Penicillin Salts Research Articles

Application of Amoxicillin in the pearl necklace test in the identification of the Anthraxic cause

Identification of the causative agent of anthrax is an integral part of the diagnosis of the disease caused by it, which is registered annually on the territory of our country among animals and people. According to the guidelines for the diagnosis of the causative agent of anthrax, one of the identification tests is to study the sensitivity of the pathogen to penicillin with the registration of the phenomenon of the pearl necklace. Currently, penicillin salts are a hard-to-reach antibacterial drug. Based on this, we used amoxicillin, a penicillin-type antibiotic with a similar mechanism of action, which was the purpose of our study. A nutrient medium with an antibiotic was prepared by analogy with a medium with the addition of penicillin, according to MUC 4.2.2413-08. Amoxicillin in the form of amoxicillin trihydrate produced by Hemofarm (Serbia) was used as an antibacterial drug. To work, amoxicillin, by analogy with penicillin, was diluted 1,000,000 times with sterile Hottinger broth and introduced into a prepared nutrient medium. The loop of the grown daily culture of the strain K-STI-79 B. anthracis was seeded in 3 ml of the prepared medium and incubated for 3 hours at 37 ° C. During the incubation time, smears were prepared from the cells and stained according to the Rebiger. The smears were prepared after 15, 30 minutes and after 1, 2 and 3 hours. As a result of the work carried out, it was found that the use of amoxicillin in the identification of B. anthracis allows us to obtain the necessary results with a characteristic picture of a "pearl necklace". At the same time, the dynamics of changes in the morphology of cells subjected to incubation in a nutrient medium containing amoxicillin was studied. It was found that changes in the cell wall and cell shape can be observed after 15 minutes of incubation. After 1 hour, the cells underwent significant deformation with the appearance of a large number of separate spherical cell forms. After 2 hours of incubation, the chains of B. anthracis began to acquire the characteristic appearance of a pearl necklace, which was traced after 3 hours.

Immunofluorescent Analysis with Magnetic Nanoparticles for Simultaneous Determination of Antibiotic Residues in Milk

An analytical system for simultaneous detection of three antibiotic residues in milk (penicillin, tetracycline, and sulfadimethoxine sodium salt) was developed. The method was based on a fluorescence immunoassay. Magnetic nanoparticles (MNPs) were prepared and then coated with 3-(aminopropyl) triethoxysilane (APTES). Antibodies, against penicillin, tetracycline, and sulfadimethoxine, were immobilized on APTES-MNPs. Two immobilization methods were used: a random and an oriented method by protein A. The fluorochrome-antigen conjugates, containing FITC, ATTO 590, and ATTO 630 were obtained. Three separate immunofluorescent analyses were investigated for penicillin, tetracycline, and sulfadimethoxine, first in buffer and then in milk. Linearity values of standard curves in milk were: for penicillin 4–15 ng mL−1, for tetracycline 50–500 ng mL−1 (using random immobilization) and 100–500 ng mL−1(using oriented immobilization), and for sulfadimethoxine 100–500 ng mL−1. The linearity and sensitivity of calibration curves of determination of penicillin, tetracycline and sulfadimethoxine in milk were very close to the obtained results for separate determination of three antibiotics. It was shown that the multiple immunofluorescence analysis for antibiotic residues in milk without preliminary treatment is effective and rapid.

Studi Kimia Adi (Fine Chemical) Industri Antibiotika

Antibiotic have been know since 1929 by Fleming. According to Fleming antibiotic is a potential subtance namely Penicilline. Antibiotic is a subtance because grew by mold or a special bacteria or made by of a Subtance use semi Synthesa/Synthesa methode, who is inhibit of other grown micro orga­nisme beside result of this self micro organisme. Indonesia still import Anti­biotic raw material namely : Penicillin salt and derivat's, Streptomycine salt and derivat's Tetracycline salt and derivat's, Chloramphenicol salt and derivat's, Erythrornycine salt and derivat's. Indonesia has been imported 12 I, l 05 Kg and 13 7 ,641 Kg Testracycline salt in 1984 and 1985. This type is the most quantity import.

