Design and Development of Novel Dual-Compartment Capsule for Improved Gastroretention

The aim of the proposed research work was to develop a novel dual-compartment capsule (NDCC) with polymeric disc for gastroretentive dosage form, which will ultimately result in better solubility and bioavailability of Ofloxacin. Floating ring caps were formulated by using different natural polymers, separating ring band and swellable polymer located at the bottom of capsule. Formulated ring caps were assessed for coating thickness, In vitro buoyancy, In vitro drug release, release kinetics and stability studies. Coating attained by the capsule shell was found to be 0.0643 mm. Depending on nature of natural polymer used, most of the formulations showed buoyancy for more than 9 hrs. Developed formulation demonstrated considerably higher drug release up to 9 hrs. The developed formulation FE2 depicted the drug release according to Korsmeyer-Peppas model. There was not any significant change in performance characteristics of developed ring caps after subjecting them to stability studies. The present study suggests that the use of NDCC for oral delivery of Ofloxacin could be an alternative to improve its systemic availability which could be regulated by the floating approach. The designed dosage system can have futuristic applications over payloads which require stomach-specific delivery.

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FORMULATION AND OPTIMIZATION OF BUOYANT IN SITU GELLING SYSTEM OF VALSARTAN USING NATURAL POLYMER

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i10.20809 ◽

2017 ◽

Vol 9 (10) ◽

pp. 128

Author(s):

S. Prasanthi ◽

M. Vidyavathi

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Natural Polymer ◽

Natural Polymers ◽

Independent Variables ◽

Drug Release Kinetics ◽

Ftir Studies

Objective: Currently natural polymers have wide spread importance in fabrication of controlled drug delivery systems. Hence in this study ocimum basilicum mucilage, (OBM) a natural polymer used to know its effect as polymer alone and in combination with HPMC K15M and Guargum in oral in situ floating gel of Valsartan using 3 full level factorial design.Methods: FTIR studies conducted to know major drug polymer interactions. OBM, HPMC K15M and Guargum were chosen as three independent variables and examined at 3 levels for in vitro buoyancy (Y1) and drug release at 10 h (Y2) as responses. By using mathematical model approach formulation variables were quantitatively evaluated, and optimized formulation (VFIG) subjected for in vitro buoyancy, density, pH, in vitro drug release, drug content, gelling capacity and drug release kinetics. In addition VFIG studied for In vivo buoyancy and release kinetics.Results: FTIR studies revealed that excipients were compatible with drug. ANOVA results shown that independent variables have significant effect (p<0.05) on both the responses. Observed responses of optimized formulation (3 % OBM, 0.88 % HPMC and 1.25 % Guar gum) were in good agreement with the experimental values. Results of all in vitro evaluations lies within the limits and drug release kinetics followed non-fickian diffusion mechanism. In vivo buoyancy study in rabbit evidenced floatation for>8 h and in vivo pharmacokinetic study exhibited increased bioavailability of optimized formulation.Conclusion: Prepared VFIG with optimized concentrations of OBM, HPMC K15M and Guargum exploiting as a promising dosage form for enhanced gastric delivery.

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Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

International Current Pharmaceutical Journal ◽

10.3329/icpj.v6i11.36435 ◽

2018 ◽

Vol 6 (11) ◽

pp. 61-80 ◽

Cited By ~ 1

Author(s):

Shashank Soni ◽

Veerma Ram ◽

Anurag Verma

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

Pharmaceutical Journal ◽

Weight Variation ◽

Zero Order Release ◽

Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

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FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1943 ◽

2018 ◽

Vol 8 (5) ◽

pp. 465-474

Author(s):

S PADMA PRIYA ◽

AN Rajalakshmi ◽

P Ilaveni

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Loading ◽

Research Work ◽

Entrapment Efficiency ◽

Polyvinyl Pyrrolidone ◽

Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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EFFECT OF FORMULATION FACTORS ON ORODISPERSIBLE TRIPTAN FORMULATIONS – NOVEL APPROACH IN TREATMENT OF MIGRAINE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i3.23401 ◽

2018 ◽

Vol 11 (3) ◽

pp. 212

Author(s):

Yella Sirisha ◽

Gopala Krishna Murthy T E ◽

Avanapu Srinivasa Rao

Keyword(s):

