Background A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue. Main text This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc.. Conclusion This review highlights the current status of triazole compounds as different multi-target pharmacological activities. From the literature survey, triazole is the most widely used compound in different potential activities.

The present study involves preparation and evaluation of floating microballoons with metformin as model drug for prolongation of gastric residence time. The microballoons were prepared by the solvent evaporation method using polymers hydroxypropylmethyl cellulose and ethyl cellulose. The shape and surface morphology of prepared microballoons were characterized by optical and scanning electron microscopy, respectively. In vitro drug release studies were performed and drug release kinetics was evaluated using the linear regression method. Effects of stirring rate during preparation, polymer concentration, solvent composition and dissolution medium on the size of microballoons, and drug release were also observed. The prepared microballoons exhibited prolonged drug release (8 hours) and remained buoyant for >10 hours. The mean particle size increased and the drug release rate decreased at higher polymer concentration. No significant effect of the stirring rate during preparation on drug release was observed. In vitro studies demonstrated diffusion-controlled drug release from the microballoons.

The purpose of this research was to prepare floating microballoons consisting of (i) calcium silicate as porous carrier; (ii) propranolol hydrochloride (PRH), an oral anti-hypertensive agent; and (iii) Eudragit S as polymer, by solvent evaporation method and to evaluate their gastro-retentive and controlled release properties. The effect of various formulation and process variables on the particle morphology, micromeritic properties, in-vitro floating behavior, percentage drug entrapment, and in-vitro drug release was studied. The gamma scintigraphy of the optimized formulation was performed in albino rabbits to monitor the transit of floating microballoons in the gastrointestinal tract. The propranolol hydrochloride-loaded optimized formulation was orally administered to albino rabbits, and blood samples collected were used to determine pharmacokinetic parameters of propranolol hydrochloride from floating microballoons. The microballoons were found to be regular in shape and highly porous. Microballoons formulation CS4, containing 200 mg calcium silicate showed the best floating ability (89 ± 4% buoyancy) in simulated gastric fluid as compared with other formulations. Release pattern of propranolol hydrochloride in simulated gastric fluid from all floating microballoons followed Higuchi matrix model and Peppas-Korsmeyer model. Prolonged gastric residence time of over 6 h was achieved in all rabbits for calcium silicate based floating microballoons of propranolol hydrochloride. The enhanced elimination half life observed after pharmacokinetic investigations in the present study is due to the floating nature of the designed formulations.

Background Acknowledging population control to be an essential step for global health promotes wide research study in the area of male contraception. Although there are a great number of synthetic contraceptives available in the market, they have plenty of adverse effects. Different potential strategies for male contraception were investigated over a long period time consisting of hormonal, chemical, and immunological interventions, although these methods showed good antifertility results with low failure rates relative to condoms. Main text This review is based upon the concept of herbal contraceptives which are an effective method for controlling the fertility of animals and humans. This review has highlighted herbal medicinal plants and plant extracts which have been reported to possess significant antifertility action in males. The review considers those plants which are used traditionally for their spermicidal and antispermatogenic activities and imbalance essential hormones for fertility purposes and plants with reported animal studies as well as some with human studies for antifertility effect along with their doses, chemical constituents, and mechanism of action of the antifertility effect of the plants. This review also explains the phases of sperm formation, hormone production, and the mechanism of male contraceptives. Conclusion As far as the relevance of the current review is discussed, it might be quite useful in generating monographs on plants and recommendations on their use. A lot of the plant species listed here might appear promising as effective alternative oral fertility-regulating agents in males. Therefore, significant research into the chemical and biological properties of such less-explored plants is still needed to determine their contraceptive efficacy and also to possibly define their toxic effects so that these ingredients can be utilized with confidence to regulate male fertility. The new inventions in this field are necessary to concentrate on modern, more potent drugs with less harmful content and that are self-administrable, less costly, and entirely reversible.

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