Journal of Pharmacy Research最新文献

The alteration of crops to improve their production was performed through the basis of selection before the creation of transgenics. This selection has been going on for thousands of years. By the year 2050, world population may reach nine billions. Food production will need to increase at the same rate or more in order to satisfy the needs of such an enormous number of people in some older centuries. So, there is a need to use the genetic techniques to improve crops over the recent decades. Through the use of transgenics, one can produce plants with desired traits and even increased yields. The transgenics would allow for more crops that last longer and withstand pests and diseases. Transgenic plant production will allow us to feed the growing population and to produce more desirable products. The future of GM crops remains a vital debate, as its applications have several advantages and disadvantages.

Background/objectives

In the present study oral extended release matrix tablets of lamivudine were formulated, characterized and evaluated for in vitro dissolution and in vivo bioavailability performance in rabbits.

Methods

Matrix tablets of lamivudine were prepared using hydroxypropyl methylcellulose K100M and its combination with polyethylene oxide as the release rate retardant polymers. The tablets were characterized for physical properties, moisture uptake studies, in vitro dissolution, accelerated stability (40 ± 2 °C and 75 ± 5% RH) testing. In vivo studies were performed by oral administration of optimized formulation in rabbits.

Results

In vitro studies revealed that the release rate decreased with increase in polymer concentration, polymer viscosity and combination of polymers. The drug release from the matrix tablets followed diffusion mechanism. Comparable correlation of in vitro drug release was observed in the initial and accelerated stability samples of lamivudine matrix tablets prepared with hydroxypropyl methylcellulose alone and its combination with polyethylene oxide. Significant bioavailability was observed in the in vivo evaluation. The C_max, t_max, AUC and K_el for F-3 matrix tablets were 1361 ng/ml, 4 h, 25,013.5 ng min/ml and 0.0719 h⁻¹ respectively. DSC and FT-IR spectra of initial and stability samples showed the absence of drug–excipient incompatibility in the formulations. The developed extended release matrix tablets of lamivudine were stable up to three months.

Conclusions

The release of the matrix tablets for prolonged periods of time employing polyethylene oxide and hydroxypropyl methylcellulose as drug rate retarding polymers could be advantageous than conventional lamivudine tablets. The study could be extended for bioavailability studies in clinical subjects.

Aim

The present study was undertaken to carry out phytochemical analysis and to investigate the antihyperglycaemic effect of aqueous slurry of Curculigo orchioides Gaertn. rhizome powder (ASCO) for 21 days.

Method

Diabetes was induced in Albino Wistar rats by single intraperitoneal administration of streptozotocin (50 mg/kg body weight). Normal as well as diabetic rats were divided into four groups to receive different treatments.

Result

Preliminary phytochemical analysis showed presence of glycosides, mucilage, tannins, steroids, flavonoids, saponins and essential oils. Phytochemical analysis using TLC showed presence of arbutin, bitter principles, cardiac glycosides, coumarins, essential oils, lignans, pungent-tasting principles, saponins, triterpenes and valepotriates. Acute toxicity study in rats did not show any signs of toxicity up to the dose of 2000 mg/kg body weight. In STZ induced diabetic rats, the daily oral treatment with ASCO (1000 mg/kg body weight) showed a significant reduction in blood glucose level. STZ administration severely deteriorated the histological structures of pancreas, kidney and liver of diabetic rats, which were found to be restored to certain extent in glibenclamide and ASCO treated animals.

Conclusion

The study indicated that ASCO is a potential antidiabetic agent and lends scientific support for its use in folk medicines.

Objective

To validate the traditional use of Cissampelos pareira as an antidiabetic agent in streptozotocin–nicotinamide induced diabetic male mice.

Methods

Antidiabetic effect of aqueous extract of C. pareira leaves (CPAE) was evaluated at 250 mg/kg and 500 mg/kg body weight, p.o. doses in male albino mice over the period of 14 days. Random blood glucose level and body weight were observed periodically. Liver glycogen level, organ coefficient and other biochemical parameters were also determined after completion of the study.

Result

Significant (p < 0.001) changes were observed in random blood glucose levels of mice after 14 days of treatment period at 500 mg/kg CPAE treatment. Aspartate transaminase, alanine transaminase, alkaline phosphatase, total bilirubin, triglycerides and creatinine levels were significantly (p < 0.05) decreased while liver tissue glycogen and serum protein levels were significantly (p < 0.05) increased after CPAE administration. No significant changes were observed in body weight and organ coefficient.

Conclusions

The present study concluded that the aqueous extract of C. pareira at 500 mg/kg body weight was capable in reducing diabetic attritions so it might be a valuable candidate for diabetes treatment.

Aim

Phosphotungestic acid (PTA), was used as titrant for the conductometric determination of loperamide hydrochloride (LOP.HCl) and trimebutine (TB) antidiarrhea drugs through ion-associated complex formation.

Method

The effect of the reagent concentration, temperature, molar combining ratio, and the solubility products of the formed ion-associates were studied and calculated.

Results

The suggested method was applied for the determination of loperamide hydrochloride and trimebutine in their pure form and pharmaceutical preparations with mean recovery values of 99.67 and 99.47 % for loperamide hydrochloride in pure form and in Imodium capsule, respectively, and 99.88 and 99.04 % for trimebutine in pure form and in Triton tablets, respectively. Relative standard deviation was less than 1.0%. The accuracy of the method was indicated by excellent recovery while low standard deviation supported the precision of the method. The sensitivity of the proposed method was discussed and the results were compared with the pharmacopeial methods.

