Original Article

Fast dissolving tablets as a novel boon for lipophilic drugs

Anupam K. Sachan*, Kamalesh Tripathi

Dayanand Dinanath College, Institute of Pharmacy, Ramaipur, Kanpur, India

*Corresponding Author. Tel.: +91 9936273358, E-mail address: anupamkrsachan@gmail.com

The objective of this paper was to review the information about Fast dissolving tablet. Methods to improve patient’s compliance have always attracted scientists towards the development of fancy oral drug delivery systems. Among them, fast dissolving drug delivery systems (FDDDS) have acquired an important position in the market by overcoming previously encountered administration problems. FDDDS have the unique property of rapidly disintegrating and/or dissolving and releasing the drug as soon as they come in contact with saliva, thus obviating requirement of water during administration. This is seen to afflict nearly 35% of the general population and associated with a number of conditions like parkinsonism, mental disability, motion sickness, unconsciousness and unavailability of water. To overcome such problems, certain innovative drug delivery systems, like ‘Fast Dissolving Tablets’ (FDT) have been developed. FDTs dissolve in saliva within a few seconds, when put on tongue. Such FDTs can be administered anywhere and anytime, without the need of water and are thus quite suitable for children, elderly and mentally disabled patients. This article describes the existing techniques for fast dissolving oral preparation, highlights their manufacturing process, various modifications in the conventional technique, evaluation parameter, future trends for these evolving forms and patients counseling points for FDDTs.

Keywords: Fast dissolving tablet, Zydis technology, Oral delivery, Freeze drying

Original Article

Development and evaluation of sustained release microparticles of Ketorolac Tromethamine

Vaibhav Rathore*, Praveen Kumar, Rajneesh K. Singh, Rajan Kaushik

Moradabad Educational Trust, Group of Institutions–Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 8449884449, E-mail address: vaibhavsrindia@rediffmail.com

The aim of the present study was to prepare and characterize microparticles for delivery of Ketorolac Tromethamine using EudragitRS100, ethyl cellulose, hydroxy propyl methyl cellulose E5 as polymeric retardant material. Microparticles were prepared by oil-in-oil emulsification method. The effect of process variables on microparticle size, percentage yield, percentage entrapment efficiency and in-vitro release characteristics of microparticles were studied. FT-IR and thin layer chromatography were performed to evaluate interaction between drug and polymer. Morphology of microparticles were characterized by scanning electron microscopy and found that the microparticles were spherical with rough surface. Mechanism of release was found Higuchi and Korsmeyer-Peppas type. This study indicated that the sustained release microparticles of Ketorolac Tromethamine could be prepared successfully by using emulsion solvent evaporation technique.

Keywords: Microparticles, Ketorolac Tromethamine, EudragitRS100, Oil-in-oil emulsification, Characterization

Original Article

Formulation and Evaluation of Mucoadhesive Nasal in-situ Gel of Diclofenac Sodium

Ashok K. Rajpoot*, Hitesh Kumar, Neelam Jain, Harish C. Verma

Moradabad Educational Trust, Group of Institutions–Faculty of Pharmacy, MIT Campus, Ramganga Vihar, Phase-II, Moradabad, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 7599186170, E-mail address: ashokraj009@gmail.com

Intranasal administration represents a viable option for local and systemic delivery of diverse therapeutic compounds. The Physiological range of the nasal mucosal temperature lies between 32-34°C. The aim of this work was to formulate and characterize thermosensitive gels based on Pluronic F127, a thermosensitive polymer, and carbopol 934P, a mucoadhesive polymer, intended for the nasal delivery of Diclofenac sodium. Nasal in-situ gel of Diclofenac sodium was prepared by cold method using different ratio of Pluronic F127 and carbopol 934P.The formulations were optimized based on gelation temperature, gelation time, drug release and mucoadhesive strength. The gelation temperature was found to be between 26.5 ± 1.52 º C to 38.16 ± 1.52 º C and pH was found to be in the range of 4.9 ± 0.814 to 6.1 ± 0.242 respectively. Pluronic F127 can be a promising in situ gelling vehicle for nasal drug delivery system. Sustained and prolonged release of the drug, good stability and biocompatibility characteristics make the in -situ gel dosage forms very reliable.

