bluuebunny/crossref_metadata_2025_split huggingface dataset:
Linagliptin loaded Solid-SMEEDS for enhanced solubility and dissolution: Formulation development and optimization by D-optimal design
Authors: Patel Madhubhai M , Patel Rahulkumar J 
Published: April 2019

The aim of the present investigation was to formulate and evaluate solid self-micro emulsifying drug-delivery systems (S-SMEDDS) to improve solubility and dissolution profile of Linagliptin. Solubility of Linagliptin in different oils, surfactants and co-surfactants was assessed and optimizations of pseudo-ternary plots were also carried out for preparation of liquid SMEDDS. D-optimal design mixture was used in the optimization of Linagliptin loaded liquid SMEEDS. The optimized SMEEDS were characterized for globule size, zeta potential, dilution stability, transmittance, pH and in-vitro release profile. The morphology of the Linagliptin SMEEDS was observed by Transmission Electron Microscopy (TEM). Among the different silicates, Nusillin US2 was used as the solid carrier/absorbent to formulate S-SMEEDS of Linagliptin. Improved in-vitro dissolution profile of optimized formulation was observed, resulting in multifold improvement in the absorption profile of Linagliptin as compared with pure drug. In a nutshell, this optimized S-SMEDD formulation holds great promise for enhancement of its physiochemical and biological attributes.
Keywords: Linagliptin, Solid Self-micro Emulsifying Drug Delivery Systems, D-optimal design, Zeta-potential, Transmission Electron Microscopy
Pharmacological Activity of a Polyherbal Formulation by Haemoglobin Glycosylation Assay
Authors: Chauhan Bhupendra , Ali Zulphikar , Naseer Md. Arif , Singh Ranjit 
Published: April 2019

Present study involves the development of a polyherbal formulation by using four different herbs i.e. Chirata (Swertia chiratia), Haldi (Curcuma longa), Neem (Azadirachta indica), Gudmar (Gymnema sylvestre), Ashwagandha (Withania somnifera), Gokharu (Pedalium murex), Methi (Trigonella foenum-graecum), Jammun (Syzygium cumini), relating to antidiabetic activity. Freshly collected and authenticated herbs were characterized by studying its morphological and pharmacognostic character. Antidiabetic and antioxidant activity of the formulation was determined by in vitro haemoglobin glycosylation assay and H2O2 radical scavenging method respectively. In the above study it was found that ethanolic extract of polyherbal formulation possess promising antidiabetic and antioxidant activity which can be consider for further biological investigation.
Keywords: polyherbal formulation, Swertia chiratia, Curcuma longa, Azadirachta indica, Gymnema sylvestre, Withania somnifera, Pedalium murex, Trigonella foenum-graecum, Syzygium cumini
Superdisintegrant: crucial elements for mouth dissolving tablets
Authors: Santosh Kumar Rada , Kumari Annu 
Published: April 2019

Mouth dissolving tablets have gained more popularity among solid oral dosage forms. They perform better than conventional tablets because of its ease of administration and patient’s compliance. It facilitates water less administration and rapid onset of action. It also helps in improving oral bioavailability. The fast disintegration followed by dissolution leads to quick therapeutic activity makes these tablets superior over available tablets and capsules. Disintegration is an important key step for any solid dosage forms to show its pharmacologic effect as any solid dosage forms should disperse into its fine particles from which it is prepared. In mouth dissolving tablets superdisintegrants are incorporated in right amount for quick disintegration with improved bioavailability. Based on the source various types of superdisintegrants are available. They are synthetic, semi-synthetic, natural, and co-processed. In this review, main emphasis is given on different types of superdisintegrants used in mouth dissolving tablets, their mechanisms and applications.
Keywords: Superdisintegrants, Mouth dissolving, Disintegration, Bioavailability
Ayuvedic approach in Primary Biliary Cholangitis (PBC): A case study
Authors: Gupta Deepika , Joshi R. K. , Padhar Bharat , Agrahari Rajesh 
Published: April 2019

