Downstream processing of polymer-based amorphous solid dispersions to generate tablet formulations.

Annona reticulata Linn. (Bullock's heart): Plant profile, phytochemistry and pharmacological properties.

Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study.

A success of formulation depends on how efficiently it makes the drug available at the site of action. Among all the newly discovered chemical entities, about 40-45% drugs fail to reach market due to their poor water solubility. Because of solubility problem, bioavailability of drugs gets affected and hence solubility enhancement becomes necessary. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of drugs. This article reviews the various preparation techniques, carriers used, advantages and limitations of solid dispersions and compiles some of the recent advances. The experience with solid dispersions over the last 10-15 years indicates that this is a very fruitful approach in improving the release rate and oral bioavailability of poorly water soluble drugs. Hence, this approach is expected to form a basis for the commercialization of many poorly water-soluble and water-insoluble drugs in their solid-dispersion formulations in the near future.

SOLID DISPERSIONS: AN APPROACH TOWARDS ENHANCING DISSOLUTION RATE Review Article

Preparation and characterization of furosemide nanosuspensions

Today synthetic indicators are the choice of acid-base titrations. But due to environmental pollution, availability and cost, the search for natural compounds as an acid-base indicator was started. The present work highlights the use of the acidified methanolic extract of the flowers of few medicinal plants as an acid-base indicator in acid-base titrations. This natural indicator is easy to extract as well as easily available. Promising results were obtained when it was tested against standard synthetic indicators. Titration shows sharp colour change at the equivalence point. This indicator was found to be useful in all type of acid-base titrations except weak acid and weak base titration. It was found very useful, economical, simple and accurate indicator for said titrations.

Use of Flower Extracts as an Indicator in Acid-Base Titrations

Domperidone is a widely used antiemetic, poorly water soluble drug, erratically absorbed in stomach and possess several dissolution-related problems thus it has poor bioavailability. Solubility of a drug plays a very important role in dissolution and hence absorption of drug which ultimately affects its bioavailability. Hence, by considering the facts related to drug, attempts have been made to formulate inclusion complexes using methylated β-cyclodextrin and also to study the effect of preparation method. Inclusion complexes were prepared using methylated β-cyclodextrin in 1:1 and 1:2 molar ratios. Kneading, ultrasonification and physical mixture method were used for preparation of inclusion complexes. All the inclusion complexes were characterized using FTIR, DSC and XRD. The solubility and dissolution results revealed that there was a considerable increase in solubility and dissolution of all inclusion complexes as compared to pure drug. It was highest in case of methylated β-cyclodextrin in 1:1 molar ratio using ultrasonification method (USM1). Stability study revealed that all complexes were stable for a period of three months.

http://ijpr.sbmu.ac.ir/article_803_f9d0ddff387dc33358d45f02d8c13b6a.pdf

Preparationa and Characterization of domperidone Inclusion Complexes with Cyclodextrin: Influence of Preparation method

Pioglitazone HCl is an antidiabetic agent with poor aqueous solubility. Inclusion complexes of pioglitazone HCl were prepared with β-cyclodextrin using various methods (physical mixing, kneading method, co-precipitation). The main aim of the present invention is to study the effect of the method of preparation on the dissolution profiles of pioglitazone HCl-β-Cyclodextrin inclusion complexes. The phase solubility profile of pioglitazone HCl with β-cyclodextrin was classified as AL-type and stability constant with 1:1 molar ratio was 115.45, calculated from the phase solubility diagram. Formation of the inclusion complex between pioglitazone HCl and β-cyclodextrin was confirmed by the Fourier Transform Infrared (FT- IR) spectroscopy. The dissolution profile of inclusion complexes were determined and compared with those of pioglitazone HCl alone and its physical mixtures.The dissolution rate of the pioglitazone HCl-β-cyclodextrin inclusion complex prepared by the co-precipitation method was six times higher when compared with the pure drug. The method of complexation of pioglitazone HCl in β-CD increased the dissolution rate of the drug in the following order: Coppt > KM > PM >Drug.

Effect of method of preparation on pioglitazone HCl-β-cyclodextrin inclusion complexes

The aim of this study was to evaluate the effect of increasing crospovidone (superdisintegrant) load on the characteristics of fast-disintegrating tablets for the potential use of the drug for its therapeutic effect. Five tablet formulations, F0, F1, F3, F7, and F10 containing 0%, 1%, 3%, 7%, and 10% (w/w) of crospovidone, respectively, frusemide and microcrystalline cellulose (PH102), were prepared by direct compression, at a different compression forces.Tablet weight variation, content uniformity, crushing strength, disintegration time, wetting time, and in vitro release were measured for each formulation at each compression force. A linear increase in compression force resulted in an exponential increase in hardness for all formulations, a linear increase in disintegration and wetting times was observed for the formulations F0, F1, F3 with the increase in compression force.The tablet formulation F7 indicated, there was no effect of compression force on disintegration and wetting time. The in vitro release of the drug was increased with increase in concentration of crospovidone irrespective the compression force. However, storage under high humidity conditions caused the softening of the tablets containing the high amount of crospovidone, leading to softening of tablets. Fast disintegration of the tablets within 1-2 min is prerequisite for improving the dissolution of frusemide, attributed to increase in speed at which maximum surface area of sparingly soluble drug is exposed to the dissolution medium. However, tablet containing high amount of crospovidone must beprotected from the atmospheric moisture because storage of these tablets at high humidity led to softening and losing the tablet characteristics.

Effect of some physical parameters and crospovidone on directly compressed frusemide tablets

In the present study, aqueous extract of leaves of Capparis zeylanica Linn, Annona reticulata Linn and Clerodendron phlomidis Linn were given at a dose of 200mg/kg, 400mg/kg (p.o.).

Screening of Some Indigenous Plants for Their Antipyretic Activity

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