Abstract: The current work aims to investigate the sudden drop of dissolution with respect to higher compression pressure and hardness of tablet with a good and comparative less significant disintegration time and to understand an affect of pressure on drug with respect to compression behavior on dissolution and other properties. Where Cefuroxime Axetil was compressed at different pressure in form of pellets and tablets using hydraulic press and compression machine respectively, and characterized to understand any physical and chemical change using X-ray powder diffraction, differential scanning calorimetry, Dissolution and Scanning Electron microscopy. Scanning electron microscopy studies of pellets revealed that the change in surface morphology from opaque to translucent clear with increase in breaking force, these different pressure compressed pellets were subjected to uniform reduction of particle size. The similarity factor f2 values of drug release profile were comparably same. The breaking force and pellet hardness had indicated a very firm intrinsic binding force exist with Cefuroxime Axetil, study had investigated the decrease in-vitro dissolution is marked by the compact binding property of individual particles of Cefuroxime Axetil between the excipient due to the increase in compression force.
Abstract: Abstract: In screening of new antibiotics, several actinomycetes were isolated from soil samples. Crowded plate technique was used for the isolation of actinomycetes. The morphological and cultural characterization of A-4 strain was performed. In medium formulation study for A-4 and A-4 mutant, various carbon and nitrogen sources were tested for maximum antibiotic production using zone of inhibition and packed cell volume (%) as parameters. Various fermentation conditions like pH, temperature and DO2 were also optimized for the maximal production of antibiotic from both A-4 and A-4 mutant. All medium formulation as well as bioprocess parameters for A-4 and A-4 mutant strains was compared. Some actinomycetes strains, showed promising antimicrobial scores against different strains of bacteria and fungi. From the six strains selected, one strain designated as A-4 showed maximum antimicrobial property against gram positive and gram negative strains as well as various fungi. Morphological and cultural studies showed that A-4 is belongs to actinomycete genus.. The strain A-4 and A-4 mutant was found to be having better antimicrobial activity in comparison with other soil isolates of actinomycetes.
Abstract: Abstract: Purpose: Two critical factors that govern the stability of pharmaceutical formulations in the tropics are humidity and temperature. This study was carried out to investigate the effect of moisture sorption at two different storage conditions on Cefaclor dry powder for oral suspension and predict the effect of moisture interaction on the reconstituted formulations Method: Cefaclor dry powder for suspension formulation was taken as a model formulation for this study. Different formulations were manufactured and placed in twelve amber coloured glass bottles for each test condition. One set of bottles was sealed by heat induction technique under vacuum to ensure the integrity of the seal while the other set was without a seal but had a child-resistant cap. Both types of bottles were stored in humidity chambers at 30°C/65%RH or 40°C/75%RH. Weight changes were monitored on a dynamic moisture balance over a period of 3 months. Results: The results were recorded in terms of moisture content, colour, and excipient interaction and their effect on product appearance. The data were analyzed using Students t-test and one way analysis of variance (ANOVA), and differences were considered statistically significant at P < 0.05. Conclusions: The study revealed that the product with enhanced packaging and also contained nonwater soluble colourants were more protected against the deleterious effects of moisture and temperature. The findings provide an insight into a possible approach for formulating moisture-sensitive pharmaceutical products, especially dry powder preparations for use in the tropics.
Abstract: A simple and accurate Reverse Phase High-Performance Liquid Chromatography (RPHPLC) method was developed to determine Etamsylate in injection formulations. The drug was chromatographed on a reversed phase C-18 column. Eluents were monitored at a wavelength of 220 nm using a mixture (40:60) Methanol: Buffer (phosphate buffer). Solution concentrations were measured on weight basis to avoid the use of an internal standard. The method was spastically validated for linearity, accuracy, precision and selectivity. Due to its simplicity and accuracy, method will be useful for routine quality control analysis.
Abstract: Leflunomide is a DMARD (Disease –Modifying Antirheumatic Drug) . It is used for the treatment of rheumatoid arthritis. It exhibits four polymorphic forms I, II, III, IV.
Leflunomide is a drug with a limited water solubility(21 mg/L). In the present study , a more soluble polymorph (form II) was formulated using a less soluble polymorph (form I)and then the rate of dissolution of the tablets of both were compared.
There was a significant difference between the melting point of both the forms. Form I and form II was 166.5°C, 83°C respectively. The crystals of form II polymorph were characterized by IR, DSC and XRPD. IR 3355 cm-1 is a characteristic band of form II.
Comparison of solubility of form I and form II was done by UV spectrophotometer. A significant increase in the solubility of leflunomide form II was seen. The absorbance solution of form II in water (10µg/ml) was found to be 0.686 at λmax 258 nm whereas absorbance of form II was found to be 0.390.There was increase in solubility of form II by 75%.
Aqueous film coated tablets of both the forms were made by using same processing parameters and compared for the rate of dissolution. The form II tablets show a significant improvement in terms of drug release and solubility. Thus, form II polymorph and tablets were successfully developed and it was concluded that form II is a desirable form for use in pharmaceutical compositions in terms of solubility and dissolution rate.
Notes: We are working on the Single Crystallographic studies.