Despite of countless facilities and highly developed technologies for the treatment of diseases in modern medical science, there are many diseases which has no medical cure other than prophylactic treatment while the disease is progressing and needs organ transplant in last stage, one such disease is Primary Biliary Cholangitis (PBC). A 65 year old female patient presenting with pain in upper abdomen (Udarshool), decrease appetite (Agnimandhyata), weakness (Daurbalyata), distension of abdomen (Kuchheradmanam), bilateral mild pedal edema (Ubhaypaad-shoth), itching (Kandu), muscular and bony pain (Mansasthishool) diagnosed as Yakritpleehodar Roga, a subtype of Udar roga was brought to Hospital National Institute of Ayurveda, Jorawarsingh Gate, Jaipur, Rajasthan. The patient was treated on the basis of Ayurvedic principles of treatment of Udar roga. According to Ayurveda, the principle of treatment of Udar roga includes Nitya Virechan (purgation), Agnideepan (increasing appetite), Yakituttejan (stimulation of Liver), Mutra Virechan (diuresis) and Ksheer Prayoga (use of milk as diet) for Balprapti (increasing strength of patient). Appreciable result were observed in the form of decreased abdominal pain, decreased abdominal girth, decreased pedal edema, decreased weakness, decreased muscular and bone pain, increased appetite, decrease in fibrotic changes of Liver, resolution of Ascites, decrease in size of Spleen along with significant improvement in other laboratory investigations.
Keywords- Ksheer Prayoga, Jalodar, Primary Biliary Cholangitis, Udar roga, Yakritpleehodar Roga.
In-Vitro antiurolithiatic activity of aqueous extract Pavonia lasiopetala
Authors: Ramprasad R. , Nilsha Anil , Hameed S. Shahul , Shifama Junuha M R , Venkateshan N. 
Published: April 2019

Background: Upto date, the scientific documentation regarding in-vitro antiurolithiatic activity of has been reported, although it has not reported for in-vitro antiurolithiatic activity up till now.
Objective: To explore anti-urolithiatic activities of Pavonia lasiopetala leaves extract by utilizing different in-vitro models.
Material and Methods: Aqueous extract of Pavonia lasiopetala fresh leaves was prepared and arranged in the different concentrations. Homogenous precipitation method was used to prepare artificial stones such as calcium oxalate and calcium phosphate and semi-permeable membrane of eggs was used as dissolution bags. Dissolution models were incubated in 72 hrs and after that, the entire content in dissolution bags was estimated spectrophotometrically. The inhibitory activity of Pavonia lasiopetala leaves extract on the nucleation of calcium oxalate crystals and the rate of aggregation in calcium oxalate crystals was determined by spectrophotometric assay. Results: In dissolution models, the extract of Pavonia lasiopetala has greater capability to dissolve calcium oxalate while Cystone standard has shown better demineralization for calcium phosphate rather than extract of Pavonia lasiopetala. Cystone exhibited strongly inhibitory action in the nucleation assay rather than aggregation assay. The extract of Pavonia lasiopetala exhibited inhibitory action in both of nucleation and aggregation assays to significant level.
Discussion: Correlation between in-vitro and in-vivo studies may be helpful to understand the molecular mechanism of litholysis process and to reveal phytochemicals of the extract responsible for dissolving or disintegrating renal calculi.
Conclusion: Pavonia lasiopetala extract exhibited significant in-vitro anti-urolithiatic activity.
Keywords: Pavonia lasiopetala, spectrophotometrically, in-vitro antiurolithiatic.
The Chemical constituents in essential oils of Pterocarpus soyauxii leaf, leaf stalk and stem bark
Authors: Moronkola Dorcas Olufunke , Oladapo Timilehin Peter , Adegbenro Fuhad Opeyemi , Ogunbanjo Oluwadamilare Oluwatimilehin , Olayinka Kehinde Ololade 
Published: April 2019