Acute paraplegia and pulmonary edema after benzathine penicillin injection

Accidental intra-arterial injection is a potentially devastating complication of the intragluteal injection of benzathine penicillin. A 35-year-old woman developed after intramuscular injection of benzathine penicillin G acute paraplegia and noncardiogenic pulmonary edema. Noninvasive positive pressure ventilation was initiated with furosemide and corticosteroids. A magnetic resonance imaging scan showed findings consistent with syringomyelia and spinal cord ischemia at T9 through T10. Vascular injury may be the result of microemboli of the injected crystals of the penicillin salts. The mechanism of noncardiogenic pulmonary edema is perhaps an immunogically mediated one. At 2-year follow-up, she had no improvement in neurologic status. The deficit is considered permanent.

Electrical Conductances of Dilute Aqueous Solutions of Sodium Penicillin G, Potassium Penicillin G, and Potassium Penicillin V in the 278.15−313.15 K Temperature Range

Systematic determinations of electrical conductivities of sodium penicillin G, potassium penicillin G, and potassium penicillin V in the 278.15-313.15 K temperature range are reported. These conductivities are examined by applying the Quint-Viallard conductivity equations and the Debye-Hückel equations for activity coefficients. Determined dissociation constants and the limiting conductances of penicillin anions are based on the assumption that in dilute aqueous solutions, penicillin salts behave as acidic salts of dibasic acids, which are the final products of degradation reactions in acidic media.

Síndrome de Hoigne

Background Hoigne's syndrome is a pseudoanaphylactic or pseudoallergic reaction that occurs after intramuscular administration of penicillin G procaine or benzathine. These are usually embolic toxic reactions possibly due to vascular occlusion by large crystals of the penicillin salts. We report a case of Hoigne's syndrome. Case report A 44-year-old woman received 1,200,000 U.I. of intramuscular procaine penicillin once daily for treatment of acute amygdalitis. Immediately after the second dose the patient developed mental confusion, visual and auditory hallucinations, perceived changes of body shape, swelling of the tongue and a fear of impending death. Penicillin allergy study (serum-specific IgE levels, skin tests and provocation test) was performed. The diagnosis of Hoigne's syndrome was confirmed by negative oral challenge test with penicillin. Conclusions Hoigne's syndrome is a pseudoanaphylactic reaction that must be differentiated from authentic anaphylactic shock due to penicillin. This distinction allows treatment to be continued in Hoigne's syndrome, whereas it is contraindicated in anaphylactic shock.

Application of capillary electrophoresis to the determination of various benzylpenicillin salts

The application of capillary electrophoresis for separation of benzylpenicillin, procaine, benzathine and clemizole was investigated. Phosphate–borate buffer supplemented with sodium dodecyl sulphate 14.4 g/l and electrophoresis voltage 18 kV seem to provide optimal conditions for micellar electrokinetic chromatographic assay of penicillin salts. This method is selective and precise. The results obtained from CE method recovery assay (above 98% for all but procaine—97% substances) and from determination of benzylpenicillin by CE compared with HPLC results, confirmed good accuracy.

Kinetic analysis of thermal decomposition for penicillin sodium salts: Model-fitting and model-free methods

A kinetic study on decomposition processes of some penicillin salts was carried out. Both isothermal and dynamic thermogravimetric curves were used. As expected by their complex structures, several steps with different energies were involved in decomposition processes. Model-fitting and -free kinetic approaches were applied to nonisothermal and isothermal data. The kinetic triplet ( f( α), A and E a) related to model-fitting method that defines a single step reaction resulted to be at variance with the multi-step nature of salts-decomposition. The model-free approach represented by the isothermal and nonisothermal isoconversional methods, gave different dependencies of the activation energy on the extent of conversion. The complex nature of the multi-step process of the studied compounds was more easily revealed using a broader temperature range in nonisothermal isoconversional method. The failure in the model-fitting method did not allow calculating shelf life and half-life times.

Inflammatory response to intramuscular implantation of polyacrylonitrile ultrafiltration probes in sheep.

