Pharmacokinetic peculiarities of drugs used in the form of rapidly dispersible tablets (oral delivery system)

2020 ◽  
pp. 7-24
Author(s):  
Zhanna Kozlova ◽  
Ivan Krasnyuk ◽  
Yuliya Lebedeva ◽  
Ekaterina Odintsova
Keyword(s):  
Oral Mucosa ◽  
Oral Delivery ◽  
Chemical Properties ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Mucosal Drug Delivery ◽  
Physical And Chemical ◽  
Pass Metabolism

Oral mucosal drug delivery is an alternative method of systemic delivery with several advantages over both injectable and enteral methods. Drugs that are absorbed through the oral mucosa directly enter the systemic circulation, passing through the gastrointestinal tract and first-pass metabolism in the liver due to oral mucosa being highly vascularised. This results in rapid onset of action for some drugs because of a more comfortable and convenient way of delivery than the intravenous one. But not all drugs can be administered through the oral mucosa due to characteristics of the oral mucosa and physical and chemical properties of the drug.

scholarly journals Sublingual Tablets : An Overview

2019 ◽  
pp. 181-187
Author(s):  
Rohit S. Nikam ◽  
Rahul P. Jadhav ◽  
Dr. Prakash D. Jadhav ◽  
Vishal D. Yadav
Keyword(s):  
Drug Delivery ◽  
Rapid Onset ◽  
Oral Route ◽  
Dosage Forms ◽  
Peroral Administration ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Evaluation Parameters ◽  
Pass Metabolism

<p>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. Peroral administration of drug has disadvantages such as Hepatic first pass metabolism and enzymatic degradation within the GI tract that limits oral administration of certain classes of drug like peptides and proteins. So, other absorptive mucosa is considered as potential sites for drug administration. Trans-mucosal routes of drug delivery (i.e. the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer several advantages over peroral administration for systemic delivery. This review highlights the sublingual dosage forms for the treatment of migraine, advantages, Disadvantages, various evaluation parameters and commercially available sublingual dosage forms.</p>

scholarly journals Nasal Delivery of Acute Medications for Migraine: The Upper Versus Lower Nasal Space

2021 ◽  
Vol 10 (11) ◽  
pp. 2468
Author(s):  
Vincent Martin ◽  
John Hoekman ◽  
Sheena K. Aurora ◽  
Stephen B. Shrewsbury
Keyword(s):  
Acute Treatment ◽  
Drug Efficacy ◽  
Hepatic Metabolism ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Nasal Delivery ◽  
Attractive Alternative ◽  
Gi Tract ◽  
Onset Of Action ◽  
First Pass

The acute treatment of migraine requires effective drugs that are well tolerated and provide rapid and consistent pain relief. Oral tablets are the most commonly used acute treatment for migraine; however, their effectiveness is limited by the rate of gastrointestinal (GI) tract absorption and first-pass hepatic metabolism, and they may not be ideal for patients experiencing GI motility issues. Nasal delivery is an attractive alternative route as it may circumvent GI tract absorption, avoid first-pass metabolism in the liver, and potentially reduce the frequency of GI adverse events. The large surface area and high vascularity within the nose may permit rapid absorption of therapeutics into the systemic circulation, allowing for rapid onset of action. However, the site of drug deposition (upper versus lower nasal cavity) may influence drug pharmacokinetics. Most approved nasal migraine therapies target the lower nasal space where the epithelium is less permeable, and they may be quickly cleared away due to increased ciliary function or dripping from the nose or swallowing, resulting in variable absorption and limited bioavailability. Together with its abundant vascularization, relative mucosal thickness stability, and low clearance rates, the upper nasal space harnesses the benefits of nasal delivery to potentially maximize drug efficacy.

scholarly journals Chitosan Nanoparticles at the Biological Interface: Implications for Drug Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1686
Author(s):  
Noorjahan Aibani ◽  
Raj Rai ◽  
Parth Patel ◽  
Grace Cuddihy ◽  
Ellen K. Wasan
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Chitosan Nanoparticles ◽  
Chemical Properties ◽  
Protein Corona ◽  
Systemic Circulation ◽  
Systemic Delivery ◽  
Toxicological Evaluation ◽  
Wide Range

The unique properties of chitosan make it a useful choice for various nanoparticulate drug delivery applications. Although chitosan is biocompatible and enables cellular uptake, its interactions at cellular and systemic levels need to be studied in more depth. This review focuses on the various physical and chemical properties of chitosan that affect its performance in biological systems. We aim to analyze recent research studying interactions of chitosan nanoparticles (NPs) upon their cellular uptake and their journey through the various compartments of the cell. The positive charge of chitosan enables it to efficiently attach to cells, increasing the probability of cellular uptake. Chitosan NPs are taken up by cells via different pathways and escape endosomal degradation due to the proton sponge effect. Furthermore, we have reviewed the interaction of chitosan NPs upon in vivo administration. Chitosan NPs are immediately surrounded by a serum protein corona in systemic circulation upon intravenous administration, and their biodistribution is mainly to the liver and spleen indicating RES uptake. However, the evasion of RES system as well as the targeting ability and bioavailability of chitosan NPs can be improved by utilizing specific routes of administration and covalent modifications of surface properties. Ongoing clinical trials of chitosan formulations for therapeutic applications are paving the way for the introduction of chitosan into the pharmaceutical market and for their toxicological evaluation. Chitosan provides specific biophysical properties for effective and tunable cellular uptake and systemic delivery for a wide range of applications.

