International Journal of Pharmaceutical Chemistry and Analysis

Page No. 193-197

Authors: Jimishaben D. Kher, Jagat Upadhyay

Uncontrolled proliferation is the hall mark of cancer and abnormal cell cycle regulation in cancer. CDK plays very important role in the control of the cell cycle and its proliferation. CDK2 is the “superstar” among the CDK family.CDK2 has cyclin A and cyclin E in its complex which the cyclin A complex require to progress through S phase regulated by phosphorylation and cyclin E require to transition from the G1 to S phase in cell cycle. Also, the mechanism of binding of CDK2 with its inhibitors as well as the changes of binding mechanisms following conformational variation of CDK2 are compared. Considering this fact, inhibition or disruption of the CDK2/cyclin complexes should be possible to suppress the hyper activation of CDK2 and hold back the infinite cell proliferation. There are main four binding site of CDK inhibitors. Competitive binding sites (site 1), Noncompetitive binding sites (site 2 and 3), Allosteric binding site (site 4). CDK inhibitors are mainly used in cancers including leukemia, melanoma, solid tumors and other types are being targeted.

Page No. 205-218

Authors: Krishna R. Gupta, Kiran Keche, Anvesha V. Ganorkar

A simple HPLC method has been developed and subsequently validated for the simultaneous determination of Eperisone hydrochloride and Diclofenac sodium. Optimum chromatographic separations among the eperisone, diclofenac sodium and stress-induced degradation products were achieved by using Waters -ODS 5 μ C18 column (250 X 4.6mm) as stationary phase with Acetonitrile and 0.05% TEA pH 3.5 (75:25% v/v) as mobile phase at a flow rate of 1.0 mL min with detection at 273 nm. ICH guidelines were used to validate the developed method. Linearity was established for Eperisone hydrochloride and Diclofenac sodium in the range of 15-75 µg/ml and 10-60 µg/ml, respectively. Eperisone hydrochloride and Diclofenac sodium were exposed to acid, base and neutral hydrolysis, oxidation and photolytic stress conditions and the stressed samples were analyzed by the proposed method. Also the kinetics of degraded sample was evaluated for all the hydrolytic conditions. As the proposed method could effectively separate the drug from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in combined dosage form.

Page No. 229-234

Authors: Manoj V. Girase, Monika L. Jadhav

The present study was undertaken with an objective to investigate in-vivo and in-vitro immunomodulatory potential of Cassia auriculata Linn. The methanolic extracts of flowers and roots of plant were investigated for their immunomodulatory potential by using in-vivo, oxazolone-induced cell mediated inflammation in rat’s model and various in-vitro immunomodulatory models. Methanolic extracts of both flowers and roots were screened scientifically through various activities models. The result of oxazolone-induced cell mediated inflammation, showed that methanolic flowers extract possesses immunomodulatory potential. While in in-vitro immunomodulatory models like NBT reduction assay by human PMN cells, methanolic flower extract showed dose dependent stimulation. With the same extract similar observation was recorded with phagocytosis of Candida albicans by human PMN. The methanolic flower extract also increased candidacidal activity in dose-dependent manner. The methanolic flower extract significantly induced human PMN cells chemotaxis and exhibited potent effects than positive control. Thus results of in-vitro studies clearly indicated that methanolic flower extract has immunostimulant effect, where as in in-vivo study of oxazolone-induced delayed type hypersensitivity, methanolic flower extract significantly reduced rat ear edema in dose dependent manner. The in-vitro assays, revealed that methanolic flower extract possess potent immunomodulatory activity due to its antioxidant potential. In all, results represented here indicated that Cassia auriculata, in addition to its reputed cytoprotected effects, also passes significant immunomodulatory activity. Thus the flavonoids rich methanolic flowers extract can be exploited in chronic inflammatory condition, such as rheumatoid arthritis usually in combination with conventional drugs to reduce the dose and dose related toxicities of later

110-116

Authors: Gunjan Rao, Anju Goyal

A stability study is a routine procedure which ensures the maintenance of pharmaceutical product safety, quality and efficacy throughout the shelf life. These pharmaceutical products are followed by the guidelines issued by International Conference on Harmonization (ICH), World Health Organization (WHO) or other agencies. Stability testing provides evidence that the quality of a drug substance or drug product under the influence of various environmental factors changes with time. Importance of various methods followed for stability testing of pharmaceutical products, guidelines issued for stability testing and other aspects related to stability of pharmaceutical products have been presented in a concise manner in the present review. This review article includes introduction about stability studies types of stability studies and chemical reactions takes place during degradation etc. This article also includes the forced degradation studies and shelf life estimation of pharmaceutical products.

