Ashok A. Hajare

Pelletization Technology: Methods and Applications-A Review

Pellets are small free flowing; spherical particulates manufactured by the agglomeration of fine powder or granules. Different types of techniques used to produce pellets are referred to as pelletization techniques. In relation to pharmaceuticals, pellets offer high degree of flexibility in design and development of oral dosage form. They offer desired dose strength, can be blended to deliver incompatible bioactive agents and can be blended to provide different release profiles. The most commonly use pelletization processes are Extrusion spheronization, Hot melt extrusion, Solution or suspension layering, Powder layering, High shear pelletization, Freeze pelletization, Cryopelletization, Crystallo-co-agglomeration, Wet spherical agglomeration, Spherical crystallization etc. In present review we will be explaining widely used pelletization techniques especially are Extrusion Spheronization and Hot Melt Extrusion in detail with methods and applications in pharmaceutical industries because these techniques represent an efficient pathway for novel drug delivery system today.

Room temperature stabilization of human serum albumin by vacuum foam drying

This article characterizes the activities required to launch a new pharmaceutical molecule into the market, summarizes studies that have attempted to pinpoint the research and development costs incurred per approved new molecule, and analyzes the various critiques levied against published R&D cost estimates. It finds that by any reckoning, R&D costs per approved molecule have risen sharply over time, most likely at a rate of approximately 7 percent per year after stripping out the effects of general economic inflation.A is a newer NSAID, used in treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Aceclofenac has shorter biological half-life around 4 h which makes it suitable for modified release to improve bioavailability and to reduce dosing frequency. Present work was aimed to develop and evaluate aceclofenac modified release (Triple Layer Tablet) TLT following direct compression technique using natural and synthetic polymers. Aceclofenac TLT containing immediate-releaselayer (IM) as first layer, controlled-release-layer (CR) as second layer and ethyl cellulose layer as barrier-layer (BL) were prepared. IM was optimized by D-optimal design where 16 formulations (IM1 – IM16) were developed by using super disintegrating agents like mannitol and SSG. CR was optimized by 32 full factorial design and 9 batches (CN1–CN9 & CS1–CS9) were developed using natural and synthetic polymers like guar gum, xanthan gum and HPMC K100 CR, HPMC K100 LVCR respectively. Drugpolymers compatibility was evaluated by Infrared spectroscopy, where all compositions were found compatible without any interaction. All formulations were evaluated for various post-compression parameters like disintegration time (DT), swelling index, hardness, friability and weight variation etc., and results were found in desirable range. IM and CR formulations were evaluated for drug release behavior in pH 6.8 phosphate buffer and best release compositions among batches were chosen to prepare TLT with BL to modify the release. Among IM formulations least DT was found in IF9 with 90.86% drug release in 10 min 21 sec so, IF9 was claimed as best composition. Among CR formulations the best compositions found were CN3 and CS6 with Time at 47.38 % and 26.42% drug release around 8 h respectively and, were then developed as triple layered tablets with IF9 where drug release was extended up to 24 h.H compounds have received considerable attention owing to their variety of biological activities, especially as inhibitors of PDE5 extracted from human platelets, HIV-1 reverse transcriptase, human EPK2, cyclin-dependent kinas. Also, heterocyclic nitrogen compounds are indispensable structural units for medicinal chemists and used as antibiotics, anthelmintics, antiviral, antidepressant, and anti-inflammatory. In view of these observations we evaluate some new poly hetero cyclic compounds which were previously synthesized according to for their analgesic, anti-inflammatory and anti-microbial activities in comparison to some reference drugs. Pyrimidines present an interesting group of compounds many of which possess wide-spread pharmacological properties such as antidepressant, antimicrobial, anticancer, and anticonvulsant activitiesM drugs combination is a promising strategy in biomedical fields, such as cancer chemotherapy, tissue engineering. The multi-drug system enables to be delivered with multiply targets and exhibits the additive or synergistic effects of drugs. However, the specific distinct drug release kinetics of the multiply drugs are required to meet the clinical needs, especially in the combined therapy of tissue regeneration and tumor chemotherapy. In order to deliver the individual drug at optimal dosages, the release behaviors of each drug in multi-drug systems should be controlled independently. Therefore, two kinds of nanoparicles with core-shell structure (PVP/PLGA and PCL/PLGA) were fabricated by coaxial electrospray in this paper. Each kind of nanoparticles can both encapsulate the hydrophilic rhodamine B and hydrophobic naproxen in one single step efficiently. The monodisperse size distribution as well as the desired core-shell structure was observed. These two multi-drug systems with dual drug loaded exhibited different distinct release profiles, attributing to the distinct core-shell structures of nanoparticles and the difference of two drugs in hydrophilic properties. Meanwhile, the release profiles of encapsulated drugs with different amount were investigated as well. The drug release behaviors were dominated by the following processes: water penetration, surface drug release, outer drug diffusion with shell polymer erosion, inner drug diffusion and nanoparticle collapse. The results suggested that the distinct release kinetics of multiply drugs fabricated by coaxial electrospray can be obtained and tuned to fulfill the clinical requirement in combination therapy.Aspirin suppositories are in commercial use, suffer with side effects such as irritation, burning sensation, rectal hemorrhage. The aim of the present work is to formulate aspirin nanoparticles loaded suppositories and to perform In vitro investigation for the prepared suppositories. Initially aspirin-chitosan nanoparticles were prepared by ionic gelation method and the nanoparticles evaluated for different In vitro evaluation studies; based on results the best formulation was selected and in order to know the diffusion efficiency, different compositions of aspirin glycerogelatin suppositories were prepared and subjected to various In vitro evaluation studies and best composition was selected. From the previously performed evaluation studies best formulation from aspirin nanoparticles incorporated in to selected glycerol gelatin bases and evaluated for In vitro characteristics. The results indicates that formulation Fa9 Aspirin nanoparticles were proved to be best formulation with 88.3±1.1 % of drug release at the end of 24hr, with zero drug release. In vitro characterization performed for aspirin suppositories indicates that Fs2, Fs4, Fs9 and Fa11 was proved to be best composition with highest percentage of drug release at the end of 60 minutes with 98.06±1, 99.3±0.45, 97.6±1.8 and 97±1 drug release and other characteristic studies performed indicates that all formulation are ideal characteristics. Previously selected bases composition used for the loading of nanoparticles based on displacement value results indicates that drug release appears with a lag phase initially and controlled for a period of 24hr.Orally dissolving tablets (ODT) provides a patient compliance solution for patients swallowing difficulties. Foam granulation is a newer technique that promises better distribution of the granulating system and better properties of the produced tablets. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor hydrophilicity of the drug results in variable dissolution rate and poor bioavailability. In this study, we tried to prepare aceclofenac ODT using the newer technique and various types of disintegrants, glidants, and lubricants. The resulted tablets were evaluated for hardness, friability, weight variation, in vitro disintegration time, and wetting time. All the formulation showed acceptable disintegration time. It was concluded that the prepared aceclofenac ODT by foam granulation technique using selective range of excipients can provide a dosage form with better patient compliance and effective therapy.