The Nigerian essential oils of fresh Pterocapus soyauxii leaf, leaf stalk and stem bark were isolated by hydro-distillation using the adapted all glass Clevenger’s apparatus designed to British Pharmacopeia specifications. Chemical compositions of the plant parts were characterized using Gas Chromatography-Mass Spectroscopy (GC-MS).
The leaf essential oil contained 12 compounds, out of which 10 were identified accounting for 93.91% of it. Leafstalk oil had 20 major compounds, which were characterised; they constitute 95.47% of the oil. 11 compounds make up 78.61% of stem bark oil, out of which 7 were characterised, responsible for 76.30% of it.
Prominent compounds in the leaf oil were cembrene (43.59%), a monocyclic diterpenoid, eremophilene (29.72%), and azulene derivatives (6.62%), which are polycyclic aromatic compounds. Leaf stalk oil was dominated by hexadecane (32.97%), cis- and trans- β-ocimene (11.60 and 7.74% respectively) and heptanol (8.39%). Major compounds in stem bark oil were neophytadiene (22.11%), 2-heptanol (19.27%) and 3,7,11,15-Tetramethyl-2-hexadecene-1-ol (14.35%). Other prominent compounds in the stem bark oil are 4-propyl-cyclohexene (4.83%), 3-Eicosyne (7.63%), 3,7,11-trimethyl-14-(1-methylethyl-[S-(E,Z,E,E)]-1,3,6,10-cyclodecatetraene (5.10%) and methyl-Z-5,8,11,14,17-Eicosapentaenoate (3.01%).
Notable compounds of biological importance and in appreciable amounts in the oils include phytol (6.93%), squalene (1.14%) and ambrial (1.97%). Fragmentation patterns in the mass spectrum of some unidentified compounds are also presented which are unique features of the oils.
Interesting classes of compounds in the three oils include monoterpenes, sesquiterpenes, diterpenes, naphthalenes, alcohols and hydrocarbons.
Evaluation of preliminary phytochemical screening, acute toxicity and antioxidant profile of Ocimum kilimandscharicum
Authors: Saxena Gaurav , Mittal Abhilasha , Siddiqui Abdul Wadood 
Published: April 2019

Nature has offered us diverse curative herbs having with powerful antioxidant phytochemicals. Ocimum (Lamiaceae) is a notable source of volatile oils and flavouring agents in general and primarily of eugenol, methyl eugenol, linalool, methyl chavicol, etc. Karpoora Thulasi is a member of this genus; nevertheless, not much literature has been reported on its safety and antioxidant potential. In this investigation, we did a pre-clinical safety assessment of concentrate of O. kilimandscharicum on Sprague Dawley rodents. Toxicological concordat of the O. kilimandscharicum concentrate was carried out following OECD guidelines 423. Further, to verify the traditional efficacy and elucidate the mechanism, the present study compared in-vitro antioxidant activity of the plant by DPPH, ABTS and Hydroxyl radical scavenging method using ascorbic acid as the standard. In acute oral toxicity, no treatment-related death or toxic signs were observed. Moreover, the study revealed that the O. kilimandscharicum extract could be well tolerated up to the dose 2000 mg/kg body weight and could be classified as Category 5. Moreover, ABTS free radical activity of the extract was 79.2148 while that of DDPH Inhibition potential was found to be 70.72758. Our findings present substantiation that the crude extracts of O. kilimandscharicum is a likely source of natural antioxidants, and this justified its long-established uses.
Keywords: Ocimum kilimandscharicum, Acute Toxicity, In-vitro Antioxidant Activity DPPH, ABTS
Fixed dose combination products as Oro-dispersible tablets: A review
Authors: Chandrasekaran Gothainayaki , Rajalakshmi A.N. 
Published: April 2019

A fixed-dose combination (FDC) drug is a one that includes two or more active pharmaceutical ingredients (APIs) combined in a single dosage form, which is manufactured and distributed in fixed doses [1]. It increases patient compliance by reducing the no. of medications that a patient has to take especially for geriatric and pediatric patients. Orally disintegrating tablets (ODTs) are solid dosage forms containing a medicinal substance or active ingredient that rapidly disintegrates upon contact with saliva, typically within 30 s, eliminating the need for swallowing. It also increases patient compliance by reducing the swallowing problems faced by the patients especially for geriatric and pediatric patients. This review is about combining the techniques of both FDC and ODT formulations which promises to have a wide range of advantages to pediatric and geriatric populations, institutionalized and psychiatric patients, those suffering from nausea and vomiting, and individuals with lack of access to water. In spite of these advantages rarely do we find FDC-ODT products in our commercial market, this review aims at analyzing all the aspects of FDC and ODT formulations thereby forming the foundation for further studies.
Keywords: Fixed-dose combinations, Orally disintegrating tablets, Patient compliance.
Preparation and characterization of azathioprine microspheres for colon specific delivery
Authors: Gonekar Rinku , Kori Mohan Lal 
Published: April 2019

