scholarly journals Selection of a Water-Soluble Salt Form of a Preclinical Candidate, IIIM-290: Multiwell-Plate Salt Screening and Characterization

ACS Omega ◽  
2018 ◽  
Vol 3 (7) ◽  
pp. 8365-8377 ◽  
Author(s):  
Vikas Kumar ◽  
Sandip B. Bharate ◽  
Ram A. Vishwakarma ◽  
Sonali S. Bharate
Keyword(s):  
Water Soluble ◽  
Soluble Salt ◽  
Salt Form ◽  
Salt Screening ◽  
Selection Of

Solid Dispersions: A Review

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Sumant Saini ◽  
Yashwant .
Keyword(s):  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Absolute Minimum ◽  
Technology Transfers ◽  
Molecular Arrangement ◽  
Water Soluble Drugs ◽  
Carrier Solvent ◽  
Preparation Techniques ◽  
Selection Of

Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. This article reviews the various preparation techniques for solid dispersion and compiles some of the recent technology transfers. The different types of solid dispersions based on the molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier, solvent and methods of physicochemical characterization, along with an insight into the molecular arrangement of drugs in solid dispersions are also discussed. In this review, it is intended to discuss the recent advances related on the area of solid dispersions.

The Influence of Hard Water on 2,4-D Formulations for the Control of Dandelion

2020 ◽  
pp. 1-31
Author(s):  
Geoffrey P. Schortgen ◽  
Aaron J. Patton
Keyword(s):  
Cropping Systems ◽  
Hard Water ◽  
Water Soluble ◽  
Soluble Salt ◽  
Synthetic Auxin ◽  
Auxin Herbicides ◽  
Acid Herbicides

The herbicide 2,4-D is used in a variety of cropping systems, especially in grasses since it is a selective postemergence broadleaf herbicide. However, the most common formulation (2,4-D dimethylamine) is antagonized when mixed in hard water. The objective of this research was to determine which formulations of 2,4-D or premixes of various formulations of synthetic auxin herbicides are subject to hard water antagonism. Formulations surveyed for hard water antagonism in the first experiment included 2,4-D dimethylamine, 2,4-D diethanolamine, 2,4-D monomethylamine, 2,4-D isopropylamine salt, 2,4-D choline salt, 2,4-D isooctyl ester, and 2,4-D ethylhexyl ester. Synthetic auxin formulation types in the second experiment included water-soluble, emulsifiable concentrates and emulsion-in-water. All formulations were mixed with both soft and hard water (600 mg CaCO3 L-1) and applied to dandelions to determine if antagonism occurred in hard water. Water-soluble (amine and choline) 2,4-D formulations were antagonized by hard water, but water-insoluble (ester) 2,4-D formulations were not antagonized. Similar results were found by formulation type with water-soluble synthetic auxin premixes antagonized but emulsifiable concentrates not antagonized. Further, water-soluble salt formulations were not antagonized when formulated in premixes with other synthetic auxin herbicides as an emulsion-in-water. This research demonstrates that all 2,4-D water-soluble formulations and water-soluble premixes with phenoxycarboxylic acid herbicides are subject to hard water antagonism. Formulations of 2,4-D containing emulsifying agents protect against antagonism by the water-insoluble nature of ingredients in their formulation.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals A systematic series of synthetic chromophoric substrates for aspartic proteinases

1986 ◽  
Vol 237 (3) ◽  
pp. 899-906 ◽  
Author(s):  
B M Dunn ◽  
M Jimenez ◽  
B F Parten ◽  
M J Valler ◽  
C E Rolph ◽  
...  
Keyword(s):  
Structure Function ◽  
Peptide Bond ◽  
Water Soluble ◽  
Animal Origin ◽  
Aspartic Proteinases ◽  
Peptide Substrates ◽  
Representative Selection ◽  
Micro Organisms ◽  
Hydrolysis Of ◽  
Selection Of

The hydrolysis of the chromogenic peptide Pro-Thr-Glu-Phe-Phe(4-NO2)-Arg-Leu at the Phe-Phe(4-NO2) bond by nine aspartic proteinases of animal origin and seven enzymes from micro-organisms is described [Phe(4-NO2) is p-nitro-L-phenylalanine]. A further series of six peptides was synthesized in which the residue in the P3 position was systematically varied from hydrophobic to hydrophilic. The Phe-Phe(4-NO2) bond was established as the only peptide bond cleaved, and kinetic constants were obtained for the hydrolysis of these peptide substrates by a representative selection of aspartic proteinases of animal and microbial origin. The value of these water-soluble substrates for structure-function investigations is discussed.

Innovative Strategies for Lipid-Based Drug Delivery

2018 ◽  
pp. 60-84 ◽  
Author(s):  
Navneet Sharma ◽  
Sabna Kotta ◽  
Mohd Aleem ◽  
Shubham Singh ◽  
Rakesh Kumar Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Absorption ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Absorption Process ◽  
Innovative Strategies ◽  
The Poor ◽  
Water Soluble Drugs ◽  
Selection Of

In the last decade, there has been a mounting concern in lipid-based formulations to deliver water-soluble drugs. Lipid-based drug delivery systems are one of the budding and promising technologies designed to tackle the poor bioavailability problems. This chapter stresses the different mechanisms of lipophilic drug absorption along with its advantages and limitations. It points out the different mechanisms of how lipid-based excipients and the different formulations interact with the absorption process. This review provides a comprehensive summary about the lipid formulation classification scheme (LFCS), a guide for the selection of appropriate formulation and commonly used excipients for lipid-based formulations, along with the important factors to be considered in formulation design and excipient selection. This review also focuses on the formulation of solid lipid-based formulations, important evaluation aspects, and commercial formulations available for the purpose.

Polymeric precipitation inhibitor as an effective trigger to convert supersaturated into supersaturable state in vivo

2019 ◽  
Vol 10 (9) ◽  
pp. 599-608
Author(s):  
Dilpreet Singh ◽  
Manmeet Singh ◽  
Abhay Tharmatt ◽  
Ashok K Tiwary ◽  
Neena Bedi
Keyword(s):  
Oral Absorption ◽  
Extended Period ◽  
Pharmaceutical Formulations ◽  
Water Soluble ◽  
Delayed Response ◽  
Supersaturated State ◽  
Drug Precipitation ◽  
Precipitation Inhibitor ◽  
Selection Of

The supersaturated state of the drug in vivo is thermodynamically unstable resulting in a delayed response and reduced efficacy. The use of polymeric precipitation inhibitor (PPI) has been demonstrated as an effective trigger for the conversion of supersaturated state to supersaturable state for improving solubilization, thermodynamic maintenance of drug concentration and oral absorption of poorly water-soluble compounds. PPI retards drug precipitation and provides a kinetically stabilized supersaturation state for an extended period in gastric and intestinal fluids. However, the selection of appropriate PPI and understanding its mechanism is a challenge for formulating a stable pharmaceutical formulation. The present review is aimed at understanding the intricacies of selecting PPIs and their applications in pharmaceutical formulations.

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