. Brooks ◽  
Spencer Heim ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Standard Of Care ◽  
Rapid Onset ◽  
Multidrug Resistant ◽  
Genetically Engineered ◽  
High Potency ◽  
Onset Of Action ◽  
New Antibiotics

There is an urgent need for novel agents to treat drug-resistant bacterial infections, such as multidrug-resistant Staphylococcus aureus (MRSA). Desirable properties for new antibiotics include high potency, narrow species selectivity, low propensity to elicit new resistance phenotypes, and synergy with standard of care (SOC) chemotherapies. Here, we describe analysis of the anti-MRSA potential exhibited by F12, an innovative anti-MRSA lysin that has been genetically engineered to evade detrimental antidrug immune responses in human patients. F12 possesses high potency and rapid onset of action, it has narrow selectivity against pathogenic Staphylococci, and it manifests synergy with numerous SOC antibiotics. Additionally, resistance to F12 and β-lactam antibiotics appears mutually exclusive, and importantly we provide evidence that F12 re-sensitizes normally resistant MRSA strains to β-lactams both in vitro and in vivo. These results suggest that combinations of F12 and SOC antibiotics could be a promising new approach to treating refractory S. aureus infections.

scholarly journals Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
K. Senthilkumar ◽  
C. Vijaya
Keyword(s):  
Pain Management ◽  
Immediate Release ◽  
Rapid Onset ◽  
Ease Of Use ◽  
Taste Masking ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Onset Of Action

Etoricoxib is a potent, orally active, and highly selective COX-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. The present research was undertaken to develop mouth dissolving films of etoricoxib to have rapid onset of action. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use, and the consequent patient compliance. Solubility enhancement and taste masking of etoricoxib were the two challenges solved by formulating drug-inclusion complex with beta-cyclodextrin (BCD). MDF prepared by solvent casting etoricoxib-BCD complex along with HPMC as film forming polymer was found to possess desirable physicomechanical properties. In vitro release of etoricoxib from MDF in simulated salivary fluid and 0.1 N HCl was more than 95% within 2 minutes. Taste masking and in vivo disintegration were in acceptable range as assessed by human volunteers. Etoricoxib MDF was further characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. The index of analgesia shown by etoricoxib MDF was comparable to that of immediate release tablets (100% activity within 40 minutes) in animal studies. Conclusively, the present study documents the development of a commercially viable formula for an MDF of etoricoxib with rapidity in pain management.

Development and Evaluation of Fast Disintegrating Tablets of Lornoxicam Solid Dispersions

2019 ◽  
Vol 12 (4) ◽  
pp. 4585-4592
Author(s):  
Hafsa Mohammadi ◽  
Hemanath Kumar V ◽  
Roshan S ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Statistical Significance ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Weight Variation ◽  
Fast Disintegrating Tablets

Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.

Efficacy and Safety of Rizatriptan Wafer for the Acute Treatment of Migraine

Cephalalgia ◽  
1999 ◽  
Vol 19 (5) ◽  
pp. 525-532 ◽  
Author(s):  
SP Ahrens ◽  
MV Farmer ◽  
DL Williams ◽  
E Willoughby ◽  
K Jiang ◽  
...  
Keyword(s):  
Pain Relief ◽  
Acute Treatment ◽  
Rapid Onset ◽  
Onset Of Action ◽  
Double Blind ◽  
Experienced Pain ◽  
Freeze Dried ◽  
New Formulation ◽  
Outpatient Study ◽  
Dosage Formulation

Rizatriptan is a potent, highly selective 5HT1B/1D agonist with rapid onset of action for acute treatment of migraine. Rizatriptan wafer1 is a novel, freeze-dried dosage formulation of rizatriptan which rapidly disintegrates on the tongue, is swallowed with saliva, and may be taken without liquids. The efficacy and tolerability of rizatriptan wafer were examined in a placebo-controlled, double-blind, outpatient study in 555 migraineurs. The primary efficacy endpoint was pain relief at 2 h. From 30 min onwards, significantly more patients experienced pain relief and became pain-free after rizatriptan 10-mg wafer compared to placebo. At 2 h, the percentage of patients with pain relief was significantly higher after rizatriptan 10-mg wafer (74%), 5-mg wafer (59%) compared with placebo (28%). Rizatriptan 10-mg wafer was superior to rizatriptan 5-mg wafer on pain relief at 1.5 and 2 h ( p<0.05). Significantly more patients were pain-free at 2 h after rizatriptan 10-mg wafer (42%), 5-mg wafer (35%) compared with placebo (10%). Both doses of rizatriptan wafer were well tolerated. Rizatriptan wafer is a convenient, highly effective new formulation for acute treatment of migraine.