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine. Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size, drug entrapment efficiency, percentage yield, shape and surface morphology and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months.
Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.
Warm-e-Lauztain (Tonsillitis): Diagnosis and Management with reference to Unani System of Medicine
Authors: AZIZ ABDUL , MANNAN ABDUL , AKHTAR MD. WASI , AZIZ YASMEEN 
Published: April 2019

Warm-e-Lauztain (Tonsillitis) being very common clinical condition affecting mostly the school going children is the one of the important reason to visit a doctor frequently. Diagnostic features and findings on clinical examination are described very clearly in classical texts of Unani medicine, e.g. if the tonsillitis is caused due to abnormality of khilt-e-dam (humour sanguine), it is expressed by severe pain in the throat, fever, redness of eyes and face, sweetish taste in mouth etc.; if it is due to khilt-e-safra (humour bile), then it is characterized by severe pain in the throat, difficulty in the swelling, high grade fever, dryness, paleness of face; if there is imbalance in khilt-e-balgham (humour phlegm), there will be soft whitish swollen tonsils associated with paresis and softness of the tongue; tonsillitis due to the abnormality in khilt-e-sauda (humour black bile) exhibit hard swelling of tonsils encroached into the tongue and surrounding tissues. On examination, if there is much congestion and redness on the tonsils or it is black in colure and hard in consistency then surgical procedure should be avoided. Always first emphasis should be given for medical treatment, if it fails then opt surgical management. When the acute inflammation (warm-e-haar) has been subsided and the base of swelling is soft and thin, than it is suitable time for tonsillectomy. Surgical procedure is also described by Abu Al-Qasim Al-Zahrawi and others in detail. Therefore it may be concluded that scholars of Unani medicine were much aware about the signs & symptoms of chronic tonsillitis; they were able to diagnose the disease clinically and were expert enough to assess the condition, whether requiring medical management or surgical intervention. Surgeons of that time knew clear-cut indications and contraindications for surgical intervention along with the procedure of tonsillectomy
Keywords: Warm-e-lauztain, Tonsillitis, Unani classical, Treatment, surgery
Formulation and evaluation of multipurpose herbal cream
Authors: DHYANI ARCHANA , Chander Vikas , Singh Nardev 
Published: April 2019

Herbal cosmetics are the preparations used to improve the individual appearance. The aim of the present study was to prepare the herbal cream for the use of moistening, nourishing and cure of various disease of the skin. Different crude drugs like Aloe barbadensis (Aloe Vera leaves), Azadirachta Indica (Neem-leaves), Curcuma longa (Turmeric-rhizomes) and Emblica Officinali (Amla) are used to formulate the cream. The selection of ingredients based on the different medicinal properties of the agents.The cream is subjected to various evaluation parameters.
Keywords: Cosmetics, herbal cream, Turmeric, Neem, Aloe Vera
Nano-cuprous oxide enhances seed germination and seedling growth in Lycopersicum esculentum plants
Authors: S Ananda , G Shobha , KS Shashidhara , Mahadimane Vishwaprakash 
Published: April 2019

