Volume 5

October-December 2013

Review Articles

Pushpendra Bhushan Mishra, Vimal Arora, Harpal Singh, Nandini Vashistha, Saurav Kumar

Sustained drug delivery systems are designed to deliver drug, at predetermined rates for predefined periods of time, and have been used to overcome the shortcoming of conventional drug formulations. And in the recent approach for the sustained drug delivery has been the development of microspheres using albumin as a polymer to sustain the release of the drug. This review deals with the methods used and the results obtained by the use of albumin (bovine serum albumin and egg albumin) as a polymer in the formulation in various research works. The in vitro studies in various research works give a very promising statement that albumin can be used as a polymer in the formulation at a large scale without much of the complications.

Keywords: Sustained Drug Delivery, Microspheres, Bovine Serum Albumin, Egg Albumin.

Research Articles

K Ofori-Kwakye, E Obese, M E Boakye-Gyasi

Sustained release diclofenac sodium matrix tablets (~100 mg) were prepared by wet granulation using blends of cashew gum, xanthan gum and HPMC as drug release modifiers. The flow properties of diclofenac sodium granules and the physical properties of the compressed matrix tablets namely, weight variation, tablet thickness, crushing strength, friability, drug content and swelling index were evaluated. In vitro dissolution studies were performed in phosphate buffer (pH 7.5) using Voltaren Retard® tablet as a reference drug. Kinetic models and difference (f1) and similarity (f2) factors were employed to evaluate the drug release data. The granules exhibited good flow properties while the physical properties of tablets generally fell within acceptable limits. Tablet formulations containing 60-100 % xanthan gum exhibited high water absorption capacities in phosphate buffer pH 7.5. Formulations F10, F12, F13 and F15 passed the dissolution test for modified release oral tablets while the rest failed the test. Formulations F7 to F15 appeared similar to the reference drug (p < 0.05; f1 ≤ 10; f2 ≥ 60) and could be used interchangeably. Drug release data fitted well to the Higuchi square root model and the Korsmeyer-Peppas equation, indicating anomalous or non-Fickian drug release. Blends of cashew gum, xanthan gum and HPMC when employed in the appropriate ratios could optimize the sustained release activity of diclofenac sodium matrix tablets.

Keywords: Natural Gums, Hydrophilic Polymers, Swelling Capacity, In Vitro Dissolution, Sustained Release.

Zaheer Abbas, Ravikiran Kanabargi

In the present investigation a novel oral drug delivery system was developed utilizing the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in the stomach and control the drug release for an extended period of time. Nizatidine microspheres were prepared by emulsification-ionic gelation technique employing sodium alginate with mucoadhesive polymers such as Carbopol 934P and Hydroxypropyl methylcellulose. The prepared formulations were subjected to particle size and shape analysis, % drug entrapment efficiency, in vitro floatability, swelling rate, in vitro mucoadhesion and in vitro drug release studies. The prepared microspheres were discrete, spherical with a mean particle size in the range of 451 ± 1.21 µm to 645 ± 2.24 µm. Entrapment efficiency was found to be in the range of 77.4 ± 3.02% to 85.2 ± 0.56%. Formulations containing Carbopol 934P showed increased in vitro mucoadhesion compared to formulations with Hydroxypropyl methylcellulose. The % in vitro floating decreased and swelling rate increased with increase in the mucoadhesive polymer content at the end of 12 h. In vitro drug release for all the formulations in 0.1N HCl was diffusion controlled gradually over a period of 12 h and followed First order kinetics. The in vitro drug release mechanism was nonfickian type controlled by swelling and relaxation of polymer. There was no significant change in physico-chemical characteristics of the microspheres stored at different storage condition after 3 months of stability study. The developed system has the dual advantages of being gastroretentive, to increase oral bioavailability and releasing drug in a controlled manner, to reduce the required frequency of administration thereby promoting patient compliance.

Keywords: Nizatidine, Mucoadhesive Microspheres, Floating Microspheres, Hollow Microspheres, Gastro Retention, Emulsification-ionic Gelation.

