scholarly journals Study of compatibility of components of a new combined drug for treatment of alcoholic intoxication and its hepatoprotective effect on a model of alcoholic liver injury

2021 ◽  
Author(s):  
Olha Rudakova ◽  
Svitlana Gubar ◽  
Nataliia Smielova ◽  
Dmytro Lytkin ◽  
Tatiana Briukhanova ◽  
...  
Keyword(s):  
Amino Acids ◽  
Ascorbic Acid ◽  
Sodium Bicarbonate ◽  
Physicochemical Properties ◽  
Acetylsalicylic Acid ◽  
Alcoholic Hepatitis ◽  
Alcohol Intoxication ◽  
Oral Solution ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients

The aim of the work is the development of a combined drug for use in alcohol intoxication based on the physicochemical properties and chemical compatibility of active pharmaceutical ingredients and excipients, and the study of the hepatoprotective effect in alcoholic hepatitis in rats. Materials and methods. During the studies, physical and physicochemical methods were used, a Specord 200 spectrophotometer (Germany), analytical scales Sartorius (SARTORIUS, Germany), class A volumetric glassware and reagents that meet the requirements of the State Pharmacopoeia of Ukraine (SPhU). Alcoholic hepatitis in rats was reproduced by intragastric administration of an aqueous 40% ethanol solution at a dose of 7 ml/kg for 1 week. Results. A new combined agent is proposed for use in alcohol intoxication in the form of an effervescent powder for the preparation of an oral solution, which contains glycine, L-glutamic acid, acetylsalicylic acid, ascorbic acid, fructose / sorbitol and sodium bicarbonate and citric acid to accelerate the dissolution of medicinal substances. To study the compatibility of the components, experimental studies of hygroscopicity, chemical interaction / chemical stability and an assessment of the redox potential of the proposed active pharmaceutical ingredients were carried out. To study the stability of the API, studies were carried out on sugaramine condensation due to the choice of amino acids and ascorbic acid in the composition of drugs. Based on the research results, it was decided to divide the API into 2 packages, separating sodium bicarbonate and glycine, which can interact with ascorbic acid / acetylsalicylic acid and ascorbic acid, respectively. In an in vivo experiment, it was found that the use of the new drug is accompanied by the normalization of the antioxidant-prooxidant status of the liver due to a likely decrease in the TBA-AP level and an increase in the RG index in the liver homogenate relative to the control group. Conclusions. Evaluation of the physicochemical properties of API allowed us to propose a new combined drug (TS-PP) for use in alcohol intoxication in the form of an effervescent powder for the preparation of oral solution. In alcoholic hepatitis in rats, it was found that the use of the studied drug largely prevents the formation of the effects of the toxic effects of ethanol on the rat organism, which is manifested by inhibition of destruction of hepatocyte membranes, a decrease in the level of LPO products, restoration of the RG index and improvement of the protein synthesizing function of the liver due to the complex effect of amino acids and ascorbic acid contained in the product

scholarly journals Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3279
Author(s):  
Ilma Nugrahani ◽  
Maria Anabella Jessica
Keyword(s):  
Amino Acids ◽  
Physicochemical Properties ◽  
Deep Eutectic Solvent ◽  
Strong Interactions ◽  
Green Method ◽  
Pharmaceutical Ingredients ◽  
Gastrointestinal Fluid ◽  
Non Covalent Interactions ◽  
Natural Deep Eutectic Solvent ◽  
Covalent Interactions

Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API’s physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, l-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially l-proline, enhances API’s solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses.

scholarly journals Structural motifs in salts of sulfathiazole: implications for design of salt forms in pharmaceuticals APIs

CrystEngComm ◽  
2018 ◽  
Vol 20 (24) ◽  
pp. 3428-3434
Author(s):  
Colin C. Seaton ◽  
Rayan R. Thomas ◽  
Eman A. A. Essifaow ◽  
Elisa Nauha ◽  
Tasnim Munshi ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Crystal Packing ◽  
Active Pharmaceutical Ingredients ◽  
Structural Motifs ◽  
Pharmaceutical Ingredients ◽  
The Creation ◽  
Salt Forms

