Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.
In recent times, focus on plant research has increased all over the world. Centella asiatica is an important medicinal herb that is widely used in the orient and is becoming popular in the West. Triterpenoid, saponins, the primary constituents of Centella asiatica are manly believed to be responsible for its wide therapeutic actions. Apart from wound healing, the herb is recommended for the treatment of various skin conditions such as leprosy, lupus, varicose ulcers, eczema, psoriasis, diarrhoea, fever, amenorrhea, diseases of the female genitourinary tract and also for relieving anxiety and improving cognition. The present review attempts to provide comprehensive information on pharmacology, mechanisms of action, various preclinical and clinical studies, safety precautions and current research prospects of the herb. At the same time, studies to evaluate the likelihood of interactions with drugs and herbs on simultaneous use, which is imperative for optimal and safe utilization of the herb, are discussed.
Reactive oxygen species are the intermediates that are formed during the normal metabolic process which are effectively neutralized by the antioxidant system of the body. Any imbalance in this neutralization process causes oxidative stress which has been implicated as one of the cause in diseases such as Alzheimer's disease, cardiovascular disorders, cancer etc. Research has enabled the use of antioxidants as therapeutic agents in the treatment of various diseases. Literature also puts forth the negative effects of using antioxidants in the treatment of diseases. This review is a compilation of both the beneficial and detrimental effects of use of antioxidants in the treatment of diseases such as cancer, cardiovascular diseases, diabetes and oral diseases.
Background: Ectopic pregnancy is a challenging and life-threatening emergency, which can cause significant maternal morbidity and mortality. The present study aims at determining the incidence, risk factors, clinical features, diagnosis, management and outcome of ectopic pregnancies in a tertiary care teaching hospital.Methods: This was a prospective study of 50 cases of ectopic pregnancies admitted to the Department of Obstetrics and Gynaecology at a tertiary care teaching hospital from August 2012 to September 2013. Relevant data of the 50 patients was tabulated and descriptive analysis was carried out.Results: The incidence of ectopic pregnancy was 6.3 per 1000 deliveries. Majority of the patients (82%) belonged to 20-30 yrs age group. 70% of the women were multiparous. The commonest site of ectopic pregnancy was fallopian tube (92 %). Past history of pelvic inflammatory disease (40%), abortions (20%), abdominopelvic surgery (14%) and IUCD usage (12%) were among the important risk factors identified. 20% of the patients had no identifiable risk factor. The classical triad of amenorrhea, bleeding per vaginum and abdominal pain was seen in 56 % of the study population. The most important signs which guided the diagnosis of ectopic pregnancy were cervical excitation pain (74%), abdominal tenderness (72%), adnexal mass or fullness (68%) and tenderness in the fornix (68%). Clinical presentation, urinary pregnancy test, culdocentesis and ultrasound were the diagnostic tools used for diagnosis of ectopic pregnancy. The incidence of ruptured ectopic pregnancy was 86%. Majority of the patients underwent salpingectomy (96%). There was no maternal mortality in our study.Conclusions: Early diagnosis, timely referral, improved access to health care, aggressive management and improvement of blood bank facilities can reduce the maternal morbidity and mortality associated with ectopic pregnancy.
Imidazole heterocycles containing oxygen or sulfur heteroatoms are of considerable pharmaceutical interest. Many synthetic strategies for imidazolidine-2-thione and imidazole-2-thione derivatives were developed in the past years. They have been well documented by a steadily increasing number of publications and patents. Substituted imidazolidine-2-thiones and imidazole-2-thiones display remarkable biological activities. For instance, imidazole-2-thione has been reported to exhibit antimicrobial, antifungal, antithyroid, antioxidant, cardiotonic, antihypertensive, Dopamine beta-Hydroxylase (DBH) inhibitory and anti-HIV properties. Imidazolidine-2-thione derivatives have been reported to exhibit antimicrobial activity, anti-HIV activity, antifungal activity and so forth. The main purpose of this review is to present a survey of the literature on the different methods of synthesis and reactions involving imidazolidine-2-thione and imidazole-2-thione during the last few decades. This article summarizes an efficient, microwave-assisted method for the liquid-phase combinatorial synthesis of 3,5-disubstituted-thiohydantoin, also reported previously. Synthesis of metal complexes of imidazolidine-2-thione and its derivatives were reported as antimicrobial agents also discussed in the article. Some of the chiral imidazolidine-2-thione N-and C-nucleoside were reported as precursors for the synthesis of azidonucleosides and fluoronucleosides known for their anti-AIDS activity. Metal complexes of heterocyclic thione ligands were reported to possess antifungal activity. Imidazolidine-2-thione and imidazole-2-thione derivatives have found applications in diverse therapeutic areas. Imidazolidine-2-thiones are also used as a chiral auxiliary and ligand for asymmetric catalysis.
Drug-resistant bacteria are now a global health threat. In the last 5 years the WHO, The House of Lords (UK), the Centre for Disease Control (USA) and many more agencies have presented reports on the scale of this problem. Microorganisms multiply very rapidly and have adapted to fill almost every available environmental niche (Rapidly growing species of bacteria under ideal conditions of growth can multiply in about 20 minutes). All members of the chemically related beta-lactam class act at the same phase in cell wall synthesis; as a result, a bacterial cell resistant to one agent is often resistant to all other analogues. The beta-peptide has two promising characteristics that distinguish it from traditional antibiotics. Firstly, bacteria may have trouble developing resistance to the beta-peptide since bacterial defenses may not recognize its unnatural amino acids. Secondly, the magainins that the beta-peptides mimic have been around for millions of years, yet bacteria have not become resistant to them. All classes of antibiotics are subject to resistance by an efflux mechanism mediated by more than one type of pump within the same organism. The bacterial cell may have a membrane pump capable of pumping a class or several classes of antibacterial agents back out of the cell. Other mechanisms of drug resistance include destruction of beta-lactam ring by beta-lactamases, impermeability of the drug into the bacterial cell wall, alteration of targets within the bacterial cells and the by-pass mechanism (bacterial cell may have acquired an alternative mechanism for achieving the essential function).
Lutein (LUT) is one of the most important carotenoid and; the most prominent being its antioxidant activity. However, its use is limited due to poor solubility and instability under adverse conditions. An attempt is made to increase the solubility and hence bioavailability of LUT using various cyclodextrins viz., betacyclodextrin (bCD), hydroxypropyl betacyclodextrin (HP-bCD) and methyl betacyclodextrin (M-bCD). Physical mixtures and spray dried inclusion complexes were prepared and characterized using spectroscopic techniques, DSC and XRD studies. From the phase solubility and dissolution studies it was found that, M-bCD significantly improved the solubility of LUT. These complexes were further subjected to in vitro anti-proliferative activity in order to validate results obtained from solubility studies. The biological results were in congruence with the results of solubility studies. Spray dried complex of LUT:M-bCD showed significant percent growth inhibition as compared to other two complexes and LUT alone. Molecular modeling studies established the hostguest stoichiometry with the lowest energy to be 2:1, with the two hexatomic rings of a LUT molecule occupying the two M-bCD cavities. The present study forms the basis for the development of oral formulations of LUT with significantly improved solubility and bioavailability.
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