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Pharmacy

Coconut husk mashi is an Ayurvedic formulation prepared by Anterdhum padhati (APM). Though Ayurvedic practitioners use coconut husk mashi, very few scientific reports are available about its claim uses. In the current study the analgesic activity of APM of unripe Cocos nucifera husk were demonstrated. The orally administered APM inhibit the acetic acid induced writhing response in mice. Tail flick and hot plate assays demonstrated that treatment of animals with APM induced attenuation in the response of heat stimulus.

School of Pharmacy

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Pharmacologyonline

Antinociceptive activity of Anterdhum padhati mashi (APM) of unripe Cocos nucifera (PALMAE) husk

The objective of present study was to develop a gastroretentive drug delivery system of propranolol hydrochloride. The biggest problem in oral drug delivery is low and erratic drug bioavailability. The ability of various polymers to retain the drug when used in different concentrations was investigated. Hydroxypropyl methylcellulose (HPMC) K4 M, HPMC E 15 LV, hydroxypropyl cellulose (HPC; Klucel HF), xanthan gum, and sodium alginate (Keltose) were evaluated for their gel-forming abilities. One of the disadvantages in using propranolol is extensive first pass metabolism of drug and only 25% reaches systemic circulation. The bioavailability of propranolol increases in presence of food. Also, the absorption of various drugs such as propranolol through P-glycoprotein (P-gp) efflux transporter is low and erratic. The density of P-gp increases toward the distal part of the gastrointestinal tract (GIT). Therefore, it was decided to formulate floating tablet of propranolol so that it remains in the upper part of GIT for longer time. They were evaluated for physical properties, in vitro release as well as in vivo behavior. In preliminary trials, tablets formulated with HPC, sodium alginate, and HPMC E 15 LV failed to produce matrix of required strength, whereas formulation containing xanthan gum showed good drug retaining abilities but floating abilities were found to be poor. Finally, floating tablets were formulated with HPMC K4 M and HPC. © 2009 American Association of Pharmaceutical Scientists.

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AAPS PharmSciTech

Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride

The present study deals with studies on Cilostazol &amp; $\beta$-cyclodextrin($\beta$CD) inclusion complexs. . The present research work describes formation of Cilostazol &amp; $\beta$-cyclodextrin complexes. using Kneading, Coevaporation &amp; physical mixture with molar proportion of $\beta$-CD (1:1). Cilostazol,6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-3,4-dihydro- 2(1H)-quinolinone.is a vasorelaxent drug &amp; act as a platelet aggregation inhibitor. Cilostazol exhibits low aqueous solubility, which accounts variability in oral bioavailability. Hence, the main objective of study was to investigate the possibility of improving the solubility &amp; dissolution rate of Cilostazol via complexation with $\beta$-CD. Phase solubility studies revealed the existence of 1:1 complex between cilostazol and $\beta$-CD.Prepared inclusion complexes were characterized by I.R, UV. In vitro release of Cilostazol from inclusion complexes were studied by dissolution study in 0.1N HCl, pH 6.8 and distilled water. It was observed that complexes exhibit higher dissolution rates than the pure drug.

International Journal of PharmTech Research

Studies on cilostazol and β-cyclodextrin inclusion complexes

The present study deals with the investigation of the neurobehavioral effects of the methanolic extract of Phoenix dactylifera (PD) fruits, studied on locomotor activity, exploratory behavior, motor coordination, hot-plate test, haloperidol-induced catalepsy, sodium nitriteinduced respiratory arrest, maximum electroshockinduced convulsions using mice. The results revealed that the extract in mice considerably reduced the exploration time in closed arms with an increased exploration in open arms, increased the time spent in mirrored chamber, increased the discrimination index, potentiated the haloperidol-induced catalepsy, reduced the onset of death in sodium nitriteinduced respiratory arrest. These results suggest that the methanolic extract of P. dactylifera fruits possess a wide range of CNS activities, which need further investigation.

Journal of Young Pharmacists

Neurobehavioral effects of phoenix dactylifera in mice

Phoenix dactylifera L (Date palm) belonging to family Arecaceae, called 'Nakhla' and the 'Tree of Life' by the Arabs, is considered as one of the oldest cultivated fruit trees. It is believed to be indigenous to the countries around the Arabian Gulf. Many Middle Easterners believe that consumption of date fruits, particularly in the morning on an empty stomach, can reverse the actions of any toxic material that the subject may have been exposed to. Different parts of this plant are traditionally claimed to be used for the treatment of a broad spectrum of ailments including memory disturbances, fever, loss of consciousness and nervous disorders. There has been a tremendous interest in this plant as evidenced by the voluminous work in last few decades. Therefore, we aimed to compile an up to date and comprehensive review of Phoenix dactylifera that covers its traditional and folk medicine uses, phytochemistry and pharmacology including various preclinical and clinical studies.

Internet Journal of Pharmacology

Phoenix dactylifera: An update of its indegenous uses, phytochemistry and pharmacology

