JPR:BioMedRx:An International Journal
ISSN NO: 2321-4988
BioMedRx journal is devoted to the promotion of Bio, Pharma and related disciplines (including medical, Nursing,Paramedical, Clinical   fields).It seeks to foster multi-disciplinary research and collaboration among scientists, pharmaceutical industries and healthcare sector as well as provide a National and international forum for the communication and evaluation of data, methods and opinions in pharmaceutical sciences and related disciplines.The Editor  welcome contributions of field relevance. Although primarily devoted to original research papers, the journal particularly welcomes reviews on current topics of special interest and relevance.

Manuscripts Published

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000290
Title: Comparative dissolution studies of an extended release formulation of Tolterodine tartrate and Tamsulosin Hcl
Category: Pharmaceutics
Section: Research Article
Country: India
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A comparative study was undertaken on dissolution studies of marketed formulations which contain Tamsulosin HCl (TAM) and Tolterodine Tartrate (TOL) in a combination of 0.4 mg and 4.0 mg respectively in an extended release form. The dissolution method developed was then used to study three marketed formulations, quantification being done using a validated HPLC method. Comparison of dissolution data was done using the Moor and Flanner model independent method which included determination of Similarity factor and Difference factor. The kinetics of the dissolution process were determined by analyzing the dissolution data using four kinetic equations; namely zero order, first order, higuchi square root and hixson Cube root equation. The results obtained were within the acceptance criteria. The kinetic study indicated that the dissolution data followed first order kinetics and hixson Crowell cube root equation as straight line were obtained with a slope of approximately one and small value of intercept.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Pha-0000289
Title: Evaluation of Acute Toxicity for Solanum Xanthocarpum Fruits
Category: Pharmacology
Section: Research Article
Country: India
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The study was designed to evaluate the acute toxicity study of powder of fruits of Solanum Xanthocarpum. The fruits were collected from the basin of river Bhima during summer season in 2012 dried in shade to a constant weight and grinded by high power electric mixture and sieved. The acute toxicity study of fruit powder is carried out as per OECD guideline in Swiss mice weighing 35 to 50 gm. The dose of 2, 4, 6, 8 and 10 gm/kg body weight plant material were administered orally in the form of aqueous slurry. The groups were almost continuously observed for mortality and behavioral changes during first 24 hrs and then daily for fortnight. The observations of changes in body weight, food and water intake as well as cage side observations were reported during acclimatization as well as during study period. There was no abnormality observed in any group. The results provide evidence that Solanum Xanthocarpum fruits were found to be nontoxic in nature.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000288
Title: Formulation, optimization and evaluation of fast disintegrating tablet of hydrochlorothiazide
Category: Pharmaceutics
Section: Research Article
Country: India
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The present study was aimed towards formulation and development of fast disintegrating tablet of hydrochlorothiazide by direct compression method using three different super disintegrating agents. The absorption rate of hydrochlorothiazide is 50-60% and the drug undergoes hepatic metabolism, so the attempt has been made to administer it as fast disintegrating tablet to increase it’s oral bioavailability. Fast disintegrating tablet was formulated using three different super disintegrants in the concentration of 3%, 4 % and 8% alone or in combination of super disintegrants. The formulation is optimized for the concentration of super disintegrants to give minimum disintegrating time with maximum drug release profile. Disintegration time, % friability and In vitro drug release were taken as the basis to optimize the fast disintegrating tablet. On the basis of results of preliminary batches, the formulation H5 containing crospovidone and croscarmellose were selected as independent variables for the 32 full factorial design as it shows less disintegration time with less percentage of friability. A 32 full factorial design was used to study the effect of croscarmellose sodium and crospovidone on disintegration time, % friability and In-vitro drug release. The responses were analyzed using ANOVA and by the polynomial equation, it was found that the concentration of croscramellose sodium and crospovidone significantly affects disintegration