scholarly journals Osmotic Activity of Drugs is an Important Factor of Their Local Action at the Injection Site: What We Don't Use to Prevent Post-Injection Abscesses

Author(s):  
Aleksandr Urakov ◽  
Natalya Urakova

It is established that very few modern high-quality drugs in the dosage form "Solution for injection" have isoosmotic activity in the range of 280-300 mosmol/l of water. The main part of solutions for injection is hypotonic or hypertonic solutions, which can have osmotic activity in the range of 0 - 4000 mosmol/l of water. The reason for this was that the osmotic activity of drugs is not included in the list of controlled indicators of drugs quality, so it is not subject to control. It is shown that the osmotic activity of drug solutions increases with an increase in the total concentration of all dissolved ingredients present in the solution.  It was found that an excessively high concentration of the drug in the solution gives it an excessively large hyperosmotic activity, which can cause a local irritant and cauterizing effect at the injection sites due to dehydration of the cells. Therefore, to exclude post-injection abscesses, it is proposed to dilute the hypertonic drug with water for injection until it is given isotonic activity.

2019 ◽  
Vol 17 (2) ◽  
pp. 79-84
Author(s):  
Alexander L. Urakov

The literature review shows that today any substance, and hence any drug, can be in such physical states as solid, liquid, gas and plasma. The classification of pharmaceutical forms of drugs, from which it follows that presently the drugs are produced in solid, liquid, soft and gaseous “dosage forms”. It is shown that the modern quality standards of drugs do not guarantee the presence of a single aggregate physical properties of all drugs produced in the same dosage forms. It is established that modern quality standards of drugs allow the production of drugs in the same pharmaceutical forms, but with different concentrations of all ingredients and with different physical and chemical properties. The ranges of concentration values of the dissolved ingredients and indicators of acid (alkaline) and osmotic activity of high-quality drugs from different pharmacological groups produced by different pharmaceutical companies in the form of “Solutions for injection” are given. From the above examples, it follows that at present qualitative “Solutions for injections” have an acidity value in the range of pH 2-12 and an osmotic activity value in the range of 0-3900 mOsmol/l of water. In addition to this, it is shown that modern drugs prepared in the pharmaceutical form “Solutions for injection” and considered to be of high quality, have a concentration of dissolved ingredients in the range of 0.01-100 %. Therefore, almost all modern medicines produced in the dosage form “Solutions for injection” have different mechanical, physical, chemical and/or physico-chemical properties that can change their pharmacological activity. Examples are given of how different concentrations of ingredients and osmotic activity of certain drugs in the dosage form “Solutions for injections” affect the severity of their local action on tissues in the range from short-term inflammation of tissues to their necrosis. It is proved that modern “solutions for injections” do not guarantee the safety of local interaction with viable tissues of the human body. The technologies of improving the safety of injection of modern “Solutions for injection” and technology to prevent tissue necrosis with “wrong” injections of drugs (by accident, ignorance, ignorance, mistake) are listed.


2020 ◽  
pp. 25-32
Author(s):  
Mariya Anurova ◽  
Elena Bakhrushina ◽  
Anna Moiseyeva ◽  
Ivan Krasnyuk

Patient compliance of drug therapy is the key factor in achieving the pharmaceutical effect. Taste masking is particularly important in pediatrics and geriatrics because the unpleasant taste negatively affects drug uptake. Patient compliance can be improved through balanced organoleptic properties of medicines. It is particularly important to choose optimal correction method for medicines with high concentration of the active substance. Hopantenic acid has been chosen as a model drug due to its bitter taste. Taste masking technologies for creating a new dosage form with optimal organoleptic properties are proposed in the article. The objective is to achieve an experimentally justified choice of technological approach to masking bitter taste of a substance and to create a new dosage form on its basis. Materials and methods. Alternative technologies were considered to solve this problem: granulation, creation of complexes with ion-exchange resins, introduction of a gel composition and taste-masking using sweeteners. Organoleptic properties in dry compositions (pure substance of hopantenic acid, granulate and resinate based on it), and also after preparation of liquid dosage forms and incorporation them into gel, were evaluated by A. I. Tentsova method. Choice of sweetener and its concentration to achieve an optimally balanced taste took place at the final stage. Hopantenic acid was chosen as a model substance. Hopantenic acid is a nootropic drug stimulating cognitive functions, nervous system, enhancing intellectual functioning, decreasing nervous system activity, with anticonvulsant action. The main therapeutic indications are mental retardation, dementia, epilepsy. Results and discussion. The study has shown that optimal technology for masking unpleasant taste of hopantenic acid is its introduction into a gel composition, and a promising dosage form is an oral gel. Compri-Zucker G sweetener (Südzucker АG, Germany) in concentration of 5 % has been chosen to create pleasant taste due to its highest taste rating. Conclusion. It has been determined as a result of the study that oral gel with active drug concentration of 5 % and sweetener concentration of 5 % has optimal organoleptic properties. Thus, this combination of active and additional substances can be considered the most perspective for developing a new dosage form of a medicine.


