Background:The osmotic drug delivery systems suitable for oral administration typically consist of a compressed tablet core that is coated with a semipermeable membrane that has an orifice drilled on it by means of a laser beam or mechanical drill. Ketorolac is a nonsteroidal agent with powerful analgesic. Oral bioavailability of ketorolac was reported to be 90% with very low hepatic first-pass elimination; the biological half-life of 4-6 hours requires frequent administration to maintain the therapeutic effect.Aim:The aim of the current study was to design a controlled porosity osmotic pump (CPOP)based drug delivery system for controlled release of an NSAID agent, ketorolac tromethamine, which is expected to improve patient compliance due to reduced frequency; it also eliminates the need for complicated and expensive laser drilling and maintain continuous therapeutic concentration.Design:The CPOP was designed containing pore-forming water-soluble additives in the coating membrane, which after coming in contact with water, dissolve, resulting in an in situ formation of a micro porous structure.Materials and Methods:The effect of different formulation variables, namely level of pore former (PVP), plasticizer (dibutyl phthalate) in the membrane, and membrane weight gain were studied.Results and Conclusion:Drug release was inversely proportional to the membrane weight but directly related to the initial concentration of pore former (PVP) in the membrane. Drug release was independent of pH and agitational intensity, but dependent on the osmotic pressure of the release media. Based on the in vitro dissolution profile, formulation F3C1 (containing 0.5 g PVP and 1 g dibutyl phthalate in coating membrane) exhibited Peppas kinetic with Fickian diffusion-controlled release mechanism with a drug release of 93.67% in 12 hours and hence it was selected as optimized formulation. SEM studies showed the formation of pores in the membrane. The formulations were stable after 3 months of accelerated stability studies. CPOP was designed for effective administration of drugs for prolonged period of time.
The present study indicates that AE of Moringa oleifera prevents dexamethasone-induced insulin resistance in peripheral tissues.
Objective: Alcoholic extract of the bark of Moringa oleifera Lam. (MO), (Moringaceae), has been experimentally evaluated previously for its insulin sensitizing potentials. In the quest to explore the possibility of the class of phytochemical(s) responsible for this experimental claim, the alcoholic extract was fractionated and evaluated for insulin sensitizing effect in rat model for insulin resistance. Methods: Alcoholic extract of MO was fractionated into, non-polar [petroleum ether (PEF)], moderately non-polar [ethyl acetate (EAF)] and polar [aqueous (AQF)] fractions. The fractions obtained were investigated for their insulin sensitizing properties in dexamethasone induced insulin resistance in rats. The bioactive fraction was analysed by spectroscopy for further characterization of phytochemical(s) present. Results: Acute treatment for 4 h with dexamethasone (1 mg/kg i.p.) in rats led to the development of impaired oral glucose tolerance. Treatment with pioglitazone and EAF abolished dexamethasone induced oral glucose intolerance (OGT). Dexamethasone (1 mg/kg s.c., once daily for 11 d) administration led to the development of insulin resistance, characterised by fasting hyperglycemia, hyperinsulinemia, hypertriglyceridemia, impaired OGT and increased HOMA IR index. Treatments with EAF (140 mg/kg p.o.) and pioglitazone [PIO (10 mg/kg p.o.)] significantly prevented dexamethasone induced metabolic changes. Similarly, treatment with AQF (95 mg/kg p.o.) also significantly prevented metabolic changes due to dexamethasone except impaired OGT. In contrast PEF (15 mg/kg p.o.) failed to prevent these metabolic changes except hypertriglyceridemia. Conclusion: The present study reveals that triterpenoid and the polyphenols (procyanidin) class of phytochemicals detected in EAF of alcoholic extract of MO bark may be responsible for the prevention of dexamethasoneinduced insulin resistance in rats.Key words: Dexamethasone, Insulin resistance, Moringa oleifera, Oral glucose tolerance test, Serum triglyceride. Key message: This is the first report which confirms and speculates the presence of polyphenols and triterpenoids respectively in EAF of MO which may be responsible for preventing the development of insulin resistance in rat model.
The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.
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