Volume 8

October-December 2016

Review Articles

Jameel Ahmed S Mulla, Shraddha C Hajare, Rajendra C Doijad

The science of small particles is known as ‘micromeritics’ and it is used extensively in many different industries, including pharmaceuticals. When you really think of how important the consistency of a drug is for it to work well, the relevance of micromeritics comes to the surface. The release and dissolution of a drug, absorption and therapeutic action, physical stability, dosage and many more are important parameters which are influenced by particle size. This review highlights the description of particle size, methods of particle size reduction, particle size determination and its significance.

Keywords: Particle Size, Particle Size Reduction, Particle Size Determination, Solubility, Absorption.

Research Articles

Veena S Belgamwar, Jatin D Dani, Anil U Tatiya, Mohan G Kalaskar, Prakash H Patil, Shailesh S Chalikwar

Atorvastatin calcium (ATR) is the choice of an anti-hyperlipidemic agent having only 12% oral bioavailability because of its poor aqueous solubility (log P 5.7) and extensive first-pass metabolism. The prime motivation for this work was to develop nanostructured lipid carriers (NLCs) to enhance solubility and avoid first-pass metabolism on oral administration of ATR. Amongst various lipids, stearic (solid) and oleic acid (liquid) were screened to prepare five different batches of ATR loaded lipidic nanoparticles (ATR-LPs) by employing hot homogenization technique for four homogenization cycles and at a pressure of 500 bar. Results concluded that as content of oleic acid increased from 0-30%, there was a decrease in particle size with increase in zeta potential, entrapment efficiency, and drug loading capacity. The optimized ATR-NLCs showed mean particle size of 147.8±7.4, PDI of 0.211±0.050 with a zeta potential of -22.5±3.64 mV. Compatibility was studied by Fourier transform infrared (FTIR) spectroscopy technique. Powder X-ray diffraction and differential scanning calorimetry studies which revealed that the crystalline ATR has converted into an amorphous form in ATR-NLCs. SEM photomicrographs confirmed the non-spherical shape of ATR-NLCs. In vitro dissolution study of ATR-NLCs established the biphasic release pattern. Triton-induced hyperlipidemic model was used for examining in vivo pharmacodynamic activity of ATR-NLCs, results of which was found to be significant than plain ATR suspension, making NLCs as a robust, promising perspective colloidal vehicles for oral delivery of ATR. Accelerated stability studies proved the robustness of ATRNLCs on three months storage at 25±2°C/60±5 % RH.

Keywords: Atorvastatin Calcium, Lipidic Nanoparticles, Nanostructured Lipid Carriers, High-Pressure homogenization, Pharmacodynamic Study, Triton-induced Hyperlipidemic Model, Accelerated Stability Studies.

Hitendra S Mahajan, Sanket B Dusunge

Purpose: The specific aim of present study was to investigate the biodegradation characteristics of xyloglucan, a natural film- forming polymer. Methods: Both in vitro as well as in vivo methods were used for assessment of the same. The in vitro degradation of xyloglucan film was followed in different fluids such as (simulated body fluid, simulated nasal fluid & simulated lung fluid) at different time intervals (0, 4, 12, 16, 20, 24, 28, 32 & 36) and in vivo by subdermal implantation in rats for up to 30 min. Rate and extent of degradation was followed in terms of film weight loss and swelling degree. Results: Although the rate of in vitro degradation was slow compared to the in vivo, xyloglucan films complete maximum degradation within 36 min following subdermal implantation in rats within 30 min. The films degraded following different rates, in vitro and in vivo, but the mechanism followed was primarily bulk degradation. Conclusions: Xyloglucan demonstrated highly in vivo biodegradable and in vitro degradation. The study provides valuable insight, which may lead to new application of xyloglucan in the field of drug delivery and challenge offers to formulator scientists.

Keywords: Xyloglucan, Swelling Degree, Weight Loss, In Vitro Degradation, In Vivo Biodegration.

Rohini S Kharwade, Nilesh M Mahajan, Rahul B Gandhe, Ujwala N Mahajan

Rosuvastatin calcium, an antilipidemic agent exhibits poor water solubility, dissolution and flow properties. Thus, the aim of the present study was to improve the solubility and dissolution rate of Rosuvastatin calcium by preparing microspheres by spray drying technique using Pullulan having low viscosity and high Tg (Glass transition temperature) value. Rosuvastatin calcium Microspheres containing different ratios of pullulan were produced by spray-drying using methanol and water (1:2) as solvent system to enhance solubility and dissolution rate. The prepared formulations containing different ratios of drug and pullulan were evaluated for solubility and in-vitro dissolution. The prepared formulations were characterized by DSC, FTIR, XRD and SEM. Dissolution profile of the prepared spray dried microspheres was compared with its physical mixture and pure sample. The Rosuvastatin calcium microspheres containing 1:3 w/w (Rosuvastatin calcium: Pullulan) showed highest % of drug release and solubility compare to other ratio, physical mixture and pure sample of Rosuvastatin calcium. Stability results showed that prepared microspheres stable for 6 month as per ICH guidelines. Hence, from the above result it can be concluded that spray dried microspheres of Rosuvastatin calcium is a useful technique to improve the solubility and dissolution of poorly water soluble drug like Rosuvastatin calcium.

Keywords: Rosuvastatin Calcium, Pullulan, Spray Drying, Microsphere, Solubility.


P S Gangane, N M Mahajan, U N Mahajan, M V Shende, G N Pawde

The objective of this study was to design and developed a capsule dosage form which contains the drug closed with plug, which is removed after a predetermined lag time and the drug is release from the insoluble capsule body early in the morning hours. This delivery system was helpful to control early morning surge in blood pressure because cardiovascular events occur more frequently in the morning. Initially core tablet was prepared by using Captopril as a model drug, which is having Angiotensin-converting enzyme inhibition activity and different concentration of crosscarmellose sodium as a super disintegrant by the direct compression method by using 6 mm flat faced punch. Formulation was developed by filling core tablets in formaldehyde treated empty capsule body and sealed by using plugs of different polymers like guar gum, HPMC K4M, Sodium alginate and Xanthum Gum. Core tablet was evaluated for different evaluation parameters and the formulation which shows least disintegration time has been selected for further study. After complete wetting of the plug, it formed a soft mass, which was then easily ejected out of the capsule body expose the core tablet of captopril to pH 6.8 phosphate buffer (simulated colonic fluid). From in vitro dissolution study it was concluded that, the drug release is directly proportional to concentration of polymer used in erodible tablet plug.

Keywords: Pulsatile Drug Delivery, Hypertension, Chronotherapy, Captopril, Lag Time.

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