scholarly journals Dry Powder Nitroimidazopyran Antibiotic PA-824 Aerosol for Inhalation

2009 ◽  
Vol 53 (4) ◽  
pp. 1338-1343 ◽  
Author(s):  
Jean C. Sung ◽  
Lucila Garcia-Contreras ◽  
Jarod L. VerBerkmoes ◽  
Charles A. Peloquin ◽  
Katharina J. Elbert ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Chemical Properties ◽  
Pulmonary Delivery ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Data ◽  
Systemic Delivery ◽  
Dry Powder ◽  
Pulmonary Administration ◽  
Particle Form ◽  
The Stability

ABSTRACT We formulated PA-824, a nitroimidazopyran with promise for the treatment of tuberculosis, for efficient aerosol delivery to the lungs in a dry powder porous particle form. The objectives of this study were to prepare and characterize a particulate form of PA-824, assess the stability of this aerosol formulation under different environmental conditions, and determine the pharmacokinetic parameters for the powder after pulmonary administration. The drug was spray dried into porous particles containing a high drug load and possessing desirable aerosol properties for efficient deposition in the lungs. The physical, aerodynamic, and chemical properties of the dry powder were stable at room temperature for 6 months and under refrigerated conditions for at least 1 year. Pharmacokinetic parameters were determined in guinea pigs after the pulmonary administration of the PA-824 powder formulation at three doses (20, 40, and 60 mg/kg of body weight) and compared to those after the intravenous (20 mg/kg) and oral (40 mg/kg) delivery of the drug. Oral and inhaled delivery of PA-824 achieved equivalent systemic delivery at the same body dose within the first 12 h of dosing. However, animals dosed by the pulmonary route showed drug loads that remained locally in the lungs for 32 h postexposure, whereas those given the drug orally cleared the drug more rapidly. Therefore, we expect from these pharmacokinetic data that pulmonary delivery may achieve the same efficacy as oral delivery at the same body dose, with a potential improvement in efficacy related to pulmonary infection. This may translate into the ability to deliver lower body doses of this drug for the treatment of tuberculosis by aerosol.

scholarly journals Sublingual spray: a new technology oriented formulation with multiple benefits

2019 ◽  
Vol 10 (4) ◽  
pp. 2875-2885 ◽  
Author(s):  
Aravindhanthan V ◽  
Anjali P B ◽  
Arun Radhakrishnan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
New Technology ◽  
Rapid Onset ◽  
Regulatory Agencies ◽  
Onset Of Action ◽  
First Pass ◽  
Delivery Technology ◽  
Pass Metabolism

Sublingual drug delivery system was a well-established platform for delivering the drug that need to exhibit quick action without any first-pass metabolic effect, but various pitfall in the regular sublingual drug delivery systems such as a tablet, capsule etc., that can be overcome by novel sublingual drug delivery technology such as particulate sublingual spray. Sublingual spray for drug administration has gained attention in the market since it proved its propensity to by-pass the first-pass metabolism and to initiate a rapid onset of action due to its atomized micro particulate nature, which is significantly higher than the other sublingual formulations. The approval of sublingual spray by the regulatory agencies may commence further research in this field by subsuming various essential drugs for indications such as cancer pain, cardiovascular issue etc. This article comprises a detailed study on the drawback of conventional sublingual drug delivery system and the approach by which these drawbacks can be overruled by spray technology in the sublingual area and the, in-depth mechanism of drug delivery through sublingual with the help of atomization followed by the entire formulation strategy along with evaluation and industrial perspective of the sublingual spray dosage form as a future tool of patient-friendly drug delivery.

scholarly journals SUBLINGUAL DRUG DELIVERY: AN INDICATION OF POTENTIAL ALTERNATIVE ROUTE

2017 ◽  
Vol 9 (6) ◽  
pp. 5 ◽  
Author(s):  
Puja Saha ◽  
Sushma Verma ◽  
Pratik Swarup Das
Keyword(s):  
Blood Vessels ◽  
Psychiatric Patients ◽  
Life Cycle Management ◽  
Ventral Surface ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Onset Of Action ◽  
The People ◽  
Short Period ◽  
Suitable Form

Sublingual literally meaning is “under the tongue”, refers to a method of administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. Sublingual route is a useful when rapid onset of action is desired with better patient compliance than orally ingested tablets. Drugs that are given sublingually reach directly in to the systemic circulation through the ventral surface of the tongue and floor of the mouth. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability. As nowadays most of the people need effective relief within a short period of time so sublingual is the most suitable form of administration. New sublingual technologies address many pharmaceutical and patient needs, ranging from enhanced life‐cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia.

scholarly journals Recent Trend In Oral Local Drug Delivery Using Buccal Mucoadhesive Formulation: A Review

