Volume 5

April-June 2013

Research Articles

Zaheer Abbas, Aditya N, Swamy N G N

Chloroquine Phosphate (CP), indicated for the treatment of infections caused by some sensitive strains of malarial protozoa is not a drug candidate feasible to be administered via oral route in unconsciousness state and nausea with vomiting symptoms. Parenteral administration is associated with numerous toxic effects. This obviates an alternative dosage form. Rectal delivery of this drug is a good substitute to parenteral administration. Conventional dosage forms like suppositories can cause patient discomfort and may reach end of the colon; causing the drug to undergo first-pass effect. In the present work, Rectal Chloroquine– Poloxamer gel systems composed of Poloxamer and bioadhesive polymers such as Polyvinyl pyrrolidone K30, Carbopol 934P and Polycarbophil were developed and evaluated. The physicochemical properties such as physical appearance, clarity, gelation temperature, gel strength, rheological studies and mucoadhesive force of various formulations were investigated. The gelation temperature for the formulations varied between 32.4 – 36.5°C, the mucoadhesive force was found to be in the range of 37.34 – 321.05 dynes/cm2 x 102 and rheological investigation revealed distinct shear thinning behaviour. Polycarbophil and Carbopol 934 P showed higher mucoadhesive strength, retardation in drug release from Pluronic F – 127 gels and significantly reduced the gelation temperature by about 6°C. The drug release was found to be matrix diffusion controlled and the release mechanism was found to be Fickian. These results prove that Pluronic F – 127 liquid suppositories containing either Carbopol 934 P or Polycarbophil are suitable alternative formulations to the conventional suppositories for being physically safe, convenient, and effective rectal dosage forms to deliver anti-malarial drugs.

Keywords: Rectal Drug Delivery, Malaria, Liquid Suppositories, Chloroquine Phosphate, Gelation Temperature, Mucoadhesive Force, Thermosensitive In Situ Gels.

V J Gadade, Dhanwantari Shivarkar, V B Suryawanshi

The objective of present work was to formulate and evaluate once a daily sustained release matrix tablet of Tramadol hydrochloride using Rice bran wax. Matrices were prepared by melt granulation technique using Rice bran wax as a release retardant. Pre-compression results revealed that granules of all formulations possessed satisfactory flow-properties and compressibility. All the tablet formulations showed acceptable Pharmacopoeial limit specifications for weight variation, drug content, hardness, thickness and friability. The in vitro release of drug from the formulations was studied in pH 1.2 acidic buffers and pH 6.8 phosphate buffer, and it was found that formulation F6 (30% of wax) exhibited good drug release pattern to provide sufficient concentration for achieving satisfactory therapeutic value for extended period of time. The formulation was optimized on the basis of acceptable tablet properties and in-vitro drug release. The release of Tramadol hydrochloride from the tablets was diffusion controlled and the release mechanism was non-Fickian. Stability studies (40±2°C/75±5% RH) for 3 months indicated that no appreciable difference was observed for the drug content and drug release.

Keywords: Tramadol Hydrochloride, Matrix Tablet, Rice Bran Wax, Sustained Release.

Dhaval Patel, S Mohan, Hiren Khatri, Hitesh Chaudhary

The present study was addressed to formulate and evaluate LOLA-loaded poly (DLlactic-co-glycolic acid) (PLGA) nanoparticles (NPs) prepared by the double emulsion solvent evaporation method and characterizes their properties. LOrnithine-L-Aspartate (LOLA) has been used in the treatment of liver diseases like Hepatic encephalopathy, having shorter biological half-life of 40 minute, thus it is a good candidate for the formulation of sustained release dosage form. The experiments were performed based on various variables; effect of poly-vinylalcohol (PVA) concentration, amount of LOLA, amount of PLGA, the volume ratio of the inner water phase and the intermediate phase, and effect of sonication time. The prepared NPs were evaluated based on their physicochemical characteristics like, particle size, zeta-potential, scanning electron microscopy (SEM). Optimized batch was produced particle size 323 nm with respect to negative zeta potential. SEM study reveals that particles were spherical in shaped and had a smooth surface. Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) study did not show any interaction between drug and polymer. In-vitro release studies were found to be zero order and followed higuchi model. In-vitro release of optimized formulation had shown 36.67% of drug release after 5 days providing sustain release of drug. It is therefore concluded that PLGA nanoparticles are capable of delivering LOLA over prolonged period achieving a sustained delivery of LOLA, thus making it a potential candidate for hepatic disease.

Keywords: L-ornithine-L-aspartate, PLGA, Nanoparticles, In-vitro Release.


Kotta Kranthi Kumar, Guru Prakash, R Nagakishore

Bilayer tablets were prepared by using combination of immediate release rabeprazole sodium along with sustained release ketorolac tromethamine. The FTIR study conducted using a combination of drugs along with excipients and polymers revealed that combination can be safely prepared. Rabeprazole sodium was formulated as immediate release layer using sodium starch glycolate, croscarmellose sodium, crospovidone as super disintegrants. The optimized rabeprazole sodium immediate release (IR 9) with highest in-vitro release was selected. Ketorolac tromethamine was formulated as sustained release layer using different grades of HPMC polymers and evaluated for in-vitro release studies. The optimized sustained release layer (F5) was selected. Bilayer tablets were prepared by double compression of optimized ketorolac tromethamine sustained release layer and rabeprazole sodium immediate release layer. All the physical parameters were in acceptable limit of pharmacopoeial specifications. Hence bilayer tablets of ketorolac tromethamine and rabeprazole sodium could be used to improve patient compliance towards the effective management of post operative pain, osteoarthritis without side effect of gastric irritation.

Keywords: Ketorolac Tromethamine, Rabeprazole Sodium, Bilayer Tablets, Immediate Release Layer, Sustained Release Layer.

Short Communications

Naren Dhiren, Catherine Leo, Sharan Saravanan, Muthu Ganesh

Gastrointestinal disorders are very common among adults; the contaminated food and water are the main sources of the organisms which can cause gastric problems. Due to the intake of antibiotic drug against the pathogen causing gastrointestinal disorders, the bacterial strains are becoming resistant to the particular. To overcome this, citrus fruit peel extract can be used to treat these disorders. The citrus fruit peel extract used Citrus paradisi Macfad (Grapefruit) Citrus sinensis (Orange), Citrus limon (Lemon), and Citrus aurantifolia (Lime) against the gastrointestinal pathogens and lesser side effects than the synthetic drugs used against gastrointestinal pathogens.

Keywords: Citrus Peel, Resistance and Prevention, Gastrointestinal Disorders.

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