Ternary Blends of some Hydrophilic and Hydrophobic Polymers in Colon Targeted Delivery of Metronidazole

Matrix tablets were prepared using blends of xanthan gum (XG), Guar gum (GG) and ethylcellulose (EC). The polymers were combined using six different ratios; 1:1:1, 1:2:1, 1:2:2, 2:2:1, 2:1:2 and 2:1:1 to produce formulations XG1GG1EC1, XG1GG2EC1, XG1GG2EC2, XG2GG2EC1. XG2GG1EC2 and XG2GG1EC1 respectively. Metronidazole was used as the model drug. The ability of the prepared matrices to target drug release predominantly at the colon under the influence of colonic bacteria was evaluated using the dissolution medium containing 4 % caecal content. Our results show that, optimum drug release was observed with formulations XG2GG2EC1 and XG2GG1EC1 with Cmax of 60 and 76 % respectively. Significant difference (P<0.05) was observed between drug release in dissolution medium with and without rat caecal contents for the batches of Metronidazole tablets. Formulations (XG2GG2EC1 and XG2GG1EC1) followed Higuchi square roots kinetics ( r2 =0.9942) via fickian diffusion ( n < 0.45 ) and Korsemeyer model (r2 = 0.9939) via non – fickian diffusion (n > 0.45) respectively. Key Words; matrix.guar, xanthan, ethylcellulose, metronidazole, colon deliver

Extraction and Nanoencapsulation of Ocimum Gratissimum Leaf Extract and Its Anti-Mycobacterial Activities

Isolation of saponin from the methanol extract of Ocimum gratissimum leaves, its identification with High-Performance Liquid Chromatography (HPLC), application of the saponin in the synthesis of nanoemulsion and their antimicrobial activities were carried out. 0.7mg was isolated from 40g of powdered leaves mixed with 70% of methanol. The methanol and saponin extracts were subjected to HPLC analysis. The methanol extracts revealed 15 peaks and the saponin revealed 8 peaks with a total elution time of 30 minutes each. The saponin was used to synthesize nanoemulsion (emulsifier). The nanoemulsion and saponin were subjected to antituberculosis activity. The nanoemulsion has better anti-tuberculosis activity than the saponin due to its Minimum Inhibitory Concentration (MIC). This goes to confirm the importance of nanomedicine in the drug delivery system and its application on diverse areas such as food, cosmetics, pharmaceuticals, and material synthesis. The biological synthesis is an eco-friendly alternative to the chemical and physical methods. Keywords: Extraction, Natural Product, Nanoencapsulation, Ocimum gratissimum, Anti-Mycobacterial, Tuberculosis. DOI: 10.7176/CMR/12-2-03 Publication date: February 29th 202

Polimerne mješavine obložene Eudragitom: Potencijalni sustav za kontroliranu peroralnu isporuku teofilina

