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

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.

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Formulation, development and evaluation of injectable formulation of Aspirin

Drugs and Therapy Studies ◽

10.4081/dts.2013.e2 ◽

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.

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