Pyrimidine incorporated semicarbazones can be regarded as a newer class of anticonvulsants. These compounds possess the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds display considerable anticonvulsant activity in both seizure models. (Ic) and (Id) of the most active compounds (Ia), (Ic) and (Id) do not show any sign of neurotoxicity. -(ALAM*, O.; MULLICK, P.; VERMA, S. P.; GILANI, S. J.; KHAN, S. A.; SIDDIQUI, N.; AHSAN, W.; Eur.
Thiadiazole Derivatives as Potential Anticonvulsant Agents. -A variety of thiadiazolyliminothiazolidinone derivatives (IX) and (XI) are synthesized, which show good potential for anticonvulsant activity and also neurotoxic effect. -(MULLICK*, P.; KHAN, S. A.; VERMA, S.; ALAM, O.; Bull. Korean Chem. Soc. 32 (2011) 3, 1011-1016, http://dx.
Considering the compliance of patients and ease of administration, the oral cavity is profoundly chosen to deliver drugs. This article focuses on mucoadhesive buccal drug delivery system providing sustained release of the drug. The drug of choice for buccal delivery is those which undergoes high first-pass metabolism or undergo acid degradation. This review article aims to focus on various aspects of buccal films, factors affecting mucoadhesion and its evaluating parameters. Different theories involved in mucoadhesion process and along with the polymers that are involved in developing different categories of films have been focused. Factors influencing the polymers involved flexibility, molecular weight, charge, etc., are also considered in this review. Most commonly used polymers in the development of mucoadhesive films are lectins, starch, pectins, and cellulose derivatives, etc. Several agents such as penetration enhancers and mucoadhesive agents are employed to develop an ideal film. These dosage forms are formulated using two processes, namely film casting method and hot-melt extrusion method. The developed films are evaluated based on multiple parameters such as surface pH, flatness, tensile strength, and peel strength. This review gives an overall view of different polymers that are used to develop the mucoadhesive films and compare their degree of mucoadhesion along with their parametric tests to evaluate the developed films.
Nowadays, solubility of active pharmaceutical ingredient (API) is one of the biggest challenges faced by the researchers during the development of pharmaceutical oral dosage form. Developing a new molecule is very expensive than formulating a dosage form of existing API. Orodispersible film (ODF) is one of the alternatives for the conventional dosage form as it dissolves and directly absorbed from the mouth. It is suitable for the delivery of poorly soluble drugs. It does not require water for the administration and gives quick absorption and high bioavailability. There are various techniques that can be used to improve the solubility of poorly soluble drugs in ODFs, namely, surfactants, superdisintegrants, and printing technology. Water-soluble polymers are used as the film former, but the different concentration and different combination of polymers and use of various additives like surfactant; superdisintegrants can show the significant effect on the solubility. It can be used for both local and systemic action. ODFs are gaining popularity and are widely accepted by the consumers, but it is still lacking in some areas due to the absence of pharmacopoeial specifications for disintegration, mechanical properties, etc.
In this study, easy and robust RP-HPLC method was developed and validated to determine acceptable residual limit of citalopram hydrobromide for cleaning procedures. The United States, Food and Drug Administration has mentioned that the acceptable limit for residues present in the equipment during processing or manufacturing should be based on logical criteria. In present study, acceptable residual limit for cleaning procedure of citalopram hydrobromide was calculated by using three approaches including therapeutic dose method, 10 ppm criteria and visual limit of inspection. The value by erapeutic dose approach was less among three calculated values hence, selected as acceptable residual limit (10.66 µg/25 cm2 ) for analytical method development and validation for the detection of this drug residues on the surfaces of manufacturing equipment. A RP-HPLC assay method was developed using C18 column and mobile phase containing mixture of methanol and ammonium acetate buffer (pH4.6) (70:30) with flow rate of 1.6 ml/min. System suitability parameters like theoretical plates and tailing factor were calculated for the validation of the developed method as per ICH Q2B guidelines. After analyzing recovery study data, it was found that stainless steel plate has minimum recovery (88.87%) and pre-analyzed tablet solution has maximum recovery (99.29%)
Liposomes, as the leading drug delivery system, have played a significant role in the formulation of anticancer drug to improve therapeutic effect. This system improves the pharmacokinetic and pharmacodynamic profiles of the therapeutic payload, promote controlled and sustained release of anticancer drugs, and exhibit very less systemic toxicity as compared to the free anticancer drug. The mechanism giving rise to therapeutic advantages of liposomes such as the ability of long-circulating liposomes to preferentially accumulate at disease sites such as tumors, site of infection, and site of inflammation. In the studies, liposomal anthracyclines have shown highly efficient drug encapsulation, resulting in significant anticancer activity with reduced cardiotoxicity. There are several methods for liposomes preparation based on lipid drug interaction and liposomes disposition mechanism including the incubation of rapid clearance of liposomes by controlling particle size and surface hydration. The liposomes are characterized with respect to physical, chemical, and biological parameters. This review discusses the recent advances in the preparation methods of liposome for the treatment of cancer.
A simple, selective and precise dissolution method was developed and validated for the Mycophenolate mofetil immediate release tablets. The method employed dissolution medium 0.1N HCl (pH1.2) and volume 900ml with USP-II apparatus (Paddle). Detection was made by measuring the absorbance on UV at the λ~max~ 250nm. The method show the linearity in the range of conc. 5[mu]g/ml to 40[mu]g/ml with r^2^=0.999. The method is also validated as per International Conference of Harmonization guidelines. The method showed the specificity with standard deviation 0.00. The method is repeatable, selective and accurate for the dissolution study of Mycophenolate mofetil immediate release tablets.
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