Purpose: To mask the bitter taste of the widely used antiallegic drug, Promethazine Hydrochloride(PMZ HCL), and to formulate it into patient-compliant and convenient fast disintegrating tablets.

Methods: Taste masking of Promethazine Hydrochloride was achieved by microencapsulation using amino alkyl methacrylate copolymers (Eudragit E100) employing the solvent evaporation technique. Taste assessment was carried out by time intensity metod. Sublimation method was used, using camphor as subliming agent, sodium starch glycolate and crosspovidone as a super-disintegrant was used to prepare fast disintegrating tablets. Tablets were evaluated with regard to a variety of pharmacopoeial tests, drug release, and disintegration time in the oral cavity.

Results: The time intensity method confirmed tasteless nature of the optimized microspheres. In vitro dissolution studies at pH 6.8 showed that no significant amount of drug is released while tablet is in mouth and approximately 92.3% of the release takes place in 15 min at gastric pH of 0.1N HCl indicating that taste-masking the drug with the pH-sensitive polymer does not affect the release of the drug in the stomach.

Conclusions: Sensory evaluation for taste by a time inetensity method on 6 healthy volunteers confirms the successful formulation of the oral palatable fast disintegrating tablets which disintegrates in the oral cavity in 15±0.4 s.

 

KEYWORDS: Eudragit E100, Fast disintegrating tablets, Superdisintegrant, Taste masking, Promethazine Hydrochloride.

[1] Jaysukh JH, Dhaval AR, Kantilal RV, Orally disintegrating tablet: A Review, Tropical journal of pharmaceutical research, 2(4), 2009, 161-172.
[2] Y. Fu, S. Yang, S.H. Jeong, Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies, Crit. Rev. Ther. Drug Carrier Syst, 2(1), 2004, 433-476.
[3] Lokesha P, Kunchu K, Tamizh Mani T, Fast disintegrationg tablet: An overview of formulation, technology and evaluation, Research Journal of Pharmaceutical, Biological and Chemical Sciences, 1(2), 2011, 589-601.
[4] Shishu A, Bhatti T, Singh, Preparation of tablets rapidly disintegrating in saliva containing bitter taste-masked granules by sublimation method, Ind. J. Pharm. Sci, 4(9), 2007, 80-84.
[5] A. Wade, P. J. Weller, Polymethacrylates in Handbook of Pharmaceutical Excipients, (The Pharmaceutical Press, London, 1994) 362-366.
[6] Kamalpreet, Varun RK, Development of taste-masked fast disintegrating tablets of tinidazole, Asian Journal of Pharmaceutical Sciences, 1(4), 39-45.

Syzygium Samarangense (red jamrul in Bangladesh) is a potential medicinal drug.We aimed to evaluate the analgesic, anti-inflammatory and CNS activities of the methanolic extract of Syzygium Samarangense bark in mice. The analgesic activity was examined by acetic acid induced writhing and formalin tests. The anti-inflammatory activity was studied using carrageenan induced hind paw edema model. The analgesic activity of the methanolic extract of Syzygium Samarangense bark was evaluated by acetic acid induced writhing and formalin tests at the dose of 100 mg/kg and 200 mg/kg, significantly (p<0.05) reduced the writhing caused by acetic acid and the number of licks induced by formalin in a dose dependent manner.The extract of Syzygium Samarangense bark caused significant (p<0.05) inhibition of carrageenan induced paw edema after 4 h in a dose dependent manner. The CNS depressant activity was evaluated by observing the reduction of locomotor and exploratory activities in the open field and hole cross tests at a dose of 100 mg/kg and 200 mg/kg body weight. The findings of the study suggested that the methanolic extract of Syzygium Samarangense bark has strong analgesic, moderate effect against inflammation and significant CNS effects, conforming the traditional use of this plant for inflammatory pain alleviation.

KEYWORDS:, Analgesic, Anti-inflammatory, Bark, CNS activities ,Methanolic extract of Syzygium Samarangense , Pain

[1] Rakh, M.S. and S.R Chaudhary, 2010. Evaluation of CNS depressant activity of Momordica dioica roxbwild fruit pulp. International Journal of Pharmacy and Pharmaceutical Sciences,2(4):124-126

[2] Kumara, N.K.V.M,.R 2001. Identification of strategies to improve research on medicinal plants used in SriLanka. a WHO symposium; University of Ruhuna, Gally, Sri Lanka .

