Informatics Publishing Limited

G. V. Ramana Reddy ¹, S. Vidyadhara ², J. Ramesh Babu ², R. L. C. Sasidhar ², A. Ramu ²

Affiliations
1 Department of Biotechnology, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur – 522 510, Andhra Pradesh, IN
2 Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Guntur - 522 019, Andhra Pradesh, IN

Abstract

Solid dispersions of lovastatin were formulated using pregelatinised starch (PGS) as super disintegrant and were further compressed into tablets by using various diluents such as lactose, dicalcium phosphate (DCP) and microcrystalline cellulose (MCC) to enhance the bioavailability. The solid dispersions were prepared by physical mixing, solvent evaporation and kneading methods. The solid dispersions were found to release the drug faster than the pure drug in dissolution media. The rapid release of poorly soluble lovastatin from solid dispersions was influenced by the proportion of polymer and the method employed for its preparation. Among the three methods employed solvent evaporation and kneading methods were found to be suitable for improving the dissolution rate of lovastatin. The release data was fitted to various kinetic models. The release was found to follow first order kinetics. Some of the dispersions prepared by the solvent evaporation method and kneading method were formulated into tablets with various diluents. The tablet preparations containing different diluents were found to release the drug in the order of DCP>MCC>Lactose. The dissolution rate of tablet formulations prepared with lovastatin solid dispersions (FK1, FS4) were found to release the drug at a faster rate than that of tablets prepared with plain drug.

Keywords

Lovastatin, Pregelatinised Starch, Solid Dispersions.

Full Text

   

S. Vidyadhara ¹, R. L. C. Sasidhar ¹, N. Ramya Krishna ¹, K. Sai Deepika ¹

Affiliations
1 Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram, Chandramoulipuram, Guntur – 522 019. Andhra Pradesh, IN

Abstract

Venlafaxine hydrochloride was formulated as oral controlled release matrix tablets using hydrophilic polymer such as hydroxypropyl methyl cellulose (HPMC K₁₅ M) along with electrolytes. In this work a new attempt was made for in situ interactions between drug and electrolytes were devised to control the release of highly water soluble drugs from oral hydrophilic monolithic systems. Electrolytes such as Calcium carbonate, magnesium trisilicate, sodium bicarbonate were used at different concentrations in various formulations, while drug and polymer concentrations were maintained constantly at 1:1 ratios in all the formulations. These electrolytes were used to monitor matrix swelling and gel properties. These findings indicated that the swelling and gel formation in the presence of ionizable species within the hydrophilic matrices provide an attractive alternative for controlled drug delivery from a simple monolithic system. FTIR studies were carried out for some selected formulations, which indicated that there were no interactions between drug and excipients used.

Keywords

Venlafaxine Hydrochloride, HPMC K₁₅M, Electrolytes, Controlled Release, Matrix Tablets.

Full Text

   

R. L. C. Sasidhar ¹, S. Vidyadhara ¹, N. T. Ramarao ², Y. Srinivasa Rao ³, K. Tejaswi ¹

Affiliations
1 Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur-522 019 (A.P.), IN
2 Chebrolu Hanumaiah institute of Pharmaceutical sciences, Chandramoulipuram, Chowdavaram, Guntur-522 019 (A.P.), IN
3 Alkem Research Center, Industrial Estate, Opposite Talons Police Station, Navi Mumbai - 410 208, Maharashtra, IN
4 Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam - 530 046, (A.P.), IN

Abstract

A simple, accurate and precise reverse phase high performance liquid chromatography (RPHPLC) method has been developed and validated for the simultaneous determination of aspirin and simvastatin in combined dosage form. Separation was performed on a C18 column [ODS column, 250mm × 4.5mm with particle size 5μm. with a mobile phase consisting of acetonitrile: methanol: phosphate buffer (55:30:15) at a flow rate of 1ml/min and UV detection was carried out at 225nm. The developed method was validated for the parameters like system suitability, specificity, linearity, accuracy and robustness according to the ICH guidelines Q2B. Retention times of aspirin and simvastatin were found to be 3.4 and 7.44 respectively. Linearity was found in the range from 10-50μg/mL for aspirin and 2-10μg/mL for simvastatin with correlation coefficients 0.9998 and 0.9999 respectively. The % recovery for 100% spiked level was 99.44 and 101.20 for aspirin and simvastatin respectively. The developed method was accurate, robust, selective, linear and repeatable which could be used for routine analysis of aspirin and simvastatin in their combined dosage forms.

Keywords

Aspirin, Simvastatin, Simultaneous, RP-HPLC.