Metformin Hydrochloride (MF) is glucose lowering agent that is widely used for management for type II diabetes. MF is reported to be absorbed mainly in upper part of GIT. It is having narrow absorption window and high water solubility and it would be more beneficial to retain the drug in stomach for prolonged duration so as to achieve maximum absorption and better bioavailability. A conventional oral CR formulation releases most of the drug content at the colon, which requires that the drug will be absorbed from the colon. The present investigation is aimed to develop novel gastroretentive (GR) drug delivery system, which releases the drug in the absorption window. As well to provide controlled release drug profile that can result patient compliance and therapeutic success. Floating tablets of MF was prepared using sodium alginate and sodium carboxymethylcellulose as a gelling agent and release modifier, respectively. Eudragit NE 30 D was used as sustained release polymer to control the initial burst release. Drug and excipients compatibility studies were monitored by thermal analysis using differential scanning calorimeter. 32 full factorial design was applied to optimize the formulation. The DSC thermogram of drug, polymer and physical mixtures revealed that there was no known interaction between drug and polymers. The prepared tablets were evaluated for in vitro dissolution, in vitro buoyancy, percentage swelling, percentage erosion and similarity factors with marketed tablets. The optimization study using a 32 full factorial design revealed that the amount of sodium alginate and sodium carboxymethylcellulose had a significant effect on t50, t90, Flag and f2. Thus, by selecting a suitable composition of release rate modifier and gel forming agent, gastroretentive system can be developed with the desired dissolution profile. This study indicated that the MF GR tablets prepared using sodium alginate and sodium carboxymethylcellulose can successfully employed as a once-a-day oral controlled release drug delivery system. {\textcopyright} 2009 Bentham Science Publishers Ltd.

Current Drug Delivery

Gastroretentive Drug Delivery of Metformin Hydrochloride: Formulation and In Vitro Evaluation Using 32 Full Factorial Design

Rubia cordifolia Linn. (family: Rubiaceae) is known as Indian madder. The present investigation was carried out to evaluate the diuretic activity of the hydroalcoholic extract of roots of Rubia cordifolia in rats to support its folklore claim. Roots of Rubia cordifolia was coarsely powdered and extracted using 70% ethanol with soxhlet extractor for 22h. Four groups of rats were treated with vehicle (normal saline: 25 ml/kg), furosemide (20 mg/kg) and two doses of extract (286 mg/kg and 667 mg/kg body weight) orally. Urine excreted was collected up to 5h post-treatment and analyzed for urine volume, Na+, K+, Cl- and creatinine content. The extract showed a significant (p<0.01) and dose dependent increase in urine volume and electrolyte excretion. Both doses of extract showed less influence on creatinine clearance than furosemide. The result indicates that hydroalcoholic extract of roots of Rubia cordifolia possess potent diuretic activity.

Diuretic activity of root extract of Rubia cordifolia Linn

Quantitative structure activity relationship (QSAR) studies of twenty four 5-cyano, N1, 6- disubstituted, 2-thiouracil derivatives were performed for their central nervous system (CNS) depressant (locomotor) activity using VlifeMDS3.5 software. Partial least square (PLS) linear regression analysis coupled with stepwise variable selection method was applied to derive QSAR models which were further validated for statistical significance and predictive ability by internal and external validation. The best QSAR model was selected, having correlation coefficient r2 = 0.9014 and cross validated squared correlation coefficient q2 = 0.8120 with external predictive ability of pred_r2 = 0.6692. The QSAR model indicated that the vdWSurfaceArea (van der Waals surface area of the molecule), dipole moment, YcompDipole (y component of the dipole moment) and T_2_F_1 (count of number of double bounded atoms (i.e. any double bonded atom, T_2) separated from fluorine atom by 1 bond in a molecule) were the important determinants for CNS depressant (locomotor) activity.

Digest Journal of Nanomaterials and Biostructures

Quantitative structure activity relationship (QSAR) studies on 5-cyano, N1, 6-disubstituted, 2-thiouracil derivatives as central nervous system depressants

An accurate, specific and precise assay level gradient reverse-phase high-performance liquid chromatographic method was developed for simultaneous determination of montelukast sodium and bambuterol hydrochloride in tablet dosage form. An inertsil ODS C-18, 5 m column having 250x4.6 mm I.D. in gradient mode, with mobile phase A, containing 0.025 M sodium phosphate buffer: methanol (85:15) and mobile phase B, containing acetonitrile:methanol (85:15) was used at different time intervals. The flow rate was 1.5 ml/min and effluent was monitored at 218 nm. The retention times of montelukast sodium and bambuterol hydrochloride were 21.2 min and 5.8 min respectively. The linearity for both the drugs was in the range of 0.25-0.75 mg/ml with correlation coefficients of 0.9999 and 0.9996 for montelukast sodium and bambuterol hydrochloride, respectively.

Indian Journal of Pharmaceutical Sciences

Determination of montelukast sodium and bambuterol hydrochloride in tablets using RP HPLC

The present investigation was carried out to study the antihypertensive activity of the two derivatives (NS1 & NS2) of novel synthetic hybrid compound [N(phenyl)N′{1′6methyl-4-(2-nitrophenyl)-2-thioxo- 1,2,3,4-tetrahydropyrimidine- 5- carboxylic acid ethyl ester} 3′ (4″ imino phenoxy) propane-2- ol thiourea] on 2K1C induced hypertensive rats. The left renal artery (LRA) was ligated by silk suture (no.4) in rats to produce two-kidney one-clip (2K1C) renovascular hypertension and kept for 6 weeks. After 6 weeks, respective treatments were started and continued for 7 days. On 7th day, 30 min after the last dose, the arterial blood pressure and heart rate (HR) of rats were measured by using data acquisition system. LRA ligated rats showed significant (P < 0.01) increment in mean arterial pressure (MAP) compared to non-ligated (normal) rats. NS1 decreased MAP and HR significantly (P<0.01) while NS2 significantly (P<0.01) decreased MAP without affecting heart rate when compared against LRA ligated rats. Standard drugs were significant (P<0.01) in reducing MAP as well as HR of LA ligated rats. In conclusion, both the derivatives (NS1 and NS2) of the novel synthetic hybrid compound showed significant reduction in the blood pressure of 2K1C induced hypertensive rats, while HR was only significantly reduced by NS1. The study needs further investigation to know the exact mechanism of antihypertensive activity of these hybrid compounds.