time and % friability. Optimized formulation H8 containing crospovidone (6%) and croscarmellose sodium (4%) showed the faster disintegration time (5 to 6 sec), less friability (0.35%) and increased % drug release (99.22% in 30 mins) as compared to other formulations. From the results of 32 full factorial design it can be concluded that crospovidone and croscarmellose sodium in combination is having better disintegrating property than alone or in combination with sodium starch glycolate. Formulation H8 containing 6% crospovidone and 4% croscarmellose sodium gives better disintegration and dissolution profile. Thus combination of crospovidone and croscarmellose sodium can be successfully used in the formulation of fast disintegrating tablets.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000287
Title: Approaches used in Colon Targeted Drug Delivery System: An Overview
Category: Pharmaceutics
Section: Review Article
Country: India
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Colon targeted drug delivery getting the importance day by day as it can be found as a potential site for systemic drug delivery of the most of proteins and peptides. The effective treatment of diseases associated with colon can be easily done with colon targeted drug delivery system. As the prevalence of diseases associated with colon increases day by day due to stress life. It is most important to treat these diseases locally with CTDDS. The present review is an attempt made to reveal the importance of CTDDS in treatment of local diseases associated with colon and the various novel approches designed to achieve desired therapeutic action and bioavailaility.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000286
Title: Novel Controlled Gastroretentive Drug Delivery Systems: A Review
Category: Pharmaceutics
Section: Review Article
Country: India
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Controlled release (CR) dosage forms have been extensively used to improve therapy with several important drugs. However, the development processes are faced with several physiological difficulties such as the inability to restrain and localize the system within the desired region of the gastrointestinal tract and the highly variable nature of the gastric emptying process. This variability may lead to unpredictable bioavailability and times to achieve peak plasma levels. On the other hand, incorporation of the drug in a controlled release gastroretentive dosage forms (CR-GRDF) which can remain in the gastric region for several hours would significantly prolong the gastric residence time of drugs and improve bioavailability, reduce drug waste, and enhance the solubility of drugs that are less soluble in high pH environment. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. Thus, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits to patients. Controlled gastric retention of solid dosage form may be achieved by the mechanisms of floatation, mucoadhesion, sedimentation, expansion or by a modified shaped system. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive dosage forms.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Pha-0000285
Title: Evaluation of Dregea volubilis leaf extract for its potential against stress induced amnesia in experimental rats
Category: Pharmacology
Section: Research Article
Country: India
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The world is focusing more upon the herbal medication for curing various ailments. The trend of validating the plants with traditional medicinal usage is increasing. The present investigation deals with the protective effect of Alcoholic extract of Dregea volubilis leaves (AEDV) against stress induced amnesia. In the present study the extract (250 and 500 mg/kg, p.o) was investigated for its Nootropic potential in normal and stress induced rats. The invitro antioxidant activity was carried out to correlate its protective affect against stress. Conditioned avoidance response using Cook’s pole climbing apparatus was used in normal and stress induced rats to assess cognitive-improving activities. The invitro antioxidant activity was carried out by reducing power assay. Daily administration of Dregea volubilis at doses of 300 and 500 mg/kg, p.o enhanced cognition in dose dependent manner in normal rats. Fast retrieval was observed in extract treated stress induced rats, compared to that of stress control group. In Ferrous reducing power assay significant increase in absorbance was observed with extract in dose dependent manner and the results were comparable with that of standard, Ascorbic acid. The present study justifies scientific support for the protective effect of Dregea volubilis against stress induced amnesia & useful in combating the stress induced CNS disorders.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-PDRS-0000283
Title: Hepatoprotective effect of methanol seed extract of Sphenostylis stenocarpa (Hoschst ex. A. Rich, Harms) against carbon tetrachloride induced liver toxicity in wistar rats