Polyacrylonitrile is used in the manufacture of dialysis membranes. These membranes are fundamental to the functioning of implantable probes for microdialysis and ultrafiltration sampling of tissue fluids. Although in vivo experimentation using polyacrylonitrile has been reported to cause little inflammatory response when implanted subcutaneously, such information is not available for intramuscular implantation in sheep. The procaine and benzathine salts of penicillin are formulated for intramuscular injection. These salts of penicillin or the formulation excipients may cause inflammatory reactions. Use of polyacrylonitrile probes to draw samples from sites at which these formulations have been injected may be compromised by inflammation or direct interaction between formulation excipients and the dialysis membrane. The aim of this project was to describe tissue responses to intramuscular implantation of polyacrylonitrile in the presence and absence of either procaine or procaine plus benzathine salts of penicillin G. Each of 20 normal sheep was implanted with two ultrafiltration probes, one at the site of an injection of procaine or benzathine plus procaine penicillin G. Similar injections were also made at remote intramuscular sites. After 8, 9, and 11 days of the experiment, sheep were killed and the injection and implantation site muscle were excised and prepared for histopathological examination. The implantation of the probe alone caused greater inflammatory response than the injection of procaine or procaine plus benzathine penicillin G at remote intramuscular sites. The histopathological lesions were greatest where the implantation site was coupled with the injection of either formulation of penicillin G. Polyacrylonitrile may not be a suitable dialysis membrane material for intramuscular implantation in sheep.

S-Aminosulfeniminopenicillins: Multimode β-Lactamase Inhibitors and Template Structures for Penicillin-Based β-Lactamase Substrates as Prodrugs

A series of novel penicillins, bearing an S-aminosulfenimine (R‘(R‘ ‘)NSN) side chain at the 6-position, have been prepared by direct reaction of a penicillin ester with sulfur diimides. A set of these structures, with the thiazolidine-ring sulfur in the sulfide oxidation state, exhibited a pattern of reactivity not previously encountered in penicillin chemistry, viz., cleavage of the β-lactam ring resulted in a rapid intramolecular displacement of the S-amino moiety as R‘(R‘ ‘)NH. This was found to be the exclusive reaction occurring consequent on cleavage of the β-lactam ring. The mechanism of this process was delineated in a detailed study in basic methanol. That a similar reactivity pattern held for a penicillin salt in aqueous solution was also verified. Thus the salt 5bm (R‘ = CH3, R‘ ‘ = p-CH3C6H4SO2) behaved as a moderate substrate for β-lactamase type I from Bacillus cereus (kcat/Km = 6.26 × 105 M-1 min-1). On enzyme-catalyzed hydrolysis of this compound, displacement of N-methyl-p-toluenesulfonamide (R‘(R‘ ‘)NH) was directly observed (1H NMR) and found to occur faster than displacement of this group from (intact) 5bm in aqueous buffer, by a factor of at least 600. These findings identified the potential of the S-aminosulfeniminopenicillin structure type to be developed as β-lactamase substrates for use as site-specific-release prodrugs. A degree of enzyme inhibition was also observed with this set of thiazolidine-ring-sulfide structures with the most potent inhibitor having the most nucleofugic S-amino moiety p-ClC6H4SO2N(CH3), indicating that displacement of this group, at the enzyme active site, played a role in their mode of inhibition. Structures with the thiazolidine-ring sulfur in the sulfone oxidation state were considerably more potent as inhibitors, with the structure 5a2 being the most active. As this compound bore the least nucleofugic S-amino moiety C2H5OC(O)NH, it indicated that the mode of inhibition of the sulfones was distinct from that of the thiazolidine-ring sulfides; it is probable that the sulfones reacted in a manner similar to that shown by sulbactam viz., rapid scission of the thiazolidine-sulfone ring after cleavage of the β-lactam ring. Synergy of action was observed with 5a2 at high concentration (78 μg/mL) against Escherichia coli when combined 1:1 with penicillin G; no synergy was observed at low concentration (4 μg/mL) when combined with pipericillin, indicating poor permeation characteristics.

