STUDIES IN OXCARBAZEPINE MICROSPHERES EMPLOYING PLACKETT AND BURMAN DESIGN

Objective: The present work was aimed to screen material and processing parameters affecting encapsulation efficiency and drug release from microspheres. Methods: Oxcarbazepine loaded microspheres were prepared employing multiple emulsion solvent evaporation technique. Ratio of chitosan to ethyl cellulose, ratio of drug to polymer, stirring speed, ratio of dichloromethane to methanol, amount of Span 80 and the volume of aqueous phase were selected as independent variables in the Plackett and Burman design. The microspheres were characterized for percentage yield, percentage encapsulation efficiency, particle size distribution and in vitro drug release. Results: The critical material and processing parameters affecting encapsulation efficiency were chitosan to ethyl cellulose ratio, volume of water, stirring speed and drug to polymer ratio. Initial burst release was affected by volume of water, temperature, dichloromethane to methanol ratio, amount of Span 80 and drug to polymer ratio. FTIR study showed compatibility of the drug with excipients. Conclusion: The outcome of the study shall be used to calculate risk priority number (RPN) and for devising suitable control strategies for the critical factors at industry

OPTIMIZATION OF BACOSIDE A LOADED SNEDDS USING D-OPTIMAL MIXTURE DESIGN FOR ENHANCEMENT INSOLUBILITY AND BIOAVAILABILITY

Objective: The objective of present study is to enhance solubility and bioavailability of poorly soluble bacoside A present in Bacopa monnieri extract using self nano emulsifying drug delivery system (SNEDDS) for the treatment of Alzheimer's disease.Methods: Solubility of the drug was assessed in various oils (edible as well as synthetic oil), surfactant and co-surfactant by saturation solubility study. Pseudo-ternary phase diagram was used to obtain appropriate concentration ranges of components include oil, surfactant and co-surfactant.Results: From the result of saturated solubility study and phase diagram, oleic acid, tween 20 and ethanol was selected as oil, surfactant and co-surfactant. The D-Optimal mixture design was used to optimize the formulation on the basis of solubility of drug and dilution potential. In vitro dissolution, study showed 89% of drug release from optimized SNEDDS formulation compared to untreated drug extract with 24% of drug release in 60 min. Ex vivo diffusion study showed more than 90% of drug diffused from optimized SNEDDS formulation compared to pure extract.Conclusion: In a nutshell, the developed SNEDDS formulation using the design of experimentation approach held great potential as a possible alternative to traditional oral formulations of poorly soluble Bacoside A to improve solubility and bioavailability

NEWER OPHTHALMIC IN SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE: OPTIMIZATION USING BOX BEHNKEN STATISTICAL DESIGN

Objective: The present research work aims at describing the formulation and evaluation of the ocular delivery system of moxifloxacin hydrochloride (MH) based on the concept of ion sensitive in situ gelations. Methods: In situ gel was prepared by a hot method using 0.6% of gelrite, 0.25% hydroxypropylmethylcellulose (HPMC K4M) and 0.023% tamarind gum as bioadhesive polymers for sustained drug release. Optimization was done by Box Behnken Design with different concentration of gelrite (X1), HPMC K4M (X2) and tamarind gum (X3) as independent variables. In situ gel was optimized based on mucoadhesion index (Y1), Gel strength (Y2) and in vitro drug release (Y3). Influence of the quantitative variable on the dependent variable was predicted by a polynomial equation. Results: Infrared spectroscopy excluded any interaction between drug and excipients. The selected independent variables significantly influenced the responses and were able to sustain the drug release. The prepared gel with a pH of 6.8 to 7.4 exhibited non-newtonian flow with no ocular irritation. The formulation remained stable with no change in pH and viscosity after 30 d of stability study. Conclusion: Thus, moxifloxacin hydrochloride (MH) in situ gel is a viable alternative to a conventional delivery system with the properties of sustained drug release, prolonged ocular retention, and improved corneal penetration

Evaluation of changes in liver function test in first, second and third trimester of normal pregnancy

Background: Understanding of physiological adaptations of normal pregnancy remains a major goal of obstetrics, and without such knowledge, it is almost impossible to understand disease processes that can threaten women during pregnancy. Aim of this study is to evaluate changes in serum liver function tests in normal pregnant women in first, second and third trimester.Methods: A hospital based cross sectional in vitro study conducted at Civil Hospital, Ahmedabad (India). A study consists of 150 pregnant women and 50 matched control. Among the 150 pregnant women, 50 were in first trimester, 50 were in second trimester and 50 were in third trimester. Serum sample was taken and assessed for routine liver function tests.Results: Serum total and direct bilirubin concentrations were significantly lower in second and third trimester. Serum ALT and AST activity was slightly but significantly increased in third trimester. Serum ALP activity was significantly higher in second and third trimester. ALP activity increases as pregnancy advances. Serum GGT values were significantly lowers in third trimester. No significant change in serum total proteins concentration, but serum albumin concentration was significantly lower and serum globulin concentration was significantly higher in all three trimester. Serum albumin/globulin ratio was significantly reduced in second and third trimester.Conclusion: Such changes in in liver function tests during normal pregnancy can be misinterpreted as pathological and can also unmask or worsen preexisting disease. So the identification and understanding of these physiological changes in pregnancy is important for the diagnosis of liver diseases during pregnancy

Rationalized Approach for Formulation and Optimization of Ebastine Microemulsion Using Design Expert for Solubility Enhancement

