New Formulation and Evaluation of Camptothecin Encapsulated and/or Dispersed Suppository

2020 ◽  
Vol 20 ◽  
Author(s):  
Sofiane Fatmi ◽  
Lamia Taouzinet ◽  
Malika Lahiani-Skiba ◽  
Mohamed Skiba ◽  
Mokrane Iguer-Ouada
Keyword(s):  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Physical Parameters ◽  
Type I ◽  
Weight Variation ◽  
New Formulation ◽  
Soluble Base

Background: Camptothecin is known for a potent anticancer activity. However, its optimal activity is reduced due to its low solubility and stability in biological media. Objective: The aim of present study is to design and characterize a camptothecin (CPT) suppository formulation. Methods: Rectal suppositories of: camptothecin alone, encapsulated with cyclodextrin (CD) and in ternary system (CPT encapsulated with cyclodextrin and dispersed in polyethylene glycol (PEG) 6000) were prepared using various hydrophobic and hydrophilic polymeric bases as semi-synthetic glyceride (Suppocire® AM Pellets) and polyethylene glycols (PEGs) mixtures. Formulations were evaluated by various parameters like weight variation, drug content, hardness and liquefaction time. In vitro release study was performed in USP type I apparatus using phosphate buffer pH 7.2 as dissolution media. Results: Suppositories were within the permissible range of all physical parameters. In vitro drug released from water soluble base (PEG) was greater than that from oil soluble base with ninety percent (90%) of drug dissolution. It was also established that drug release from various formulations was by diffusion mechanism according to Higuchi’s equation. Conclusion: This new formulation offers a new approach to colorectal cancer treatment by offering an alternative and simple drug administration route.

scholarly journals Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
V. J. Kapure ◽  
V. V. Pande ◽  
P. K. Deshmukh
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Weight Variation ◽  
Liquisolid Compacts ◽  
Rosuvastatin Calcium

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

Design and Evaluation of Rectal Suppositories of Carvedilol

2009 ◽  
Vol 2 (3) ◽  
pp. 654-660
Author(s):  
P. V. Swamy ◽  
Laeeq Farhana ◽  
S. B. Shirsand ◽  
Md.Younus Ali ◽  
Ashokgoud Patil
Keyword(s):  
Drug Release ◽  
Significant Degree ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation ◽  
Rectal Suppositories

Carvedilol (non-cardio selective b-blocker) is an antihypertensive used in management of hypertension, angina pectoris and heart failure.  But its oral bioavailability is about 25-35% only due to significant degree of first pass metabolism.  It has gastrointestinal side effects such as diarrhea, gastric pain and irritation.  Hence, rectal suppositories of carvedilol were developed by using different water-soluble polymeric bases like gelatin and agar-agar using propylene glycol as plasticizer. The gelatin suppositories were disintegrating/dissolving type while gelatin–agar based suppositories were non-disintegrating/non-melting. All the formulations were evaluated for various physical parameters like weight variation,  drug content uniformity, liquefaction time, micro-melting range, in vitro dissolution, short-term stability and drug-excipient interaction (FTIR).  The mechanism of drug release was diffusion controlled and follows first order kinetics in majority of cases. The results suggested that when gelatin is replaced up to 25% w/w with agar, liquefaction time and drug release were not appreciably affected; higher proportions of agar exhibited incomplete and slow release.  Stability studies conducted at 25±3º C and 60±5% relative humidity for three months indicated that the formulations were stable in the drug-content and in vitro drug release rate (p<0.05).

scholarly journals Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Weight Variation ◽  
Vitro Release

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

scholarly journals Design of Extended Release Matrix Tablet of Tramadol hydrochloride Using Combination of Hydrophobic and Hydrophilic Polymer

2017 ◽  
Vol 9 (05) ◽  
Author(s):  
Sunil Kumar Shah ◽  
Prabhakar Bhudholiya ◽  
Supriya Pandey ◽  
Sujata Kushwaha ◽  
Firoz Khan
Keyword(s):  
Extended Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Physical Parameters ◽  
Matrix Tablet ◽  
Hydrophilic Polymer ◽  
Tramadol Hydrochloride ◽  
Hydrophobic Polymer ◽  
Weight Variation

