MIT-World Peace University (MIT-WPU) is a top educational institute located in Pune, India. It is recognized within&nbsp;UGC under Government of Maharashtra Act No. XXXV 2017.&nbsp;

It is part of the MIT group of institutions (established in 1983) which covers 10+ campuses across India and has more than 50,000+ students enrolled across various disciplines at a given point of time. The institute houses 15 schools ranging from Engineering &amp; Technology, Design, Pharmacy, Commerce, Governance among others. It offers undergraduate, postgraduate and PhD programs among different disciplines.&nbsp;

&nbsp;

MIT World Peace University

School of Pharmacy

Floating pulsatile is combined approach designed according to circadian rhythm to deliver the drug at right time, in right quantity and at right site as per pathophysiological need of disease with prolong gastric residence and lag phase followed by burst release. As the migraine follows circadian rhythm in which headache is more painful at the awakening time, the dosage form should be given during night time to release drug when pain get worsen. Present work deals with formulation and optimization of floating pulsatile tablet of sumatriptan succinate. Core tablet containing crospovidone as superdisintegrant (10%) showed burst release. Lag time was maintained using swellable polymer as polyoxN12K and xanthum gum. 32 experimental design was carried out. Developed formulations were evaluated for physical characteristics, in vitro and in vivo study. Optimized batch F2 with concentration of polyox N12K (73.43%) and xanthum gum (26.56%) of total polymer weight showed floating lag time 15±2 sec, drug content 99.58±0.2 %, hardness 6±0.2 Kg/cm2 and drug release 99.54±2% with pulsatile manner followed lag period of 7±0.1h. In vivo x-ray study confirms prolong gastric residence of system. Programmable pulsatile release has been achieved by formulation F2 which meet demand of chronotherapeutic objective of migraine. {\textcopyright} 2014 Bentham Science Publishers.

Pharmacy

World University root node

Current Drug Delivery

Development and Optimization of Press Coated Floating Pulsatile Drug Delivery of Sumatriptan Succinate

Biophytum sensitivum (L.) DC (Family: Oxalidaceae) is a medicinal plant widely used in the treatment of various health aliments throughout the world. The plant extract showed the presence of flavonoids, saponins, tannins, terpenes, steroids, amino acids, essential oil, polysaccharides and pectin. The plant has been extensively studied by various researchers for its biological activities and therapeutic potentials such as analgesic, anti-pyretic, anti-inflammatory, immunomodulatory, antitumor, antidiabetic, antioxidant, antibacterial, antihypertensive, chemoprotective, radioprotective and antifertility. The present review is an effort to provide detailed information on folkloric uses, chemical compositions, pharmacological activities of the extracts and isolated compounds and safety profile of Biophytum sensitivum for further research studies.

International Journal of Pharmacy and Pharmaceutical Sciences

Phytochemical and pharmacological profile of biophytum sensitivum (L) DC

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, primarily used for the treatment of hypertension, congestive heart failure and heart attack. It belongs to BCS class III having a half-life of 12 hrs and 25% bioavailability. The purpose of the present work was to develop a press-coated, floating-pulsatile drug delivery system. The core tablet was formulated using the superdisintegrants crosprovidone and croscarmellose sodium. A press-coated tablet (barrier layer) contained the polymer carrageenan, xanthan gum, HPMC K4M and HPMC K15M. The buoyant layer was optimized with HPMC K100M, sodium bicarbonate and citric acid. The tablets were evaluated for physical characteristics, floating lag time, swelling index, FTIR, DSC and in vitro and in vivo behavior. The 5% superdisintgrant showed good results. The FTIR and DSC study predicted no chemical interactions between the drug and excipients. The formulation containing xanthan gum showed drug retaining abilities, but failed to float. The tablet containing HPMC K15M showed a high swelling index. The lag time for the tablet coated with 200 mg carrageenan was 3±0.1 hrs with 99.99±1.5% drug release; with 140 mg HPMC K4M, the lag time was 3±0.1 hrs with 99.71±1.2% drug release; and with 120 mg HPMC K15M, the lag time was 3±0.2 hrs with 99.98±1.7% drug release. The release mechanism of the tablet followed the Korsmeyer-Peppas equation and a first-order release pattern. Floating and lag time behavior have shown good in vitro and in vivo correlations. {\textcopyright} Jagdale et al.

