Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride

Pandit, Vinay; Pai, Roopa S; Yadav, Vivek R.; Devi, Kshama; Surekha, Bhavya; Inamdar, Mohd N; Suresh, Sarasija

doi:10.3109/03639045.2012.662503

Cited by 30 publications

(23 citation statements)

References 17 publications

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“…Floating ethyl cellulose microspheres containing metformin HCl was prepared by emulsion solvent evaporation method using different drug:polymer concentration ratio (1:1-1:6), and then, its pharmacokinetic and pharmacodynamic properties were evaluated (Pandit et al, 2013). The production yield values of all microsphere formulations were higher than 85%, and the entrapment efficiency values were in the range of 45-82%.…”

Section: Metformin-loaded Microparticles and Nanoparticlesmentioning

confidence: 99%

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Çetin

Şahin

2015

Drug Delivery

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Context: Metformin hydrochloride is a biguanide derivative widely used for the treatment of type 2 diabetes, prescribed nearly to 120 million people worldwide. Metformin has a relatively low oral bioavailability (about 50-60%). Although the major effect of metformin is to decrease hepatic glucose output as an antihyperglycemic agent, its inhibitory effects on the proliferation of some cancer cells (e.g. prostate, breast, glioma cells) have been demonstrated in the cell culture studies. Development of novel formulation (e.g. microparticles, nanoparticles) strategies for metformin might be useful to improve its bioavailability, to reduce the dosing frequency, to decrease gastrointestinal side effects and toxicity and to be helpful for effective use of metformin in cancer treatment. Objective: The main aim of this review is to summarize metformin HCl-loaded micro-and nanoparticulate drug delivery systems. Method: The literature was rewieved with regard to the physicochemical, pharmacological properties of metformin, and also its mechanism of action in type 2 diabetes and cancer. In addition, micro-and nanoparticulate drug delivery systems developed for metformin were gathered from the literature and the results were discussed. Conclusion: Metformin is an oral antihyperglycemic agent and also has potential antitumorigenic effects. The repeated applications of high doses of metformin (as immediate release formulations) are needed for an effective treatment due to its low oral bioavailability and short biological half-life. Drug delivery systems are very useful systems to overcome the difficulties associated with conventional dosage forms of metformin and also for its effective use in cancer treatment.

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Section: Metformin-loaded Microparticles and Nanoparticlesmentioning

confidence: 99%

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Çetin

Şahin

2015

Drug Delivery

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“…2 Penggunaan MH dengan dosis yang besar dan secara berulang memungkinkan terjadinya gangguan gastrointestinal dan toksisitas sebanyak 30%. 3 Efek samping yang dapat ditimbulkan yaitu seperti perut terasa tidak nyaman, mual dan diare.…”

Section: Pendahuluanunclassified

Optimasi Konsentrasi Etil Selulosa dan Lama Pengadukan dalam Preparasi Microspheres Metformin Hidroklorida

Sukmaningrum

Sari

Irawan

2017

IJPST

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AbstrakMetformin hidroklorida (MH) merupakan obat pilihan pertama yang digunakan dalam terapi diabetes mellitus tipe 2, namun dapat menimbulkan efek samping pada saluran pencernaan sehingga MH tepat dipreparasi menjadi sediaan microspheres. Banyak faktor yang mempengaruhi hasil preparasi microspheres di antaranya adalah konsentrasi etil selulosa (EC) dan lama pengadukan yang digunakan. Penelitian ini bertujuan untuk mengetahui komposisi terbaik konsentrasi EC dan lama pengadukan yang dapat menghasilkan microspheres MH-EC dengan entrapment efficiency (EE) tertinggi menggunakan optimasi desain faktorial. MH digunakan sebagai bahan aktif, EC digunakan sebagai polimer serta non-aqueous solvent evaporation method sebagai teknik yang dipilih dalam preparasi microspheres. Hasilnya microspheres yang menggunakan konsentrasi EC sebanyak 4.500 mg dan lama pengadukan selama 2 jam menghasilkan EE sebesar 84,6 ± 0,557% dengan nilai verifikasi EE sebesar 98,1%, drug loading sebesar 12,7 ± 0,173% dan yield sebesar 95,1 ± 0,612%. Microspheres memiliki bentuk sferis dan morfologi permukaan yang relatif halus dan cerah serta ukuran partikel sebesar 173,8 ± 4,41µm. Hasil analisis FTIR menunjukkan bahwa tidak ada perubahan gugus fungsi spesifik pada MH sebagai bahan aktif. Kata kunci: microspheres, metformin hidroklorida, etil selulosa Optimization of Ethyl Cellulose Concentration and Stirring Time on Metformin Hydrochloride Microspheres AbstractMetformin hydrochloride (MH) has been used as a first line for treatment of diabetes mellitus type 2. It could cause gastrointestinal side effects, therefore it is appropriate to be prepared as microspheres. Many factors affect the result of microspheres preparation, such as EC concentration and stirring time which used in preparation. This research was aimed to find the best composition of ethyl cellulose (EC) concentration and stirring time to produce MH-EC microspheres with the highest entrapment efficiency (EE) using factorial design optimization. MH was used as a drug, EC was used as a polymer and non-aqueous solvent evaporation method was chosen for technique of microspheres preparation. The result of microspheres preparation used 4,500 mg of EC and 2 hours stirring time produced 84.6 ± 0.557% EE, 98.1% EE verification, 12.7 ± 0.173% drug loading and 95.1 ± 0.612% yield. The microspheres had spherical structure and a relatively smooth and bright surface morphology. The particle size was 173.8 ± 4.41 μm. FT-IR analysis indicated that there were no changes in the spesific functional groups on MH as an active substance.