The creation of salts is a frequently used approach to modify physicochemical properties of active pharmaceutical ingredients. This work prepares a collection of sulfathiazole salts to probe the influence of counterion structure on crystal packing.

scholarly journals Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 195
Author(s):  
Ana Santoveña-Estévez ◽  
Javier Suárez-González ◽  
Amor R. Cáceres-Pérez ◽  
Zuleima Ruiz-Noda ◽  
Sara Machado-Rodríguez ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Stability Study ◽  
Active Pharmaceutical Ingredients ◽  
Adherence To Treatment ◽  
Pharmaceutical Ingredients ◽  
Antituberculosis Treatment ◽  
Maximum Stability ◽  
Ph Conditions ◽  
The Stability

(1) Background: First-line antituberculosis treatment in paediatrics entails the administration of Isoniazid, Pyrazinamide, and Rifampicin. This study examines the possibility of developing a combined dose liquid formulation for oral use that would facilitate dose adjustment and adherence to treatment for younger children. (2) Methods: The active pharmaceutical ingredients stability under in vitro paediatric digestive pH conditions have been checked. The samples were studied as individual or fixed combined paediatric dosages to determine the pH of maximum stability. The use of hydroxypropyl-β-cyclodextrin to improve Rifampicin solubility and the use of ascorbic acid to increase the stability of the formulation have been studied. (3) Results: Maximum stability of combined doses was determined at pH 7.4, and maximum complexation at pH 8.0. Taking this into account, formulations presented the minimum dose of two active pharmaceutical ingredients dissolved. The addition of ascorbic acid at 0.1% w/v enables the detection of a higher remaining quantity of both drugs after three days of storage at 5 °C. (4) Conclusions: a formulation which combines the minimum paediatric dosages dissolved recommended by WHO for Isoniazid and Rifampicin has been developed. Future assays are needed to prolong the stability of the formulation with the aim of incorporating Pyrazinamide to the solution.

Continuous-flow protocol for the synthesis of enantiomerically pure intermediates of anti epilepsy and anti tuberculosis active pharmaceutical ingredients

2019 ◽  
Vol 17 (6) ◽  
pp. 1552-1557 ◽  
Author(s):  
Renata M. Aguiar ◽  
Raquel A. C. Leão ◽  
Alejandro Mata ◽  
David Cantillo ◽  
C. Oliver Kappe ◽  
...  
Keyword(s):  
Amino Acids ◽  
Continuous Flow ◽  
Building Blocks ◽  
Active Pharmaceutical Ingredients ◽  
Enantiomerically Pure ◽  
Pharmaceutical Ingredients ◽  
Chiral Intermediates

Continuous-flow production of chiral intermediates plays an important role in the development of building blocks for Active Pharmaceutical Ingredients (APIs), being α-amino acids and their derivatives widely applied as building blocks.

Multicomponent Crystals of an Artemisinin Derivative and Cinchona Alkaloids for Use as Antimalarial Drugs

CrystEngComm ◽  
2021 ◽  
Author(s):  
Qi Jiang ◽  
David A. Hirsh ◽  
Yifan Tu ◽  
Laibin Luo
Keyword(s):  
Physicochemical Properties ◽  
Antimalarial Drugs ◽  
Cinchona Alkaloids ◽  
Active Pharmaceutical Ingredients ◽  
Artemisinin Derivative ◽  
Pharmaceutical Ingredients

Pharmaceutical multicomponent crystals (MCCs) including salts and co-crystals of active pharmaceutical ingredients (APIs), are an active focus of research to improve various physicochemical properties of drugs. In this work, we...

scholarly journals Determination of the glucose residues on pharmaceutical equipment surfaces by both methods: polarimetry and HPLC