Category: Plant Drugs Related Study
Section: Research Article
Country: India
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The present study was carried out to evaluate the effect of methanol seed extract of Sphenostylis stenocarpa (African yam bean) on some antioxidant and liver marker enzymes of rats treated with CCl4 as well as the acute toxicity test of the extract. Twenty four (24) Wistar rats were randomly distributed into 6 groups of 4 rats each. Group 1 rats were not induced with CCl4 and were given normal rat feed and water (normal control). Groups 2-6 were induced with CCl4. Group 2 rats received no treatment (negative control) and those in group 3 received 300 mg/kg body weight of ascorbic acid (standard drug). Groups 4, 5 and 6 were treated respectively with 200, 400 and 800 mg/kg body weight of S. stenocarpa methanol seed extract. The acute toxicity test (LD50) of the extract showed no toxicity up to 5000 mg/kg body weight. This showed that the seed of the plant is safe for human and animal consumption. The glutathione concentration, catalase and superoxide dismutase activity of the rats increased significantly (p<0.05) in a dose dependent manner in all the treatment groups. The methanol seed extract had a positive effect on the antioxidant enzymes of rats treated with CCl4. There were no significant (p>0.05) increase in the alanine aminotransferase, Aspartate aminotransferase and alkaline phosphatase activity of rats in all the treatment groups. These suggest that S. stenocarpa seeds possess some antioxidant and non-hapatotoxic properties.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000282
Title: Hydrogel based biodegradable enteric coated alginate beads for colon targeted drug delivery of embelin
Category: Pharmaceutics
Section: Research Article
Country: India
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Alginate, a natural polysaccharide has been extensively used as a matrixing agent for number of allopathic drugs. In the present investigation attempt is made to develop a sustained release multi particulate dosage form containing herbal molecule. Embelin, a well-proven anthelmentic from herbal origin was formulated in to gel beads of sodium alginate. A 23 full factorial design has been adopted for optimization of cross-linked sodium alginate beads containing embelin. Sodium alginate (10% w/v) was used as a polymer. Based on preliminary studies, the constraints of independent variables X1 (concentration of cross linking agent), X2 (type of hardening agent) and X3 (drying temperature for beads) have been fixed. The dependent variable that has been selected was Y1 (time taken for 80% drug release from beads, T80). The application of factorial design gave systematic approach in optimization on formulation variables. Concentration of cross linking agent (10% and 20% CaCl2) and type of hardening agent (Isopropyl alcohol and Glutaraldehyde) were found to be effective in controlling the gel bead size and T80. The drug release was found to follow Korsmeyer model of diffusion. A USP dissolution guideline, similarity factor f2 for drug release from gel beads with and without colonic fluid showed dissimilarity in drug release pattern. Further, optimized gel beads were film coated with HPMC phthalate to prevent the early release of embelin in upper GI tract and allowing majority of drug to release in lower intestine.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-HPRS-0000281
Title: A prospective clinical evaluation of quality of life and co–morbidity of patients with chronic blood transfusion and chelation therapy
Category: Hospital Pharmacy Related Study
Section: Research Article
Country: India
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The patient with hemoglobinopathy like Thalassemia major (TM), Bone marrow dysfunction, and Sickle cell disease are requiring chronic blood transfusion in their life time to survive. Among these, thalassemia major is one of the most common hemoglopinopathy in world wide. This study was done to assess the quality of life of the patients with chronic blood transfusion and chelation therapy. The Quality of Life Scores were obtained through the self-administered SF-36 questionnaire. The study subjects were asked to answer the SF-36 questionnaire every three months once. After 6 months the SF 36 General Health mean score was 63.58 ± 12.98 (P < 0.05). The highest mean score was 69.37 ± 11.61. The mean difference after the final reviews was statistically significant. The preponderance of scores used to assess quality of life suggests that there is a direct and independent effect on quality of life when treated with transfusion and ironchelation therapy.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-IALI-0000280
Title: Preliminary phytochemical analysis, antibacterial activity and GC-MS analysis of Kalanchoe floribunda Wight&Arn.