[3] Joshi, B., S. Lekhak and A. Sharma, 2009. Antibacterial property of different medicinal plants Ocimum sanctum, Cinnamomum zeylanicum , Xanthoxylum armatum and Origanum majorana. Kathmandu University Journal of Sciences Engineering and Technology, 5(1): 143-150.

[4] Sivarajan, V.V. and I. Balachandran, 2002.Ayurvedic drugs and their plant sources. Oxford and IBH publishing Co. Pvt. Ltd., New Delhi, pp: 271-272

[5] Clore;J.N;Stillman, j;Sugerman,H.Glucose-6-phosphate flux in vitro is increased in type 2 diabetes.Diabetes 2000,49,969-974.

[6] Resurreccion-Magno,M; Villasenor,I,Harada,N;Monde,K.Antihyperglycaemic flavonoids from Syzygium Samarangense (Blume) Merr. And perry. Phytother.Res 2005,19,246-251

"Local or regional anaesthesia may be defined as a regional loss of sensation to a painful stimulus as well as loss of all other sensations including temperature, pressure and touch etc resulting from a reversible interruption of peripheral conduction along a specific neural pathway" Malamed1 .Local anesthetics are chemicals that block nerve conduction in a specific, temporary and reversible manner, without affecting the patient's consciousness. The molecule consists of two poles: a hydrophilic tertiary or secondary amino group and a lipophilic aromatic ring. According to the type of intermediate alkyl linkage between them, they are classified in ester-type anesthetics, with an amino-ester bond and whose prototype is procaine, and the amide-type with an amino-amide bond and whose prototype is lidocaine2.The choice of anesthetic solution should be based on three main clinical considerations: anesthetic potency, latency (time to onset of anesthesia), and duration of the anesthetic effect.1,3,4,5. A number of local anesthetic agents are available that provide rapid onset of surgical anesthesia and adequate duration of anesthetic effect6 Vasoconstrictors have been added to local anesthetic solutions to increase the quality and duration of anesthesia, avoid excessive intraoperative bleeding, and decrease systemic toxicity.

 

[1] Malamed SF. HandBook of Local Anesthesia. 4th ed. St Louis: CV Mosby; 1997.
[2] Milam SB, Giovannitti JA Jr. Local anesthetics in dental practice. Dent Clin North Am. 1984;28:493-508.
[3] Berini-Aytés L, Gay-Escoda C. Anestesia Odontológica. 2nd ed. Madrid: Ediciones Avances Medico-Dentales, S.L.; 2000.
[4] Mehra P, Caiazzo A, Maloney P. Lidocaine toxicity.
[5] Anesth Prog 1998;45:38-41.
[6] Daublander M, Muller R, Lipp MD. The incidence of complications associated with local anesthesia in dentistry. Anesth Prog 1997;44:132-41.

Endostatin is an endogenous inhibitor of angiogenesis. It was first found secreted in the media of no-metastasizing mouse cells from a hemangioendothelioma cell line in 1997 and was subsequently found in humans. The sequence of endostatin gene (AC: AF257775) has been downloaded from NCBI database and via Conserved Domain Database (CDD), DNA Motif Searching Database (DMSD), DNA binding-site database predicator, the similar domains, motif, DNA binding-site, has been recognized. The result showed in this sequence important motif includes: EGF_1, CTCK_1, and VWFC_1 and 2FE2S_FER_1. Our result showed in this study a total of 10 domain structures which were similar with endostatin protein sequence has been identified.

 

KEYWORDS: endostatin, Mus musculus, computational analysis

 

[1] Huang XJ, Wong MKK, Zhao Q, Zhu ZY, Wang KZQ, Huang N, Ye CS, Gorelik E (2001) Li MF (2001) Soluble recombinant endostatin purified from Escherichia coli: antiangiogenic activity and antitumor effect (vol 61, pg 478). Cancer Res 61(15):5956.
[2] Deininger MH, Wybranietz WA, Graepler FTC, Lauer UM, Meyermann R, Schluesener HJ (2003) Endothelial endostatin release is induced by general cell stress and modulated by the itric oxide/cGMP pathway. Faseb J 17(10):1267–1276.
[3] Sorensen DR, Read TA, Porwol T, Olsen BR, Timpl R, Sasaki T, Iversen PO, Benestad HB, Sim BKL, Bjerkvig R (2002) Endo- statin reduces vascularization, blood flow, and growth in a rat gliosarcoma. Neuro-Oncology 4(1):1–8
[4] Zhu, J.K. ( 2002). Salt and drought stress signal transduction in plants. Annu. Rev. Plant. Biol. 53, 247–273.
[5] Lloyd, G., Landini, P., Bushby, S. (2001). Activation and repression of transcription initiation in bacteria. Essays Biochem. 37, 17–31

