Indian Journal of Pharmaceutical Sciences
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Scientific Publication of the Indian Pharmaceutical Association
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   1993| July-August  | Volume 55 | Issue 4  
 
 
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Preformulation studies of a prodrug of ciprofloxacin.
AG Swaminathan, SP Agarwal
July-August 1993, 55(4):159-161
A prodrug of Ciprofloxacin was synthesized by reacting the free base with aqueous formaldehyde solution in a 1:1 mixture of methylene chloride and methanol. The colourless, crystalline Nhydroxymethyl derivative, m.p. 238-242 degree C showed enhanced solubility and a three fold increase in the dissolution rate over parent drug. The degradation kinetics, pH-rate profile and antimicrobial activity of the prodrug were also determined.
[ABSTRACT]   Full text not available   
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Antihepatotoxic activity of some ayurvedic prepartions.
BP Reddy, CK Kokate, D Rambhau, V Venkateshwarlu, VN Murthy
July-August 1993, 55(4):137-140
In Ayurveda, various preparations are used for liver disorders. Abhrak bhasma (100 puts), Praval bhasma agniputi), Mandur bhasma, Loha bhasma and Arogyavardhini Rasa No.1 were screened for antihepatotoxic activity in albino rats treasted with CCl4, using the liver to body weight ratio,pentobarbitone sleeping time and serum levels of SGPT, SGOT, alkaline phosphatase and bilirubin. Abhrakbhasma and Arogyavardhini were found to have good hepatoprotective activity.
[ABSTRACT]   Full text not available   
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Preparation and evaluation of flurbiprofen and diclofenac sodium transdermal films.
UV Singh, S Pandey, N Udupa
July-August 1993, 55(4):145-147
Transdermal Films of Flurbiprofen and Diclofenac Sodium were prepared using HPMC and Beta Cyclodextrin. The films were evaluated for physicochemical characteristics, release pattern, Pharmacodynamic activity and Bioavailability.
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Invitro release and anti fungal activity of commercial clotrimazole creams.
MJ Prasad, D Rambhau, SS Apte, G Venkateshwarlu, V VS Rao, BR Rao, V Sarveswar V, Ramesh Rao B
July-August 1993, 55(4):119-123
Three commercial creams of clotrimazole (CLTZ) were tested for in vitro release and anti fungal activity. Release and anti fungal activity showed an inverse relation, indicating that these parameters are governed by two independent mechanisms. Release was related to particle size according to Noye's Whitney hypothesis, but it was inversely related to Electrokinetic potential (EKP) indicating that electrical double layer is a barrier retarding the release. A linear relationship between anti fungal activity and EKP reveals that, since EKP is a measure of spreadability and dispersibility of creams, via these factors it is influencing the anti fungal activity. As the release data fitted well in to Higuchi's square root law and Hixson-Crowell equation, it is inferred that both matrix type and diffusion controlled mechanisms are governing release.
[ABSTRACT]   Full text not available   
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Synthesis, reactions and biological activities of some fluorine containing 3' -phenylspiro [3h-indole-3,2' -thiazolidine]-2,4' (1h) -diones.
A Dandia, V Kaur, P Singh
July-August 1993, 55(4):129-136
Several fluorine containing 3' -phenylspiro [3H- indole-3, 2' -thiazolidine]-2, 4' (1H)-dions were synthesised. Reaction of 2-mercaptopropionic acid/mercaptoacetic acid with fluorinated 3-aryyliminoindole-2-ones,prepared in situ from indole-2, 3-diones (isatins) and fluorinated anilines, afforded the title compounds. Alkylation of spiro compounds under Phase- Transfer-Catalysis yielded exclusively N-alkylated indole. The spiro compounds were converted into corresponding thiones. Representative compounds were screened for antifungal,antibacterial and insecticidal activities. Enhanced antifungal, antibacterial and insecticidal activities were recorded when sulphur was added to the representative compounds.
[ABSTRACT]   Full text not available   
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Pharmacokinetics of naproxen in presence of dapsone.
JS Kumar, DR Krishna
July-August 1993, 55(4):115-118
Neproxen 500 mg (2 x 250 mg tablets) alone and in combination with dapsone 100 mg tablet was administered to seven healthy human volunteers in a sequential design. Plasma concentrations were determined during a 48 hr. period following drug (s) administration. The plasma levels and pharmacokinetic parameters such as C max, t max, AUC, t1/2, V,CL and MRT of naproxen were not affected significantly (p>0.05) in presence of dapsone. In vitro protein binding interaction between naproxen and dapsone was studied by equilibrium dialysis method using bovine serum albumin. No significant variation in protien of naproxen was observed in presence of different concentrations of dapsone.
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Some aspects of polarographic wave of ascorbic acid and its determination from some synthetic and medicinal samples.
SN Gupta, MN Ray
July-August 1993, 55(4):124-128
The ascorbic acid oxidizes electrochemically at the surface of the dropping mercury electrode. Oxalic acid which is used as extracting agent for ascorbic acid does not influence the anodic wave and does not react with it. Defined anodic waves are obtained if the potential range of polarogram is kept in the range 0-300m V. pH 4.0 was found to be the most satisfactory for determination of ascorbic acid. The ascorbic acid in synthetic and various medicinal samples was determined by internal addition method.
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Evaluation of ciprofloxacin hydrochloride ocular preparations.
UR Kamath, UV Singh, N Udupa
July-August 1993, 55(4):148-150
An ocular drug delivery device of Ciprofloxacin was designed with the aim to overcome the drawbacks of conventional eye medications. The drug release pattern and stability of these devices were studied.
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In vitro anti-inflammatory effect of indomethacin encapsulated in liposomes.
BM Trivedi, RH Parikh
July-August 1993, 55(4):157-159
The anti-inflammatory activity of liposomal indomethacin was compared with that of free indomethacin in female albino rats. A statistically significant difference was found between the anti-inflammatory effect of free and liposomal indomethacin in reducing carrageenan-induced oedema in rats.
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Spectrophotometric determinations of phenothiazine derivatives.
SL Bhongade, AV Kasture
July-August 1993, 55(4):151-154
Two spectrophometric methods are described for the determinations of Phenothiazine tranquillizers based on the formation of chloroform extractable complexes exhibiting absorption maxima at 520 nm with Amaranth and Fast red-E in acidic medium. The ion-pair methods has been applied to the determination of promethazine HCL, chlorpromazine HCL, thioridazine HCL, trifluoperazine HCL, triflupromazine HCL, methdilazine HCL and fluphenazine HCL as raw materials and from their pharmaceutical formulations.
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Extractive spectrophotometric determinations of nortriptyline hydrochloride.
SL Bhongade, AV Kasture
July-August 1993, 55(4):155-157
Two senstive methods for the determination of Nortriptyline HCI based on the formation of coloured complexes of the drug with regents such as Light Green FCF at pH 5.0 and Orange- ll at pH 2.0 are described in bulk samples and in pharmaceutical preparations. The ion-pair complexes formed are quantitatively extracted into chloroform under the experimental conditions.
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Some biological activity of aryloxypropanolamins of bisphenol derivatives.
HH Garchar, RC Srimal, PH Parsania
July-August 1993, 55(4):141-144
Epoxy resins and hydrochloride salts of aryloxypropanolamines of bisphenol derivatives were synthesised and characterised by elemental, IR, 1H NMR spectral data. All the compounds were screened for their antibacterial, antifungal and hypotensive activities.
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