Tablet Formulation and Enhancement of Aqueous Solubility of Efavirenz by Solvent Evaporation Co-Crystal Technique (original) (raw)
The aim of the work was to improve the dissolution properties of the poorly soluble drug, Efaverinz by the liquisolid compaction technique. The study demonstrated with confidence that the liquisolid technique is promising approach for improvement of solubility of poorly soluble drugs. In vitro drug release of Efaverinz compacts showed increase in dissolution rate of Efaverinz. So PEG 400, PG, Tween 80 could be economic substitute as dissolution enhancing agent. Stability studies showed that there were no significant changes in physical and chemical properties of formulation F5 after 2 months. Propylene glycol in 1:0.25 ratios (F5) was showing best release. F5 was compared with marketed and prepared conventional formulation and result shows better dissolution profile.
Co-Crystallization: A Novel Approach to Enhance the Dissolution of Poorly Soluble Drugs
2019
Approximately 40% of newly synthesized drugs are not able to enter market due to biopharmaceutical issues like poor solubility and poor permeability. Most number of drugs marketed is administered orally hence solubility enhancement plays a major role. There are different techniques to upgrade the dissolvability of inefficiently soluble drugs including pro-drug approach, salt formation, particle size reduction, complexation and solid dispersion. Out of all other techniques, salt formation is one of majorly used technique to improve physicochemical characteristics of drugs which includes formation of ionic bond. But nowadays development of co-crystals has evolved as a suitable technique towards improving the dissolvability and bioavailability of ineffectively soluble drugs that includes non-ionic bond formation. In this paper a brief and accurate precis of pharmaceutical co-crystals is stated with specific spotlight on co-crystal preparation methodologies, mechanism of co-crystal form...
New Trends in the Co-crystallization of Active Pharmaceutical Ingredients
Journal of Applied Pharmaceutical Science
Pharmaceutical materials science being a fundamental branch that continuously provides important insights, theories, and technologies to formulation sciences. The recent advances in this area have brought the possibility to produce pharmaceutical materials by design. In particular, the formation of co-crystals, i.e. crystalline molecular complexes of two-or more neutral molecules, represents a potential route to achieve pharmaceutical materials with improved properties of interest, including dissolution rate and stability under conditions of high relative humidity. Co-crystals consists of API and a stoichiometric amount of a pharmaceutically acceptable co-crystal former. Pharmaceutical co-crystals are nonionic supramolecular complexes and can be used to address physical property issues such as solubility, stability and bioavailability in pharmaceutical development without changing the chemical composition of the API. These can be constructed through several types of interaction, inc...
American Journal of PharmTech Research
Co-crystallization is an emerging approach for enhancing physicochemical properties like solubility, stability, bioavailability of poorly soluble drugs of BCS class II in pharmaceutical development without changing the chemical composition and considered better alternatives to optimize drug properties. Co-crystal is a crystalline entity consists of API and a stoichiometric amount of a pharmaceutically acceptable co-crystal former formed by intermolecular interactions like Hydrogen bonding, π-π stacking and Van der Waals forces. In this article, an overview of pharmaceutical cocrystals will be presented along with the intermolecular interactions (Chemistry of Co-crystals), methods of their preparations, characterization of co-crystals altered physicochemical properties. Furthermore, this article also gives a brief explanation about newer trends in co-crystals with application of co-crystals in medicines and industries.
Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications
Advanced Pharmaceutical Bulletin, 2020
Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administrati...
International Journal of Applied Pharmaceutics, 2023
Over the past few decades, co-crystal Drug Delivery System (DDS) has attracted interest due to their potential to increase the solubility, stability, and bioavailability of medications that aren't sufficiently soluble. In this study, we factualized to develop a co-crystal chemical delivery system utilizing an experimental model. We utilized caffeine and succinic acid as model chemicals and prepared co-crystals utilizing different methods, including solvent evaporation, grinding, and spray drying. The co-crystals have been characterized utilizing X-ray powder diffraction, Fouriertransform infrared spectroscopy, and differential scanning calorimetry. The solubility and dissolution rate of the co-crystals has been evaluated in simulated digestive and intestinal juices. The outcomes showed that when compared to co-crystals made utilizing the solvent evaporation and spray drying procedures, those organized utilizing the grinding approach exhibited the maximum solubility and dissolution rate. This study underlines the potential of co-crystals as a workable method for enhancing the administration of pharmaceuticals that are not adequately soluble and provides a helpful experimental paradigm for the development of co-crystal chemical delivery systems.
Indian Journal of Pharmaceutical Sciences, 2009
Yadav, et al.: Co-crystals to Modify Physicochemical Properties of API's Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical form and formulation tends to exhibit the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for the enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co-crystals. The physicochemical properties of the active pharmaceutical ingredients and the bulk material properties can be modified, whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of cocrystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies. The intellectual property implications of creating co-crystals are also highly relevant.
Iranian Journal of Pharmaceutical Research
Background: Efavirenz nanosuspensions (EZ-NSs) were developed by the wet milling method as the most promising top-down nanosizing technique. Different process and formulation parameters were studied and optimized to produce appropriate EZ-NS in suitable conditions to enhance drug dissolution. Methods: In the preliminary studies, various polymeric stabilizers, including Pluronic F68, sodium carboxymethylcellulose (CMC), hydroxypropyl methylcellulose (HPMC), and polyvinyl alcohol (PVA), as well as different sizes and weight of milling beads were used to prepare NSs. The effect of sodium lauryl sulfate (SLS) concentration on the NS properties was also evaluated. The influence of other formulation and process parameters, including polymer concentration, milling speed, and milling time, on the particle size and distribution of NSs were investigated using Box-Behnken design. The optimized freeze-dried nanosuspension was characterized by redispersibility, physicochemical properties, and st...
Pharmaceutics
Despite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efavirenz (EFV) as a drug model. EFV solubility was assessed in water, Labrafac Lipophile and medium chain triglycerides oil (MCT oil). EFV turned out to be more soluble in the two latter dissolving media (solubility > 250 mg/mL); hence, given its affordability, MCT oil was used for LNC formulation. LNC were prepared using a low-energy method named phase inversion, and following a design of experiments process. This one resulted in polynomial models that predicted LNC particle size, polydispersity index and zeta potential that were, respectively, around 50 nm, below 0.2 and below −33 mV, for the optimized formulations. Once synthesized, we were able to achieve an encapsulation efficacy of...