Keywords: Diclofenac sodium, Pluronic F127, Carbopol 934 P, Nasal in-situ gel

Original Article

Synthesis and anticonvulsant evaluation of benzothiazole derivatives

Laxmi Tripathi^a, Rashmi Juneja^b,a,*

^aMoradabad Educational Trust, Group of Institutions–Faculty of Pharmacy, MIT Campus, Ramganga Vihar, Phase-II, Moradabad, Uttar Pradesh, India.

^b*Department of Pharmaceutical Chemistry, S.D. College of Pharmacy & Vocational Studies, Muzaffarnagar, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 8534954084, E-mail address: rashmi.mpharma.21@gmail.com

A series of substituted N-benzothiazole derivatives and substituted N-benzthiazole2-yl-hydrazides were synthesized and their anticonvulsant activity was evaluated after oral administration in the MES model. The synthesized derivatives showed moderate to minor protection in anticonvulsant screening. Among the synthesized derivatives only BZT-4, BZT-5, BZT-11 and BZT-12 showed moderate activity in MES test. None of the compounds showed neurotoxicity at the maximum administered dose.

Keywords: Benzothiazole, Benzothiazole hydrazide, Anticonvulsant activity

Original Article

Curative Effect of Extractive Phytoconstituents of Psidium Guajava Leaves on Ethylene Glycol Induced Urolithiasis in Experimental Animals

Hemant K. Nagar^a,*, Harinarayan S. Chandel^a, Pawan Rathore^a, Amit K. Srivastava^b, Girjesh Vishwakarma^b, Rajnish Srivastava^c,Mahendra S. Ranawatd^d

^aDepartment of Pharmacology, Truba Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

^bDepartment of Pharmacology, Sapience Bio-analytical Research Lab, Bhopal, Madhya Pradesh, India.

^cMoradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

^dBhupal Nobles’ College of Pharmacy, Udaipur, Rajasthan, India.

*Corresponding Author. Tel.: +91 9993633755, E-mail address:hemant_nagar81@yahoo.co.in

The aim of this study was to investigate the curative effect of extractive phytoconstituents of Psidium guajava leaves on ethylene glycol induced urolithiasis in experimental animals. Urolithiasis was induced in Wistar albino rats by 0.75% Ethylene glycol (v/v) in drinking water for 28 days and preventive effect of ethanolic extract of Psidium guajava leaves (EEPG) was evaluated. The animals were divided into six group’s i.e. normal control, negative control, positive control (Cystone, 750 mg/kg body weight, p.o.) and test (EEPG, 100, 150, and 200 mg/kg body weight, p.o.). All extracts and standard drug were given once daily by oral route from 15th to 28th day. Evaluation parameters such as body weight, urinary volume, urine and serum calcium, oxalate, creatinine, urea and uric acid were evaluated. Kidneys from each animal were removed on the 28th day for histopathological examination. EEPG prevents the reduction in body weight and significantly increased the urine volume. EEPG treatment significantly (P < 0.05) decreased the elevated urinary and serum creatinine, urea, uric acid, calcium and oxalate level. Histopathological examination of EEPG treated showed decreased degenerative changes in the kidney tissue like epithelial cell dissociation, interstitial inflammation within the renal tissue and proximal tubules dilation. Extractive phytoconstituents of Psidium guajava leaves was found to show potential anti-urolithiatic activity.

Keywords: Antiurolithiatic activity, Ethylene glycol, Hyperoxaluria, Psidium guajav

Original Article

Ameliorative effect of Jasminum grandiflorum (L.) leaves against cyclophosphamide (CTX) induced renal and liver toxicity

Deepaa^a,*, Arun Lodhi^a, Rajnish Srivastava^b, Amit K. Srivastava^c, Hemant Nagar^d

^aDepartment of Pharmacology, NRI Institute of Pharmaceutical Sciences, Bhopal-462030, Madhya Pradesh, India.

^bMoradabad Educational Trust, Group of Institutions–Faculty of Pharmacy, Moradabad-244001, (U.P) India.