Category: Instrumental analysis led to identification
Section: Research Article
Country: India
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Traditional medicine also known as indigenous or folk medicine comprises medical knowledge systems that developed generations with in various societies before the era of modern medicine. In the present study deals with the phytochemical, antibacterial activity and GC-MS analysis of the medicinal plant Kalanchoe floribunda Wight & Arn. Qualitative phytochemical analysis of these plants confirms the presence of various secondary metabolites like alkaloids, phenols, proteins, saponins, sterols. Antibacterial activity of Kalanchoe floribunda leaf extracts (Ethyl acetate, Ethanol and Distilled Water) on pathogenic bacterial strains (Enterobacter aerogenes, Escherichia coli, Klebsiella oxytoca, Proteus mirabilis and Salmonella typhi) was tested by agar well diffusion method. Ethyl acetate leaves were also should maximum inhibition on Enterobacter aerogenes (10mm) and Klebsiella oxytoca (10mm). Seven compounds were identified in the ethyl acetate extract of Kalanchoe floribunda by Gas Chromatography Mass Spectrometry (GC-MS) analysis.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Pha-0000278
Title: Toxicity testing strategies – current innovations and future outlook
Category: Pharmacology
Section: Review Article
Country: India
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Humans are often exposed to chemicals in the form of pharmaceutical substances, household products, pollutants and it is vital to screen these chemicals for their toxicity so that it can be used safely without subjecting human lives at risk. Scientific advancements in the field of toxicology paved a better platform for evaluating these chemicals. A plethora of techniques are used for this purpose which includes toxicity test using animals, in vitro testing methods for enhanced toxicity testing (cell culture systems, stem cells, toxicogenomics, in silico techniques - Toxicity database, QSARs, Human knowledge-based methods) etc. These techniques vary in their scope, use, reliability, limitations so a search is needed to find out a testing method which fulfils all aspects of a testing method. This review highlights the general toxicity testing approaches, current developments in the field of toxicology, basics and significance of alternative testing methods in toxicological research for enhanced toxicity testing.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000277
Title: Formulation and evaluation of venlafaxine hydrochloride mouth dissolving tablets by effervescent technique
Category: Pharmaceutics
Section: Research Article
Country: India
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Venlafaxine hydrochloride is used in the treatment of depression and anxiety disorders. The objective of the present study was to prepare the mouth dissolving tablets of venlafaxine hydrochloride by effervescent method. sodium bicarbonate, citric acid and tartaric acid were used as effervescent agents. Tablets are prepared by direct compression process with crosscaremellose sodium and sodium starch glycolate as super disintegrants and mannitol as bulking agent. The prepared tablets were evaluated for hardness, friability, in vitro dispersion time, weight uniformity, wetting time and for in vitro drug release. Further the tablets were characterized by Fourier Transform Infra Red Spectroscopy and by Differential Scanning Calorimetry. Among all the formulations the tablets prepared by with sodium starch glycolate as super disintegrant and tartaric acid and sodium bicarbonate as effervescent agents showed faster disintegration and rapid drug release.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-PDRS-0000276
Title: In vitro evaluation of the anthelmintic and antibacterial activities of three nigerian medicinal plants
Category: Plant Drugs Related Study
Section: Research Article
Country: India
