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ISSUE 26

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                     October - December 2015, Volume 10 No 26 pp 121-260

Table of Contents

About the Cover

Insulin is used medically to manage diabetes mellitus by frequent subcutaneous injections have turned into a part of life can be enormously distressing for patients. Hence, we anticipate to getting rid of the usage of subcutaneous injections completely. Virtual screening method (for selection of carriers), Toxtree tool (for toxicity evaluation of carriers) and Discovery Studio tool (for Pharmacopore designing, ADMET analysis, designing oral Insulin conjugates and Interaction studies between Insulin Receptor and oral Insulin conjugates) were used for proposed study. We have screened 14 competent drugs delivering agents (DDAs) from 7 chemical compound databases. The ADMET and Pharmacophoric properties of DDAs were analyzed by drug-informatics’ tools. Consequently, the DDAs were mono, di & poly conjugated by covalent bonding with various binding sites of Monomeric and hexameric form of human insulin and insulin-lispro (Humalog®) individually; and novel oral-insulin conjugates (OICs) were generated. Its binding efficiency and biological activity with Insulin-receptor were determined. Inulin and Vitamin- B1 are considered as novel, safe and proficient carriers for oral delivery of Insulin. Insulin Lispro is the remarkable option for oral delivery than other Insulin forms (Ref: Seenivasagam R. Designing novel oral-Insulin conjugates for the development of oral-Insulin tablet: Inulin- Insulin conjugate is an efficient form for oral-Insulin tablet. Drug Discovery, 2015, 10(26), 121-249).

RESEARCH

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Designing novel oral-Insulin conjugates for the development of oral-Insulin tablet: Inulin-Insulin conjugate is an efficient form for oral- Insulin tablet

Seenivasagam R

Insulin is used medically to manage diabetes mellitus by frequent subcutaneous injections have turned into a part of life can be enormously distressing for patients. Hence, we anticipate to getting rid of the usage of subcutaneous injections completely. Virtual screening method (for selection of carriers), Toxtree tool (for toxicity evaluation of carriers) and Discovery Studio tool (for Pharmacopore designing, ADMET analysis, designing oral Insulin conjugates and Interaction studies between Insulin Receptor and oral Insulin conjugates) were used for proposed study. We have screened 14 competent drugs delivering agents (DDAs) from 7 chemical compound databases. The ADMET and Pharmacophoric properties of DDAs were analyzed by drug-informatics’ tools. Consequently, the DDAs were mono, di & poly conjugated by covalent bonding with various binding sites of Monomeric and hexameric form of human insulin and insulin-lispro (Humalog®) individually; and novel oral-insulin conjugates (OICs) were generated. Its binding efficiency and biological activity with Insulin-receptor were determined. Inulin and Vitamin-B1 are considered as novel, safe and proficient carriers for oral delivery of Insulin. Insulin Lispro is the remarkable option for oral delivery than other Insulin forms.

Drug Discovery, 2015, 10(26), 121-249

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COMMUNICATION

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FDA approved drugs – June 2015

Vidhya V

Kengreal is specifically indicated as an adjunct to percutaneous coronary intervention for reducing the risk of periprocedural myocardial infarction, repeat coronary revascularization, and stent thrombosis in patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor. It is supplied as a sterile white to off-white lyophilized powder for reconstitution into an IV infusion. The recommended dosage is a 30 mcg/kg IV bolus followed immediately by a 4 mcg/kg/min IV infusion. Initiate the bolus infusion prior to PCI.

Drug Discovery, 2015, 10(26), 250-251

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FDA approved drugs – July 2015

Vidhya V

Entresto is specifically indicated to reduce the risk of cardiovascular death and hospitalization for heart failure in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It is supplied as a tablet for oral administration. The recommended starting dose of Entresto is 49/51 mg (sacubitril/valsartan) twice-daily.

Drug Discovery, 2015, 10(26), 252-256

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FDA approved drugs – August 2015

Vidhya V

Addyi is specifically indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD) as characterized by low sexual desire that causes marked distress or interpersonal difficulty. It is supplied as a tablet for oral administration. The recommended dosage is 100 mg taken once daily at bedtime. It should be dosed at bedtime because administration during waking hours increases risks of hypotension, syncope, accidental injury, and central nervous system (CNS) depression. Discontinue treatment after 8 weeks if no improvement is observed.

Drug Discovery, 2015, 10(26), 257-260

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