scholarly journals Gastroretentive Drug Delivery System of Levo-Salbutamol Sulphate: Formulation and in vitro Evaluation

Author(s):  
Kamanashis Das ◽  
Md. Yasin ◽  
Ishrak Jahan ◽  
Tahira Akter ◽  
Saiful Islam ◽  
...  

In order to prepare the sustained release tablet with levo-salbutamol sulphate we have used these excipients methylcellulose, PVPK30, magnesium stearate, talc, isopropyl alcohol, microcrystalline cellulose, lactose, HPMCK100, HPMCK4M. Here our approach was for making the sustained released matrix tablet by two ways, one is to make the tablet granules floating and the second one is by retarding the release of the levo-salbutamol sulphate from the matrix. We have already discussed the relationship with delaying the gastric transit time and the active drug absorption, if the tablet granules are floating in our introduction part. Since the above mentioned excipients are floating in nature so formulations with those excipients are supposed to be floating. We also showed a list of excipients those are used in the preparation of floating tablets. Now the second observation which was the release rate, among the three different formulations (mentioned in the introduction) we found different types of release. Since our objective is to prepare a sustained released tablet which will give a prolong release time, in that prospect two among the three formulations were disqualified (though we have not done the kinetic study). We observed desired effect in the formulation-2 during the preparation of experiment.

Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.


Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.


2020 ◽  
Author(s):  
Darren J. Beriro ◽  
Mark R. Cave ◽  
Joanna Wragg ◽  
Russell Thomas ◽  
Christopher Taylor ◽  
...  

<p>The current research builds on the findings of a systematic literature review by the authors which recommends the need to work towards a standardised method for measuring the in vitro dermal absorption of HMW-PAH in soils. One part of the method is understanding the partitioning of the high molecular weight polycyclic aromatic hydrocarbons (HMW-PAH) from soil to sebum found in skin. In vitro HMW-PAH soil-sebum partition coefficients (KSS) were measured for twelve soils collected from former UK gasworks.  Concentrations of ∑16 USEPA PAH in the soils ranged from 51 to 1440 mg/kg, benzo[a]pyrene ranged from 3.2 to 132 mg/kg. Time series extractions (0.5, 1, 2, 4, 8 and 24 h) at skin temperature (32°C) of HMW-PAH from sebum to soil for two samples were conducted to determine the maximum release time-step. The maximum HMW-PAH release time-step was determined as 4 h, which was subsequently used as the extraction time for the remaining samples. Evaluation of KSS data for the 4 h extractions showed that soil type and selected HMW-PAH properties (literature based molecular weight and octanol-carbon partition coefficients) affect the amount of HMW-PAH released from soil into sebum. Characterisation of soil properties was limited to total organic carbon, which showed no relationship to KSS. Selected soils showed distinctly higher K¬SS than others. The relationship between MW and KSS was statistically significant while the relationship between KOC and KSS was not statistically significant. Further research effort is required to improve our understanding of which soil and HMW-PAH properties affect the release of HMW-PAH from soil into sebum and the reasons why.</p>


Author(s):  
Vidya Viswanad ◽  
Shammika P ◽  
Aneesh Tp

ABSTRACTObjective: The current research deals with the formulation and evaluation of synthesized quinazolinone derivative for colon site specific delivery.Methods: The synthesized quinazolinone derivative was enteric coated 5% Eudragit L-100 with by wet granulation method using guar gum, pectin,and guar gum pectin combination as hydrophilic polymer. The prepared matrix tablet was characterized by differential scanning calorimetry andevaluated for different pre-compression and post-compression studies and drug release profiles.Results: All the matrix tablets were within the range of pharmacopeial limits with better flow properties. All the six formulations of matrix tablets haddisintegrated within 5-6 minutes. The optimized formulation selected was F6 formulation combination of guar gum and pectin with 95.79% of drugrelease than compared to the remaining formulation. The optimized matrix tablets followed zero order kinetics with Fickian diffusion.Conclusion: The results proposed that the combination of guar gum and pectin coated tablet with 5% Eudragit L-100 of synthesized quinazolinonederivative is a promising colon site specific delivery.Keywords: Quinazolinone derivative, In vitro drug release, Disintegration time, Guar gum, Pectin, 5% Eudragit L-100, Colon site-specific delivery, Wetgranulation, Compression.


2015 ◽  
Vol 71 (3-4) ◽  
pp. 187-202
Author(s):  
Jasmina Moskovljevic-Popovic

The main purpose of this paper is to analyze different co reference relations which can be established in a complex sentence between one of the arguments of the matrix clause and the understood/implicit subject of the complement clause introduced by the complementizer ?da?. Various patterns of control relations which are present in contemporary Serbian - obligatory, non-obligatory, and shared control - have been enumerated and exemplified. Different types of constructions and different classes of verbs which introduce (or may introduce) control relations have been identified and patterns of control instantiated by them have been described. It has been argued that the analysis of the Serbian data indicates that a type of the matrix predicate is not the only factor which determines the control relations established in a complex sentence, but that a type of situation/event described in the complement clause, as well as the relationship between the events denoted by the matrix and the complement clauses have their influence too.