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The methanol extracts of the leaves of Asystasia gangetica, roots of Urtica dioica and whole plant of Spigelia anthelmia were screened for anthelmintic and antibacterial activities using in vitro models. Anthelmintic test was done using the local earthworm Nsukkadrilus mbae, while antibacterial activity against laboratory strains of Eschericia coli, Staphylococcus aureus and Bacillus subtilis were evaluated by agar diffusion technique. Extracts of the three plants caused a significant (P<0.05) concentration-related reduction in time of onset of paralysis and death of Nsukkadrilus mbae compared to piperazine. The magnitude of anthelmintic effect was in the order S. anthelmia > A. gangetica > U. dioica. In the antimicrobial activity test, only S. anthelmia inhibited microbial growth with magnitude of susceptibility in the order E. coli > S. aureus > B. subtilis, and minimum inhibitory concentrations (MIC) of 11.69, 12.59 and 14.42 mg/ml respectively. In conclusion, extracts of A. gangetica, U. dioica and S. anthelmia have significant anthelmintic activity, while S. anthelmia also possesses antibacterial activity against E. coli, S. aureus and B. subtilis.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-PDRS-0000275
Title: GC-MS analysis, antioxidant and antibacterial activities of Thespesia populnea Linn. Leaf – in vitro study
Category: Plant Drugs Related Study
Section: Research Article
Country: India
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Thespesia Populnea (T. populnea ) Linn has been used conventionally to treat various diseases like rheumatism, diabetes and also as an anti-inflammatory agent. In this study, ethanolic extract of T. populnea leaves was screened for chemical constituents (Chemical methods and GC-MS analysis) and pharmacological properties such as antioxidant capacity (DPPH and ABTS models) and antibacterial property (Agar-well diffusion and micro broth dilution methods) by in vitro assays. The leaf extract showed significant antioxidant and antibacterial activities. Preliminary phytochemical screening discloses the presence of bioactive constituents including flavanoids phenols and alkaloids. Results of GC-MS analysis showed 19 different phytocompounds. The present results suggest that the ethnopharmacological role of T. populnea could be attributed from active principles.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-PDRS-0000274
Title: Effect of geographical properties on the phytochemical composition and antioxidant potential of Moringa oleifera flowers
Category: Plant Drugs Related Study
Section: Research Article
Country: India
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Moringa oleifera is a major tropical plant with highly valued nutritional and medicinal properties. The present study is undertaken to analyze the phytochemistry and antioxidant activity of the flowers of this plant and study the influence of the geographical properties on them. Antioxidant activities of extracts of M. oleifera flowers from four different districts of Tamilnadu, India with varying geographical properties, were investigated. Free radical scavenging potential was evaluated in vitro by using diphenyl-picryl-hydrazyl (DPPH) assay. Other antioxidant assays like Hydroxyl radical scavenging assay, Superoxide Anion Radical scavenging assay, Metal chelating assay, Phosphomolybdenum assay, Ferric thiocyanate (FTC) method, Thiobarbituric acid (TBA) method were also adopted. Phytochemicals in the flower extracts were screened qualitatively. Phenol and flavonoid contents of the samples were estimated. Significant differences were observed in the antioxidant machinery of the extracts. Though the presence of phytochemicals among the samples remained the same, their quantity varied as noticed from their phenol and flavonoid contents which correlated to their antioxidant activities. The methanol extract of M. oleifera flowers from Tirunelveli district with loamy red soil, moderate monsoon and less pollution, exhibited the highest antioxidant potential. Its phenol and flavonoid contents also seemed to be maximum when compared with the other samples. Results suggested the profound effect of geographical properties on the phytochemical composition which further influenced the antioxidant potential of M. oleifera flowers.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-PDRS-0000273
Title: Isolation and Characterization of Bioactive Compounds from the Petroleum Ether Extracts of Leaves of Xanthium Strumarium Linn.