Conclusion

The proposed procedure was simple, rapid, sensitive, and accurate and can be applied for the routine measurements of the cited drugs.

Aims/objective

Oral SR gastroretentive dosage forms offer many advantages for drugs having absorption from upper GIT and improve the bioavailability of medications that are characterized by narrow absorption window. Cefdinir is a third generation cephalosporin with broad spectrum of activity with low bioavailability (20–30%) and short biological half life (1–2 h). It has better absorption from upper part of gastrointestinal tract. The purpose of present study was to formulate and develop a new GRDDS using bilayered tablet technology for cefdinir as a model drug.

Methods

Cefdinir bilayer tablets (CBT) were prepared by using double compression cup and core method. First layer, floating matrix layer contained different rate retarding polymers and effervescent mixture. Second layer is loading layer contained cefdinir and fast releasing components (soluble starch, sodium bicarbonate and citric acid). All CBT were evaluated for their pre and post compression parameters.

Results

Precompression and post compression parameter of all CBT were within the pharmacopeial limits. In vitro buoyancy behavior and matrix integrity study revealed that FLT of optimized formulation was 1.57 ± 0.52 min and the tablet remained floatable throughout the study. In vitro drug release of optimized CBT follows initially first order release upto 30 min (till their release of loading layer), then zero order release upto 12 h and kinetic profile followed the Peppas (R² = 0.9838) and zero order (R² = 0.9986). FTIR studies revealed no drug–excipients interactions. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, floatability, matrix integrity.

Conclusion

Kinetics of CBT showed biphasic release in the first phase, immediate dose was released in less than 60 min and second phase was released from matrix layer as a controlled zero order fashion. Cefdinir is a suitable drug for development of gastroretentive bilayer tablet.

Aims

The present study was aimed to study the in vitro antioxidant property by DPPH, superoxide, and hydroxyl radical scavenging assays, in vivo hepatoprotective activity by CCl₄ induced hepatotoxicity in albino rats, formulation of polyherbal hepatoprotective tablets containing equal quantities of methanolic extract of roots of Begonia laciniata Roxb., whole plant of Cuscuta epithymum (L.) L and whole plant of Dendrobium ovatum (L.) Kraenzl., which were used traditionally in Chittoor and Khammam districts of Andhra Pradesh, India.

Methods

Formulation was developed by direct compression method using super tab-11SD, primojel, talc and magnesium stearate as excipients and then subjected to evaluation of precompression and post compression parameters.

Results and conclusion

All the selected plants showed dose dependant antioxidant property, highest at 360 μg dose and significant dose dependant hepatoprotective activity, highest at a dose of 400 mg/kg b.w compared to standard drug silymarin, the histopathological studies also confirmed protective effects of extracts against CCl4-induced liver injuries. The observations from formulation support the ideal properties of compressed tablets and its feasibility for large-scale commercial production.

The present study clearly indicated that the crude ethanol extract of Boerhavia diffusa did produce anthelmintic activity against Indian earthworm Pheretima posthuma. The plant possesses significant anthelmintic activity at 100 mg/ml concentration measured by time taken for paralyze/death of the earth worms. The current investigation leads to conclusion that the leaves of B. diffusa have potent anthelmintic activity of conventionally used drug. The results did not, however, exclude the possibility that doses of the extract with lower anthelmintic activity in this study might be efficacious against other species of helminths. Further studies using in vivo models and to isolate active constituents from extract are required to carry out and established the effectiveness and pharmacological rational for the use of B. diffusa as an anthelmintic drug.

Aim

To study the key pharmacophore requirements for heparanase inhibition and design of new molecules.

Method

Three dimensional quantitative structure activity relationship (3D QSAR) methodologies namely Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) were applied, PLS analysis was performed and QSAR models were generated for a set of 43 bezoxazol-5-yl acetic acid derivatives and 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea reported as potent inhibitors of heparanase.

Result

QSAR model showed good internal and external statistical reliability that is evident from the $q_{\text{loo}}^2$, $r_{\text{ncv}}^2$ and $r_{\text{pred}}^2$. CoMFA model provides a correlation of steric and electrostatic field with biological activities. CoMSIA model provides a correlation of steric, electrostatic, acceptor, donor and hydrophobic fields with biological activities.

Conclusion

The identified key features enabled us to design novel symmetrical 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea derivatives.

Aim

A selective, and sensitive LC–MS/MS method has been developed and validated for quantification of donepezil in human plasma using donepezil D7 as an internal standard (IS).

Methods

The analyte and IS were extracted by liquid–liquid extraction using dichloromethane and hexane mixture and separated by isocratic elution on C18 analytical column with 0.1% formic acid and methanol in the ratio of 70:30 (flow rate of 1 ml/min) as the mobile phase in the positive ion mode. Multiple Reaction Monitoring transitions for donepezil and internal standard are 380.2/91.2 and 387.2/98.2 respectively.

Results

The lower limit of quantification was 50 pg/ml with the linearity range of 50 pg/ml–25,000 pg/ml and the method was validated as per international regulatory guidelines for its selectivity, stability, accuracy, precision, and recovery.

Conclusion

The method can be readily applicable to pharmacokinetic and bioequivalence studies to support different regulatory submissions.