Sustained release (SR) dosage forms enable prolonged and continuous deposition of the drug in the gastrointestinal (GI) tract and improve the bioavailability of medications characterized by a narrow absorption window. In this study, a new strategy is proposed for the development of SR dosage forms for theophylline (TPH). Design of the delivery system was based on a sustained release formulation, with a modified coating technique and swelling features aimed to extend the release time of the drug. Different polymers, such as Carbopol 71G (CP), sodium carboxymethylcellulose (SCMC), ethylcellulose (EC) and their combinations were tried. Prepared matrix tablets were coated with a 5 % (m/m) dispersion of Eudragit (EUD) in order to get the desired sustained release profile over a period of 24 h. Various formulations were evaluated for drug concentration and in vitro drug release. It was found that the in vitro drug release rate decreased with increasing the amount of polymer. Coating with EUD resulted in a significant lag phase in the first two hours of dissolution in the acidic pH of simulated gastric fluid (SGF) due to decreased water uptake, and hence decreased driving force for drug release. Release became faster in the alkaline pH of simulated intestinal fluid (SIF) owing to increased solubility of both the coating and matrixing agents. The optimized formulation was subjected to in vivo studies in rabbits and the pharmacokinetic parameters of developed formulations were compared with the commercial (Asmanyl®) formulation. Asmanyl® tablets showed faster absorption (tmax 4.0 h) compared to the TPH formulation, showing a tmax value of 8.0 h. The cmax and AUC values of TPH formulation were significantly (p < 0.05) higher than those for Asmanyl®, revealing relative bioavailability of about 136.93 %. Our study demonstrated the potential usefulness of eudraginated polymers for the oral delivery of the sparingly soluble drug theophylline.Pripravci za produljeno oslobađanje (SR) omogućavaju produljeno i kontinuirano oslobađanje lijeka u gastrointestinalnom (GI) traktu i poboljšavaju bioraspoloživost lijekova s uskim apsorpcijskim prozorom. U radu se predlaže nova strategija za razvoj formulacija s produljenim oslobađanjem teofilina (TPH), koja se temelji na sustavu za produljeno oslobađanje, kojem je u svrhu produljenja vremena oslobađanja modificiran način oblaganja i bubrenja. Korišteni su različiti polimeri, kao što su Carbopol 71G (CP), natrijeva karboksimetilceluloza (SCMC), etilceluloza (EC) i njihove kombinacije. Pripravljene matriks tablete obložene su 5-postotnom (m/m) disperzijom Eudragita (EUD) kako bi se postiglo produljeno oslobađanje tijekom 24 h. U pripravljenim formulacijama određena je koncentracija lijeka i in vitro oslobađanje. Rezultati pokazuju da se povećanjem udjela polimera smanjuje brzina oslobađanja in vitro. Oblaganje s EUD značajno je produljilo lag fazu tijekom prva 2 sata otapanja u kiselom pH simuliranog želučanog soka (SGF). Naime, oblaganje usporava ulazak vode i tako smanjuje pogonsku silu za oslobađanje lijeka. Zbog povećane topljivosti obložnog sloja i matriksa u lužnatom mediju, oslobađanje u simuliranoj intestinalnoj tekućini (SIF) je brže. Optimizirana formulacija ispitana je in vivo na zečevima. Farmakokinetički parametri novih formulacija uspoređivani su s komercijalnim pripravkom Asmanyl®. Asmanyl® tablete pokazuju bržu apsorpciju (tmax 4,0 h) u odnosu na TPH formulaciju (tmax 8,0 h). cmax i AUC vrijednosti TPH formulacije bile su značajno (p < 0,05) više od onih za Asmanyl®, što ukazuje na relativnu bioraspoloživost od oko 136,93 %. Stoga smatramo da su polimeri obloženi eudragitom potencijalno korisni za oralnu upotrebu teško topljivog lijeka teofilina

Ternary Blends of some Hydrophilic and Hydrophobic Polymers in Colon Targeted Delivery of Metronidazole

Matrix tablets were prepared using blends of xanthan gum (XG), Guar gum (GG) and ethylcellulose (EC). The polymers were combined using six different ratios; 1:1:1, 1:2:1, 1:2:2, 2:2:1, 2:1:2 and 2:1:1 to produce formulations XG1GG1EC1, XG1GG2EC1, XG1GG2EC2, XG2GG2EC1. XG2GG1EC2 and XG2GG1EC1 respectively. Metronidazole was used as the model drug. The ability of the prepared matrices to target drug release predominantly at the colon under the influence of colonic bacteria was evaluated using the dissolution medium containing 4 % caecal content. Our results show that, optimum drug release was observed with formulations XG2GG2EC1 and XG2GG1EC1 with Cmax of 60 and 76 % respectively. Significant difference (P&lt;0.05) was observed between drug release in dissolution medium with and without rat caecal contents for the batches of Metronidazole tablets. Formulations (XG2GG2EC1 and XG2GG1EC1) followed Higuchi square roots kinetics ( r2 =0.9942) via fickian diffusion ( n &lt; 0.45 ) and Korsemeyer model (r2 = 0.9939) via non – fickian diffusion (n &gt; 0.45) respectively. Key Words; matrix.guar, xanthan, ethylcellulose, metronidazole, colon deliver

Učinak molekulske mase karboksimetilceluloze i nekih polimera na usporeno oslobađanje teofilina iz hidrofilnih matriksa