Fulltext

Scientia Pharmaceutica

Development of press-coated, floating-pulsatile drug delivery of lisinopril

{\textcopyright}2014 Bentham Science Publishers.Purpose: The objective of the present work was to develop a site specific gastro-retentive floating tablet of Troxipide for the treatment of peptic ulcer. Troxipide is a novel anti-ulcer agent having an elimination half-life of 7.4 hrs and mainly absorbed from the gastrointestinal tract.Methods: 32factorial design was applied. Dependant variables were swelling index, hardness and % drug release. Pluronic acid F127 and HPMC K 15M were used as rate controlled polymer. Optimized formulations were evaluated for physical characteristics, buoyancy, buoyancy lag-time, drug content, in- vitro drug release, floating behavior and in-vivo X-ray study.Results: Formulation H5 (20% Pluronic acid F127 and 78% HPMC K 15M) showed a floating lag time 60 ±2 sec with a desired controlled release profile over a period of 10 hrs. FTIR and DSC studies confirmed no chemical interactions. In-vivo X-ray study for optimized formulations showed gastro retention for 6 hrs.Conclusion: Results demonstrate feasibility of development of gastroretentive floating tablet of Troxipide.

Current Drug Therapy

Development and Optimization of Troxipide Floating Delivery for Treatment of Peptic Ulcer

{\textcopyright}2014 Bentham Science Publishers.The present work aimed to develop and study the effect of HPMC on compression-coated floating - pulsatile delivery of Bisoprolol. Inner core tablet contains bisoprolol and a super disintegrant. Outer shell contains HPMC K4M and HPMC K100M as erodible layer along with a gas generating agent. Compression-coated tablet of bisoprolol with 120mg HPMC K4M (B2) showed a lag time of 3.40±0.1 hrs with 99.81% drug release. Whereas 110mg HPMC K100M (B5) showed a lag period 4.0±0.1 hrs with 98.91% drug release. A 32factorial design was applied. HPMC K4M CR and K100M were independent variables whereas drug release, lag time at 4 hrs and swelling index were dependent variables. To understand the interaction of independent variables on dependent variables three dimensional surface response plots were drawn. The responses exhibited by batch F4 (55 mg HPMC K4M and 65 mg K100M) showed lag time 4.20 hrs following the sigmoidal release pattern. Optimized batch F4 gave good in-vitro in -vivo correlation.

Study on the Effect of HPMC on Compression Coated Floating Pulsatile Delivery of Bisoprolol

Development and evaluation of polymeric micelles for targeted anticancer drug delivery

A simple, economic, accurate and precise stability indicating method for Timolol Maleate was developed as per ICH guidelines Q1A(R2) and subsequently validated as per ICH guidelines Q2R(1). Chromatographic evaluation was carried out on C18 column of Kromasil (250 mm × 4. 6 mm, 5$\mu$m particle size) with a mobile phase consist of phosphate buffer: methanol (60:40 v/v). The pH of buffer was maintained to 3. 5 by using O-phosphoric acid. Flow rate was maintained to 1ml/min. Timolol Maleate was found to be stable in all conditions except in alkaline condition. In alkaline condition two degradation products were observed. Method was validated for different parameters like Linearity (calibration curve), accuracy, precision, robustness, recovery study. LOD and LOQ was found to be 0. 724 and 2. 19$\mu$g/ml respectively. The optimized and validated method can be used for estimation of Timolol Maleate in bulk and also in finished product.