Author(s):  
Otgonsuren D ◽  
Davaasuren Ts ◽  
Enkhtuul B ◽  
Wang Huang ◽  
Bao Liming ◽  
...  

Monoammonium glycyrrhizinate of Glcyrrhiza root has been used as an expectorant, detoxificator, anti-allergic, and antioxidant. Japanese researchers have been determined its anti-hepatitis A, B, C, D viruses activity. Therefore, we isolated mono-ammonium glycyrrhizinate from Glycyrrhiza root, grown in Mongolia and developed controlled release matrix tablet. Appropriate excipients were chosen for matrix tablet: lactose as a diluent, 5% of PVP-K30 as a binder, HPMC as a matrix former, 3% of talc and 1% of magnesium stearate as a glidiant or lubricant. We prepared matrix tablet by wet granulation method and pressed by 2.5 kPa pressure. Formulation 5 (F5) was determined the most qualified tablet design and it released drug constantly in vitro. For the determining of hepatoprotective effect, we studied influence on hepatocytolis of preparation in vivo by the histological method. Results of the study showed that the Licozinat matrix tablet was appropriate at a 52 mg/kg dose once daily. Ликозинат матрикс шахмалын чанарын болон элэг хамгаалах үйлдлийн судалгаа Хураангуй: Чихэр өвсний үндсэнд агуулагдах моноаммонийн глициризинат нь цэр ховхлох, хордлого тайлах, харшлын эсрэг, антиоксидант үйлдэлтэй. Японы эрдэмтдийн судалгаагаар моноаммонийн глициризинат нь элэг хамгаалах болон А, В, С, D вирүсээр үүсгэгдсэн элэгний үрэвсэлд вирүсийн идэвхжлийг саатуулдаг нь тогтоогдсон байна. Бид өөрийн оронд ургадаг Уралын чихэр өвсний үндэснээс моноаммонийн глицирризинатыг цэврээр ялган авч эмчилгээний өндөр ач холбогдол бүхий матрикс хэлбэрийн шахмал гарган авч практикт нэвтрүүлэх нь зүйтэй гэж үзлээ.Бид эмийн бодисоо зохицуулалттай чөлөөлдөг матрикс шахмалын тохирох дүүргэгч бодисоор лактоз, холбогч бодисоор PVP-K30 5% концентрациар, матрикс үүсгэгчээр НРМС, гулсуулагч тослох бодисоор тальк 3%, магнийн стеарат 1%-ийн холимгийг сонгох нь тохиромжтой болохыг тогтоов.In vitro нөхцөлд эмийн бодисын чөлөөлөгдөлтийг тодорхойлоход F5 загварын шахмал нь эмийн бодисоо жигд хурдтайгаар чөлөөлж байв. Туршилтын амьтанд in vivo нөхцөлд бэлдмэлийн элэг хамгаалах үйлдлийг элэгний эсийн задралд хэрхэн нөлөөлж буй болон гистологийн аргаар судлахад Ликозинат матрикс шахмал эмийг 52 мг/кг тунгаар өдөрт нэг удаа уулгах нь тохиромжтой болохыг тогтоолоо. Түлхүүр үгс: Чихэр өвс, моноаммонийн глицирризинат, матрикс шахмал, элэг хамгаалах идэвх


2012 ◽  
Vol 1 (11) ◽  
pp. 376-383 ◽  
Author(s):  
M Mallikarjuna Gouda ◽  
A Ramakrishna Shabaraya ◽  
S M Shanta Kumar

Current study is to develop the colon targeted matrix tablet using the natural polysaccharide sterculia gum as carrier and model drug ciprofloxacin HCl. The matrix tablets were prepared by wet granulation technology using the various proportions of sterculia gum with carbopol 934 P, sterculia gum and ethyl cellulose polymer blends. Granules of all formulations were evaluated for rheological, post compressional properties and in vitro dissolution study in different pH buffers of pH 1.2 , pH 7.4 , pH 6.8 (saline phosphate buffer) without and with 4% rat cecal content in order to mimic GIT condition . Formulation SGC2 to SGC4 and SGE7 to SGE9 has released 13.6% to 38.9% in the initial 5h and released more amount of drug in stomach and small intestine than colon. Formulation SGC5 containing 45% of sterculia gum and 25% carbopol 934 p and Formulation SGE10 containing 45% of sterculia gum and 25% ethyl cellulose has released minimum 10.91 % to 13.04 % in the initial 5h and sustained the drug release up to 24 h and at the end of study released 75% to 79.99%. Formulations with 4% rat cecal content at the end of 24 h study drug released is 90.44% to 95.33% indicating higher amount of drug release is due to enzymatic break down of sterculia gum in the matrix tablet. Hence the above results conclude that the formulation SGC5 and SGE10 are potential in targeting the drug to colon to treat irritable bowel disease.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12064 International Current Pharmaceutical Journal 2012, 1(11): 376-383


