Formulation Development and Evaluation of Aqueous Injection of Poorly Soluble Drug Made by Novel Application of Mixed Solvency Concept

It is commonly recognized in the pharmaceutical industry that on average more than 40% of newly discovered drug candidates are poorly water-soluble. The objective of present research is to explore the application of mixed solvency technique in the injection formulation of poorly soluble drugs and to reduce concentration of individual solubilizers (used for solubility enhancement) to minimize the toxic effects of solubilizers. In the present work poorly soluble drugs Ofloxacin are selected as model drugs. Ofloxacin is an antibiotic drug tried to formulate the aqueous injection by the use of various physiologically compatible solubilizing agent like Lignocaine Hydrochloride, Niacinamide, Sodium benzoate, Sodium citrate, PEG 400, PEG 4000, PVP 40000, Ethanol, and Propylene Glycol. For expected synergistic enhancement effect on solubility of these poorly soluble drugs various blends of solubilizers shall be tried to decrease the amounts of Solubilizer employed for a desired solubility enhancement ratio. The study further opens the chances of preparing dry powders for injection of drug which are not stable in aqueous solution, ready to use injection. Key word- Mixed solvency solubilization, Ofloxacin, solubility enhancement, synergistic enhancement effect

Formulation Development and Evaluation of Aqueous Injection of Poorly Soluble Drug Made by Novel Application of Mixed Solvency Concept

It is commonly recognized in the pharmaceutical industry that on average more than 40% of newly discovered drug candidates are poorly water-soluble. The objective of present research is to explore the application of mixed solvency technique in the injection formulation of poorly soluble drugs and to reduce concentration of individual solubilizers (used for solubility enhancement) to minimize the toxic effects of solubilizers. In the present work poorly soluble drugs Ofloxacin are selected as model drugs. Ofloxacin is an antibiotic drug tried to formulate the aqueous injection by the use of various physiologically compatible solubilizing agent like Lignocaine Hydrochloride, Niacinamide, Sodium benzoate, Sodium citrate, PEG 400, PEG 4000, PVP 40000, Ethanol, and Propylene Glycol. For expected synergistic enhancement effect on solubility of these poorly soluble drugs various blends of solubilizers shall be tried to decrease the amounts of Solubilizer employed for a desired solubility enhancement ratio. The study further opens the chances of preparing dry powders for injection of drug which are not stable in aqueous solution, ready to use injection. Key word- Mixed solvency solubilization, Ofloxacin, solubility enhancement, synergistic enhancement effect

Preparation and Evaluation of Spray Dried Mucoadhesive Microspheres of Metoclopramide Hydrochloride for Nasal Delivery

&#x0D; There is increasing interest in drug delivery through nasal mucosa because of the ability of drug particles to cross membrane due to their particle size in nano or submicron range. The present study was aimed to prepare and evaluate microspheres of metoclopramide hydrochloride (MH) by using HPMC E4M and Carbopol 934P. Microspheres were prepared using spray drying method and particle size was found in the range of 1.62 µm. Drug loaded microspheres of HPMC E4M and Carbopol 934P and combination of HPMC E4M: Carbopol 934P were evaluated for various parameters for optimized batch were drug entrapment (61.73%), mucoadhesive strength (1959.30 g/cms2), and in-vitro diffusion studies (95.61%). Optimized batch also evaluated for SEM, TEM, X-ray diffraction study. Amorphous form of optimized batch was confirmed by X-ray diffraction study. Particles were spherical and discrete confirmed by SEM study. Particle size range was confirmed by TEM. The drug release of optimized batch was carried out by using sheep nasal membrane. Histopathological studies have shown no toxicity to the sheep nasal membrane and hence optimized formulation was found to be safe. The optimized formulation was found to be stable in the accelerated stability studies. It was found that drug entrapment was in the order of HPMC E4M&gt; Carbopol934P &gt; Carbopol 934P: HPMC E4M, mucoadhesive strength Carbopol 934P: HPMC E4M &gt; Carbopol 934P &gt; HPMC E4M, In-vitro drug release Carbopol 934P: HPMC E4M &gt; HPMC E4M &gt; Carbopol 934P. In conclusion, these studies indicate the feasibility and superior pharmacokinetic profile of the metoclopramide nasal system.&#x0D;  </jats:p