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INDONESIA
INDONESIAN JOURNAL OF PHARMACY
Published by Universitas Gadjah Mada
ISSN : 23389427     EISSN : 23389486     DOI : -
Core Subject : Health,
Medicine & Pharmacology
Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas Gadjah Mada (UGM) Yogyakarta Indonesia in collaboration with IAI (Ikatan Apoteker Indonesia or Indonesian Pharmacist Association) and only receives manuscripts in English. Indonesian Journal of Pharmacy is Accredited by Directorate General of Higher Education (DGHE) DIKTI No. 58/DIKTI/Kep/2013.
Arjuna Subject : -
Articles 2 Documents
 1 
Search results for , issue " Vol 26 No 4, 2015" : 2 Documents clear
SYNTHESIS, COMPUTER AIDED SCREENING AND PHARMACOLOGICAL EVALUATION OF 2/3-SUBSTITUTED-6(4-METHYLPHENYL)-4,5-DIHYDROPYRIDAZIN3(2H)-ONES, AND PYRIDAZINE SUBSTITUTED TRIAZINE Khokra, Sukhbir Lal; Seth, Sonakshi; Garg, Shama S; Kaushik, Pawan; Ahmad, Aftab; Khan, Shah Alam; Husain4, Asif
INDONESIAN JOURNAL OF PHARMACY Vol 26 No 4, 2015
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (15.106 KB) | DOI: 10.14499/indonesianjpharm26iss4pp200

Abstract

The present research work involved synthesis of some new pyridazine derivatives and evaluation of their analgesic and anti-inflammatory activities in experimental animals to obtain safer non-steroidal anti-inflammatory agents (NSAIDs). Friedel-Crafts acylation reaction of succinic anhydride with toluene in the presence of anhydrous aluminum chloride gave 4-(4-methylphenyl)-4-oxo-butanoic acid (1). The aryl propionic acid 1 on reaction with phenyl hydrazine and hydrazine hydrate yielded the pyridazinone derivative 2 and 3, respectively. Reaction of the compound 3 with phosphorus oxychloride (POCl3) produced the corresponding chloropyridazine derivative 4. A 4-hydroxymethyl derivative of dihydropyridazinone (5) was synthesized by condensing 3 with methanol and formaldehyde (HCHO). The compound 5 on further treatment with guanidine hydrochloride in ethanol gave the pyridazino-triazine (6). The synthesized compounds were investigated for their analgesic activity in mice and anti-inflammatory activity in Wistar albino rats. The molecular, pharmacokinetic and toxicity properties of the synthesized compounds were calculated by Molinspiration and Osiris property explorer software. The results of in-vivo anti-inflammatory studies revealed that the compound. 4 showed maximum inhibition in paw edema volume followed by compound 3 while the compound 4 exhibited excellent  peripheral analgesic activity (74%) followed by the compound 5. Compound s 4 and 5 also showed good central analgesic effect increased the reaction time to 90 minutes. All the title compounds except compound 5 are predicted to be safe by Osiris online software and are likely to have good oral bioavailability as they obey Lipinski’s rule of five for drug likeness.Keywords:  Pyridazinone, Hydrazine derivatives, Chloropyridazine, Triazin-2-imine.
DESIGN AND EVALUATION OF GUARGUM - BASED TIMOLOL MALEATE OCULAR INSERT Kumar, Sunil; Issarani, Roshan; Nagori, B P
INDONESIAN JOURNAL OF PHARMACY Vol 26 No 4, 2015
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (15.106 KB) | DOI: 10.14499/indonesianjpharm26iss4pp177

Abstract

The objective of this study was to prepare ocular inserts of timolol maleate using guar gum as a polymer. Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v , 75 % w/v and 1.0% w/v). The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage moisture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation. In-vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell. The inserts were found to be of uniform thickness (ranging from 41.12±0.04µm to 79.90±0.03µm) and weight (0.84±0.07 mg to 2.11±0.09 mg). The % drug content in the inserts was found to be varied between 98.69±0.58to 96.37±0.58. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24 h. In-vitro transcorneal study revealed that an increase in concentration of polymer slows down the release of timolol maleate from the formulation. Ocular inserts using guar gum as a polymer were successfully prepared and can be effectively used for sustain ocular delivery over a period of 24 h.Key words: Guar gum, in vitro transcorneal permeation study, ocular insert, timolol maleate, sustained release

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