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.

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 Salts of Therapeutic Agents: Chemical, Physicochemical and Biological Considerations

2018 ◽  
Author(s):  
Deepak Gupta ◽  
Deepak Bhatia ◽  
Vivek Dave ◽  
Vijaykumar Sutariya ◽  
Sheeba Varghese Gupta
Keyword(s):  
Dosage Form ◽  
Selection Process ◽  
Therapeutic Agents ◽  
Active Pharmaceutical Ingredients ◽  
Salt Form ◽  
Pharmaceutical Ingredients ◽  
Salt Selection ◽  
Pharmaceutical Properties ◽  
Positive Effect ◽  
Salt Forms

Choice of the salts of therapeutic agents or active pharmaceutical ingredients (API) is based on the physicochemical properties of API and the dosage form considerations. The appropriate salt can have positive effect on overall therapeutic and pharmaceutical effects of API. However, the incorrect salt form can negatively affect the overall pharmaceutical outcomes of the API. This review addresses various criteria for choosing appropriate salt form along with the effect of salt forms on API’s pharmaceutical properties. In addition to comprehensive review of the criteria, this review also gives a brief historic perspective of the salt selection process.

scholarly journals Interconvertible Hydrochlorothiazide–Caffeine Multicomponent Pharmaceutical Materials: A Solvent Issue

Crystals ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 1088
Author(s):  
Cristóbal Verdugo-Escamilla ◽  
Carolina Alarcón-Payer ◽  
Antonio Frontera ◽  
Francisco Javier Acebedo-Martínez ◽  
Alicia Domínguez-Martín ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Intermolecular Forces ◽  
Active Pharmaceutical Ingredients ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Great Stability ◽  
X Ray ◽  
Pharmaceutical Ingredients ◽  
Interesting Approach ◽  
Pharmaceutical Materials

The design of new multicomponent pharmaceutical materials that involve different active pharmaceutical ingredients (APIs), e.g., drug-drug cocrystals, is a novel and interesting approach to address new therapeutic challenges. In this work, the hydrochlorothiazide-caffeine (HCT–CAF) codrug and its methanol solvate have been synthesized by mechanochemical methods and thoroughly characterized in the solid state by powder and single crystal X-ray diffraction, respectively, as well as differential scanning calorimetry, thermogravimetric analyses and infrared spectroscopy. In addition, solubility and stability studies have also been performed looking for improved physicochemical properties of the codrug. Interestingly, the two reported structures show great similarity, which allows conversion between them. The desolvated HCT–CAF cocrystal shows great stability at 24 h and an enhancement of solubility with respect to the reference HCT API. Furthermore, the contribution of intermolecular forces on the improved physicochemical properties was evaluated by computational methods showing strong and diverse H-bond and π–π stacking interactions.

scholarly journals The Lisbon Supramolecular Green Story: Mechanochemistry towards New Forms of Pharmaceuticals

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2705
Author(s):  
João Luís Ferreira da Silva ◽  
M. Fátima Minas da Piedade ◽  
Vânia André ◽  
Sofia Domingos ◽  
Inês C. B. Martins ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Physicochemical Properties ◽  
Mechanochemical Synthesis ◽  
Crystal Engineering ◽  
Short Review ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Polymorphic Forms ◽  
Derivatives Of

This short review presents and highlights the work performed by the Lisbon Group on the mechanochemical synthesis of active pharmaceutical ingredients (APIs) multicomponent compounds. Here, we show some of our most relevant contributions on the synthesis of supramolecular derivatives of well-known commercial used drugs and the corresponding improvement on their physicochemical properties. The study reflects, not only our pursuit of using crystal engineering principles for the search of supramolecular entities, but also our aim to correlate them with the desired properties. The work also covers our results on polymorphic screening and describes our proposed alternatives to induce and maintain specific polymorphic forms, and our approach to avoid polymorphism using APIs as ionic liquids. We want to stress that all the work was performed using mechanochemistry, a green advantageous synthetic technique.

scholarly journals An Overview of Pharmaceutical Co-Crystal

2019 ◽  
Vol 7 (2) ◽  
pp. 39-46
Author(s):  
Rahul Kumar Ancheria ◽  
Saloni Jain ◽  
Deepak Kumar ◽  
Sankar Lal Soni ◽  
Mukesh Sharma
Keyword(s):  
Hydrogen Bonding ◽  
Physicochemical Properties ◽  
Pharmaceutical Compounds ◽  
Physicochemical Characteristics ◽  
Supramolecular Complexes ◽  
Active Pharmaceutical Ingredients ◽  
Therapeutic Activity ◽  
Pi Stacking ◽  
Pharmaceutical Ingredients ◽  
Future Aspect

Pharmaceutical co-crystals are nonionic supramolecular complexes and supramolecular chemistry. Pharmaceutical co-crystal consists of active pharmaceutical ingredients and coformers. Pharmaceutical co-crystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity. Co-crystals can be constructed through several types of interaction, including hydrogen bonding, pi-stacking, and vander Waals forces. Pharmaceutical co-crystals could play a major role in the future of API formulation. Pharmaceutical co-crystal can be improvement future aspect problems related physicochemical properties of API

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 Application of 1-Hydroxy-4,5-Dimethyl-Imidazole 3-Oxide as Coformer in Formation of Pharmaceutical Cocrystals

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 359 ◽  
Author(s):  
Aneta Wróblewska ◽  
Justyna Śniechowska ◽  
Sławomir Kaźmierski ◽  
Ewelina Wielgus ◽  
Grzegorz D. Bujacz ◽  
...  
Keyword(s):  
Solid State Nmr ◽  
Ball Mill ◽  
Barbituric Acid ◽  
Crystal Packing ◽  
Thiobarbituric Acid ◽  
Active Pharmaceutical Ingredients ◽  
X Ray ◽  
Pharmaceutical Ingredients ◽  
Tautomeric Forms ◽  
Biological Studies

Two, well defined binary crystals with 1-Hydroxy-4,5-Dimethyl-Imidazole 3-Oxide (HIMO) as coformer and thiobarbituric acid (TBA) as well barbituric acid (BA) as Active Pharmaceutical Ingredients (APIs) were obtained by cocrystallization (from methanol) or mechanochemically by grinding. The progress of cocrystal formation in a ball mill was monitored by means of high-resolution, solid state NMR spectroscopy. The 13C CP/MAS, 15N CP/MAS and 1H Very Fast (VF) MAS NMR procedures were employed to inspect the tautomeric forms of the APIs, structure elucidation of the coformer and the obtained cocrystals. Single crystal X-ray studies allowed us to define the molecular structure and crystal packing for the coformer as well as the TBA/HIMO and BA/HIMO cocrystals. The intermolecular hydrogen bonding, π–π interactions and CH-π contacts responsible for higher order organization of supramolecular structures were determined. Biological studies of HIMO and the obtained cocrystals suggest that these complexes are not cytotoxic and can potentially be considered as therapeutic materials.

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