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“…A hatóanyag elnyújtott felszívódására további technológiai módosításokat -ozmotikus felszívódás késlelteté-sét [16], mikroszféra-szerkezetet [17] − is kifejlesztettek, ezek azonban szélesebb körben nem terjedtek el. Újabb elhúzódó felszívódású változatával (delayed reabsorption -DR) biztató -fázis II − vizsgálatokat folytatnak (kifejlesztésének elméleti hátterére a későbbiekben viszszatérünk) [14].…”

Section: A Metformin Farmakokinetikájának Főbb Adataiunclassified

Metformin – újabb adatok egy megbízható és hatékony „régi” vércukorcsökkentő készítményről

Winkler

2016

Orvosi Hetilap

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A metformin a 2-es típusú diabetes vércukorcsökkentő kezelésének alapgyógyszere: a hatályos kezelési irányelvek szerint ellenjavallat/intolerancia hiányában adását a betegség egész tartamában fenn kell tartani, inzulinkezelés bevezetését követően is. Az utóbbi időben mind több részlet vált ismertté hatásai molekuláris hátterét illetően, a megismeréssel párhuzamosan nőtt azonban a megválaszolásra váró újabb kérdések száma is. Az áttekintő közlemény a szer klinikai farmakológiájával és hatásspektrumával kapcsolatos már kikristályosodott, illetve újabb adatokat járja körül. Röviden kitér a hatását potenciálisan befolyásoló genetikai polimorfizmusokra és gyógyszer-interakciókra is. Orv. Hetil., 2016, 157(23), 882-891.Kulcsszavak: metformin, farmakokinetika, farmakodinamika, molekuláris mechanizmusok, genetikai polimorfizmusok, gyógyszer-interakciók Metformin -new data of an "old", but efficient, safe and reliable antidiabeticsMetformin is the basic drug of antihyperglycemic therapy in type 2 diabetes: according to actual therapeutic guidelines, it should be given in the absence of contraindications or intolerance during the whole course of the disease even after the initiation of insulin therapy. Recently more and more details have been explored regarding the molecular background of its effects, however, in parallel with the enormous growing knowledge, the number of questions still waiting to be answered has also grown. This review article deals with data already crystallized as well as with details not definitely cleared up. Genetic polymorphisms as well as potential drug interactions influencing the effects of metformin are also briefly summarized. ÖSSZEFOGLALÓ KÖZLEMÉNYRövidítések 5-HT3 = 5-hidroxi-triptamin-3; ADP = adenozin-difoszfát; AgRP = (Agouti-related protein) Agouti-szerű fehérje; AMP = adenozin-monofoszfát; AMPK = AMP-vel aktiválódó kináz; ATP = adenozin-trifoszfát; CART = (cocaine-amphetamine retard transcript) kokain-amfetamin függő termék; CI = (confidence interval) megbízhatósági tartomány; CIN = (contrastinduced nephropathy) kontrasztanyag kiváltotta vesekároso-dás; CYP = citokróm P450 mikroszomális enzimrendszer; DR = (delayed reabsorption) késleltetett felszívódású gyógy-szerváltozat; FDA = (Food and Drug Administration) (amerikai) Élelmiszer-és Gyógyszerfelügyelet; GFR = glomerularis filtrációs ráta; GLP-1 = (glucagon-like peptide) glükagonszerű peptid-1; HIF = hypoxia indukálta faktor; ICAM = (intercellular cell adhesion molecule) intercelluláris sejtadhéziós molekula; IR = (immediate release) azonnal oldódó gyógyszerválto-

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Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride

Cited by 30 publications

References 17 publications

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Optimasi Konsentrasi Etil Selulosa dan Lama Pengadukan dalam Preparasi Microspheres Metformin Hidroklorida

Metformin – újabb adatok egy megbízható és hatékony „régi” vércukorcsökkentő készítményről

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