Evaluation of the kinetics of the release of active substance in the oral cavity after the use of orodispersible tablets against sore throat

Pharmateca ◽  
2019 ◽  
Vol 1_2019 ◽  
pp. 65-69
Author(s):  
V.V. Smirnov ( Smirnov ◽  
) ) ◽  
E.A. Egorenkov () Egorenkov ◽  
◽  
Materials ◽  
2019 ◽  
Vol 12 (8) ◽  
pp. 1202 ◽  
Author(s):  
Dorota Wojcik-Pastuszka ◽  
Justyna Krzak ◽  
Bartosz Macikowski ◽  
Ryszard Berkowski ◽  
Bogdan Osiński ◽  
...  

Implants are readily applied as a convenient method of therapy. There is great interest in the prolonged release of active substances from implants. The objective of this work was to evaluate the dissolution kinetics of steroidal anti-inflammatory preparation (SAP) released from novel implants, and to test the influence of the technology on SAP release kinetics. The proposed long-acting preparations may overcome difficulties resulting from repeated injections and often visits to ambulatory clinic, as the stabilizing function of the artificial ligament would be enriched with pharmacological activity. The potential advantages provided by the new coatings of knee implants include the continuous, sustained, and prolonged release of an active substance. The study was carried out using a modified United States Pharmacopoeia (USP) apparatus 4. The amount of SAP was measured spectroscopically. It was revealed that the transport of the drug was mainly a diffusion process. The drug release kinetics was analyzed using zero-, first-, and second-order kinetics as well as Korsmeyer-Peppas, Higuchi, and Hixon-Crowell models. The highest values of the release rate constants were k0 = (7.49 ± 0.05) × 10−5 mg × min−1, k1 = (6.93 ± 0.05) × 10−6 min−1, and k2 = (7.70 ± 0.05) × 10−7 mg−1 × min−1 as calculated according to zero-, first-, and second-order kinetics equations, respectively. The values of the rate constants obtained for the slowest process were k0 = (3.63 ± 0.06) × 10−5 mg × min−1, k1 = (2.50 ± 0.03) × 10−6 min−1, and k2 = (2.80 ± 0.03) × 10−7 mg−1 × min−1. They may suggest the possibility of sustained release of betamethasone from the system. Due to the statistical analysis, differences were observed between most of the studied implants. Incubation, temperature, time of stabilization of layers, and the method of SAP deposition on the matrix affected the drug release.


2002 ◽  
Vol 126 (1) ◽  
pp. 31-39 ◽  
Author(s):  
John B Morris ◽  
Peter Symanowicz ◽  
Ramesh Sarangapani

STED JOURNAL ◽  
2019 ◽  
Vol 1 (2) ◽  
Author(s):  
Davut Lacin ◽  
Ayse Zehra Aroguz ◽  
Vesna Teoflović ◽  
Olga Govedarica ◽  
Jelena Pavličević ◽  
...  

Recently, controlled drug release systems have been garnering a lot of attention, due to more targeted and effective approach for delivering drugs to a specific tissue. Because of a specific structure and natural abundance, clays are being added to those systems in order to increase its efficiency and minimize costs. In this study, controlled release kinetics of the drug active substance 5-Fluorouracil was studied, using halloysite clay/polymer drug carriers. For this purpose, the halloysite clay was initially modified with cetyltrimethyl ammonium bromide (CTAB). Drug carriers were prepared by adding modified halloysite clays in the mixtures of polyvinyl alcohol (PVA) and sodium alginate. Firstly, the swelling behaviour of the prepared substances was studied in buffer solutions at different pH. The drug release kinetics from the drug carriers, loaded with 5- Fluorouracil, was observed under a UV-spectrophotometer at 266 nm. Release profiles of the active substance were obtained by studying its release in buffer solutions at different pH. The results showed that the prepared drug carriers with modified halloysite clay were suitable for carrying and releasing of the 5-Fluorouracil.


Slovene ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 314-337
Author(s):  
Tatyana A. Agapkina ◽  
Elena L. Berezovich

The article considers the word duboglot, which functions in the Russian dialects (mainly South Russian) in the meanings of ‘strong dry cough, usually accompanied by a sore throat,’ ‘angina.’ Semantic and motivational reconstruction of this word is carried out based on its role in the text. The authors conclude that the word got into the dialect system from the folklore (mainly from the charms), where it refers to diseases related to inflammation of the oral cavity, pharynx and lower respiratory tract, and accompanied by a strong cough, pain. It is established that most often the word appeared in the texts as a part of the formula “X (a tree), take your Y (duboglot), otherwise I will eat you / swallow you,” which is initially addressed to an oak tree as a convenient “recipient” of diseases that are expelled from the speaker’s space. The authors suggest that the word duboglot is “induced” by the logic of unfolding the text: this is “the oak glot” (glot is the ability to swallow – from the Russian verb glotat’ ‘to swallow’), which should belong to an oak, not a sick person. The word creation within the framework of a spoken construction is supported by the capabilities that are inherent in the language system. Firstly, it is the image of an oak “mouth” (throat), which is formed on the basis of the natural properties and features of oak. This image could be fixed in the internal form of the word itself, which is a controversial issue, but it certainly is seen in the stable compatibility of dub ‘oak’ ↔ duplo ‘hollow’, and at the synchronous level is also supported by the phonetic proximity of these words. The image of a tree, secondly, has another facet: the image of roots of a tree and its crown is projected on the idea of the growth of a tumour (including one in the throat); roots and crown of a tree simultaneously seem to be a “tool” for clearing the throat. Yet another facet of the image is related to how the native speaker sees the properties of a bark: there is a productive model for the Russian language that fixates the connection between the designations of wood (oak) bark and tumours on the human body (including throat tumours); oak bark itself is generally an “archetype” of a bark, hard, rough, stripped from the surface of a tree (which corresponds to “tearing” sensations with a sore throat).