Deepali Gawale, Raju Onkar Sonawane, Vishal Vijay Pandey, Pradum Pundlikarao Ige

The present study involves preparation and characterization of extended release matrix pellets by using Lornoxicam as a model drug for prolong release of drug for extended period of time after predetermined lag time for the chronotherapy of rheumatoid arthritis. The pellets were prepared by the Extrusion and Spheronization method using as release retarding polymers like xanthan gum, xyloglucan and is combination with PVP K-30 and MCC PH-101 as pelletization aid. Matrix Pellets had characterized by flow properties, differential scanning calorimetry, scanning electron microscopy, particle size, circularity, roundness, aspect ratio, crushing strength, percent drug content, percent production yield, percent friability and in vitro drug release. The effects of various formulation variables on the size and drug release were also investigated. In this study, the feasibility and influence of incorporation of natural gums by itself and in combination with other gums on the ability to form spherical pellets by extrusion spheronization techniques. Matrix pellets containing 30% xanthan gum, 30% of xyloglucan and 30% combination of XG: Xg which showed sustained release of lornoxicam for15 h.

Keywords: Multiple Unit, Matrix Pellets, Lornoxicam, Natural Gums, In-Vitro Drug Release.


Sujan Banik, Md Masud Kaisar, Mohammad Salim Hossain

This work reports a simple, rapid, accurate and precise UV-spectrophotometric method for the assay of Linagliptin in bulk and marketed tablet dosage form has been developed. The method was linear in the range of 5 and 30 µg/ml presenting a good correlation coefficient (r=0.999). Method is validated as per ICH guideline and this study is statistically significant as all the statistical parameters are within the acceptance range (% RSD < 2.0 and SD < 2.0) for both accuracy and precision.

Keywords: Linagliptin, Tablets, UV-Spectrophotometer, Validation.

Vinayaka K S, Karthik S, Nandini K C, Prashith Kekuda T R

Diabetes mellitus is an endocrinal chronic disease caused by altered carbohydrate metabolism and characterized by elevated blood glucose levels. The present study was conducted to determine amylase inhibitory activity of methanol extract of six macrolichens namely Everniastrum cirrhatum (Fr.) Hale, Usnea sinensis, Ramalina conduplicans Vain, Ramalina hossei, Parmotrema pseudotinctorum (des. Abb.) Hale and Parmotrema tinctorum collected from Western Ghats, Karnataka. The lichens were collected, powdered and extracted using methanol. The inhibitory activity of extracts of the lichens was determined against fungal amylase. The extracts caused a dose dependent inhibition of amylase activity. Among lichens, R. conduplicans caused higher inhibition of enzyme activity followed by R. hossei, P. tinctorum, U. sinensis, E. cirrhatum and P. pseudotinctorum. The inhibitory efficacy of lichens could be related to the presence of secondary metabolites present. The lichens of Karnataka could be exploited in the development of agents active in regulating postprandial glucose level and hence the lichens could possibly used to manage diabetes.

Keywords: Bhadra Wildlife Sanctuary, Macrolichens, Amylase Inhibitory Activity, Secondary Metabolites, Type II Diabetes.

D C Nwachukwu, C N Okwuosa

The hepatoprotective effect of leaf extract of Clerodendrum polycephalum was investigated using albino wistar rats. Carbon tetrachloride (CCl4) was used to induce liver damage. Preliminary phytochemical analysis revealed the presence of Resins, Saponins, Tannins, Terprenoids and Steroids. Acute toxicity study showed an oral LD50 greater than 400mg/Kg in rats. The rats were divided into five groups (A- E) of 5 rats each. Group A served as the normal control group and received no treatment; Groups B-D served as the experimental treatment groups and received 100, 200, and 400mg/Kg daily of the extract while group E was the control treatment and was administered 50mg/Kg of silymarin daily. Treatment lasted for two weeks before CCl4 intoxication. Blood was collected via retro-orbital puncture for liver marker enzyme studies. Total protein and serum albumin levels were also estimated. Results showed a significant decrease (p<0.001) in the levels of alkaline phosphatese (ALP), alanine transaminase (ALT) and aspartate aminotransfarase ( AST) in the treatment groups which appears to be dose-dependent but total protein and serum albumin levels increased. Methanol extract of Clerodendrum polycephalum demonstrated significant hepatoprotective activity and improved liver function.

Keywords: Clerodendrum polycephalum, CCl4, Hepatotoxicity, Liver Maker Enzymes, Serum Albumin, Total protein.

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