2018 ◽  
pp. 83-89
Author(s):  
A. А. Fedosenko ◽  
Yu. V. Scrypynets ◽  
I. I. Leonenko ◽  
A. V. Yegorova ◽  
S. N. Kashutskуy ◽  
...  
Keyword(s):  
Good Manufacturing Practice ◽  
Oral Solution ◽  
Process Equipment ◽  
Cross Contamination ◽  
Active Pharmaceutical Ingredients ◽  
Rapid Methods ◽  
Membrane Filters ◽  
Pharmaceutical Ingredients

Cleaning of equipment in the production of medicines is an important requirement of good manufacturing practice (GMP). As a rule, the same process equipment is used for the production of a number of different drugs that may result in cross-contamination. In order to prevent the contamination there is need in efficient cleaning of equipment used with the validation methods for each part of equipment. There is need as well to prove and establish acceptable residual limits of active pharmaceutical ingredients (API) on the surface of the equipment after purification (purity acceptance criteria) based on the therapeutic dose of API, toxicity, volume of series, the surface area of the used equipment. The aim of this work is the development of the simple and selective polarimetry and HPLC methods for determining residual amounts of glucose in washings from surfaces of pharmaceutical equipment after production of the drug. The object of the research is glucose, which is a part of the drug Regidron, powder for oral solution of 18.9 g per sachet. The swab Alpha® Sampling Swab TX715; membrane filters 0.20 µm; Minisart RC 15 «Sartorius» (Germany) were used. The polarimetric and HPLC methods for determination of glucose residues in washings from surfaces of pharmaceutical equipment after production the Regidron were developed. The recovery rates of glucose from swabs and pharmaceutical equipment surfaces are more than 90%. The proposed simple and rapid methods are characterized by satisfactory metrological characteristics and can be recommended to determine the residues of glucose in controlling the quality of cleaning pharmaceutical equipment.

scholarly journals Fiber-Array-Based Raman Hyperspectral Imaging for Simultaneous, Chemically-Selective Monitoring of Particle Size and Shape of Active Ingredients in Analgesic Tablets

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4381 ◽  
Author(s):  
Timea Frosch ◽  
Elisabeth Wyrwich ◽  
Di Yan ◽  
Juergen Popp ◽  
Torsten Frosch
Keyword(s):  
Particle Size ◽  
Acetylsalicylic Acid ◽  
Hyperspectral Imaging ◽  
Active Pharmaceutical Ingredients ◽  
Active Ingredients ◽  
Fiber Array ◽  
Size And Shape ◽  
Pharmaceutical Ingredients ◽  
Particle Size And Shape ◽  
Chemically Selective

The particle shape, size and distribution of active pharmaceutical ingredients (API) are relevant quality indicators of pharmaceutical tablets due to their high impact on the manufacturing process. Furthermore, the bioavailability of the APIs from the dosage form depends largely on these characteristics. Routinely, particle size and shape are only analyzed in the powder form, without regard to the effect of the formulation procedure on the particle characteristics. The monitoring of these parameters improves the understanding of the process; therefore, higher quality and better control over the biopharmaceutical profile can be ensured. A new fiber-array-based Raman hyperspectral imaging technique is presented for direct simultaneous in-situ monitoring of three different active pharmaceutical ingredients- acetylsalicylic acid, acetaminophen and caffeine- in analgesic tablets. This novel method enables a chemically selective, noninvasive assessment of the distribution of the active ingredients down to 1 µm spatial resolution. The occurrence of spherical and needle-like particles, as well as agglomerations and the respective particle size ranges, were rapidly determined for two commercially available analgesic tablet types. Subtle differences were observed in comparison between these two tablets. Higher amounts of acetaminophen were visible, more needle-shaped and bigger acetylsalicylic acid particles, and a higher incidence of bigger agglomerations were found in one of the analgesic tablets.

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