Solubility Studies and Validation of Lovastatin using High Performance Liquid Chromatography Method

This study aimed to determine the solubility of lovastatin (LV) in different oil, surfactant, and co-surfactant using the high-performance liquid chromatography method. LV was solubility studies in different vehicle. The different vehicle used almond oil, sunflower oil, oleic acid, olive oil, soybean oil, and corn oil, isoprophyl myristate, myoglyol, tween 80, tween 20, and cremophor R.H. 40, propylene glycol, and PEG 400. Each of them was added lovastatin until saturated. The mixtures were mixing, sonicating, putting in the water bath and standing for 24 hours, then centrifugated. Each of the aliquot 2 µL diluted with acetonitrile and determination of concentration lovastatin using HPLC, with detector ultraviolet at 237 nm. Before determinate LV validated, and curve calibration at range 2-16 µg/mL was made. This study using the HPLC method with detector UV 237 nm, Agilent C 18 (4.6 x 150 mm 5 µ) column, and acetonitrile: water (70:30 v/v) as mobile phase. Calibration curve of lovastatin at the range 2-16 µg/mL with linear regression 0.999. Accuracy and precision showed that. Lovastatin has high soluble in oleic acid, tween 80, and PEG 400.

Development and Validation of Tramadol Hydrochloride in Bulk and Pharmaceutical Dosage Form by Ultraviolet Spectroscopy

A simple, rapid, accurate, precise and economic spectrophotometric technique for estimation of tramadol hydrochloride in 0.1N HCl have been developed. Tramadol Hydrochloride exhibit absorbance most 270nm when 0.1N HCl used as solvent proportion, so absorbance was once measured at the identical wavelengths for the determination of Tramadol Hydrochloride obeys Beer Lambert’s law in the concentration range of 20-180µg/ml. The present study describes development and validation of simple and economic UV spectrophotometric method for the estimation of Tramadol Hydrochloride in bulk and injection dosage form using absorbance maxima method. Solubility studies indicated that a Tramadol Hydrochloride shows better solubility in proposed diluents i.e., 0.1N HCl solution the ? max of Tramadol Hydrochloride was found to be 270nm. Because of cost effective and minimal maintenance, the present UV spectrophotometric methods can be preferred at small scale industries as compared to other reported methods.

Formulation and Evaluation of Liquisolid Compacts of BCS Class II Drug Ketoprofen

Aims: The main objective of the current research work is to develop liquisolid compacts of BCS Class II drug ketoprofen with an intention to enhance the solubility of drug by applying liquisolid technique. Place and Duration of Study: Smriti College of Pharmaceutical Education between June 2018 June 2019. Methodology: Initially liquid medication was obtained by dissolving drug in suitable solvent. Saturation solubility studies were performed in various hydrophilic non-volatile solvents to select the solvent showing highest solubility for drug. This liquid medication was admixed with calculated amounts of carrier material (Avicel PH 102) and coating material (Cab-O-Sil) using Spireas mathematical model in order to obtain liquisolid formulations. Further, this powder mass of liquisolid system was compressed to form Ketoprofen liquisolid compact formulations ranging from TK1 to TK9. They were further subjected to post compression evaluation tests such as weight variation, hardness, friability, content uniformity, disintegration and in vitro dissolution studies. Results: Based on the solubility studies, PEG 400 was selected as solvent for ketoprofen drug. Rheological properties for the prepared liquisolid powder system were performed for all the formulations and they showed acceptable flow properties. The results obtained for the post compression evaluation tests of all the prepared liquisolid compacts were present within the acceptable limits. The disintegration time observed for all formulations were within 5 minutes. The results of in vitro release of all the liquisolid compacts showed enhanced release rates compared to that of directly compressed tablet. Lquisolid compact formulation TK7 showed maximum release of 97.62% of drug within 12 minutes in pH 7.4 phosphate buffer which was much higher when compared to that of directly compressed tablet. The SEM and PXRD studies for TK7 revealed conversion of crystalline to molecularly dispersed form of drug in the obtained liquisolid formulation. DSC and FTIR studies also revealed that there was no presence of any significant interaction between drug and excipients involved in the formulation. Conclusion: Finally, it could be concluded that Liquisolid technique was successful in enhancing the solubility and further dissolution profile of BCS Class II drug Ketoprofen.

Development of the Binary and Ternary Atorvastatin Solid Dispersions: In Vitro and In Vivo Investigations

The object of this study was to prepare binary and ternary solid dispersions of atorvastatin (ATR) by the melting method using PEGs and poloxamer 188 (P188) as the carriers, singly and in combination with each other. Dissolution behavior, solubility studies, X-ray diffractometry, differential scanning calorimetry, and Fourier transform infrared spectroscopy were studied. Furthermore, antihyperlipidemic activities of formulations were compared to each other by serum lipid analyses in hyperlipidemic rats. Based on the results, the highest dissolution efficiency ( DE 30 = 83 % ) was obtained by binary systems consisted of ATR and P188. Also, no additional improvement was observed in dissolution properties of ternary solid dispersion formulations. Solubility studies showed enhancement of ATR phase solubility in water and a buffer solution containing P188 or PEG 10000. Furthermore, saturated solubility of ATR in the buffer solution improved more than twofold in the optimized ternary dispersion system. No crystalline changes occurred in PEG-based formulations; meanwhile, partial amorphization happened in the ATR-P188 combination. Finally, the in vivo study in hyperlipidemic rats exhibited a rapid decrease in the lipid profile of all formulations compared to ATR (after 7 days). Moreover, reduction of serum triglycerides and total cholesterol on the 14th day in the ATR group ( p value < 0.01) was less than solid dispersion or physical mixing preparations ( p value < 0.001). These findings proved the appropriate influence of using PEG and P188 in solid dispersion systems for the improvement of the therapeutic efficiency of ATR.

Growth, optical, spectral, thermal and mechanical investigations of organic NLO crystal cis-2, 6-bis(4-chlorophenyl)-3, 3-dimethylpiperidin-4-one

The single crystal of cis-2,6-bis(4-chlorophenyl)-3,3-dimethylpiperidin-4-one (4C3DMPO) has been grown using a slow evaporation technique. 4C3DMPO is a non-centrosymmetric crystal which crystallizes in the orthorhombic system with space group Pna21. Benzene is used as a solvent for the crystal growth based on solubility studies. The mechanical studies, using microhardness methods, have also been carried out. The compound is characterised using UV, FT-IR and NMR spectral studies. Furthermore, the thermal stability of the crystal is established by TG/DTA. The nonlinear optical studies (SHG) of the crystal have been determined using the Kurtz and Perry powder technique and the activity observed is 2.5 times greater than that of KDP.

Simultaneous improvement of ketoconazole solubility, antifungal and antibiofilm activity by multicomponent complexation

Background: A novel multicomponent complex (MC) of ketoconazole (KET) with β-cyclodextrin (β-CD) and N-acetylcysteine (NAC) was developed with the purpose of improving the solubility as well as the antifungal and antibiofilm activity of KET against Candida albicans. Results & methodology: The interactions among the components were studied using nuclear magnetic resonance, thermal analysis, powder x-ray diffraction, infrared spectroscopy and scanning electron microscopy. Phase-solubility studies demonstrated a considerable increase in the solubility of the MC. An enhancement in antibiofilm and antifungal activity of MC was determined against C. albicans by XTT assay and microbiological studies. Conclusion: This MC, with improvements in the drug pharmaceutical performance, might have an important potential in the development of new pharmaceutical formulations of KET.