Physicochemical Properties Of Active Pharmaceutical Ingredients Research Articles

Amorphous Solid Dispersions: Implication of Method of Preparation and Physicochemical Properties of API and Excipients.

The present study investigated the effect of different polymers and manufacturing methods (hot melt extrusion, HME, and spray drying, SD) on the solid state, stability and pharmaceutical performance of amorphous solid dispersions. In the present manuscript, a combination of different binary amorphous solid dispersions containing 20% and 30% of drug loadings were prepared using SD and HME. The developed solid-state properties of the dispersions were evaluated using small- and wide-angle X-ray scattering (WAXS) and modulated differential scanning calorimetry (mDSC). The molecular interaction between the active pharmaceutical ingredients (APIs) and polymers were investigated via infrared (IR) and Raman spectroscopy. The in vitro release profile of the solid dispersions was also evaluated to compare the rate and extend of drug dissolution as a function of method of preparation. Thereafter, the effect of accelerated stability conditions on the physicochemical properties of the solid dispersions were also evaluated. The results demonstrated higher stability of Soluplus® (SOL) polymer-based solid dispersions as compared to hydroxypropyl methylcellulose (HPMC)-based solid dispersions. Moreover, the stability of the solid dispersions was found to be higher in the case of API having high glass transition temperature (Tg) and demonstrated higher interaction with the polymeric groups. Interestingly, the stability of the melt-extruded dispersions was found to be slightly higher as compared to the SD formulations. However, the down-processing of melt-extruded strands plays critical role in inducing the API crystal nuclei formation. In summary, the findings strongly indicate that the particulate properties significantly influence the performance of the product.

The effect of polymorphism on active pharmaceutical ingredients: A review

Active pharmaceutical ingredients (API) are the main components in the production process of pharmaceutical products. If the API has a good quality, then it will lead to good pharmaceutical products. API consists of more than one different crystal form which, then forms a polymorph through the process of polymorphism. Until now, API polymorphism is still a big challenge in the pharmaceutical industry. That is because the nature of polymorphism is difficult to predict. One of them is by crystallizing molecules in one or many crystalline forms or combining with other molecules to form stable co-crystal. This process will lead to several polymorph forms of one certain API. Sometimes, these forms will have characteristics that differ one to another. Each polymorph has different mechanical, physical, thermal, and chemical properties that will affect the solubility, dissolution, bioavailability, stability, bioequivalence, and manufacturing of the API. Therefore to know the nature of an API, it is necessary to characterize the polymorphic form of the API before. If the form is not incompatible with the formulation, it can cause a failure in the production process. This review will discuss the effect of polymorphism on the physicochemical properties of API. It is hoped that this review can become the basis for improving the stability and effectiveness of pharmaceutical products.

Development of gel composition and technology based on pyrimidine substance

Background: This work was conducted in the framework of quality by design project involving the production of a pharmaceutical gel. Preliminary work included the identification of the quality target product profiles from historical values for previously laboratory batches, which were used to construct a D-optimal experimental design. Fungal disease of mycoses has long been known, since the days of antiquity. Our research gel high pharmacological effect (antifungal) in comparison with the drugs “Flucytosine” and “Fucis”. Aims and Objectives: The purpose of this study is to develop the optimal composition and rational gel technology under the conventional name “Antiсandid” on the basis of the substance piperidinylethanone with an antifungal effect. Materials and Methods: Thermogravimetric analysis and rotational viscometry, which affect the process of the formation of carbopol, were taken. Based on the physicochemical properties and technological properties of the gel, an optimal solvent system is selected that corresponds to the maximum solubility of the drug substances and ensures polymer swelling. At the same time, the materials dimexide (DMSO), propylene glycol (PG), carbol-floor, and triethanol were taken into account, which improve the process of solubility and gelling. Results: The results were obtained, which, when the active substance is administered in the dissolved state, is the most therapeutic effect on the gel base. At the same time, active pharmaceutical ingredients (APIs) were dissolved in different solvents with gradual heating. The ratio of solvents DMSO-PG-water (1:4:1) at which the developed dosage form will be more structured, stable, and thixotropic is established. Conclusion: Fungal skin diseases are one of the most frequently discussed problems in various dermatological forums and in the pages of scientific journals. The relevance of this topic is determined by the high prevalence of this pathology, which, according to the literature, accounts for 37-42% of all skin diseases. The results of the studies on the study of the microbiological, physicochemical properties of APIs, and carbopol Ultrez 20 for the development of optimal composition are taken into account. It was found that the gel model with an active substance content of 3% is more effective and has high antifungal activity.

Co‐crystallization: An approach to improve the performance characteristics of active pharmaceutical ingredients

Co‐crystal chemistry has recently attracted supramolecular scientists. Co‐crystals are comprising of hydrogen boding assembly between different molecules. Many issues related to performance characteristics of an active pharmaceutical ingredient (API) can be resolved using co‐crystallization approach. Proper understanding of crystal structure of an API is required for successful formation of co‐crystals with the selected co‐former. This review article focus on explanation about co‐crystals, intellectual property rights, their advantages and limitations. Co‐crystallization can be achieved using different methods like co‐grinding slurry based, solvent evaporation method, etc. Methods of co‐crystallization are simple and increase the purity of the final product. Co‐crystallization can be applied to the drugs prescribed in combination therapy. Stoichiometric composition of different drugs used in combination therapy can be co‐crystallize to form one solid state form. Physicochemical properties of APIs such as solubility and stability can be improved using co‐crystallization approach. With due regards co‐crystallization should be used with caution because of some issues during manufacturing of final product. Key words: Chiral switch, crystal engineering, hydrogen bonding, intellectual property rights, polymorphism

Estudo das propriedades físico-químicas da glibenclamida e excipientes que influem sobre resultados do ensaio de dissolução para medicamento similar e genérico

Some active pharmaceutical ingredients (API) might present polymorphism at any stage of the industry production process. In caseit is not characterized and specified, a different polymorph might be erroneously used during the manufacturing procedure. Polymorphisms cause some variations in the physicochemical properties of APIs, especially in solubility. Therapeutic inefficacy was detected in some glyburide drug products, and the occurrence of polymorphs might be one of the possible reasons. This study analyzed five drug products and five APIs., The characteristic pharmaceutical equivalence tests were used for analyzing the drug products. The techniques employed to evaluate the APIs showed no differences in polymorphism, no significant changes in the physicochemical properties or in the intrinsic dissolution rate. However, the dissolution profiles of the drug products, mainly between two similar products A and B, showed significant differences in the f2 factor values, being 20 and 42, respectively, indicating that these values were related to the occurrence of different excipients, such as mannitol.