Full Text

   

S. Vidyadhara ¹, R. L. C. Sasidhar ¹, B. Venkateswara Rao ¹, P. Ratna Kumari ¹

Affiliations
1 Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram, Guntur – 19, Andhra Pradesh, IN

Abstract

The aim of the present work is to develop a simple, accurate, precise and reproducible UV spectrophotometric method for the simultaneous determination of Tenofovir, Efavirenz and Lamivudine in bulk and pharmaceutical dosage form. The stock solutions of the standard drugs were prepared in methanol followed by the further required dilutions with distilled water. This method involves the formation and solving of simultaneous equations at 260nm, 347nm and 272 nm, as absorbance maxima of Tenofovir, Efavirenz and Lamivudine respectively. Beer's law obeyed the concentration range of 10 - 40mcg/mL, 5 - 20 mcg/mL and 5 - 20 mcg/mL for Tenofovir, Efavirenz and Lamivudine respectively. The results of analysis were validated statistically and by recovery studies. The % RSD for the recovery study was less than 2. The proposed method can be effectively used for the simultaneous estimation of these three drugs in bulk and combined tablet dosage form.

Keywords

Tenofovir, Efavirenz and Lamivudine, Simultaneous Equation Method, Method Validation.

Full Text

     

B. Venkateswara Rao ¹, P. Vijetha ¹, S. Vidyadhara ¹, K. Kavitha ¹

Affiliations
1 Department of Pharmaceutical Analysis, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram, Guntur, Andhra Pradesh, IN

Abstract

A simple, precise, accurate, reproducible and economical stability- indicating reverse phase liquid chromatography method was developed and validated for the quantitative simultaneous estimation of Pioglitazone and Glimepiride in marketed formulations. Estimation of drugs in this combination was done with a C₁₈ column (Kromasil 100-5 column, 250mm x 4.6mm) using mobile phase of composition phosphate buffer pH 7: Acetonitrile in ratio 60:40 v/v. The flow rate was 0.8 ml/min and the effluents were monitored at 230 nm. The retention time of Pioglitazone and Glimepiride were 6.71 min and 8.38 min respectively. The method was found to be linear over a range of 10-50 μg/ml for Pioglitazone and 3-15 μg/ml for Glimepiride. The established method proved as reproducible one with a % RSD value of less than 2 and having the robustness and accuracy within the specified limits. Assay of marketed formulation was determined and find with 96% and 98% for Pioglitazone and Glimepiride respectively. The method was validated according to the guidelines of International Council for Harmonization (ICH) and was successfully employed in the estimation of commercial formulations. This liquid chromatographic method can be applied for the qualitative and quantitative determination of selected drugs by the modern chemist.

Keywords

Pioglitazone, Glimepiride, RP-HPLC and Method validation.

Full Text

     

P. Srinivasulu ¹, Ramesh Babu ¹, P. Pavan Kumar ¹, CH. Aruna Kumar ¹, S. Vidyadhara ¹

Affiliations
1 Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Guntur, A.P, IN

Abstract

Background: Co administration of two or more medications to a patient is called polypharmacy. Hence, much attention is required to study the possible drug interaction in the prescription, to reduce the influence of one drug action on the another. Accordingly, the effect of candesartan cilexetil was studied on the blood glucose levels of glimepiride treated normal and diabetic rats. Method: Effect of blood glucose levels were studied by using Candesartan cilexetil and Glimepiride in normal and diabetic albino male rats at a dose of 1.44 mg/kg and 0.09 mg/kg, respectively. The blood samples were collected during the study at the time intervals of 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12 and 24 hours. The samples were subjected to estimation of blood glucose levels using glucometer. Results: The present study was conducted in both normal and diabetic rats. Glimepiride showed its hypoglycemic effect at the 4^th hour, whereas candesartan cilexetil doesn’t show any changes in blood glucose levels in both normal and diabetic rats. In normal rats, candesartan cilexetil doesn’t affect on the blood glucose levels of glimepiride in both single and multiple dose studies. In diabetic rats, the candesartan cilexetil showed significant action on blood glucose levels of glimepiride in multiple dose interaction study but the insignificant effect of candesartan cilexetil in single dose interaction on glimepiride. Hence, the interaction was carefully monitored in type-2 diabetes mellitus patients. Conclusion: The study suggested that candesartan cilexetil has a profound effect on blood glucose levels of glimepiride on long term use; the possible mechanism for the cause is either angiotensin converting enzyme inhibitors improve insulin sensitivity or inhibition of CYP2C9. The study also recommended that caution must be taken while prescribing with the combination of candesartan cilexetil and glimepiride or its analogs.

Keywords

Diabetes, Polypharmacy, Blood Glucose Levels, Candesartan Cilexetil, Glimepiride, Albino Male Rats.