The impact and mechanism of ampakine CX1739 on protection against respiratory depression in rats

2020 ◽  
Vol 12 (23) ◽  
pp. 2093-2104
Author(s):  
Dian Xiao ◽  
Fei Xie ◽  
Xin Xu ◽  
Xinbo Zhou
Keyword(s):  
Respiratory Depression ◽  
Ampa Receptors ◽  
Emergency Treatment ◽  
Rapid Onset ◽  
High Dose ◽  
Opioid Agonist ◽  
Onset Of Action ◽  
Sedative Drugs ◽  
The Impact

Background: Abuse of analgesic and sedative drugs often leads to severe respiratory depression and sometimes death. Approximately 69,000 people worldwide die annually from opioid overdoses. Purpose: This work aimed to investigate whether CX1739 can be used for emergency treatment of acute respiratory depression due to drug abuse. Results: First, the results clarify that CX1739 is a low-impact ampakine that can safely activate α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors without causing excito-neurotoxicity. Second, CX1739 rapidly crossed the blood–brain barrier (Tmax = 2 min), which meets the requirement of rapid onset of action in vivo. Our work provides preliminarily confirmation that high-dose intravenous administration of CX1739 can immediately reverse respiratory depression in animal models of respiratory depression caused by opioid agonist 030418, pentobarbital sodium and ethanol.

Morphological effects and tegumental alterations induced by mefloquine on schistosomula and adult flukes ofSchistosoma mansoni

Parasitology ◽  
2009 ◽  
Vol 137 (1) ◽  
pp. 85-98 ◽  
Author(s):  
T. MANNECK ◽  
Y. HAGGENMÜLLER ◽  
J. KEISER
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Rapid Onset ◽  
Current Treatment ◽  
Current Evidence ◽  
Onset Of Action ◽  
Tegumental Surface ◽  
Scanning Electron

SUMMARYThere is a pressing need to develop novel anti-schistosomal drugs, as current treatment relies largely on praziquantel (PZQ). To further strengthen current evidence of the anti-schistosomal properties of mefloquine (MQ), we studied the temporal effect of this compoundin vitroandin vivo, and examined alterations on the tegumental surface of schistosomula and adults ofS. mansoniby means of scanning electron microscopy (SEM). Schistosomula and adults were each incubatedin vitrousing MQ over a wide concentration range (1–100 μg/ml). In addition, mice infected with adultS. mansoniwere treated with a single oral dose of 400 mg/kg MQ, and worms were recovered 24, 48, 72, 96 and 120 h following treatment. MQ showed a rapid onset of action on schistosomulain vitro; 100 and 75 μg/ml of MQ killed schistosomula immediately; the minimal lethal and effective concentrations of MQ on schistosomula after 1 h were 25 and 5 μg/ml, respectively. Adult worms incubated with 100 and 10 μg/ml of MQ were dead after 1 h and 24 h of incubation, respectively. A hepatic shift of adult schistosomes was observed in mice already 24 h after treatment, and 120 h following treatment >98% of all worms had translocated to the liver. SEM observations revealed extensive tegumental destruction, including blebbing, shrinking and sloughing, particularly followingin vitroincubation and on the tegument of female worms.

Nanovesicles System for Rapid-Onset Sublingual Delivery Containing Sodium Tanshinone IIA Sulfonate: In vitro and In Vivo Evaluation

2013 ◽  
Vol 102 (7) ◽  
pp. 2332-2340 ◽  
Author(s):  
Hongda Zhu ◽  
Jianjun Hao ◽  
Huabing Chen ◽  
Shanshan Jiang ◽  
Mingxing Liu ◽  
...  
Keyword(s):  
Rapid Onset ◽  
Tanshinone Iia ◽  
In Vivo Evaluation ◽  
Sodium Tanshinone Iia Sulfonate ◽  
Sublingual Delivery

Platelet Aggregation in Diabetes Mellitus and the Effect of Insulin in Vivo on Aggregation

1972 ◽  
Vol 27 (01) ◽  
pp. 114-120 ◽  
Author(s):  
A. A Hassanein ◽  
Th. A El-Garf ◽  
Z El-Baz
Keyword(s):  
Platelet Aggregation ◽  
Rapid Onset ◽  
Control Group ◽  
Diabetic Patients ◽  
Fasting State ◽  
Clotting Time ◽  
Cholesterol Levels ◽  
Platelet Disaggregation ◽  
Aggregation And Disaggregation

SummaryADP-induced platelet aggregation and calcium-induced platelet aggregation tests were studied in 14 diabetic patients in the fasting state and half an hour after an intravenous injection of 0.1 unit insulin/kg body weight. Platelet disaggregation was significantly diminished as compared to a normal control group, and their results were negatively correlated with the corresponding serum cholesterol levels. Insulin caused significant diminution in the ADP-induced platelet aggregation as a result of rapid onset of aggregation and disaggregation. There was also a significant increase in platelet disaggregation. In the calcium-induced platelet aggregation test, there was a significant shortening of the aggregation time, its duration, and the clotting time. The optical density fall due to platelet aggregation showed a significant increase. Insulin may have a role in correcting platelet disaggregation possibly through improvement in the intracellular enzymatic activity.

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