2013 ◽  
Vol 3 (2) ◽  
pp. 41-44
Author(s):  
M Gupta ◽  
R Shrivastava ◽  
R Ahuja ◽  
M Gupta ◽  
A Aggarwal ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Mucosa ◽  
Recent Trend ◽  
Local Drug Delivery ◽  
Oral Diseases ◽  
Systemic Delivery ◽  
First Pass Metabolism ◽  
First Pass ◽  
Therapeutic Peptides ◽  
Pass Metabolism

In this 21st century pharmaceutical science has been focused on the delivery of drugs through the oral mucosa. The buccal mucosa has been investigated for mucoadhesive local drug therapy and the systemic delivery of therapeutic peptides and other drugs that are subjected to first-pass metabolism or are unstable within the rest of the gastrointestinal tract. This review focuses on the permeability features of oral mucosa and new potential mucoadhesive local delivery systems to treat oral diseases. DOI: http://dx.doi.org/10.3329/bjdre.v3i2.16612 Bangladesh Journal of Dental Research & Education Vol.3(2) 2013: 41-44

A review of rapid-onset opioids for breakthrough pain in patients with cancer

2014 ◽  
Vol 10 (3) ◽  
pp. 207 ◽  
Author(s):  
Steven M. Simon, RPh, MD ◽  
Lee S. Schwartzberg, MD, FACP
Keyword(s):  
Breakthrough Pain ◽  
Immediate Release ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Abrupt Onset ◽  
Onset Of Action ◽  
Duration Of Action ◽  
Patients With Cancer ◽  
Duration Of Effect ◽  
Effective Pain Relief

Pain management in patients with cancer remains suboptimal. Breakthrough pain (BTP) is characterized by abrupt onset of severe pain in a background of otherwise stable managed pain and presents a substantial burden to patients, as it disrupts activities and quality of life. Rapid-onset opioids (ROOs), with an appropriate onset and duration of effect, provide new options for effective and well-tolerated management of BTP. All currently available ROOs are various formulations of transmucosal immediate-release fentanyl (TIRF) and, although they were originally developed and approved for use in children before painful procedures, are only approved for use in opioid-tolerant adult patients with cancer and BTP. The formulation options include oral lozenge, buccal tablet, buccal film, sublingual tablet, nasal spray, and a sublingual spray; each has practical considerations that vary with the product and route of administration. All have the common advantage of rapid entry into the systemic circulation via transmucosal absorption, avoiding hepatic and intestinal first-pass metabolism and allowing a rapid onset of action that rivals intravenous injections. Rapid onset and short duration of action allow good patient control of analgesia. The pharmacokinetic and analgesic properties of ROOs may allow reduction of the total opioid burden and associated adverse effects, while still providing effective pain relief. The shared TIRF risk evaluation and mitigation strategy program implemented in March 2012 has simplified enrollment and administration of these products to help mitigate the risks of abuse and misuse and to help ensure safe use in patients with cancer suffering from BTP.

Statistical criteria of stellar population types

1966 ◽  
Vol 24 ◽  
pp. 101-110
Author(s):  
W. Iwanowska
Keyword(s):  
Stellar Population ◽  
Chemical Properties ◽  
Spectrophotometric Study ◽  
Physical And Chemical Properties ◽  
Population Type ◽  
The Galaxy ◽  
Distribution Parameters ◽  
Physical And Chemical ◽  
Statistical Criteria ◽  
And Chemical Properties

In connection with the spectrophotometric study of population-type characteristics of various kinds of stars, a statistical analysis of kinematical and distribution parameters of the same stars is performed at the Toruń Observatory. This has a twofold purpose: first, to provide a practical guide in selecting stars for observing programmes, second, to contribute to the understanding of relations existing between the physical and chemical properties of stars and their kinematics and distribution in the Galaxy.

Biophysical Measurement of Molecular Weight of Foot-and-Mouth Disease RNA Fragments

1974 ◽  
Vol 32 ◽  
pp. 262-263
Author(s):  
Sydney S. Breese ◽  
Howard L. Bachrach
Keyword(s):  
Chemical Properties ◽  
Foot And Mouth Disease ◽  
Mouth Disease ◽  
Distilled Water ◽  
Bovine Plasma ◽  
Mouth Disease Virus ◽  
Foot And Mouth ◽  
Carbon Coated ◽  
Rna Fragments ◽  
Physical And Chemical

Continuing studies on the physical and chemical properties of foot-and-mouth disease virus (FMDV) have included electron microscopy of RNA strands released when highly purified virus (1) was dialyzed against demlneralized distilled water. The RNA strands were dried on formvar-carbon coated electron microscope screens pretreated with 0.1% bovine plasma albumin in distilled water. At this low salt concentration the RNA strands were extended and were stained with 1% phosphotungstic acid. Random dispersions of strands were recorded on electron micrographs, enlarged to 30,000 or 40,000 X and the lengths measured with a map-measuring wheel. Figure 1 is a typical micrograph and Fig. 2 shows the distributions of strand lengths for the three major types of FMDV (A119 of 6/9/72; C3-Rezende of 1/5/73; and O1-Brugge of 8/24/73.

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