Full Text

   

Pottella Srinivasulu ¹, Padarthi Pavan Kumar ², Ch. Aruna Kumar ², S. Vidyadhara ³, Janga Ramesh Babu ³

Affiliations
1 Acharya Nagarjuna University, Guntur – 522510, Andhra Pradesh, IN
2 Department of Physiology and Pharmacology, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram – 522019, Andhra Pradesh,, IN
3 3Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram – 522019, Andhra Pradesh, IN

Abstract

Bioactive compounds have been a significant therapeutic agent for decades, but the use of bio-active natural metabolites in traditional medicines and the discovery of drugs are still active. Anthraquinones are one of the secondary metabolites that are responsible for colour, fragrance and flavour to the plant; also used as colouring agents in the food and textile industries. The present aim of the study was to evaluate the cytotoxicity of Quinizarine (QNZ) and 2-Methyl Anthraquinone (MAQ) in C8-B4 (microglia cell lines, Mouse), SH-SY-5Y (Neuroblastoma cell lines, Human). As well, the study extended to determine the acute toxicity of these compounds on rat Sprague Dawley. Inhibitory concentration (IC50) was determined for both compounds as well as acute toxicity of MAQ was determined in Sprague Dawley (SD) rat. The IC50 values of MAQ and QNZ were 88.66 μg/ml, 55.33 μg/ml on C8-B4 and 88.68 μg/ml, 108.89 μg/ml on SH-SY-5Y, respectively. The acute toxicity study of fixed doses was carried out in female SD rats for both compounds. The LD50 of QNZ and MAQ were found to be greater than 5000 mg/kg and less than 300 mg/kg, respectively. The haematological investigation did not show any significant variation changes among treated rats. The following biochemical parameters were investigated to include Kidney Function Tests (KFTs), Liver Function Tests (LFTs), lipid profile, electrolytes and Random Blood Glucose (RBG) were found no significant changes in the QNZ treated group as compared with the sham group but elevation of Na+, creatinine and SGOT levels in MAQ treated animals. Gross necropsy showed non-significant alteration upon QNZ administration but Lung inflammation was found in the MAQ group. The histopathological finding suggested no significant alteration in tissue histology in QNZ group but infiltration of neutrophils, lymphocytes and macrophages in MAQ treated group. A high dose of both compounds for Single oral administration did not produce any significant alteration in morphological and behavioural parameters. The histopathological finding also supports the safety of both compounds in SD Female rats.

Keywords

Acute Toxicity, C8-B4, Quinizarine, SH-SY-5Y, 2-methyl Anthraquinone

Full Text

     

Pottella Srinivasulu ¹, Padarthi Pavan Kumar ², Ch Aruna Kumar ², J. Venkateswara Rao ³, S. Vidyadhara ³, Janga Ramesh Babu ³

Affiliations
1 Acharya Nagarjuna University, Guntur – 522510, Andhra Pradesh,, IN
2 Department of Physiology and Pharmacology, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram – 522019, Andhra Pradesh,, IN
3 Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram – 522019, Andhra Pradesh,, IN

Abstract

The present study was intended to screen the antibacterial activity of anthraquinones i.e. 2-Methyl Anthraquinone (MAQ) and Quinizarine (QNZ), isolated from roots of Rubia cordifolia Linn. Minimum Inhibitory Concentration (MIC) of isolated anthraquinones was evaluated against selected gram-positive [Bacillus subtilis (BS) and Staphylococcus aureus (SA)] and gram-negative [Serratia marcescens (SM) and Escherichia coli (EC)] bacterial strains. The MIC was determined by micro broth dilution method using Tryptone Soya Broth (TSB) in 96 well plates as well as by measuring zone of inhibition using nutrient agar medium by the cup-plate method. Absorbance values after micro broth dilution revealed the significant MIC of MAQ as 40 μg/mL against BS, 40 μg/mL of MAQ against SA and 80 μg/mL of MAQ against SM. Whereas, The MIC of QNZ was 20 μg/mL against EC. Percentage zone of inhibition after cup-plate method revealed the significant MIC of MAQ as 39.8% against BS when compared with vancomycin, 88.33% against SA when compared with linezolid, 53.37% against SM when compared with amikacin. Whereas, percentage zone of inhibition revealed the significant MIC of QNZ as 53.76% against EC when compared with ciprofloxacin. Based on the MIC results after both micro broth dilution and cup-plate method, we observed that MAQ has shown considerable antibacterial activity against selected bacteria.

Keywords

MIC, Micro Broth Dilution, Quinizarine, 2-Methyl Anthraquinone.

Full Text