124-132

Authors: Nilesh Prajapati, Mayank Dalal, Hasumati A. Raj

A simple, specific, precise, and accurate RP-HPLC method has been developed and validated for Xylometazoline Hydrochloride. The mobile phase has been used for separation consisting of buffer (Acetate buffer in water, pH adjusted to 5 with triethyl amine)-Acetonitrile (30: 70, v/v) using phenomenax C18 column with flow rate 1.0 ml/min. Detection wavelength was 240 nm. The method has been linear for the range of 1 – 300 μg/mL with r2 0.999. Drug has been shows 99 to 101 % recovery. ICH Q2R1 guideline has been used for validation of developed analytical method. Drug was exposing to forced degradation condition like hydrolysis, oxidation, thermal and photolytic. Method can well resolve all degraded product as compare to Xylometazoline. The isolate alkali degraded product was characterized by NMR, MASS and IR data. Developed method can routinely used for the estimation of Xylometazoline drug from the dosage form and also for stability sample

143-149

Authors: Kakadiya Dipesh, Malleshappa N. Noolvi

This study was aimed at investigating the antitumor activity of novel 5-substituted 2-oxindole derivatives. A series of oxindole derivatives of N-(1,3,4-thiadiazol-2-yl)benzo[d]thiazol-2-amine were prepared and confirmed by 1H NMR, mass and IR data. These compounds were evaluated for their anticancer activity at National Cancer Institute (NCI), USA by single High dose (10-5 M) in full NCI 60 cell panel. Primary in vitro one dose anticancer assay was performed in full NCI 60 cell panel representing leukaemia, melanoma and cancers of lung, colon, brain, breast, ovary, kidney and prostate. Among them compound 1[D] has showed moderate anticancer activity while compound 3[A-2] has showed significant anticancer activity with overall mean growth percent 38.25. These findings prompt us to further explore the oxindole structure as leading scaffold to design new molecules with potent antitumor activity.

162-167

Authors: Narendra Joshi, Anju Goyal

Introduction: Quinazoline is an important moiety found natural and used for their biological activity, quinazoline always attract scientist due to its broad therapeutic value. In the present research article we prepared a series of fifteen compound by conjugating to prominent therapeutic active moiety to produce synergistic effect to mimic the antidepressant activity of quinazoline. Methods: In the process firstly we synthesized substituted 1, 2, 4-triazole and added to the benzoxazine moiety to synthesized derivatives of quinazolines. all the synthesized compound was screened for antidepressant activity by using The Porsolt forced swimming test, The synthesized compounds (20 mg/kg), imipramine (20 mg/kg), and Fluoxetine (20 mg/kg) suspended in aqueous tween 80 (0.5%), were injected as intraperitoneally (i p) and the mouse forced to swim in water cylinder and the vigorous activity observed. Result: From the synthesized compound Qazo7, Qazo9 and Qazo11 show prominent activity the duration of Immobility is 29.6±0.80, 29.5±1.41 and 29.5±0.62 respectively, compare to standard Fluoxetine and Imipramine. Conclusion: It can be stated that combination of quinazoline with triazole provide effective antidepressant activity, the synthesized compound may be help to develop potent and safe antidepressant moiety.

174-182

Authors: Shweta Sharma, Smrita Singh, Mymoona Akhter, Sarvesh Paliwal

Introduction: The present investigation was undertaken to understand the overlaying problems of mutation in HIV virus leading to failure to combat AIDS. Materials and Methods: In present study Multiple Linear Regression (MLR) analysis was carried on a series of 71(sulfonyl) benzene analogs reported as viral nucleocapsid protein zinc finger modulators for HIV. Results: The MLR model obtained using carbo method (N*N) similarity showing good predictive ability, r 2 (training) = 0.655, r 2 (test) = 0.605. Conclusion: The results indicated that Refractivity Similarity (polarizability and volume) and Shape Similarity are important parameters in predicting the activity of viral nucleocapsid protein zinc finger inhibitors.

66-72

Authors: Sonal S. Khatavkar, Trupti P. Deshpande, Sameer Zayed, Manoj Zingraji Misal, Pranita Kate

In paediatric patients midazolam and ketamine are commonly used as premedicants. This prospective randomized study was conducted to compare the efficacy of oral midazolam versus combination of midazolam and ketamine as premedicants in paediatric age group in 60 childrens. 30 in each group, aged 2-6 years, undergoing major and intermediate surgery were included in the study. Forty five (45) minutes prior to surgery group A received oral midazolam (0.5mg/kg) and group B received oral midazolam 0.25mg/kg and oral ketamine (3mg/kg) in recovery room. The observations included onset of sedation, reaction to emotions, sedation score, response to intravenous cannulation and face mask acceptance. The data was analysed using chi-square test and unpaired t-test. The results observed in midazolam and ketamine group were statistically significant than in midazolam group alone. Intraoperatively, haemodynamic parameters were comparable in both the groups. There was significant post-operative analgesia in midazolam and ketamine (M+K) group. Thus we conclude oral premedication allays anxiety significantly and results in a calm and co-operative patient. Midazolam as well as midazolam and ketamine (M+K) offers sedation of superior quality. No significant side effects were observed in both the groups. Aims: Midazolam and Ketamine are used in children commonly for premedication. Aim of our study was to find premedicant effects of oral midazolam and midazolam with ketamine in children and any advantages of combination of oral midazolam with ketamine. Methods and Material: Sixty children of age group 2–6 years of A.S.A grade 1and 2 were selected. Group A-midazolam [0.5mg/kg] Group B- midazolam [0.25 mg/kg + ketamine 3mg/kg] Both groups received drug orally 45min before surgery in recovery room with monitored anesthesia care. Onset of sedation, reaction to emotions, score of sedation, mask acceptance and intravenous cannula acceptance were studied. Statistical analysis used: Chi square test and Unpaired t-test. Results: Sedation score, anxiolysis, attitude, reaction to Intravenous cannulation, face mask acceptance, reaction to emotions were studied in both groups. Midazolam and ketamine group results were significant than midazolam group. Intra operatively in both groups pulse rate, oxygen saturation, respiratory rate had no significant difference also post operatively no significant difference was observed in above parameters, post-operative analgesia was significantly better in midazolam with ketamine group. Conclusions: Oral premedication provides good pre-operative condition in terms of co-operation and anxiety. Midazolam as well as combination of Midazolam with ketamine offers sedation of superior quality. No significant side-effects were observed in both groups.