1998 ◽  
Vol 38 (3) ◽  
pp. 95-102 ◽  
Author(s):  
G. Mazzolani ◽  
F. Pirozzi ◽  
G. d'Antonoi

Numerical models for the prediction of turbulent flow field and suspended solid distribution in sedimentation tanks are characterized by refined modeling of hydrodynamics, but apparently weak modeling of settling properties of suspensions. It is known that sedimentation tanks typically treat highly heterodisperse suspensions, whose concentrations range from relatively high to low values. However, settling is modeled either by considering one or more particle classes of different settling velocity, without accounting for hindered settling conditions, or by treating the suspension as monodisperse, even in regions of low concentration. A new generalized settling model is proposed to account for both discrete settling conditions in low concentration regions of the tanks and hindered settling conditions in high concentration regions. Settling velocities of heterodisperse suspensions are then determined as a function of particle velocities in isolation and their total concentration. The settling model is used in the framework of a transport model for the simulation of hydrodynamics and solid distribution in a rectangular sedimentation tank. Results show that solid distribution is mainly affected by particle interactions in the inlet region and by settling properties of individual particles in the outlet region. Comparison of the proposed settling model with other settling models suggests that a generalized approach of the modeling of settling properties of suspensions is a primary concern to obtain reliable predictions of the removal rate.


2021 ◽  
Vol 14 (2) ◽  
pp. 1037-1045
Author(s):  
Xiaona Shang ◽  
Ling Li ◽  
Xinlian Zhang ◽  
Huihui Kang ◽  
Guodong Sui ◽  
...  

Abstract. Oxidative stress can be used to evaluate not only adverse health effects but also adverse ecological effects, but limited research uses eco-toxicological assay to assess the risks posed by particle matters to non-human biomes. One important reason might be that the concentration of toxic components of atmospheric particles is far below the high detection limit of eco-toxic measurement. To solve the rapid detection problem, we extended a versatile aerosol concentration enrichment system (VACES) for ecotoxicity aerosol measurement and firstly used VACES to provide a comparison of ecotoxicity between non-concentrated and concentrated aerosols in ambient air. In this study, the total concentration (number or mass), the concentration of chemical components and the ecotoxicity were all increased by approximately 7 to 10 times in VACES, making the detection of ecotoxicity above the baseline. The comparison of ecotoxicity data and PM2.5 concentration showed that low concentration was not matched with ecotoxicity, although high concentration corresponded to higher ecotoxicity. In addition, the higher saturation temperature in VACES caused a loss of particulate matter, of which nitrate accounted for about 18 %.


2019 ◽  
Vol 90 ◽  
pp. 102784 ◽  
Author(s):  
Diana H. Bacon ◽  
Catherine M.R. Yonkofski ◽  
Christopher F. Brown ◽  
Deniz I. Demirkanli ◽  
Jonathan M. Whiting

2014 ◽  
Vol 32 (No. 1) ◽  
pp. 69-76 ◽  
Author(s):  
H. Zhao ◽  
F. Zhou ◽  
P. Dziugan ◽  
Y. Yao ◽  
J. Zhang ◽  
...  

The effect of malolactic fermentation (MLF) on the flavour quality of cider was examined. Leuconostoc mesenteroides subsp. mesenteroides Z25 was used to start MLF taking place at 25°C for 12 days after the completion of alcoholic fermentation (AF) by Saccharomyces cerevisiae. Strain Z25 showed good activity in starting MLF of cider with 10% alcoholic concentration. The content of malic acid, whose high concentration gives negative organoleptic characteristics to the cider, dropped significantly from 4.0 g/l to 0.25 g/l via MLF. The concentration of lactic acid increased significantly from 0.99 g/l to 3.50 g/l, contributing to volatile acidity. The acetic acid content of the ciders was 0.74 g/l. Among 51 volatile compounds detected by GC-MS, higher alcohols, esters, and carbonyl compounds were formed in ciders through MLF. The total concentration of aromatic substances doubled compared to the controls. The occurrence of MLF started by strain Z25 enabled the cider containing more volatile compounds and an acceptable adjustment of organic acids. This is the first report on using L. mesenteroides subsp. mesenteroides strain Z25 to start the MLF of apple wine improving the flavour quality of the cider produced.  


