Solubilizing Systems for Parenteral Formulation Development—Small Molecules

2007 ◽  
pp. 309-339 ◽  
Author(s):  
JAMES E. KIPP
Keyword(s):  
Small Molecules ◽  
Formulation Development ◽  
Parenteral Formulation

scholarly journals FORMULATION OPTIMIZATION AND CHARACTERIZATION OF AQUEOUS INJECTION CONTAINING POORLY SOLUBLE DRUG USING MIXED HYDROTROPIC SOLUBILIZATION

2021 ◽  
pp. 100-107
Author(s):  
NEELKUMAR K. DARAJI ◽  
VIPUL P. PATEL ◽  
VINODKUMAR D. RAMANI
Keyword(s):  
Quality Control ◽  
Mefenamic Acid ◽  
Peak Plasma ◽  
Aqueous Solubility ◽  
Cost Effective ◽  
Stability Study ◽  
Formulation Development ◽  
Parenteral Formulation ◽  
Cost Effective Treatment ◽  
Hydrotropic Agent

Objective: Mefenamic acid (MFA) is an NSAID that exhibits anti-inflammatory analgesic and antipyretic activity. Peak plasma levels are attained in 2-4 h and the elimination half-life approximates 2 h, repetitive administration of tablets for 3-5 times a day is desired. It is supplied only in the form of tablets for oral administration. In acute conditions drug administered parenterally could give rapid relief from severe symptoms like pain. Thus, formulation of injectable formulation of MFA could be better alternative compared to conventional tablet dosage form. The low aqueous solubility of MFA precludes its use in parenteral formulation development. Methods: In this work attempt were made to enhance the aqueous solubility of mefenamic acid using mixed solvency technique. For that different hydrotropic agents such as Urea, Sodium acetate, sodium benzoate, sodium citrate and their blends were evaluated. Optimal concentration of hydrotropic agent in blend was determined using D-optimal mixture experimental design. The optimized bled was used to develop the aqueous injection of mefenamic acid. The developed injection was subjected for various quality control tests and stability of developed formulation was also evaluated. Results: The aqueous solubility in optimized blend of hydrotropic agent batches (U: SA: SB: SC, 4:4:23:9 %w/v) showed 835.71-fold compared to MFA solubility in distilled water. The quality control tests for parenteral formulation and accelerated stability study were found to be within prescribed limits and stable. Conclusion: The inadequate solubility of MFA was overcome, and aqueous injection was successfully developed which can be serve as cost effective treatment in various indications.

scholarly journals Formulation, development and evaluation of injectable formulation of Aspirin

2013 ◽  
Vol 3 (1) ◽  
pp. 2
Author(s):  
Rakesh P. Patel ◽  
Kaushal P. Patel ◽  
Kushal A. Modi ◽  
Chirayu J. Pathak
Keyword(s):  
Aqueous Solubility ◽  
Solvent System ◽  
Water Soluble ◽  
Stability Studies ◽  
Formulation Development ◽  
Parenteral Formulation ◽  
Polyethylene Glycol 400 ◽  
Accelerated Stability ◽  
Aqueous Solvent ◽  
Water Soluble Drugs

The objective of this study was to develop and manufacture a stable parenteral formulation for Aspirin, a non steroidal anti-inflammatory agent. The solubility and stability of the drug was determined. Solubility studies suggested that Aspirin exhibited poor aqueous solubility but showed appreciable solubility in non-aqueous solvents. Based on the preformulation studies, a lyophilized parenteral formulation containing 25 mg/mL of Aspirin was prepared in a solvent system containing of 80% v/v water and 20% v/v polyethylene glycol-400 (PEG-400). Rubber closures, filter membranes, and liquid transfer tubing were selected on the basis of compatibility studies. The formulation was subjected to accelerated stability studies. After reconstitution with sterile water for injection, Aspirin injection was stable for a period of 8 hr at 2°C to 8°C. Accelerated stability studies suggested that the lyophilized product should be kept at controlled room temperature for longterm storage. The proposed non-aqueous solvent concentration used, are known to safe hence, toxicities/safety related issues may not raise. The proposed techniques would be economical, convenient and safe. Thus, the study opens the chances of preparing lyophilized formulation of poorly-water soluble drugs.

Bexarotene nanocrystal—Oral and parenteral formulation development, characterization and pharmacokinetic evaluation

2014 ◽  
Vol 87 (1) ◽  
pp. 160-169 ◽  
Author(s):  
Lijiang Chen ◽  
Yongjie Wang ◽  
Jiaozhen Zhang ◽  
Leilei Hao ◽  
Hejian Guo ◽  
...  
Keyword(s):  
Formulation Development ◽  
Parenteral Formulation ◽  
Pharmacokinetic Evaluation

Gap junctions in the prothoracic glands of the tobacco hornworm, Manduca sexta

1992 ◽  
Vol 50 (1) ◽  
pp. 706-707
Author(s):  
Ji-da Dai ◽  
M. Joseph Costello ◽  
Lawrence I. Gilbert
Keyword(s):  
Gap Junctions ◽  
Small Molecules ◽  
Manduca Sexta ◽  
Freeze Fracture ◽  
Cell Communication ◽  
Cellular Level ◽  
Thin Sections ◽  
Prothoracic Glands ◽  
Polyhydroxylated Steroids ◽  
Stimulation Of

Insect molting and metamorphosis are elicited by a class of polyhydroxylated steroids, ecdysteroids, that originate in the prothoracic glands (PGs). Prothoracicotropic hormone stimulation of steroidogenesis by the PGs at the cellular level involves both calcium and cAMP. Cell-to-cell communication mediated by gap junctions may play a key role in regulating signal transduction by controlling the transmission of small molecules and ions between adjacent cells. This is the first report of gap junctions in the PGs, the evidence obtained by means of SEM, thin sections and freeze-fracture replicas.

Fusion and Fission Processes in Exocytosis: Possible Roles for Synexin and Osmotic Lysis in the Two Events

1980 ◽  
Vol 38 ◽  
pp. 594-597
Author(s):  
H.B. Pollard ◽  
C.E. Creutz ◽  
C.J. Pazoles ◽  
J.H. Scott
Keyword(s):  
Small Molecules ◽  
Chromaffin Cells ◽  
Adrenal Glands ◽  
General Concept ◽  
Extracellular Calcium ◽  
Large Protein ◽  
Granule Membrane ◽  
Osmotic Lysis ◽  
Per Se ◽  
Chemical Evidence

Exocytosis is a general concept describing secretion of enzymes, hormones and transmitters that are otherwise sequestered in intracellular granules. Chemical evidence for this concept was first gathered from studies on chromaffin cells in perfused adrenal glands, in which it was found that granule contents, including both large protein and small molecules such as adrenaline and ATP, were released together while the granule membrane was retained in the cell. A number of exhaustive reviews of this early work have been published and are summarized in Reference 1. The critical experiments demonstrating the importance of extracellular calcium for exocytosis per se were also first performed in this system (2,3), further indicating the substantial service given by chromaffin cells to those interested in secretory phenomena over the years.

Sign in / Sign up

Export Citation Format

Share Document