^cDepartment of Pharmacology, Sapience Bio-analytical Research Lab, Bhopal-462021, Madhya Pradesh, India.

^dDepartment of Pharmacology, Truba Institute of Pharmacy, Bhopal-462030, Madhya Pradesh, India.

*Corresponding Author. Tel .: +91 9027422094, E-mail address: chaudharydeepa22141@gmail.com

In the present study, first we screened the ethanolic extract of Jasminum grandiflorum leaf (EEJG) through the in-vitro DPPH free radical scavenging method for its possible antioxidant activity and was found to posses good antioxidant potential. After that, ameliorative effect of the EEJG was evaluated against Cyclophosphamide (CTX) induced renal and hepatic toxicity. Wistar albino rats were divided into five groups, Group-I, control (0.5% w/v, Carboxy Methyl Cellulose); Group-II, negative control (CTX, 30 mg/kg, i.p, for 15 days); Group-III, (EEJG, 100 mg/kg, b.w., p.o., + CTX 30 mg/kg, b.w., i.p, for 15 days); Group-IV, (EEJG, 200 mg/kg, b.w., p.o. + CTX, 30 mg/kg, b.w., i.p, for 15 days) and Group-V, (received only EEJG, 200 mg/kg, b.w., p.o, for 15 days). Extract and CTX were given once daily for 15 days. Administration of CTX (30 mg/kg, b.w., i.p.) for 15 days induced renal and liver damage as indicated by the serum marker enzymes of liver alanine aminotransferase (SGPT), aspartate aminotransferase (SGOT), alkaline phosphatase (ALP), bilirubin and biochemical parameters for kidney function such as serum creatinine, urea and uric acid. Equivalent to these changes CTX also alters the hematological parameters like RBC, total WBC count and hemoglobin level. Concurrent treatment with EEJG (100 and 200 mg/kg, b.w., p.o.) effectively ameliorate the toxicological changes induced by the CTX through scavenging of free radicals. The Jasminum grandiflorum has potential as adjuvant treatment option to CTX for circumventing the side-effects associated with its antineoplastic applications.

Keywords: Jasminum grandiflorum, Toxicity, Liver, Cyclophosphamide, Flavonoids

Original Article

Hepatoprotective activity of ethanolic extract of stem bark of Berberis aristata against carbon tetrachloride (CCl4 ) induced hepatotoxicity on albino wistar rats

Bhawana Rathi^a,*, Juhi Sahu^a, Sameksha Koul^a, R.L. Khosa^a, Prashant Raghav^b

^aSchool of Pharmacy, Bharat Institute of Technology, Partapur, By-Pass Road, Meerut, Uttar Pradesh, India.

^bPES, College of Pharmacy,50-feet Road, Hanumanthnagar, Srinagar, Bangalore, Karnataka, India.

*Corresponding Author. Tel.: +91 9411483282, E-mail address: bhawanarathi41@gmail.com

Berberis aristata DC (Berberidaceae) is used in Indian traditional medicine. The hepatoprotective activity of Berberis aristata stem bark suspension was studied using CCl4 overdose induced liver damage in rats. The activity was assessed by monitoring various liver functions testing enzymes viz, Serum Glutamate Pyruvate transaminase (SGPT), Serum Glutamate Oxaloacetate Transaminase (SGOT), Serum Alkaline Phosphates (SALP) and total and direct bilirubin in blood serum. When the vehicle treated group l was compared with control group 2 (treated with CCL4 ), there was a significant rise in the level of serum marker enzyme ALP, but no significant difference observed between the vehicle treated group and standard drug treated group. Increased levels of serum SGOT, SGPT, ALP and Bilirubin were observed in CCL4 treated control group. But in different dose levels of EEBA (100 & 300 mg/kg of body weight) treated groups, a significant (p<0.001) reduction of serum SGOT (94.5 ± 3.09, 90.20±0.04), SGPT (45.67 ± 1.58, 43.65 ± 0.08), ALP (61.23 ± 1.59, 58.8 ± 3.25) and bilirubin (total & direct 1.30±0.02, 1.10 ± 0.01) & (0.81±0.02, 0.53±0.03) were observed.