2015 ◽  
Vol 19 (2) ◽  
pp. 123-128 ◽  
Author(s):  
Sadhana Pradhanang

A five-step sequential extraction procedure was applied for the determination of the distribution of four elements (Cr, Mn, Fe, and Ni) in sediment of the Karra River. Sediment samples were collected from 16 different sites in the Karra River (upstream, industrial belt, downstream). The distribution of trace metals among exchangeable, carbonate, reducible, oxidizable and residual fractions were determined. The total concentration of metals varies in the range of Cr 72–4339.54 mg kg?1, Mn 22–411.93 mg kg?1, Fe 2967.23-32423.0 mg kg?1 and Ni 31.70-180.74 mg kg?1. The accuracy evaluated by comparing total trace metal concentrations with the sum of the five individual fractions proved to be satisfactory. The chemical speciation of Cr, Mn, Fe, and Ni in most sampling stations were in the order of residual > reducible > oxidazable > carbonate> exchangeable. Fractionation analysis showed that dominant metals are in residual fraction. The highest metal concentrations were observed at the most polluted sites of the industrial belt. High concentration of chromium was found in the Fe-Mn oxide and organic fraction in some of the sites of industrial belt.Journal of Institute of Science and Technology, 2014, 19(2): 123-128


2014 ◽  
Vol 644-650 ◽  
pp. 2137-2142
Author(s):  
Jian Wang ◽  
Yan Liu ◽  
Zhi Guang Zhang ◽  
Zhan Jiang Yu ◽  
Bao Gui Wang ◽  
...  

A new kind of human-imitate shooting platform is needed, so that the automation and standardization of small arm experiment could be realized. And the main part of shooting platform design is the modeling of human-gun interaction system. The main object of this paper is modeling human-gun interaction system by testing the model of the system. Firstly, the testing scheme is promoted for testing interaction between gun and human shoulder, and high quality test data is collected. Then, the model parameter of human-gun system is calculated by the method of model parameter identification. 3D model of human-gun system is built. At last, the dynamic simulation is made by ADAMS. And human-gun model built by experiment method is verified.


Antibodies ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 36
Author(s):  
Vaneet K. Sharma ◽  
Bijay Misra ◽  
Kevin T. McManus ◽  
Sreenivas Avula ◽  
Kaliappanadar Nellaiappan ◽  
...  

The discovery of numerous potent and broad neutralizing antibodies (bNAbs) against Human Immunodeficiency Virus type 1 (HIV-1) envelope glycoprotein has invigorated the potential of using them as an effective preventative and therapeutic agent. The majority of the anti-HIV-1 antibodies, currently under clinical investigation, are formulated singly for intra-venous (IV) infusion. However, due to the high degree of genetic variability in the case of HIV-1, a single broad neutralizing antibody will likely not be sufficient to protect against the broad range of viral isolates. To that end, delivery of two or more co-formulated bnAbs against HIV-1 in a single subcutaneous (SC) injection is highly desired. We, therefore, co-formulated two anti-HIV bnAbs, 3BNC117-LS and 10-1074-LS, to a total concentration of 150 mg/mL for SC administration and analyzed them using a panel of analytical techniques. Chromatographic based methods, such as RP-HPLC, CEX-HPLC, SEC-HPLC, were developed to ensure separation and detection of each antibody in the co-formulated sample. In addition, we used a panel of diverse pseudoviruses to detect the functionality of individual antibodies in the co-formulation. We also used these methods to test the stability of the co-formulated antibodies and believe that such an approach can support future efforts towards the formulation and characterization of multiple high-concentration antibodies for SC delivery.


1991 ◽  
Vol 261 (4) ◽  
pp. H1197-H1204 ◽  
Author(s):  
S. Yamada ◽  
M. DePasquale ◽  
C. S. Patlak ◽  
H. F. Cserr

Dynamics and pathways of 125I-labeled albumin (RISA) outflow from brain to deep cervical lymph have been studied in anesthetized rabbits between 4 and 25 h after microinjection of 1 microliter RISA into the internal capsule or midbrain. Lymph from the jugular lymph trunks was collected for periods of 2-11 h. RISA was cleared from brain with half-times of disappearance from internal capsule and midbrain of 18.2 and 11.9 h, respectively. RISA was distributed in high concentration to subarachnoid arteries that supplied the tissue injection site; this was consistent with RISA drainage from brain via perivascular spaces. Outflow through lymph rose to a maximum value 15-20 h after tracer injection. Mean recovery of RISA from lymph over the 25-h collection period accounted for 22% of total loss from internal capsule and 18% from midbrain. This result compares with mean recoveries from caudate nucleus and cerebrospinal fluid of 47% and 30%, respectively [M.W.B. Bradbury, H.F. Cserr, and R.J. Westrop, Am. J. Physiol. 240 (Renal Fluid Electrolyte Physiol. 9): F329-F336, 1981]. These are minimal estimates of total outflow to lymph because of the 15- to 20-h delay in RISA passage from brain to lymph.


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