Category: Plant Drugs Related Study
Section: Research Article
Country: India
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Objective: Xanthium strumarium Linn. belonging to the family compositae, commonly known as ‘burweed’ and chotagokhru in hindi contains a number of phytoconstituents such as alkaloids, phytosterols, glycosides, bioflavonoids, phenols, terpenoids and sugar. The objective of the present study was to isolate and characterize phytoconstituents from the petroleum ether extract of leaves of Xanthium strumarium Linn. Methods: Petroleum ether extract was saponified with alcoholic KOH and then subjected to column chromatography and eluted with different solvents of increasing polarity, composed of hexane, chloroform, ethyl acetate to isolate the constituents. Isolated compounds were purified by PTLC, CC and recrystallization method. The structure of the isolated compounds was established on the basis of spectroscopic evidences (IR, UV, 1HNMR, 13CNMR, MS). Results: Phytosterol such as stigmasterol, β-sitosterol and two long chain alcohols pentatriacontan-1-ol and tritriacontanol isolated from the petroleum ether extract of leaves of the plant. Conclusions: Xanthium strumarium contains stigmasterol, β-sitosterol, pentatriacontan-1-ol and tritriacontanol which are responsible for various pharmacological activities of the plant.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Pha-0000272
Title: In vitro antioxidant activity of Sophora interrupta by ABTS and hydrogen peroxide method
Category: Pharmacology
Section: Research Article
Country: India
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The aim of the study was to evaluate the antioxidant property of Sophora interrupta which belongs to the family Fabaceae. To carry out this study, the methanolic extract of the whole plant was used. The methods used were hydrogen peroxide and ABTS methods. In both methods Ascorbic acid was used as the standard. In Hydrogen peroxide method, the IC50 value of the extract was found to be 112µg and the IC50 of Ascorbic acid was found to be 37µg. In ABTS method, the IC50 of the extract was 135µg and Ascorbic acid was 37µg.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000271
Title: Diclofenac potassium–loaded dika fat solid lipid microparticles: in vitro and in vivo characterisation
Category: Pharmaceutics
Section: Research Article
Country: India
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The aim of the work was to formulate diclofenac potassium-loaded SLMs and evaluate the in vitro and in vivo properties of the solid lipid microparticles (SLMs). Diclofenac potassium-loaded SLMs were prepared by hot homogenization technique using admixtures of Phospholipon® 90G and dika fat (1:1, 1:2 and 2:1 %w/w) as the lipid matrix. Characterisation based on particle size, particle morphology, pH, drug content and encapsulation efficiency were carried out on the lipospheres. In vitro release was carried out in simulated intestinal fluid (SIF) without enzymes (pH 7.4) using the USP paddle method. Anti-inflammatory and ulcerogenic properties of diclofenac potassium-loaded SLMs were studied. From the results, the photomicrographs revealed spherical particles that ranged from 1.82 – 2.90 µm. SLMs formulated with lipid matrix 2:1 and containing 0.25 % diclofenac potassium had the highest encapsulation of 72 % and was significantly different from the other batches (p < 0.05). The in vitro release showed that SLMs having higher ratios of phospholipid (LM 2:1) i.e. batches C1 to C3 had more prolonged drug release rate with maximum drug release at 100 min, while SLMs formulated with lipid matrix having equal concentration of phospholipid and dika fat (A1 – A3) or having higher amount of dika fat (B1 – B3) exhibited faster release of drug with maximum drug release at 90 min. Diclofenac potassium SLMs prepared exhibited good anti-inflammatory properties and also inhibited the ulcerogenic potentials of diclofenac potassium. Therefore, diclofenac potassium-loaded SLMs exhibited good in vitro and in vivo properties.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000279
Title: Formulation development and evaluation of terbutaline sulphate mucoadhesive buccal tablets
Category: Pharmaceutics
Section: Research Article
Country: India
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Mucoadhesive drug delivery system is bind to the gastric mucin or epithelial cell surface are useful in drug delivery for increasing the intimacy and duration of contact of drug with the absorbing membrane, this helps in sustained release of drug and prevent the metabolism of drug in gastric pH condition for the drug sensitive for acidic condition. In this work, the attempt has made to develop and evaluate the Mucoadhesive Buccal tablets of Terbutaline sulphate with natural polymers gaur gum, with ethyl cellulose as back layer of bilayer tablets. Terbutaline sulfate is a white to gray-white crystalline powder. It is odorless or has a faint odor of acetic acid. Terbutaline sulfate is indicated in for the prevention and reversal of bronchospasm in patients 12 years of age and older. With asthma, COPD and reversible bronchospasm associated with bronchitis and emphysema. Because of its first pass metabolism its bioavailability is in the range of 30 to 50% by orally. I R Spectroscopy did the compatible study between polymers and Terbutaline sulphate and No interaction was found between drug and polymers. Different formulations of oral Mucoadhesive buccal tablets of Terbutaline Sulphate (TS) were prepared using polymer Gaur gum, in different concentrations by direct compression. Post compressed evaluation studies, hardness, thickness, friability; weight variation and drug content, mucoadhesive strength of tablets were studied. The in-vitro release of TS was studied in buffer pH 6.8 at 370C. All parameters of TS buccal tablets are passed the standard of mucoadhesive buccal tablets. It was found that mucoadhesive natural polymers exhibited better adhesiveness and mucoadhesiveness. The in vitro study of TS exhibited greater drug release profile with release of in the range of 80.57 to 100.81%.

