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Enhanced Pharmacokinetics of Omeprazole when Formulated as Gastroretentive Microspheres along with Piperine
(Asian Pacific Journal of Tropical Disease, 2014-01-01) Boddupalli, Bindu Madhavi; Anisetti, Ravinder Nath; Ramani, Ramalingam; Malothu, Nagulu
Objective: To investigate the formulation of gastroretentive microspheres of omeprazole along with piperine and estimate the pharmacokinetic parameters in comparison with omeprazole alone.
Methods: In our present investigation, gastroretentive microspheres of omeprazole were prepared with the inclusion of piperine. Pharmacokinetic parameters like Cmax, Tmax and area under curve were estimated by administering the prepared microspheres to rabbits and the results were
compared with omeprazole alone.
Results: There was a significant increase in area under curve from 3.441+-1.093 mg·h/mL to 14.422 +_0.708 mg·h/mL along with an increase in Cmax.
Conclusions: This clearly shows the increased absorption and decreased metabolism of omeprazole when administered along with piperine as gastroretentive microspheres.
Enhanced Transdermal Drug Penetration of Curcumin via Ethosomes
(Universiti Sains Malaysia, 2013) Madhavi, Boddupalli Bindu; Vennela, Kallem Siri; Masana, Prasad; Madipoju, Bhavana
The objective of the present research work is to overcome the barriers of poor oral bioavailability through transdermal drug delivery (TDD). Among the available transdermal systems, ethosomes are the promising ones with increased penetration effect due to the combination of lipid bilayer and ethanol in its structure. Curcumin has poor oral bioavailability and can be given as transdermal ethosomes to enhance bioavailability along with local action of antiinflammation. Curcumin ethosomes were prepared and optimised for lipid and ethanol concentrations based on entrapment efficiency, vesicular size and drug penetration. Drug penetration capability of the ethosomes was
compared with aqueous, ethanolic and liposomal solutions. The optimised ethosomes were compared for the cumulative drug penetration (74.2±0.236%) into skin with aqueous (5.61±0.263%), ethanolic (62.31±0.263%), liposomal (59.3±0.44%) and ethosomal curcumin-β-cyclodextrin complex (78.01±0.22). It was found that the penetration was enhanced and maximum in ethosomes
incorporated with curcumin-β-cyclodextrin complex because of combined effects of ethanol, lipid bilayer along with increased dissolution of curcumin with β-cyclodextrin complex. This formulation will be suitable to treat local skin inflammations with enhanced penetration via ethosomes incorporated with curcumin-β-cyclodextrin complex.
In-vitro Anti-denaturation and Antibacterial Activities of Zizyphus oenoplia
(Scholars Research Library, 2010-07-28) Ramalingam, R.; Madhavi, B. Bindu; Nath, A. Ravinder; Duganath, N.; Sri, E. Udaya; Banji, David
Zizyphus oenoplia mill belongs to the family Rhamnaceae. The fruits of the plant are used as stomach-ache pills and root bark decoction is used to promote the healing of fresh wounds. Plant has shown the presence of cyclopeptide alkaloids. Aerial parts of the plant were reported to have
anti-inflammatory and anticholinergic activities. Bark and leaves of the plant were reported for antibacterial activity. No biological and antibacterial activities were reported on root part of Zizyphus oenoplia. The aim of the study was to investigate the Anti-denaturation and antibacteriial activities for various extracts of the Zizyphus oenoplia. Root part of Zizyphus oenoplia was extracted with ethyl acetate, 90% ethanol and water using soxhlet apparatus. The solvents were evaporated under reduced pressure below 400C using rotary evaporator to obtain dry extracts. These crude extracts were subjected to investigation for anti-denaturation study and
antibacterial study by using a method designed by William’s et al and agar ditch diffusion method respectively. Phytochemical analysis revealed the presence of carbohydrates, alkaloids, phenolic compounds, tannins and saponins. All the extracts of Zizyphus oenoplia protected Bovine Serum Albumin (BSA) from denaturation more than 97% at 1µg/ml concentration. Only ethanolic extract showed antibacterial activity against Staphylococus aureus.
Free Radical Scavenging and Antiepileptic Activity of Leucas Lanata
(Journal of pharmacy research, 2013-03-01) Ramalingam, Ramani; Nath, Anisetti Ravinder; Madhavi, Boddupalli Bindu; Nagulu, Malothu; Balasubramaniam, Arumugam
Objective:Oxidative stress was found to be the underlying mechanism in many disorders especially in neurodegenerative disorders like epilepsy. The main aim of the investigation was to evaluate invitro free radical scavenging potential and invivo antiepileptic activity of selected fraction of Leucas lanata.
Methods Ethanolic extract of L. lanata was taken for its phytochemical screening, invitro free radical scavenging, cytotoxic studies, fractionation with ethyl acetate and its HPTLC studies. Further the fraction was evaluated for invivo acute toxicity studies and antiepileptic activity in mice.
Results:After the estimation of 64.412 ± 8.44 mgGAE/g of phenolic and 63.723 ± 8.01 mgRE/g of flavonoids contents, invitro free radical scavenging studies of ethanolic extract of the plant revealed its almost equal potential as quercetin. HPTLC studies of ethyl acetate fraction of extract revealed the presence of 3 unknown flavonoids with Rf values of 0.03, 0.48 and 0.93. In animal studies there was a decrease in the duration of hind limb extension like 7.8 ± 0.1 s, 7.4 ± 0.2 s and 7.1 ± 0.2 s linearly with doses. In forced swim test animals were found to be active without any decreased locomotory activity indicated by more immobilized time in diazepam treatment (233.33 ± 5.03 s) and less immobilized time with the treatment of fraction (161.66 ± 5.686 s). From the studies of malondialdehyde estimation, there was a comparative decrease in the content which was not linear with dose.
Conclusion:From the results of invitro and invivo studies it can be concluded that, flavonoid and phenolic rich ethyl acetate fraction of L. lanata can be used to treat epilepsy without any induction of depression.
Dissolution Enhancement of Efavirenz by Solid Dispersion and PEGylation Techniques
(International Journal of Pharmaceutical Investigation, 2011-01) Madhavi, B. Bindu; Kusum, B.; Chatanya, CH. Krishna; Madhu, M. Naga; Harsha, V. Sri; Banji, David
Efavirenz is the preferred nonnucleotide reverse transcriptase inhibitor for first-line antiretroviral treatment
in many countries. It is orally active and is specific for human immunodeficiency virus type 1. Its effectiveness can be attributed to its long half-life, which is 52–76 h after multiple doses. The drug is having poor water solubility. The formulation of poorly soluble drug for oral delivery will be one of the biggest challenges for formulation scientists in the research field. Among the available approaches, the solid dispersion technique has often proved to be the most commonly used method in improving dissolution and bioavailability of the drugs because of its simplicity and economy in preparation and evaluation. Materials and Methods: Solid dispersions were prepared by solvent evaporation and physical mixture methods by using polyethylene glycol as the hydrophilic carrier and PEGylated product was also prepared. The prepared products were evaluated for various parameters, such as polymer interaction, saturation solubility study, and drug release studies. The drug release data were analyzed by fitting it into various kinetic models. Results: There is an improvement in the dissolution from 16% to 70% with solid dispersion technology. Higuchi model was found to be the
best fit model. Conclusion: Solid dispersion is the simple, efficient, and economic method to improve the dissolution of the poorly water-soluble drugs.
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