International Journal of Pharmaceutical Chemistry and Analysis

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.

154-160

Authors: Pritam S. Jain, Prashant V. Bhadane, Harshal P. Chaudhari, Sanjay J Surana

A simple, rapid, accurate and economical Area under Curve method has been developed for estimation of Midodrine hydrochloride from bulk and pharmaceutical formulation. The λ max of Midodrine hydrochloride in water was found to be 289 nm. The drug follows linearity in the concentration range 12-84 μg/ml with correlation coefficient value 0.999. The proposed method was applied to pharmaceutical formulation and % amount of drug estimated 97.00% – 101.00% 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 97.00% – 101.00%. 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.

170-181

Authors: Palaniappan Senthilkumar, Kullampalayam Krishnasamy Sivakumar, Gayam Krishnareddy, Sanju Kaladharan

Eight hybridized pyrazolone analogs were designed, docked, synthesized by microwave technique and evaluated for their in-vitro antimicrobial property against four Gram positive, four Gram negative bacterial strains and two fungal strains. Chalcone derivatives of pyrazolone moiety 5a, 5b, 5f, 5g and 5h shows good antibacterial activity aganist Gram positive strains (Percentage zone of inhibition range 68 to 100% with MIC range 12.5-50 μg/mL) compared with Ciprofloxacin (bacteria) and Clotrimazole (fungal). Compound 5h showed good binding at the active site of the protein with docking score -8.69 and shows hydrogen bonding with Arg 58, Arg 136 and electronic interactions with Asp 34, Glu 38. All other compounds shows mild to moderate activity against all the screened micro-organisms tested.

187-191

Authors: Shapali Anil Bagde, Namrata Jadhav, Nikhil Mali, Manisha Karpe

Clinical efficacy of topical antifungal therapy depends on the drug ability to penetrate into the stratum corneum (SC) and the duration of treatment. The mechanism of action for antifungal activity of the bifonazole (BFZ) is the inhibition of ergo sterol biosynthesis, an essential step in the membrane formation of fungal cells. BFZ is indicated in the treatment of superficial fungal infections of the skin such as dermatophytoses, cutaneous candidiasis and pityriasis versicolor. Thus, topical gel of bifonazole with increased bioavailability will be favorable for the treatment of fungal infections and symptomatic relief. The objective of the present work is to compare the antifungal activity of BFZ gel formulated using two drug delivery system; micro emulsion and micro sponge drug delivery system. Microemulsion was prepared by oil titration method. Quassi emulsion solvent diffusion-evaporation technique was used for the preparation of micro sponges. The formed micro emulsion and micro sponges are then incorporated into gel. In vitro antifungal activity of micro sponge based gel and micro emulsion based gel was compared using cup plate method.

120-122

Authors: Asif Husain, Aftab Ahmad, Shah Alam Khan, Mymoona Akhter

The aim of this study was to evaluate the in vitro anthelmintic activity of 2-Arylidene-4-(substituted aryl) but-3-en-4-olides (I-IX) against Indian earthworm i.e. Pheretima posthuma. The anthelmintic activity of nine butenolide derivatives was determined by recording the mean paralyzing and death times of the worms at concentration of 2 mg/mL. The results indicated that few of the tested butenolide derivatives possess significant anthelmintic activity comparable to positive control, albendazole.

130-135

Authors: Pankaj Baboo, S.K.Gupta

Ethyl N-Succinimido acetate was synthesized by equimolar condensation of succinimide and ethylchloroacetate by refluxing in presence of anhydrous potassium carbonate. Then Ethyl N-succinimido acetate was refluxed with hydrazine hydrate in presense of 1, 4-dioxane to obtain N-Succinimido acetylhydrazide, which was further treated with benzaldehyde to get phenyl succinimido acetylhydrazide, this compound was cyclized with mercaptoacetic acid to get the 3-(2-phenyl 4-oxo-1,3-thiazolidine) acetamido succinimide which was reacted with various aldehyde to get the 5-Arylidene-3-(2-phenyl 4-oxo-1,3-thiazolidine) succinimido aceto hydrazide. The formation of title compounds confirmed by physical and spectral data. The synthesized compounds were subjected to microbiological screening.

139-142

Authors: Sankalp Yadav, Gautam Rawal

The low income countries are having a number of issues related to public health. One such very important issue is the practice of self-medication which is prevalent in such countries. There are multiple factors present in these countries that have led to widespread self-medication. The present article highlights this grave problem prevalent in the low income countries.