Journal: JPR:BioMedRx:An International Journal, Volume: 1, Issue: March
Article Id: JPRS-Ph-0000284
Title: Factorial Studies on Enhancement of Solubility and Dissolution Rate and Formulation Development of Efavirenz Tablets Employing β Cyclodextrin and Soluplus
Category: Pharmaceutics
Section: Research Article
Country: India
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Efavirenz, a widely prescribed anti retroviral drug belongs to class II under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limited and it requires enhancement in the solubility and dissolution rate for increasing its oral bioavailability. The objective of the study is to enhance the solubility and dissolution rate of efavirenz by cyclodextrin complexation along with Soluplus and to evaluate the individual main effects and combined (or interaction) effects of β cyclodextrin (βCD) and surfactant (Soluplus) on the solubility and dissolution rate of efavirenz in a series of 22 factorial experiments. The solubility of efavirenz in four selected fluids containing βCD and Soluplus as per 22 factorial study was determined. Solid inclusion complexes of efavirenz-βCD were prepared with and without Soluplus by kneading method as per 22-factorial design and were evaluated. The feasibility of formulating the drug- βCD- Soluplus complexes into compressed tablets was also evaluated in a 22 factorial study . The individual and combined effects of βCD and Soluplus in enhancing the solubility, dissolution rate and dissolution efficiency of efavirenz were highly significant (P < 0.01).βCD alone gave a 2.14 fold increase in the solubility of efavirenz. Combination of âCD with Soluplus resulted in a much higher enhancement in the solubility of efavirenz, 86.96 fold than with âCD alone. Soluplus alone gave a much higher enhancement (289.49 folds) in the solubility of efavirenz. Combination of βCD with Soluplus also gave significantly higher dissolution rates (K1) and dissolution efficiency (DE20) when compared to βCD alone. βCD alone gave 2.00 fold increase and in combination with Soluplus, it gave 7.34 fold increase in the dissolution rate of efavirenz. Efavirenz – βCD, Efavirenz – Soluplus and efavirenz –βCD – Soluplus inclusion complexes could be formulated into compressed tablets by direct compression method. Efavirenz dissolution was rapid and higher from the tablets formulated employing drug- βCD- Soluplus inclusion complexes when compared to the tablets containing efavirenz alone. The tablets formulated employing drug- βCD- Soluplus inclusion complexes fulfilled the official (I.P 2010) dissolution rate test specification of NLT 70 % in 30 min prescribed for efavirenz tablets. The individual as well as combined effects of the two factors involved i.e., βCD (factor A) and Soluplus (factor B) were highly significant (P< 0.01) in enhancing the dissolution rate (K1) and dissolution efficiency (DE 30) of efavirenz. Soluplus alone also gave a higher enhancement in the dissolution rate and dissolution efficiency of efavirenz and efavirenz tablets. Hence a combination of βCD with Soluplus and / or Soluplus alone is recommended to enhance the solubility, dissolution rate and dissolution efficiency of efavirenz, a BCS class II drug and its tablet formulations.