scholarly journals Co-crystals: A novel approach to modify physicochemical properties of active pharmaceutical ingredients

2009 ◽  
Vol 71 (4) ◽  
pp. 359 ◽  
Author(s):  
AV Yadav ◽  
AS Shete ◽  
AP Dabke ◽  
PV Kulkarni ◽  
SS Sakhare
Keyword(s):  
Physicochemical Properties ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Novel Approach

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 Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 234
Author(s):  
Chiluba Mwila ◽  
Roderick B. Walker
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Active Pharmaceutical Ingredients ◽  
Acidic Media ◽  
Pharmaceutical Ingredients ◽  
Novel Approach ◽  
Improved Stability ◽  
Input Variables ◽  
The Impact ◽  
Sustained Release Microspheres

The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin.

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

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