Author(s):  
Mona Semalty ◽  
T Bisht ◽  
A Semalty

The aim of the present study was to develop sustained release, multilayered-matrix tablet of aceclofenac using natural polymers-guar gum (GG) and xanthan gum (XG) as carrier for core matrix and hydroxyl propylmethyl cellulose (HPMC K-15M), sodium carboxymethylcellulose (NaCMC) and ethyl cellulose (EC) and polyvinylpyrrolidone (PVP-K30) for preparing bottom and top layers. The formulated tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, swelling index and in vitro drug release. The physicochemical properties of tablets were found within the limits. The physiochemical investigation showed that aceclofenac matrix tablet prepared with xanthan gum showed better dissolution profile as compared to that of guar gum. Matrix tablets of xanthan gum with 6% W/V xanthan gum (MTX1) showed the highest percent drug release (88.98%), while matrix tablets of guar gum with 6% W/V guar gum (MTG1) showed the highest percent drug release (73.89%) at the end of 8 hours in pH 6.8 phosphate buffer. Among the matrix tablet of xanthan gum MTX4 (with 24% W/V of xanthan) showed the lowest percent drug release (49.6%) and while among the guar gum tablets MTG4  (with 24% W/V of guar gum) showed the lowest percent drug release (48.65%) at the end of 8 hours. It was concluded that increasing the concentration of gum from 6% W/V to 24% W/V in the formulation decreased the amount of drug release from the tablet. The xanthan gum based matrix tablets of aceclofenac were found to be superior to that of guar gum matrix tablets for potential therapeutic uses. 


2020 ◽  
Vol 10 (12) ◽  
pp. 942
Author(s):  
Anna Volnova ◽  
Vassiliy Tsytsarev ◽  
Maria Ptukha ◽  
Mikhail Inyushin

Epilepsy remains one of the most common brain disorders, and the different types of epilepsy encompass a wide variety of physiological manifestations. Clinical and preclinical findings indicate that cerebral blood flow is usually focally increased at seizure onset, shortly after the beginning of ictal events. Nevertheless, many questions remain about the relationship between vasomotor changes in the epileptic foci and the epileptic behavior of neurons and astrocytes. To study this relationship, we performed a series of in vitro and in vivo experiments using the 4-aminopyridine model of epileptic seizures. It was found that in vitro pathological synchronization of neurons and the depolarization of astrocytes is accompanied by rapid short-term vasoconstriction, while in vivo vasodilation during the seizure prevails. We suggest that vasomotor activity during epileptic seizures is a correlate of the complex, self-sustained response that includes neuronal and astrocytic oscillations, and that underlies the clinical presentation of epilepsy.


2012 ◽  
Vol 10 (1) ◽  
pp. 1-7
Author(s):  
Md Saiful Islam ◽  
Md Ziaur Rahman Khan ◽  
Masuda Khatun ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza

Controlled release matrix tablets of Theophylline anhydrous and Theophylline sodium glycinate were prepared with different types of bio-adhesive polymers e.g. HPMC 15 & 50 cps, Gelatin, PVP K-30, Na-CMC and Xanthan gum. Tablets, prepared by direct compression method were subjected to in-vitro drug dissolution for 8 hours in 0.1 N hydrochloric acid (pH 1.2) using a thermal shaker at 50 rpm at 37 ± 0.5ºC. The bio-adhesive property was investigated in terms of retention time following in-vitro wash-off method by Lehr et al. The anhydrous and corresponding salt form was used to investigate whether physical variation of Theophylline molecule can cause any change in release and bio-adhesion property or not. In most of the cases it is found that salt form releases greater percentage of active drug than its corresponding anhydrous form. Irrespective of drug’s physical property and amount of polymer, bio-adhesive strength of Xanthan gum was proved to be maximum followed by HPMC- 50 cps, Na-CMC and HPMC- 15 cps, whereas gelatin and PVP K-30 showed little or poor muco-adhesion. Xanthan gum, Na-CMC and HPMC based formulations showed nearly zero-order release; on the contrary PVP K-30 based formulation showed a burst release within one hour of dissolution.DOI: http://dx.doi.org/10.3329/dujps.v10i1.10008DUJPS 2011; 10(1): 1-7


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