Drug Release ◽

Factorial Design ◽

Release Kinetics ◽

Research Work ◽

Angle Of Repose ◽

Compatibility Study ◽

In Vitro Drug Release ◽

Orodispersible Tablets ◽

Croscarmellose Sodium

Objective: The present research work is an attempt to determine the effect of various diluents and superdisintegrants on drug release of eletriptan orodispersible tablets and designs an optimized formulation using 22 factorial design. Further, evaluate the tablets for various pre-compression and post-compression parameters.Methods: The drug excipient compatibility study was conducted by infrared spectroscopy, differential scanning colorimetry and X-ray diffraction studies were conducted to test the purity of the drug. The tablets were formulated by direct compression method using spray dried lactose, mannitol, microcrystalline cellulose, starch as diluents and crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants. The powder formulations were evaluated for pre-compression parameters such as bulk density, tapped density, Carr’s Index, Hausner’s ratio, and angle of repose. The tablets were evaluated for post-compression parameters such as the hardness, thickness, friability, weight variation, and disintegrating time in the oral cavity, in vitro drug release kinetics studies, and accelerated stability studies. The formulations were optimized by 22 factorial design.Results: The drug and excipients were compatible, and no interaction was found. The drug was pure, and all the pre-compression parameters were within Indian Pharmacopoeial Limits. Post-compression parameters were also within limits. The disintegration time was found to be 27 s for the formulation F29 containing Croscarmellose sodium (5%) and Mannitol as diluent, and in vitro drug release was found to be 99.67% in 30 min and follows first-order kinetics. This was also the optimized formulation by 22 factorial design with a p=0.013.Conclusion: The orodispersible tablets of eletriptan were successfully formulated, and the optimized formulation was determined that can be used in the treatment of migraine.

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DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE MUCOADHESIVE MICROBEADS CONTAINING SIMVASTATIN WITH DIFFERENT CROSS LINKING AGENTS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i6.38913 ◽

2020 ◽

pp. 118-126

Author(s):

VENKATA RAMANA REDDY K. ◽

NAGABHUSHANAM M. V. ◽

PAMULA REDDY B. ◽

RAVINDAR NAIK E.

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

Aluminium Chloride ◽

In Vitro Dissolution ◽

Cross Linking ◽

Stability Studies ◽

Study Results ◽

Curing Agents

Objective: The aim of the present work was to prepare and examine drug release of the oral controlled release microbeads using different curing agents by emulsification internal ionic gelation technique. Methods: Cross-linked alginate microbeads were prepared with different cross linking agents by using mucoadhesive properties. The formation and compatibility of microbeads were confirmed by compatibility studies. Prepared microbeads evaluated for encapsulated efficiency, micromeritic properties, drug loading, in vitro wash off studies, in vitro dissolution studies, drug release kinetics and stability studies Results: The in vitro drug release was influenced by both type of curing agents and type of polymers and no significant changes in characterization parameters was observed after 3 mo stability studies. The sustained release profile of optimized batch was found to be 99.66±0.18% in comparison to pure drug profile of 28.64±0.02% at 12 h release study. Results of both wash-off and in vitro studies suggests that batch (SF2) prepared with aluminium chloride has shown better mucoadhesive property. Drug release of optimized batch follows zero order with non fickian mechanism according to Korsmeyer-Peppas equation. Conclusion: The data suggest the use of simvastatin mucoadhesive cross linked microbeads to offer the potential for oral controlled drug delivery with improved gastric retention and capable to provide sustained drug release by using cross linking agents.

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APPLICATION OF NOVEL NATURAL POLYMER FOR CONTROLLING THE RELEASE OF FENOVERINE FROM CONTROLLED RELEASE MATRIX TABLETS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i2.16318 ◽

2017 ◽

Vol 9 (2) ◽

pp. 1 ◽

Cited By ~ 1

Author(s):

Ajit Kulkarni ◽

Trushali Mandhare ◽

Nagesh Aloorkar

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Kinetics ◽

Methyl Cellulose ◽

Matrix Tablets ◽

Natural Polymer ◽

In Vitro Drug Release ◽

Dissolution Studies ◽

Drug Content

Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices.Methods: In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study.Conclusion: Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.Keywords: Pullulan, Fenoverine, Hydroxypropyl methyl cellulose, Controlled release, In vitro

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DEVELOPMENT OF MUCOADHESIVE TABLET OF PENTOXIFYLLINE USING A NATURAL POLYMER FROM MANILKARA ZAPOTA LINN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i4.32177 ◽

2019 ◽

pp. 88-91

Author(s):

GNANASEKARAN JOHN SELVARAJ ◽

ARUL BALASUBRAMANIAN ◽

KOTHAI RAMALINGAM

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Natural Polymer ◽

High Concentration ◽

In Vitro Drug Release ◽

Manilkara Zapota ◽

Mucoadhesive Polymer ◽

Weight Variation ◽

Release Studies

Objective: The present study was designed to develop a mucoadhesive tablet of pentoxifylline using the mucoadhesive natural polymer from the plant Manilkara zapota Linn. Methods: The tablets were formulated with three different concentrations of the isolated polymer and evaluated for thickness, weight variation, friability, hardness, swelling index, mucoadhesive strength and in vitro drug release. The swelling index was indirectly proportional to the mucoadhesive polymer of Manilkara zapota (MAPMZ) concentration. Results: The tablets formulated with a high concentration of MAPMZ showed good mucoadhesion strength in 5 min contact time. The in vitro drug release studies indicated that the drug release was directly proportional to MAPMZ concentration. The release kinetics indicated that the drug release was followed the zero-order. Conclusion: The MAPMZ showed the controlled release of pentoxifylline for a period of 12 h.