Keywords: Berberis aristata, Hepatoprotective activity

Original Article

Comparative pharmacognostic investigation of stems and barks of Albizia lebbeck

Vipin Agarwala^a,*, Bhupendra Chauhan^b, Himanshu Chaurasia^b, Peeyush Bhardwaj^b

^aAdarsh Vijendra, Institute of Pharmaceutical Sciences, Shobhit University, Gangoh, Saharanpur, Uttar Pradesh, India.

^bInstitute of Pharmacy, Bundelkhand University, Jhanshi, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 8859909070, E-mail address: vip.sanjivani@gmail.com

The standardization of Albizia lebbeck was carried out as per Ayurvedic Pharmacopoeia of India, Pharmacopoeial standard for Ayuvedic Formulation and as per the W.H.O. parameters of quality control for medicinal plants. Albizia lebbeck is wild plant having a number of ethnomedicinal applications. In the present study, the stem and bark of the plant were subjected to comparative pharmacognostical investigation. The study includes macroscopy, microscopy, preliminary phytochemical screening, physicochemical evaluation and fluorescence analysis. Qualitative analysis of plant metabolites like alkaloid, carbohydrates, protein, resins, starch have been carried out.

Keywords: Albizia lebbeck, Pharmacognostic, Phytochemical, Fluorescence analysis

Review Article

Implications of patents on cost of medicines in pharmaceutical industries

Anu Singhai^a,*, A.K. Singhai^b

^aAmity University Rajasthan, Jaipur, Rajasthan, India.

^bLakshmi Narain College of Pharmacy, Bhopal, Madhya Pradesh, India.

*Corresponding Author. Tel.: +91 9826526960, E-mail address: singhaiak@rediffmail.com

The Indian pharmaceutical industry with a market capital of 7.5 billion in 2011- 2012 offers more than 27000 brands of medicines including average new launches of about 2000 products in year. Surprisingly, for the common ailment of pain alone over 3325 brands are available and choosing the most safe and effective drug amongst them is practically not possible by the poor patient. After Supreme Court’s decision in the V.P. Shanta Case[1], medical profession has been brought u/s 2(1) (o) of the CPA 1986. With implementation of the Patent (Amendment) Act 2005, the cost of medicine would be dearer to patients. In 2007, Madras High Court rejected the writ by Novartis which had challenged the validity of the Indian Patent Law. This lead cost benefits through cheaper medicines by Indian Companies like Cipla & Bayer, Delhi HC 2010 paved the way for cost relief to patients after litigating patent issues.

Keywords: Patent, Pharmaceutical industry, Medicines, Trademark, Indian patent law

Original Article

An empirical study on oral contraceptive pills in Moradabad region

Roshani Rajvansh*, Swetam Singh

Moradabad Educational Trust, Group of Institutions–Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

*Corresponding Author. Tel.: +91 9917269050, E-mail address: rajvansh1991@gmail.com

Oral Contraceptive pills (OCPs) are medications taken by mouth for the purpose of birth control. They consist of one or more synthetic female sex hormones (estrogen and progestin or progestin only) that prevent pregnancy by blocking the normal process of ovulation. Centchroman is a nonhormonal oral birth control pill developed that is available in India marketed under the brand Saheli. A market survey was done among the gynecologists and the drug market of Moradabad region on the use of OCPs. Parameters selected were the success rate of OCPs over other contraceptive methods, preferred hormonal combination used by OCP manufacturing units and the preferred active ingredient and brands of emergency OCPs used. It was found that OCPs were the most effective contraceptives than any other method of contraception with very low side effect profile and additional advantage of preventing various types of cancers in women. Pharmaceutical companies prefer cyproterone acetate and ethinylestradiol combination in their combined OCPs as these both hormones together work better in preventing pregnancy. Most of the emergency OCPs contained levonorgestrel as the active ingredient. Among them i-pill (Piramal Life Science) was the most used emergency OCP brand.

Keywords: Oral contraceptive pills, Market survey, Success rate, Emergency OCPs