Randomized evaluation of benzathine penicillin V twice daily versus potassium penicillin V three times daily in the treatment of group A streptococcal pharyngitis

In a randomized, prospective, multicenter study the clinical and bacteriological efficacies of three dosage schedules with two different salts of oral penicillin V suspensions (regimen 1: potassium salt of penicillin V, 50,000 U/kg of body weight per day in three divided doses; regimen 2: benzathine salt of penicillin V, 50,000 U/kg of body weight per day in two divided doses; and regimen 3: benzathine salt of penicillin V, 100,000 U/kg of body weight in two divided doses) for the treatment of streptococcal pharyngitis were evaluated. Children with clinical signs of acute pharyngitis and a positive throat culture for group A beta-hemolytic streptococci (GABHS) were eligible. There was no difference between the treatment groups with respect to the overall clinical success rate. Eradication of the original serotype of GABHS from throat cultures was achieved in 87.1% (regimen 1), 85.5% (regimen 2) and 87.7% (regimen 3) of patients. The incidence of potential drug-related adverse events was significantly higher in patients treated with regimen 3. The results of this and earlier studies strongly suggest that oral penicillin given twice daily should be the recommended treatment for the initial treatment of pharyngitis due to GABHS. Doubling the total daily dose is not beneficial in the usual clinical setting. Because of its favorable pharmacokinetics, the benzathine salt of penicillin V appears to be well suited for a twice-a-day dosage schedule.

Effect of teat dipping and dry cow therapy on mastitis in a commercial dairy herd in China

One hundred and nine Holstein cows were divided at random into two groups: a trial group and a control group. Teat dipping with Dianxiaoling (containing 0.5% available iodine) after milking and dry cow therapy with TA-125 (mainly containing benzathine penicillin and cloxacillin) at drying off were applied in the trial group of 53 cows. The other 56 cows in the control group were not dipped, but their quarters were infused following the last milking with solutions of penicillin salt and dihydrostreptomycin. After a 22-month experiment, the incidence of subclinically mastitic quarters in the trial group was reduced about 50% in comparison with that in the control group ( P < 0.01). The incidences of clinical mastitis and of blind teats were also significantly reduced.

Intravascular Injuries from Intramuscular Penicillin

Benzathine penicillin, procaine penicillin, and mixtures of both are opaque preparations for intramuscular injection. Visualization of aspirated blood, the fail-safe for avoiding intravascular injection, is predictably problematic. A spectrum of injuries, sometimes permanent, to the gluteal region, distal extremities, perineum, and spinal cord probably results from inadvertent intra-arterial injection, possibly due to vascular occlusion by large crystals of the penicillin salt(s). Since the arterial injurie disproportionately affect infants, use of these preparations in that age group should be minimized. The corresponding intravenous injection probably is Hoigne's syndrome, a procaine-induced central nervous system syndrome. Though usually brief and transient complications may be profound, including coma, convulsions, and death. Careful attention to details of anatomy and manufacturer's recommendations is critical.

Ion Chromatographic Determination of the Principal Inorganic Ion in Bulk Antibiotic Salts

Two ion-chromatographic procedures were developed for determining the principal inorganic ions in bulk antibiotic salts. The anion system enables sulfate determination in sulfate salts of polymyxin, neomycin, streptomycin, and dihydrostreptomycin, with typical analysis times of 8 min/sample and a relative precision of ±2% (95% confidence interval). The cation system is applicable to sodium or potassium analysis in the respective penicillin salts in 9-16 min with a relative precision of ±2.5%. These methods offer speed, specificity, and easy sample preparation compared with traditional assays.

The effect of penicillin- and tetracycline-containing medicaments on the microhard-ness of human dental enamel: An in vitro study

While the sugar content of various medicaments has been accepted as a hazard to dental health, the possible detrimental effect of the medicaments per se has been largely overlooked. In the present study the microhardness of dental enamel was examined before and after the exposure to various salts of penicillin, to tetracycline chloride, and to human saliva. The Vickers hardness index was found to 1. remain stable or increase slightly in enamel exposed to saliva, nonaqueous penicillin suspensions and certain watery solutions of phenoxymethylpenicillin calcium. 2. decrease to a moderate degree in most aqueous penicillin solutions, and 3. decrease drastically in tetracycline solutions and in phenoxymethylpenicillin calcium solutions containing citrate. The results indicate that a direct reaction may take place between the dental enamel and the medicament and/or its degradation products when antibiotic compounds are taken per os.