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PREPARATION AND CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ANTI-HYPERTENSIVE DRUG’’

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v9i4.777 ◽

2020 ◽

Vol 9 (4) ◽

Author(s):

Anukumar E ◽

Nagaraja T S ◽

Yogananda R ◽

Bharathi D R

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Release Kinetics ◽

Stability Studies ◽

In Vitro Drug Release ◽

Hypertensive Drug

The present work is to prepare and characterization of self nano emulsifying drug delivery system containing Anti-hypertensive drug. Losartan is a competitive antagonist and inverse agonist of angiotensin 2 receptor. The SNEDDS is prepared by Sonication method using a components of SPAN 60/Eudragit RS 100 as a surfactant, PVA as a Co-surfactant, Iso propyl alcohol as a solvent and DCM as a co-solvent. The prepared SNEDDS was evaluated for Fourier transform infrared spectroscopy, Surface morphology, particle size, zeta potential, drug entrapment efficiency, visual assessment, self-emulsification time, Robustness to dilution, in-vitro drug release and short term stability studies. The in-vitro drug release data of all the formulations were found to be zero order over a period of 24 h and Formulation F7 shows good results for the drug release kinetics as controlled release. The stability studies data was found that there was no such difference in drug EE and in-vitro drug release.

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Disintegration, In vitro Dissolution, and Drug Release Kinetics Profiles of k-Carrageenan-based Nutraceutical Hard-shell Capsules Containing Salicylamide

Open Chemistry ◽

10.1515/chem-2020-0028 ◽

2020 ◽

Vol 18 (1) ◽

pp. 226-231

Author(s):

Pratiwi Pudjiastuti ◽

Siti Wafiroh ◽

Esti Hendradi ◽

Handoko Darmokoesoemo ◽

Muji Harsini ◽

...

Keyword(s):

Drug Release ◽

Rate Constant ◽

Release Rate ◽

Release Kinetics ◽

Zero Order ◽

Dissolution Profile ◽

Natural Polymers ◽

Drug Release Kinetics ◽

Hard Shell

AbstractThe release of drugs from solid drug delivery materials has been studied intently in recent years. Quantitative analyses achieved from in vitro dissolution becomes easier if a zero-order mathematical model is used. Non-gelatin nutraceutical hard-shell capsules of zero size (approximately 0.7-0.8 cm) were produced from carrageenan-based natural polymers, namely carrageenan-alginate (CA) and carrageenan-starch (CS). Disintegration, dissolution and zero-order drug release kinetics of hard-shell capsules containing 100 mg of salicylamide were studied. The disintegration time of CA and CS were observed to be less than 30 min for both CA and CS. In vitro dissolution profile showed that the percentage dissolution of CA capsules was better at pH 4.5, while that of CS was poor at pH 1.2, 4.5 and 6.8. Determination of drug release kinetics profiles of carrageenan-based hardshell capsules utilized the Noyes-Whitney and Peppas-Sahlin modification rules for zero-order. The drug release from carrageenan-based capsules followed zero-order kinetics, especially at pH 6.8, and was compared to the Higuchi model. Salicylamide in CA hard-shell capsules at a pH 6.8 had a release rate constant (kH) of 2.91 %(ppm/ ppm) min-1/2, while the release rate constant of CS was 0.36 %(ppm/ppm) min-1.

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Formulation and Evaluation of Sustained Release Tablets of Nateglinide by Using natural polymers

International Journal of Advances in Pharmaceutical Sciences ◽

10.5138/09761055.2065 ◽

2017 ◽

Vol 9 (1) ◽

pp. 8 ◽

Cited By ~ 1

Author(s):

Pavani Chowdary ◽

T Sravani ◽

MD Basheeruddin

Keyword(s):

Drug Release ◽

Sustained Release ◽

Bulk Density ◽

Guar Gum ◽

Chemical Interaction ◽

Research Work ◽

Fickian Diffusion ◽

Natural Polymers ◽

Sustained Release Tablets

The purpose of this research work was to formulate and evaluate the sustained release tablets of Nateglinide 500mg, an antidiabetic drug. Nateglinide is an oral hypoglycemic agent. The tablets are prepared by direct compression method. The formulations were optimized by incorporating varying composition of Xanthan gum and guar gum as polymers, lactose as flow aid and magnesium stearate as lubricant. All the excipients are tested for compatibility with drug, which revealed that there was no physical and chemical interaction occurred. The Preformulation parameters such as bulk density, tapped density, compressibility index and Hausner’s ratio were analyzed. The friability, drug content, loss on drying, bulk density and percentage yield was evaluated for tablets. The effect of these variables on drug release also studied. The In-Vitro drug release studied were Performed in the USP dissolution apparatus-II using pH 0.1N HCl as dissolution media at 75 rpm speed and temperature of 37oc ± 5oc. The sampling was done at periodic time intervals of 1,4,8,12,16,20 and 24 hours and was replaced by equal volume of dissolution media after each withdrawal. The cumulative amount of drug release at different intervals is estimated using UV method. Based on the evaluation result the formulations F-7 was selected as best formulation. The tablets were found to follow first order kinetics and Higguchi mechanism of drug release, ‘n’ value is less than 0.5 which confirms that the drug release through the matrix was fickian diffusion.

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