Karnataka

A recent advance in Novel Drug Delivery System (NDDS) aims to enhance safety and efficacy of drug molecule by formulating a convenient dosage form for administration and to achieve better patient compliance. Mouth dissolving tablets or fast dissolving tablets have received ever-increasing demand during the last decade, and the field have been rapidly growing in  the pharmaceutical industry and gaining popularity due to ease of administration  and better patient compliance to all age groups. MDDDS have the unique property of dissolving and/or rapidly disintegrating and releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. This review focusses on various formulations and also technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. The target population for these new fast dissolving/ disintegrating dosage forms have generally been pediatric, geriatric, and bedridden or developmentally disabled patients. Patients with persistent nausea, who are in traveling, or who have little or no access to water are also good candidates for MDDTs.

Asteracantha longifolia (L.) Nees. belonging to the family Acanthaceae is known as Talmakhana in Unani and Kokilasha in Ayurveda system of medicine. It is found in India, Srilanka, Burma and Nepal. The plant contains alkaloids, flavonoids, terpenoids, essential oil and phytosterols. It has been using in traditional systems of medicine since centuries for the treatment of diseases like low libido, premature ejaculation, ascites, jaundice and diseases of urogenital tract etc. Many pharmacological studies have been conducted on Asteracantha longifolia which proved its aphrodisiac, hepatoprotective, antioxidant and analgesic activities etc. In this review, an attempt has been made to present its phytochemical, pharmacological and other important aspects. Key words: Asteracantha longifolia, Talmakhana, aphrodisiac, Ayurveda, Unani.  

Several pharmacological activities like antitubercular, analgesic, anti-cancer, anti-inflammatory, antiasthmatic, antioxidant and antibacterial activities have been attributed to pyrazoles. The above observations prompted us to synthesize some novel pyrazole derivatives as possible antimicrobial agents. A series of novel 1,3,5-trisubstituted pyrazole derivatives (P1-P15) have been synthesized by the reaction of substituted chalcones (C1-C15) with succinichydrazide. The starting material, chalcones were prepared by claisen Schmidt condensation of acetophenone with aldehydes in the presence of sodium hydroxide in ethanol. Succinichydrazide was synthesized by condensing succinic acid with hydrazine hydrate. The cycloaddition of chalcones with succinichydrazide gives 1,3,5-trisubstituted pyrazole derivatives. The structures of synthesized derivatives were confirmed by IR, 1HNMR and Mass spectrum. The synthesized compounds were screened for their antibacterial and antifungal activity. The antibacterial activity data of the synthesized derivatives revealed that the compound P4, P13 and P7, P14 were effective against gram positive and gram negative organisms respectively. The antifungal activity data revealed that the compound P7 and P8 showed good activity against tested fungi.

Granisetron hydrochloride is a novel serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. It is well absorbed from the gastrointestinal tract, but its oral bioavailability is low (60%) due to extensive first-pass metabolism which makes it an ideal candidate for rapid release drug delivery system. Hence, an attempt was made to prepare and evaluate fast dissolving oral films containing Granisetron hydrochloride as a model drug by solvent casting method using natural and synthetic polymers. Various formulations were developed with varying concentration of polymers like, CMC, HPMC and Pullulan. Citric acid was used as a disintegrating agent and Propylene glycol as a plasticizer. The prepared oral films were evaluated for their physicochemical and mechanical parameters such as Physical appearance, surface texture, Weight uniformity, surface pH, ,thickness uniformity, percentage moisture absorption, loss on drying, disintegration time, drug content uniformity, folding endurance, tensile strength, percentage elongation, in-vitro drug release, and stability studies. In-vitro release rate of Granisetron hydrochloride was studied in phosphate buffer pH 6.8. F7, F10 showed maximum release rate about 93.95% and 95.29% in 180 seconds respectively, whereas F3 showed 60.98%. The mechanism of drug release of fast dissolving oral film was found to be to be non-fickian diffusion following first order kinetics. The selected fast dissolving oral films were found to be superior to marketed conventional tablet. Short term stability studies of selected films indicated that there is no significant change with respect to physical appearance, disintegration time, drug content and in-vitro drug release.

The advent of highly active antiretroviral (ARV) agents has led to striking reduction in plasma viral load, opportunistic infection and mortality from AIDS. Unfortunately most of these drugs have poor physiochemical, metabolism or transport properties that result in poor or variable absorption and side effects, which are often related to the accumulation of the drug at inappropriate sites. Various classes of antiretroviral agents are available, though monotherapy in HIV positive individuals can develop resistance more quickly as compared to combinational therapy or fixed dose combination or highly active antiretroviral therapy. The currently available ARV drugs mostly oral formulations, which are associated with several disadvantages and inconveniences to the HIV patients. The delivery of drugs via oral route suffers from significant first-pass effect, variation of absorption and degradation in the gastrointestinal, erratic bioavailability, limited duration of drug action, metabolism/elimination and transport barriers reducing the effect of anti-HIV drugs reaching the target site. Also half-life of several ARV drugs is short, which requires frequent administration of doses leads to poor patient compliance. Therefore, the usage of novel drug delivery systems is a logical approach to circumvent these problems and effectively treat the HIV infection. Various novel drug delivery techniques were tried or on trial for ARV drugs. Among the recent approaches of novel drug delivery system for anti-HIV drugs, controlled/sustained and targeted/intracellular drug delivery are the important ones. In this review the need for novel drug delivery, advantages, and recent development in drug delivery system of antiretroviral drugs were discussed, which may useful for further research in future.