Identification of an Imidazolinium salt, the major Product from Reaction of Benzathine with Iodine

The isolation and identification of an imidazolinium salt are described. Unambiguous determination of structure was accomplished by independent synthesis. The isolated product interferes in the iodometric assay of the benzathine salts of penicillin.

The bioavailability of oral penicillin V. A comparative study of the absorption of different salts of penicillin V in children.

Different salts of penicillin V (pc-V): potassium pc-V (Calciopen and Kåvepenin), calcium pc-V (Penicals) and benzathine pc-V (Meropenin) were given to 37 children (age 2 months to 4 years) with upper respiratory infections. The gastro-intestinal absorption of the drug given in a mixture was followed for three hours after administration by determination of the serum levels from capillary samples. Administration of the mixtures containing the potassium pc-V resulted in a more rapid absorption and in significantly higher plasma concentrations at 30 min than did administration of the preparations containing the calcium and benzathine salts. In four children with coeliac disease, verified by intestinal biopsy, the absorption of potassium pc-V (Calciopen) was compared with that of calcium pc-V (Penicals). A decreased absorption was found and this was most pronounced when the calcium salt was given.

Epileptogenic Effects of Several Penicillins and Penicillin‐Related Compounds in Rat Neocortex

Several penicillins and penicillin-related compounds were tested for their ability to produce epileptiform activity in rat neocortex. (1) Alterations in the side chain of penicillin G decreased epileptogenic capability in all the compounds tested in this study: Phenoxymethylpenicillin produced a primary focus but no mirror focus, suggesting a dissociation of the mechanisms underlying these two processes. Ampicillin, 6-aminopenicillanic acid, and potassium 6-aminopenicillanic acid, and potassium 6-aminopenicillanic acid produced little or no epileptiform activity. All these compounds have free amino grounds and are amphoteric. (2) Breaking the beta lactam ring of penicillin G (potassium penicillin G penicilloate) eliminated epileptogenic capability. (3) Potassium salts of penicillin or its derivatives (potassium penicillin G, propicillin, potassium 6-aminopenicillanic acid, potassium penicillin G penicilloate) consistently suppressed cortical activity, regardless of the ability of the compound to produce spike discharges. Thus, mechanisms underlying these two properties can be dissociated. (4) Antibiotic activity of penicillins bears no relationship to epileptogenic capability.

Oral Absorption Efficiency of Acid-Labile Antibiotics from Lipid-Drug Delivery Systems

The utility of cholesterol, cholesteryl acetate, and β-sitosterol in protecting and improving the oral absorption efficiency of acid-labile antibiotics is discussed. The potassium salts of penicillin G and penicillin V and erythromycin lactobionate were studied. The stability of the two penicillins in simulated gastric fluid was determined iodometrically. The rank order of acid protective activity was: cholesteryl acetate > β-sitosterol > cholesterol. Oral administration of erythromycin lactobionate coated with cholesteryl acetate produced a twofold increase in human urinary excretion of erythromycin when compared with the uncoated material. Potassium salts of penicillin G and penicillin V coated with cholesteryl acetate yielded 1.6- and 2-fold higher urine levels, respectively, as compared with the uncoated candidates.

ChemInform Abstract: STUDIES ON THE EFFECTS OF GAMMA RADIATION ON HEXA‐AMINOPENICILLANIC ACID AND ITS DERIVATIVES BY THE EPR‐METHOD

AbstractDie EPR‐Spektren der bestrahlten Proben [6‐Amino‐penicillansäure, Kalium‐ Benzylpenicillin, Procain‐Benzylpenicillin, Na‐3‐(o‐chlorphenyl)‐5‐methyl‐4‐ isoxazolyl‐Penicillin) weisen auf das Vorhandensein von Radikalen mit ungepaarten Elektronen am Sund von durch Decarboxylierung entstandenen Radikalen hin.