80-83

Authors: Santosh V. Gandhi, Rasika R. Korhale, Swati U. Kolhe

The present work was done to evaluate pharmacokinetic parameters of ritonavir standard, ritonavir crystallo co agglomerates and marketed formulation of ritonavir. The aim of formulation of Ritonavir crystallo co agglomerates was immediate drug release and solubility enhancement. The analysis was carried out by HPLC. The parameters evaluated were Cmax, Tmax, area under curve (AUC 0-t, AUC 0-∞), t1/2, k elimination (ke).

90-98

Authors: Gandla Kumaraswamy, Repeudi Lalitha, K. Vijayaprakash

The present work was aimed at method development and validation for simultaneous estimation of Rosuvastatin Calcium and Aspirin by UV-Spectrophotometric method in pharmaceutical dosage form. In UV method 0.1N NaoH as solvent and λmax of Rosuvastatin Calcium and Aspirin were found to be 232 nm and 222 nm respectively. Concentration ranges were found to be 4-20µg/mL for both drugs. The R2 values were found to be 0.996 and 0.999 for Rosuvastatin Calcium and Aspirin respectively. The method was validated statistically and by recovery studies. Percentage Assay and Recovery were found to be 95-105% for Rosuvastatin Calcium and Aspirin. LOD and LOQ ranges were found to be 0.177 and 0.539µg/mL and 0.298 and 0.903µg/mL for Rosuvastatin Calcium and Aspirin respectively. This method was validated using ICH guidelines.

13-17

Authors: Pritam S. Jain, Harshal P. Chaudhari, Pankaj R. Bari, Sanjay J. Surana

A simple, rapid, accurate and economical AUC method has been developed for estimation of Rizatriptan benzoate from bulk and pharmaceutical formulation. The λmax of rizatriptan benzoate in water was found to be 280 nm. The drug follows linearity in the concentration range 6-36 μg/ml with correlation coefficient value 0.999. The proposed method was applied to pharmaceutical formulation and % amount of drug estimated 98.00% – 102.00% was found in good agreement with the label claim. The accuracy of the method was checked by recovery experiment performed at three different levels i.e., 80%, 100% and 120%. The % recovery was found to be in the range 98.00% – 102.00%. The low values of % RSD are indicative of the accuracy and reproducibility of the method. The precision of the method was studied as an intra-day, inter-day variations and repeatability. The % R.S.D. value less than 2 indicate that the method was precise. Ruggedness of the proposed method was studied with the help of two analysts. The above method was a rapid and cost-effective quality-control tool for routine analysis of Rizatriptan benzoate in bulk and in pharmaceutical dosage form.

25-42

Authors: Chaskar Swati G., Chaskar Akshay G., Avhad Pawan S

International Journal of Pharmaceutical Chemistry and Analysis (IJPCA) is the Official Journal of Innovative Publication and is Being Published Since 2014. IJPCA is an international, peer reviewed Quarterly Journal which is devoted to Publish Research and reviews articles in field of pharmacy and the related disciplines of pharmaceutical chemistry. It also publishes Editorial, Short Communications, Case series, case report and letter to editors in all the related fields of Analytical and Pharmaceutical Chemistry. IJPCA Describes the Field of Pharmaceutics is a science of preparing and dispensing drugs. It describes the process involved in turning a new chemical entity into Pharmaceutical.

49-52

Authors: Manoj V. Girase, Monika L. Jadhav, Ashish S. Jain

The Prosopis spicigera Linn. is locally known as Khejri one of the most common medicinal plant of the Indian desert. The plant is very useful and famous especially in desert area due to its spread ability and importance. The plant is known as “Golden tree” or “Wonder tree” of the desert. It is an important herbal plant as mentioned in ancient literature. It is used traditionally in the treatment of various infirmities like leukoderma, leprosy, asthma, dyspepsia etc. The numbers of phytoconstituents like tannins, steroids, flavone derivatives, alkaloids etc. has been isolated from the plant. Pharmacological activities like anti-inflammatory, anticonvulsant, antifungal, anticancer, antidiabetic, hypolipidemic, abortifacient, antioxidant, antimicrobial and wound healing properties have been reported of different plant extracts. The present review deals with phytoconstituents and potential pharmacological activities of Prosopis spicigera.