Ebastine is available as an oral antihistamine formula for allergic disorders such as tablets and syrup. Oral ebastine causes unfavorable effects on heart like QT prolongation, severe gastric distress, decreased tear production, resulting in dryness of the ocular surface, which exacerbates ocular discomfort and increasing susceptibility of eye to irritation. To avoid systemic side effects and ocular discomfort, topical ocular therapy could prove to be superior to systemic therapy in treating ocular allergies. Hence, topical formulation was developed to achieve onsite exposure of ebastine for ocular allergies. Moreover, conjunctiva is more accessible to hydrophilic molecules than lipophilic molecules. This creates challenge for a lipophilic molecule such as ebastine for topical ocular development. Successful dissolution of ebastine in o/w microemulsion allows its use in more convenient soluble form. Initially, solubility of drug in various oils, surfactant and cosurfactant was determined, followed by pseudo-ternary phase diagram to find microemulsion area. The D-optimal mixture design was employed for optimization of formulation. The optimized microemulsion formulation was characterized for its transparency, drug content, droplet size, zeta potential, viscosity, isotonicity, osmolarity and surface tension etc. The optimum physicochemical properties were observed to be eye-fitting. Carboxy methyl cellulose and sodium hyaluronate were used as gelling agents at different concentrations to increase residential time at the site of action. In vitro drug release study revealed that ebastine release from microemulsion gel in a sustained manner up to 24 hrs. for the purpose of providing prolonged therapy for ocular allergy. Hence, prepared microemulsion had great potential as an alternative to customary oral formulations of poorly soluble drug. Keywords:  Ebastine, Microemulsion, D-optimal mixture design, Solubilit

Enhancement of Solubility of Artemisinin and Curcumin by Co-Solvency Approach for Application in Parenteral Drug Delivery System

The aim of present study was to enhance solubility of poorly soluble antimalarial drugs, Artemisinin and Curcumin by adopting  Co-solvency approach and to develop parenteral aqueous injectable solution. Solubility enhancement of both drugs was achieved using co-solvency approach. The parenteral injection was prepared by using a ternary co-solvent system which comprised of benzyl alcohol, PEG 400 and tween 80 (as surfactant). Solubility of Artemisinin and Curcumin was found to be higher in benzyl alcohol and PEG 400. Co-solvent system comprising of  benzyl alcohol, PEG 400 and tween 80 in volume fraction of 0.3, 0.9 and 0.2 respectively showed the minimum required solubility of Artemisinin (90 mg per ml) and Curcumin (180 mg per ml). The parenteral injectable formulation was characterized for pH, clarity, viscosity, osmolarity and sterility and the stated parameters were found in acceptable range.  In-vitro erythrocyte toxicity study showed that intravenous administration of optimized formulation will be safe. In-vitro antimalarial assay indicated that efficacy of artemisinin and curcumin parenteral formulation was greater than quinine and combination of Artemether and Lumefantrine. Stability study of the optimized batch showed no change in physical and chemical characteristics. Based on study, one can conclude that Artemisinin and Curcumin can be successfully formulated as parenteral injectable formulation by co-solvency approach for the effective treatment of malarial infectio

गुजरात के सागर तट की समुद्री शैवाल विविधता

गुजरात के सागर तट की समुद्री शैवाल विविधत

Razvoj metformin hidroklorida za izravnu kompresiju metodom sušenja raspršivanjem

Metformin hydrochloride exhibits poor compressibility during compaction, often resulting in weak and unacceptable tablets with a high tendency to cap. The purpose of this study was to develop directly compressible metformin hydrochloride by the spray drying technique in the presence of polymer. Metformin hydrochloride was dissolved in solutions containing a polymer, namely polyvinylpyrrolidone (PVP K30), in various concentrations ranging from 0-3 % m/V. These solutions were employed for spray-drying. Spray-dried drug was evaluated for yield, flow property and compressibility profile. Metformin hydrochloride spray-dried in the presence of 2 % PVP K30 showed an excellent flow property and compressibility profile. From the calculated Heckel’s parameter (Py = 2.086), it was demonstrated that the treated drug showed better particle arrangement in the initial compression stage. Kawakita analysis revealed better packability of the treated drug compared to the untreated drug. Differential scanning calorimetry and Fourier transform infrared spectroscopy experiments showed that the spray-dried drug did not undergo any chemical modifications. Tablets made from the spray-dried drug (90 %, m/m) were evaluated for crushing strength, friability and disintegration time and the results were found satisfactory.Metformin hidroklorid se teško komprimira zbog čega nastaju slabe tablete neodgovarajuće kvalitete s velikom tendencijom kalanja. Cilj ovog rada je prirediti metformin hidroklorid za izravnu kompresiju metodom sušenja raspršivanjem u prisutnosti polimera. Metformin hidroklorid je otopljen uz dodatak različitih količina (03 % m/V) polivinilpirolidona (PVP K30). Dobivene otopine sušene su raspršivanjem, a tako pripravljenom metformin hidrokloridu određivano je iskorištenje, tečnost i kompresibilnost. Metformin hidroklorid pripravljen u prisutnosti 2 % PVP K30 ima izvrsnu tečnost i kompresibilnost. Izračunati Heckelovi parametri (Py = 2,086) pokazuju da tako obrađeni metformin hidroklorid tvori veće čestice na početku kompresije. Analiza po Kawakiti ukazuje na to da se obrađeni lijek bolje preša od neobrađenog. Diferencijalna pretražna kalorimetrija (DSC) i Fourierova transformirana infracrvena spektroskopija (FTIR) pokazuju da sušenje raspršivanjem nije uzrokovalo nikakve kemijske promjene. Iz obrađenog metformina izrađene su tablete (90 % m/m) sa zadovoljavajućom lomljivošću, drobivošću i vremenom dezintegracije