Freeze Dried Fenugreek Seed Mucilage as disintegrant for Fast Dissolving Tablets of Valsartan

The objective of the research work was to formulate fast dissolving tablet of valsartan using freeze-dried fenugreek seed mucilage as disintegrant. An attempt was made to extract the mucilage from fenugreek seeds and Ocimum tenuiflorum linn seeds and was evaluated for its various physicochemical characteristics. Fast dissolving tablets of valsartan was formulated by direct compression using different concentrations of fenugreek gum and Ocimum tenuiflorum gum as a natural superdisintegrants and compared with synthetic superdisintegrants like crospovidone. The tablets formulated using fenugreek gum and Ocimum tenuiflorum were evaluated for various physical tests like friability, weight variation, hardness. In vitro dissolution study showed 93.32% and 91.46% drug release, 42, and 53 seconds disintegration time, respectively for fenugreek and Ocimum tenuiflorum gum tablets. Natural gums like fenugreek and Ocimum tenuiflorum have better disintegration properties with improved disintegration time, when used in combination with synthetic disintegrants.

Development and Validation of RP-HPLC Method for Determination of Doxorubicin Hydrochloride from Vacuum Foam Dried Formulation

A rapid reversed phase (RP) high performance liquid chromatography (HPLC) method was developed and validated for quantitative estimation of Doxorubicin hydrochloride (Dox) from the prepared vacuum foam dried formulation. Chromatographic runs were performed on C18 column with mobile phase comprising of acetonitrile: 0.01M o-phosphoric acid (40: 60) pH 2 at a flow rate of 0.75mL.min−1. Dox was detected at a wavelength of 234nm. The method was shown to be specific, linear in the range of 0–10μg.mL−1 with correlation coefficient of 0.9999, precise at the intra-day level as reflected by relative standard deviation, accurate at recovery rate 99.60±0.13 and robust to change mobile phase and column brand. The detection and quantitation limits were 0.091μg.mL−1 and 0.2758μg.mL−1, respectively. The proposed method could be advantageous in estimation of Dox quantitation in pharmaceutical dosage form in the presence of excipients.

COMPARATIVE EFFICIENCY OF FORMULATION TECHNIQUES FOR DEVELOPMENT OF SALBUTAMOL SULPHATE LOADED LIPOSOMES

Present study investigate d most efficient technique for the develop ment of salbutamol sulphate loaded liposom es . Salbutamol sulphate is a selective β 2 adrenoceptor agonist widely used in the treatment of bronchial asthma, chronic bronchitis and emphysema. Our work is mainly focused on in vitro st udies of liposomal formulation encapsulated with salbutamol sulphate which may have high drug entrapment, sustained drug release and effective vesicle size. Drug loaded liposome s were prepared by ethanol injectio n and thin film hydration techniques using s oyaphosphatidyl choline and cholesterol in various molar ratios . Liposomes were evaluated for vesicle size, entrapment efficiency, transmission electron microscopy, zeta potential and drug release parameters. The particle size of drug loaded liposomes prep ared by ethanol injection technique was 423 ‐ 527 nm whereas it was 160 - 174.2 nm when prepared by thin film hydration technique. Z eta potential of liposomes prepared by thin film hydration technique was enough to stabilize over six month s . Optimized batches of s albutamolsulphate loaded liposomal formulations prepared by ethanol injection and thin film hydration technique have shown drug release as 94.59 % and 88.03 %, respectively . On the basis of observed a verage particle size, percent drug entrapment and dr ug release profiles, thin film hydration technique was emerged as superior technique over ethanol injection technique.