PREPARATION AND EVALUATION OF TRANSNASAL MICROEMULSION OF VIGABATRIN

Introduction: The objective of this study was to develop novel transnasal microemulsion containing Vigabatrin for treatment of epilepsy. Method: Oleic acid was selected as oil while Tween 80 and ethanol were selected as surfactant and co-surfactant respectively based on solubility results. Optimized ratio of Tween 80 and Ethanol was selected after developing pseudoternary phase diagrams for different ratio and microemulsions were prepared. The prepared microemulsions were evaluated for globule size, viscosity, pH, and % transmittance. Ex-vivo diffusion study for optimized microemulsion was performed through goat nasal mucosa where in diffusion flux and permeability coefficients were determined. Pharmacological performance was screened in rats by electrically induced seizures. Result: It was found that op mized microemulsion was stable and transparent. Pharmacological evaluation indicated significant reduction (p<0.001) of seizures in rats treated with optimized formula on in comparison to rats treated with oral Vigabatrin microemulsion and nasal Vigabatrin solu on which suggested Vigabatrin transnasal delivery system as an effective alternate therapy for treatment of epilepsy. Conclusion: Transnasal microemulsion of Vigabatrin was successfully formulated using Tween 80 as surfactant and ethanol as co-surfactant in the formula on to treat epilepsy. Key words: Epilepsy; Transnasal Microemulsion; Vigabatrin

PREPARATION AND EVALUATION OF TRANSNASAL MICROEMULSION OF VIGABATRIN

Introduction: The objective of this study was to develop novel transnasal microemulsion containing Vigabatrin for treatment of epilepsy. Method: Oleic acid was selected as oil while Tween 80 and ethanol were selected as surfactant and co-surfactant respectively based on solubility results. Optimized ratio of Tween 80 and Ethanol was selected after developing pseudoternary phase diagrams for different ratio and microemulsions were prepared. The prepared microemulsions were evaluated for globule size, viscosity, pH, and % transmittance. Ex-vivo diffusion study for optimized microemulsion was performed through goat nasal mucosa where in diffusion flux and permeability coefficients were determined. Pharmacological performance was screened in rats by electrically induced seizures. Result: It was found that op mized microemulsion was stable and transparent. Pharmacological evaluation indicated significant reduction (p<0.001) of seizures in rats treated with optimized formula on in comparison to rats treated with oral Vigabatrin microemulsion and nasal Vigabatrin solu on which suggested Vigabatrin transnasal delivery system as an effective alternate therapy for treatment of epilepsy. Conclusion: Transnasal microemulsion of Vigabatrin was successfully formulated using Tween 80 as surfactant and ethanol as co-surfactant in the formula on to treat epilepsy. Key words: Epilepsy; Transnasal Microemulsion; Vigabatrin

Comparison between nalbuphine propofol and dexmedetomidine propofol for laryngeal mask airway insertion

Aims and Objectives: The aim of the present study was to compare the laryngeal mask airway (LMA) insertion conditions using either nalbuphine - propofol or dexmedetomidine - propofol. Materials and Methods: Sixty female patients aged 25–35 years posted for interval tubal ligation were randomly allocated in two groups of 30 each. Group N received intravenous injection nalbuphine 0.2 mg/kg over 5 min, and Group D received injection dexmedetomidine 1 μg/kg over 5 min. Later, all the patients were induced with injection propofol 2 mg/kg and 90 s after induction, classic LMA of number 3 was inserted in all the patients. LMA insertion conditions were assessed using various parameters. Heart rate, mean arterial pressure, respiratory rate, and SpO2were recorded before induction and at 1, 3, 5, and 10 min after LMA insertion. Incidence and duration of apnea were also recorded. Observations and Results: Demographic data were comparable in both the groups. LMA insertion conditions were comparable in both the groups (P = 0.15), and both the groups had excellent LMA insertion conditions. The apnea duration was slightly more in dexmedetomidine group (140 s) as against nalbuphine group (120 s). The reduction in heart rate was more in Group D and the difference was statistically significant at 1 and 3 min after induction (P < 0.001). Conclusion: Nalbuphine combined with propofol provides similar conditions of LMA insertion as that of dexmedetomidine - propofol combination with advantage of better maintenance of hemodynamic stability

Nanosuspension Technology for Delivery of Poorly Soluble Drugs and Its Applications: A Review

Now a days, many drug candidates are water insoluble hence they show a limited drug release and poor bioavailability. It is difficult to formulate these drugs by conventional dosage form. Nanosuspension technology is a promising approach to solve the problems of poorly soluble and less bioavailable drugs. Nanosuspension is a very finely colloidal, biphasic, and uniformly dispersed solid drug particles in a suitable aqueous vehicle, having a particle size below 1 μm stabilized by suitable surface active agents and polymers. Nanosuspensions are prepared by various suitable techniques for drug delivery applications. Due to reduced particle size at the nano scale, surface area, saturation solubility, dissolution velocity and bioavailability of BCS class II and class IV drugs are increased sufficiently. Nanosuspension is suitable to administration via various routes such as oral, intravenous, topical, pulmonary and ocular delivery systems. Nanosuspension can be also used for targeting purpose in various diseases such as cancer, HIV and production of sustained and extended release products by choosing suitable polymers. Production and manufacturing are not complicated, easy to scale up. Top down and bottom technologies are used for the preparation of nanosuspensions. It includes methods such as high-pressure homogenization, by milling media method, precipitation method, probe sonication, dry-co-grinding, supercritical fluid method, and lipid emulsion method. Formulation consists of stabilizers, surfactant, and solvents. Nanosuspension can be stored in the form of dry powder using spray drying, freeze drying techniques. This review describes the advantages, various methods of preparation, formulation consideration and characterization of nanosuspension.  </jats:p

UHPLC-UV Method for Simultaneous Determination of Perindopril Arginine and Indapamide Hemihydrate in Combined Dosage Form: A Stability-Indicating Assay Method

Perindopril arginine and Indapamide hemihydrate in combination were proven to have a synergistic antihypertensive impact when compared with the use of each component alone. Therefore, a new Ultra-High Performance Liquid Chromatography coupled with Ultraviolet detector (UHPLC-UV) method has been developed and subsequently validated for simultaneous determination of the anti-hypertensive combination of Perindopril arginine and Indapamide hemihydrate. The separation of Perindopril arginine and Indapamide hemihydrate was achieved using a BEH C18 (1.7 μm, 2.1 × 50 mm) analytical column (Waters® Acquity UPLC) and a mobile phase composed of 0.01% v/v formic acid in water adjusted to pH 4 with acetic acid and acetonitrile (40:60 v/v). The method was able to separate Perindopril arginine and Indapamide hemihydrate within less than 4.5 min with high accuracy, precision, resolution, and sensitivity. The content of Perindopril arginine and Indapamide hemihydrate present in the dosage form Coversyl Plus® (5000 µg of Perindopril arginine/1250 µg of Indapamide hemihydrate) was determined in triplicate to give a concentration of 4991 µg and 1247 µg, respectively, from the manufacturer’s stated amounts with Relative Standard Deviation (%RSD) of ±0.63% for Perindopril arginine and ±0.84% for Indapamide hemihydrate. Moreover, the degradation products of the combination were elucidated by UHPLC-Quadrupole Time of Flight-Mass spectrometry (UHPLC-QToF-MS) under acidic, basic, and thermal conditions. In conclusion, the developed UHPLC-UV method was sensitive, rapid, and precise. Furthermore, forced degradation studies were performed and the degradants were identified by UHPLC-Electro-Spray Ionization-QToF (UHPLC-ESI-QToF)