Onset of action of a topical antihistamine as assessed by histamine challenge-induced plasma exudation responses

2006 ◽  
Vol 96 (2) ◽  
pp. 345-348 ◽  
Author(s):  
Magnus Korsgren ◽  
Morgan Andersson ◽  
Lars Larsson ◽  
Marie Aldén-Raboisson ◽  
Lennart Greiff
Keyword(s):  
Onset Of Action ◽  
Plasma Exudation ◽  
Histamine Challenge

An Evaluation of the Antihistamine Activity of Acrivastine and Its Onset in Human Skin

1992 ◽  
Vol 20 (2) ◽  
pp. 106-111 ◽  
Author(s):  
V K Manna ◽  
P Marks ◽  
J R Gibson
Keyword(s):  
Crossover Study ◽  
Healthy Volunteers ◽  
Human Skin ◽  
Treatment Plan ◽  
Onset Of Action ◽  
Double Blind ◽  
Time Points ◽  
Antihistamine Activity ◽  
Flare Response ◽  
Histamine Challenge

In a double-blind, two-period crossover study, 24 healthy volunteers were evaluated to establish the time of onset of action of activity of acrivastine in suppressing the weal and flare response to intradermally injected histamine. Volunteers received single doses of 8 mg acrivastine and placebo according to a fully randomized, balanced treatment plan. Acrivastine significantly ( P < 0.002) reduced the flare response induced by 0.4 μg histamine challenge 15 min after oral acrivastine dosing when compared with placebo. A significant ( P < 0.001) reduction of the weal response was noted at 25 min, although trends in this direction were already present at earlier time points. Dans d'une étude croisée à deux phase, réalisée en double aveugle et ayant porté sur 24 volontaires sains, on a tenté d'établir le moment du début de l'action de l'acrivastine dans la suppression de la réponse inflammatoire consécutive à l'injection intradermique d'histamine. Les volontaires ont reçu des doses uniques de 8 mg d'acrivastine et de placebo, selon un plan de traitement entièrement randomisé et équilibré. L'acrivastine a réduit significativement ( P < 0,002) la réponse de rubéfaction induite par 0,4 μg d'histamine 15 minutes après l'administration orale d'acrivastine, par rapport au placebo. Une réduction significative ( P < 0,001) de la réponse d'enflure a été notée à 25 minutes, bien qu'une tendance en ce sens ait déjà été observée à un stade plus précoce.

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

Invivo Activity of Polyherbal Gels Prepared Using Carbopol

2020 ◽  
Vol 10 (3) ◽  
pp. 63-66
Author(s):  
Parasakthi N ◽  
Deepika R ◽  
Sivanathan C ◽  
Abubackkar Sithiq PD ◽  
Venkateshan N
Keyword(s):  
Physiological Stress ◽  
Defense Responses ◽  
The Body ◽  
Peptic Ulcers ◽  
Onset Of Action ◽  
Standard Drug ◽  
Root Extracts ◽  
Carbopol 940 ◽  
Anti Inflammatory ◽  
Rich Countries

Pain and inflammation are the basic defense responses of the body that the result of the injury and any other damage to the body. During the years the concerns were raised towards the inflammation that is caused to the oxidative damage that is resulted in the physiological stress due to oxidation. There are a lot of drugs that are used to treat the condition effectively and the typical examples are NSAID’s and SAID’s which have a noted mechanism to show the anti-inflammatory activity. They have serious problems with the side effects like Gastrointestinal irritation, Gastric pain, Gastric perforations and peptic ulcers. Herbs have been used as better alternatives that are used to treat diseases. The significance of the medicinal plants had been emphasized significantly in tradition rich countries like India and all over the world. The research proof of those herbs for their activities and their traditional claims were proven. Poly Herbal Gels were prepared using the root extracts of the plant Corchorus olitorius. The gels were prepared using the Carbopol 940 and the prepared gels were investigated for their anti-inflammatory property and the gels showed a significantly better activity compared to the plant extract and the standard drug too. The addition of other drugs in to the gels added and advantage to the increase in the activity and faster onset of action as the gel was applied directly in the place of the inflammation.

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.

Topical Analgesic Formulations: Following the Transdermal Treatment Paradigm Only?

2019 ◽  
Author(s):  
Jan M Keppel Hesselink
Keyword(s):  
Ad Hoc ◽  
Active Pharmaceutical Ingredient ◽  
Mechanisms Of Action ◽  
Onset Of Action ◽  
Good Tolerability ◽  
Short Commentary ◽  
Topical Analgesics ◽  
The Usa ◽  
Treatment Paradigm ◽  
Topical Analgesic

Topical analgesics are regarded as new inroads to treat peripheral neuropathic pain, with a number of advantages over oral treatments. Topical treatment reduces systemic induced side-effects and have good tolerability, without problems of misuse or abuse, or dependency. Furthermore, the onset of action is fast, mostly within 30 minutes. The mechanism of action of topical analgesics is either via transdermal delivery of the analgesic, or via intradermal mechanisms of action. In the latter case, plasma levels of analgesics in the blood are absent or very low. This perspective is missing in the approach of the ad hoc committee of the National Academies of Sciences, Engineering, and Medicine in the USA, installed by the FDA. In this short commentary, we plead for a more comprehensive approach of topical analgesics, including those formulations which explicitly are not based on transdermal penetration of the active pharmaceutical ingredient, but on intradermal mechanisms of action.

Design, Optimization and Evaluation of Fast-Dissolving Oral Films of Ropinirole

2018 ◽  
Vol 11 (1) ◽  
pp. 3958-3967
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 4000 ◽  
Oral Films

The main objective of this study was to develop fast dissolving oral films of ropinirole HCl to attain quick onset of action for the better management of Parkinson’s disease. Twenty-seven formulations (F1-F27) of ropinirole oral dissolving films by solvent-casting method using 33 response surface method by using HPMC E15, Maltodextrin PEG 4000 by using Design of experiment software. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F4 showed minimum disintegration time 11 sec, maximum drug was released i.e. 99.68 ± 1.52% of drug within 10 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 92.77 ± 1.52 after 50 min. Therefore, it can be a good alternative to conventional ropinirole for immediate action. In vitro evaluation of the ropinirole fast dissolving films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of ropinirole. The oral dissolving film is considered to be potentially useful for the treatment of Parkinson’s disease where quick onset of action is desired

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.

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

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