The bioactive aromatic aldehyde, vanillin (3-methoxy 4-hydroxy benzaldehyde) is isolated from stem bark of the medicinal plant Mimusops elengi for the first time. Elucidation of structure is achieved with the help of spectral data derived from GC-MS, FTIR, 1HNMR and 13CNMR analysis. The structure of 3-methoxy 4-hydroxy benzaldehyde is examined by use of the HF (6-31G* level), Density Functional Theory, DFT (6-31G* level) and hybrid functional B3LYP. Using the optimized structure of this compound IR, 1HNMR and 13CNMR data is calculated and compared with the experimental data. The results are discussed in this article. It shows good relation between theoretically calculated and observed values for IR wave numbers. The chemical shifts are in good comparison for 1HNMR and 13CNMR spectra too.

 

Key words: 3-methoxy 4-hydroxy benzaldehyde, FTIR, NMR, HF (6-31G* level), DFT.

 

[1.] Wealth of India, Raw Materials Vol.6, 383, CSIR, New Delhi, India, 1962.
[2.] Database on Med. Plants Used in Ayurveda Vol. 1 65, 2000.
[3.] P. P. Joy, J. Thomas, Samuel Mathew, Baby P. Medicinal Plants, 126,1998.
[4.] S.G. Joshi, Medicinal Plants, Oxford and IBH Publ. Co. Pvt. Ltd., 362, 2000.
[5.] Chakraborti, N. ; Madal, L.; Banerjee, G. C. Indian Vet. J., 65 (2), 145-9, 1988.
[6.] Mandal, B.; Maity, C. R., Acta Aliment, 20 (2), 103-7 , 1991
[7.] Mali R.G., Mahajan S.G. and Mehta A.A.; Phcog Mag. 3 (10), 73-75, 2007

Isotretinoin is a known teratogen affecting the neuronal differentiation in developing brain. Apart from its effects on brain and other craniofacial malformations, it is also known to cause failure of detachment of the lens from the surface ectoderm. Interestingly very little is known about the teratogenic effect of isotretinoin on the development of eye. Hence in the present study we evaluated the morphometric and histopathological changes in developing cornea and lens in rats during postnatal development.The pregnant rats received16mg/kg dose of isotretinoin during gestation day 1to 7 or 12 to 18. The control group received equivalent volume of vegetable oil instead of isotretinoin. The pups were sacrificed on day 7 or 14 or 30 for histopathological and morphometric analysis using haematoxylin and eosin staining.The results of the study clearly demonstrate that prenatal isotretinoin severely affects the development and growth of the cornea in both treatment regimes. There was also a considerable damage to the morphology of the lens.This preliminary animal study clearly demonstrates the teratogenic effect of isotretinoin on developing cornea and lens.

 

KEY WORDS: Developing rat cornea, Developing rat lens, Prenatalisotretinoin, Rat eye development

 

[1] Berarda A, Azoulay L, Koren G, Blais L, Perrealt S &Oraichi D. Isotretinoin, pregnancies, abortions and birth defects: a population-based perspective. Br J ClinPharmacol63, 2007, 196-205.
[2] Eleny BR, Karina GS, Maria AJ. Effect of isotretinoin on tooth germ and palate development in mouse embryos. Braz. Dent. J, 12,2001,115-19.
[3] O'Reilly KC, Shumake J, Gonzalez-Lima F, Lane MA, Bailey SJ. Chronic administration of 13-Cis-Retinoic Acid Increases Depression-Related Behavior in Mice. Neuropsychopharmacology, 31, 2006,1919-27.
[4] Cook CS and Sulik K.K. Laminin and fibronectin in Retinoid-induced keratolenticulardysgnesis. Investigative ophthalmology and Visual Science, 31, 1990,751-57.
[5] Divya P, Sampath M, V, Jai A, Teresa J, Sudhanshu S. Effect of Prenatal Isotretinoin Exposure on Neuronal Population of Prefrontal Cortex in Rats. Research Journal of Pharmaceutical, Biological and Chemical Sciences, 4, 2013, 902- 11.
[6] Cook CS and Sulik KK. Sequential scanning electron microscopic analyses of normal and spontaneously occurring abnormal ocular development in C57BI/6J mice. Scanning Electron Microsc, 3, 1986,1215