International Journal of PharmTech Research

Development and validation of stability indicating reverse phase high performance liquid chromatography method for timolol maleate

Drug-cyclodextrin complexes improve aqueous solubility and dissolution rate of poorly water-soluble drugs. Solubilisation followed by buccal delivery of poorly water-soluble drugs can be advantageous for increasing drug absorption. Darifenacin is an antispasmodic used against urinary incontinence and specifically blocks M3 muscarinic acetylcholine receptors in smooth muscle. M3 receptors are mainly located in exocrine glands, smooth muscle and vascular endothelium. The oral absorption of darifenacin is poor owing to its low solubility. It also has poor bioavailability (15-19%) due to a high rate of first-pass metabolism. Complexation with beta-cyclodextrin was carried out to enhance solubility. The best results were obtained by co-grinding in a 1:1 molar ratio of drug: ??-cyclodextrin. The solid inclusion complexes were characterized by DSC, X-ray diffractometry and FTIR. Inclusion complexes showed higher dissolution rates than the pure drug. Controlledrelease mucoadhesive patches were prepared with two hydroxypropyl methylcellulose (HPMC) polymers, K100M CR and K15. The patches were assessed for surface pH, folding endurance, swelling, mucoadhesive properties, in-vitro residence time, vapor transmission test and in-vitro (cellophane, egg membrane) and exvivo (goat buccal mucosa) release. Formulations Ha2 (2%) HPMC K100M CR and Pa4 (4%) HPMC K15 showed good mucoadhesive strength, in-vitro and exvivo residence times, with controlled release for 10 hours.

Revista de Ciencias Farmaceuticas Basica e Aplicada

Development of buccal patches for delivery of darifenacin from beta-cyclodextrin complexes

Objective: The objective of the present study was to develop colon targeted pulsatile drug delivery system of Rizatriptan benzoate for the treatment of migraine. Method: Drug excipient interaction was carried by UV spectroscopy, FT-IR and DSC. Granules were prepared by wet granulation method. Physicochemical characteristics of Rizatriptan benzoate was carried out by flow properties and drug content. From the obtained results the formulation was selected for further preparation of pulsatile capsule with 100mg hydrogel plug. Prepared pulsincap was coated with 5% CAP. The pulsincap was evaluated for in-vitro dissolution studies and release kinetics. Results: F6 formulation was optimized. FTIR and DSC has shown no interaction between polymer and Rizatriptan benzoate. Cross-linked gelatine capsule were evaluated and confirmed that 8 hrs formaldehyde treatment was sufficient.100mg hydrogel plug was optimized Hardness and thickness of the plug controlled lag time. Granules showed good flow properties and drug content were found to be in the range of 95.4±0.56 to 98.3±0.56%. The results indicated that drug content was uniform. In-vitro release studies revealed that increasing the polymer content resulted in sustained release. Value of n in Korsmeyer-Peppas Equation is greater than 1 hence, formulation were follows swelling controlled super case II transport. Conclusion: Present pulsincap formulation study conclude that optimized F6 batch of Rizatriptan benzoate successfully targeted to colon for the treatment of migraine. Drug release over a period of 5-18 hrs, can be achieved from treated gelatine capsule and hydrogel plug.

Formulation and evaluation of modified pulsincap drug delivery system of rizatriptan benzoate

Migraine follows circadian rhythm in which headache is more painful at the awakening time. This needs administration of dosage form at night time to release drug after lag period when pain gets worse. Sumatriptan succinate is a drug of choice for migraine. Sumatriptan succinate has bitter taste, low oral bioavailability and shorter half-life. Present work deals with application of design of experiment for polyox and xanthan gum in development of press coated floating pulsatile tablet. Floating pulsatile concept was applied to increase gastric residence of the dosage form. Burst release was achieved through immediate release tablet using crospovidone as superdisintegrant (10%). Pulse lag time was achieved using swellable polymer polyox WSR205 and xanthan gum. 32 experimental design was applied. Optimized formulation was evaluated for physical characteristics and in-vitro and in-vivo study. From results, it can be concluded that optimized batch F8 containing polyox WSR205 (72.72%) and xanthan gum (27.27%) of total weight of polymer has shown floating lag time of 55 ± 2 sec, drug content of 100.35 ± 0.4%, hardness of 6 ± 0.1 Kg/cm2 and 98.69 ± 2% drug release in pulse manner with lag time of 7 ± 0.1 h. Optimized batch showed prolong gastric residence which was confirmed by in-vivo X-ray study.