One of the challenges faced by scientific community is that of adverse and deterioting side effects of psychotropic agents, which are popularly known as neuroleptic induced extrapyramidal adverse effects. Neuroleptic induced movement disorders pose a significant burden to patients, often resulting in non-adherence, disease relapse, and decreased quality of life. Evidence indicates that drugs which potentiate or attenuate neuroleptic induced catalepsy in rodents might aggravate or reduce the extrapyramidal signs respectively in human beings. It is being appreciated that many plant drugs can be explored for their protective nature against such adverse and toxic effects on account of their ascribed effects.

This present review is progress in selected nanotechnology topics and some possible applications. This attempt mainly focused on Different Classes of Nanoparticles (Ceramic nanoparticles, Metallic particles, Carbon nanomaterials, Quantum dots) and Applications of Nanotechnology in Pharmaceuticals (Diagnosis, Pharmacology and Therapy, Molecular Diagnosis) and Nanoparticle Drug Delivery Systems and Toxicity of Nanoparticles. Nanoparticles mainly use aims to minimize drug degradation upon administration, prevent undesirable side effects, and increase drug bioavailability and the fraction of the drug accumulated in the pathological area.

The structural and therapeutic diversity coupled with commercial viability of small heterocyclic molecules has fascinated organic and medicinal chemist. So, a great deal of research was carried out in the field of heterocyclic containing sulphur and nitrogen, because of their immense biological importance. The thiadiazole derivatives posses’ different pharmacological and biological activity. Hence, the search for never effective antimicrobial agents is imperative. It focuses on the problems of cross resistance and better activity against variety of infections. The majority of 1, 3, 4-thiadiazoles are based on the cyclisation of thiaosemicarbazide derivative incorporating this basic structural unit. The structure of new compounds prepared during present investigation has been authentically established by their IR, 1H NMR and Mass spectral studies. The antimicrobial activity of thiadiazole derivatives also reported some of these derivatives exhibit significant and broad spectrum antimicrobial activity. All the synthesized compounds were screened for antibacterial activity against Bacillus subtilis, Bacillus pumilus, E coli and Pseudomonas aureginosa by Disc diffusion method using ciprofloxacin as a standard against Gram positive and Gram negative bacteria. Key Words: Thiadiazole, Thiosemicarbazide, Antimicrobial, Cyclization, Screening 

To evaluate the use of tricyclic antidepressants, selective serotonin reuptake inhibitors and benzodiazepines in elderly patients aged over 60 years. Prospective, cross sectional, descriptive type of study was carried out in the general medicine department of a 640 bedded multispecialty tertiary care teaching hospital, South India. Benzodiazepines were prescribed in 79.6% patients, selective serotonin reuptake inhibitors in 12.3% and tricyclic antidepressants in 8.27%. The study identified 81.7% inappropriateness in prescriptions. Initiation of treatment with high dose after admission contributed to 32.6% while prescribing without proper indication accounted for 31.7%. Significant reduction of inappropriateness (48%) was observed during the post implementation phase, especially in the number of prescriptions of tricyclic antidepressants. The initial dose of alprazolam was reduced to 0.25 mg in all elderly patients. Prescribing benzodiazepines without proper indication reduced from 31.7% to 22%. Long acting benzodiazepines were not prescribed during this phase. The study demonstrated an overall improvement in the prescribing pattern of tricyclic antidepressants, selective serotonin reuptake inhibitors and benzodiazepines in elderly patients. Key Words: Antianxiety agents, tricyclic antidepressants, selective serotonin reuptake inhibitors, benzodiazepines, elderly, prescriptions.

The changes in polyphenols and caffeine alkaloid compositions of black tea, due to the variations of fermentation temperature were investigated. Black tea was manufactured by fermentation at various temperatures such as 26oC (Control) 30o, 36o and 40o where the tea leaves were fermented initially for 45-50 minutes at an private factory. During this oxidation process, withered and rolled leaf looses its green colour acquiring copper red to brown colour. Drying terminates these biochemical changes and remove moisture thereby the colour of fermented leaves turns from copper red to black and fermentation is arrested. Total polyphenols content were determined colorimetrically using Folin-Ciocalteau method and caffeine was isolated from all the samples by Liquid-Liquid extraction using chloroform. The results showed that increase in fermentation temperature significantly increases caffeine content whereas polyphenols content showed a great reduction at 30o, 36o and 40o. However further studies are needed to evaluate the organoleptic characters such as taste and aroma.