2019 ◽  
pp. 102-104
Author(s):  
V. V. Smirnov ◽  
E. A. Egorenkov

Acute respiratory viral infection (ARVI) is one of the most common causes of morbidity in Russia. The incidence rate is high regardless of age or social group [1]. Sore throat is the most common symptom during ARVI, prevalence rate is 95%[2]. Symptomatic treatment of ARVI requires the use of various drugs, including drugs for pain in the throat. Such preparations are widely represented on the market, while they have a different form and different composition. One of the most popular are sprays containing benzydamine hydrochloride. Professional associations recommend using Benzydamine hydrochloridewhile sore throat, also in paediatric practice [3].In connection with a large number of generics, the issue of standardization of such sprays is topical. To compare the range of the actual concentration of the active substance in interchangeable preparations with different trade names, a comparative determination of the concentrations of benzydamine hydrochloride in sprays of 4 trade names was carried out in 6 different series in each. The quantitative determination was carried out by HPLC with a UV detector. As a result, the active substance concentration ranges were determined in 6 batches of the preparation of each trade name, and the coefficient of variation of concentrations was calculated and conclusions were made on the difference in the indicated indices among preparations of various manufacturers.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 651 ◽  
Author(s):  
Neel Desai ◽  
Andrew Redfearn ◽  
Graeme MacLeod ◽  
Catherine Tuleu ◽  
Ben Hanson ◽  
...  

Orodispersible tablets (ODTs) offer rapid disintegration of the dosage form when placed on the tongue, which leads to fast release of the active pharmaceutical ingredient. Despite increased use in diverse patient populations, there have been numerous challenges associated with ODTs. One such concern is the lack of standardised assessment of disintegration behaviour. In the European Pharmacopoeia, ‘orodispersibles’ are defined as such if disintegration time is faster than 3 min. Common in vitro measurement methods only provide single time point data and have limited physiological accuracy. To determine more bio-predictive disintegration kinetics, a bench-top in vitro oral cavity model (OCM) was modified and piloted to assess disintegration of three ODTs of differing hardness. All ODTs disintegrated similarly within the OCM—surface breakdown/swelling, initial ‘wash away’ and final ‘wash away’. The distinct advantage presented within this pilot study using the OCM is the opportunity to ascertain disintegration behaviour profiles of ODTs by evaluating changes in the observable area during simulated oral processing. The model could be implemented as a decision-support tool during the early stages of the drug design process to improve acceptability and further understand ODT disintegration behaviour.


Author(s):  
Rajitha K ◽  
Shravan Kumar Y ◽  
Adukondalu D ◽  
Ramesh Gannu ◽  
Madhusudan rao Y

Buspirone is a classical anxiolytic agent. The present investigation deals with formulation of orodispersible tablets (ODT) of buspirone that disintegrate in the oral cavity upon contact with saliva and thereby should improve therapeutic efficacy. 


Author(s):  
R. Alrouhayya ◽  
T.F. Sheshko ◽  
E.B. Markova ◽  
V.S. Boldyrev ◽  
A.A. Razvodova ◽  
...  

The low solubility of a biologically active substance in an aqueous medium is often the main reason for the reduced therapeutic effect of drugs. The most common approach to solve this problem is to obtain a watersoluble salt of the active substance and an appropriate preparatory formulation based on it. In this case, the solubility of the obtained compound in hydrophobic systems decreases dramatically, which decreases the rate of transmembrane transport and changes the pharmacokinetic laws of the process. In practice, not only the dependence of the therapeutic effect on the salt compound properties, but also a complete loss of the drug active ingredient activity can be observed. The use of biologically active compound solid dispersions in watersoluble polymers is the most promising approach to increase the therapeutic effect of drugs while maintaining the hydrophobic nature of the active component, to reduce the dose load on the patient’s body and obtain prolonged action. In experiments we obtained solid dispersions of mefenamic acid in polyvinylpyrrolidone and studied kinetic regularities of solubility of this promising drug form in aqueous solution of phosphate buffer. By means of mathematical modelling it was found that the phenomenon under study is well described by Ritger --- Peppas model, which considers diffusion of biologically active component into solution according to Fick's law with possible influence on mass transfer at swelling and degradation of polymer matrix


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