The objective of this study was to investigate the influence of the molecular size of carboxymethylcellulose (cmc) and some hydrophobic polymer additives on the release properties of theophylline from the tablet matrices. The cmc matrices were prepared by the conventional wet granulation method. The granules were evaluated for angles of repose, bulk density, compressibility index, and porosity, while the tablets were subjected to hardness, friability and compression characteristics. All the tablet formulations showed acceptable pharmacotechnical properties. Low molecular size cmc (cmc-L) had the fastest drug release t50% values of 27 min, for medium size cmc (cmc-M) 55 min and high molecular size cmc (cmc-H) 200 min. Overall, results showed that drug release rate decreases with increase in molecular size of cmc. All the polymer additives ethylcellulose (ETC), cellulose acetate phthalate (CAP) and Eudragit l-100 (EUD) retarded theophylline release from cmc-L and cmc-H, with ethylcellulose having the most pronounced effect on cmc-L. Kinetic studies using Hixson-Crowell and Peppas-Ritger equations showed that different drug release mechanisms were involved in controlling drug dissolution from the tablets. Drug release mechanism was influenced by both the molecular size of cmc and the presence of polymer additives.U radu je ispitivan učinak molekulske mase karboksimetilceluloze (cmc) i nekih hidrofobnih polimera kao aditiva na profil oslobađanja teofilina iz tabletnih matriksa. Matriksi s cmc pripremljeni su uobičajenom metodom vlažne granulacije. Granulama je određivana sipkost, gustoća, poroznost i indeks kompresivnosti, dok je tabletama ispitivana tvrdoća, rastrošljivost i kompresibilnost. Sve priređene tablete imala su prihvatljiva farmakotehnološka svojstva. Najbrže vrijeme oslobađanja t50% od 27 min postignuto je iz pripravka cmc male molekulske mase (cmc-L), 55 min iz pripravka cmc srednje molekulske mase (cmc-M) 55 min i 200 min iz pripravka cmc velike molekulske mase (cmc-H). Rezultati ukazuju da se brzina oslobađanja smanjuje povećanjem molekulske mase cmc. Svi polimerni aditivi, etilceluloza, celuloza acetat ftalat i Eudragit l-100 usporili su oslobađanje teofilina iz cmc-L i cmc-H pripravka, a najveći učinak imala je etilceluloza na cmc-L. Kinetičke studije provedene pomoću Hixson-Crowell-ove i Peppas-Ritger-ove jednadžbe ukazuju da su u oslobađanju teofilina iz tableta uključeni različiti mehanizmi. Na mehanizam oslobađanja utjecali su i molekulska masa cmc i prisutnost polimernih aditiva

Total Quality Management in a Resource-Starved Nation

Total quality management (TQM) is defined as management approach, which empowers employees to adequately satisfy the customer needs. For efficient TQM, management is required to be fully committed, focused and goal-driven. The needs of employees such as tools and resources required for efficiency, self-improvement and corresponding recognition to reward for hard work are paramount in TQM; to achieve this in a resource starved nation such as Nigeria is a huge challenge. In 2016, the National Institute for Pharmaceutical Research and Development (NIPRD) decided that it was adopting TQM in its research and development activities. The challenge, however, was lack of infrastructure and trained personnel in this highly specialized and sensitive area. Respite came when the United States Agency for International Development (USAID) through the United States Pharmacopoeia Convention Promotion of Quality Medicines (USP/PQM) agreed to provide support. Two years later (2018), NIPRD laboratory has been accredited by the American National Accreditation Board (ANAB) as the only academic institution and probably the only academic-based research institute in West Africa. We discuss herein TQM in a resource starved nation like Nigeria and propose that developing countries should collaborate in all areas of TQM with a view to upgrading institutions to international standards

History, Evolution and Future of Starch Industry in Nigeria

Starch industry has progressed into a business that is worth billions of dollars globally, as they have been found useful in the food, textile, biofuel, plastic and the pharmaceutical industries. Nigeria can be the largest producer of starch in the world. Her major sources are roots and tubers (cassava, yam, cocoyam and potato), cereals (maize, sorghum, millet and rice) and fruits (banana, plantain and breadfruit). Although, all the starch crops are abundantly produced in Nigeria, only less than 1% is processed into high quality starch for industrial processes. This chapter therefore examines the past, the progression and the current state of the starch industry in Nigeria and the roles the government and relevant stakeholders must play in order to revolutionize the industry in Nigeria