This study was carried out to determine the influence of cuprous oxide nanoparticles (Cu2O NPs) biosynthesised from leaf extracts of Flacourtia montana on the tomato Lycioersicum esculentum seed germination, seedling growth and vigour index. Here we examined the promotory and phytotoxic effect of Cu2O NPs (0-160ppm) on tomato seeds resulted in dosage dependent response. The highest germination percentage (95%) was observed at 20ppm Cu2O NPs, however, above 20ppm Cu2O NPs, there is a reduction in the seed germination. The tomato seedlings showed increased root and shoot elongation up to 20ppm Cu2O NPs concentration, further increase in NPs concentration caused the negative effect on plants growth and development. The leaf pigments showed increasing trend in tomato plants after treatment with Cu2O NPs up to 20ppm as compared to control. Phytotoxicity of Cu2O NPs in tomato seedlings demonstrated by lower contents of chlorophyll a, b and carotenoid pigments. The study of effect on antioxidant enzymes showed increases in activity with increase in Cu2O NPs concentration for two enzymes, Super oxide dismutase (SOD) and Glutathione Peroxidase (GPX) out of five enzymes treated. High antioxidant activity of enzymes is followed by the increased lipid peroxidation and decrease in free radical scavenging activity by the DPPH. The activity of Catalase, Pheny Alanine Aminolyase and Poly Phenol Oxidase enzymes were found to increase up to 20ppm as compared to control and above this, all three enzymes showed decrease in activity. Uptake of Cu2O NPs nanoparticle by tomato seedlings was confirmed by atomic absorption spectroscopy.
Key words: Nano-Cuprous Oxide, Flacourtia montana, Tomato, antioxidant enzymes, lipid peroxidation
In-vitro assessment of CYP3A4 and CYPC29 inhibition potential of Lupeol using human liver microsomes
Authors: KHATAL LAXMAN DATTU , More Harinath 
Published: April 2019

Background: Lupeol is a dietary triterpene, possesses numerous biological activities. Lupeol is currently under development for chemotherapy and chemoprevention. The aim of present study was to determine the potential inhibitory effect of Lupeol on cytochrome P450 (CYP3A4 and CYP2C9 isozymes) activities in human liver microsomes (HLM).
Methods: The inhibition studies were conducted using testosterone 6β-hydroxylase (CYP3A4), and diclofenac 4’-Hydroxylase (CYP2C9) activity assay using positive control Ketoconazole and Sulphaphenazole, respectively. Inhibition study was performed by incubating lupeol (0 to 20 μM) with human liver microsomes, and the metabolite formation was analyzed by liquid chromatography-Tandem Mass Spectrometry (LC-MS/MS).
Results: Luepol did not inhibit CYP3A4 and CYP2C9 isozymes mediated activities in human liver microsomes up to a maximum tested concentration of 20µM based on solubility under tested invitro conditions.
Conclusions: Lupeol is not an inhibitor of the CYP3A4 and CYP2C9 isozymes. IC50 is greater than highest tested concentration as well as physiological concentration, where effect was measured with confidence. Therefore, clinically relevant pharmacokinetic herb-drug interactions are unlikely to occur between Lupeol and co-administered substrates of these CYP isozymes. Looking at the spectrum of biological activities and CYP inhibition potential of Lupeol; Lupeol can be used as adjuvant/ chemotherapy agent/ chemopreventive agent in therapy.
Keywords: Lupeol, HLM, CYP3A4 and CYP2C9, Inhibition, herb–drug interactions
Preparation and characterization of Starch–Urea–Borate: A new floating polymer
Authors: Santosh Kumar Rada , Chowdary K.P.R. 
Published: April 2019

In recent years considerable attention has been focused on the development of new drug delivery systems known as controlled release drug delivery systems. Such interest is based largely on the fact that the controlled release products have established and retained place in the market based on their uniqueness and their clinical advantages in the practices of medicine. The major types of controlled release systems include matrix tablets, floating tablets, swellable tablets, coated beads, microcapsules and microspheres, mucoadhesive systems, ion exchange resin complexes, osmotic pressure controlled release systems, transdermal systems etc. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Several polymers such as various viscosity grades of hydroxypropylmethyl cellulose (HPMC), Carbopol 934P, Eudragit RL, calcium alginate, chitosan, xanthan gum, guar gum, ethyl cellulose etc., have been used in the design of floating tablets of various active pharmaceutical ingredients (APIs). Though these polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets.The overall objective of the investigation is to develop new, efficient and safe polymer as floating matrix former for floating systems.
Keywords: Floating, Matrix, Polymers, Starch-urea-borate.