The aim of design of oral extended drug delivery system is to achieve a prolonged therapeutic effect by continuously releasing medicament over an extended period of time after administration of a single dose. An attempt was made to formulate Tramadol Extended Release (ER) matrix tablet using combination of hydrophobic and hydrophilic polymer consisting of ethyl cellulose, HPMC K15M, carbopol, and xanthan gum. The polymeric concentration of hydrophobic and hydrophilic polymer was optimized and was found that drug to polymeric ratio (hydrophobic and hydrophilic) of 1:0.75:0.75 was appropriate for the formulation of Tramadol ER tablet. The concentration of hydrophobic polymer was kept constant were as the combination of hydrophilic polymer was attempted and combined to hydrophobic polymer to retard the drug release for 24-hour from the matrix tablet. A total of nine formulations (F1-F9) of Tramadol matrix tablet, with different concentration of hydrophobic and hydrophilic polymer were used with other excipients. The tablets were compressed by direct compression method after subjecting the blend to blend physical parameters studies like studies like angle of repose, bulk density, tapped density, Carr’s index. The results obtained were satisfactory. Post compression parameters like hardness, weight variation, friability, drug content analysis and in-vitro release profiles of drug from all the formulations could be best expressed by Higuchi’s equation, as the plots showed high linearity (R2: 0.942-0.995). To confirm the diffusion mechanism, the data were fit into Korsmeyer equation. The formulations F-1 to F-6 showed good linearity (R2: 0.961 to 0.993), which indicate the mechanism is diffusion coupled with erosion.

scholarly journals Formulation and evaluation of matrix tablets of Eperisone hydrochloride

2020 ◽  
Vol 1 (4) ◽  
pp. 131-136
Author(s):  
Peruboina Neelima ◽  
Maddula Venkata Ramana
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Hepatic Metabolism ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Spinal Reflexes ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Weight Variation

The aim of the present research is to develop and optimize Eperisone Hydrochloride extended release matrix tablets. Eperisone Hydrochloride is an antispasmodic drug mainly used to relieve pains it acts by relaxing the skeletal and smooth vascular muscles by blocking spinal reflexes drug which has oral bioavailability of 70% due to hepatic metabolism. Sustained release matrix tablets of Eperisone Hydrochloride were prepared through wet granulation technique by using HPMC K4M and EC as polymers, PVPK30 as binder, Magnesium stearate as lubricant and Talc as glidant. The granules of different formulations were determined for pre compression parameters. The prepared granules along with the excipients were then compressed. The formulated tablets were evaluated for physical characteristics viz. Hardness, Thickness, % Weight variation, Friability and the drug content. Furthermore the tablets evaluated for the in vitro release studies. Out of all the 8 formulations F7 showed desired characteristics in the physical parameters and in vitro drug release of 85.48% in 12hrs.The F7 dissolution data was best fitted to the Zero order model. The prepared Eperisone Hydrochloride matrix tablets found to be having a potential extended drug release.

EFFECT OF HYDROPHILIC POLYMERS ON CONTROLLED RELEASE MATRIX TABLETS OF ACYCLOVIR

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (01) ◽  
pp. 42-49
Author(s):  
P Ashok Kumar ◽  
◽  
S. Damodar Kumar
Keyword(s):  
Controlled Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Fickian Diffusion ◽  
Sem Images ◽  
Weight Variation ◽  
Karaya Gum

Acyclovir was formulated as oral controlled release matrix tablets using natural and synthetic polymers separately or in combinations. Tablets were prepared by direct compression method. The tablets were evaluated to thickness, weight variation test, drug content, hardness, friability and in vitro release studies.All the formulations showed compliance with pharmacopoeal standards. The tablets prepared with various combination of hydroxy propyl methylcellulose (HPMC K100), locust bean gum (LBG) and karaya gum (KG) failed to produce the desired controlled release. Dissolution studies indicated that formulation F5 was most successful of the study. The formulation F5 exhibited anomalous (non-Fickian) diffusion mechanism. Based on the results of in-vitro studies it was concluded that the hydrophilic polymers canbe used as an effective matrix former to provide controlled release of acyclovir. SEM images of tablet after dissolution showed pore formation. FT-IR and DSC study did not show any possibility of interaction between acyclovir and excipients.

Formulation and Development of Divalproex Sodium Bi-Layered Tablets using Superdisintegrants and Release Retardant Polymers

2017 ◽  
Vol 10 (2) ◽  
pp. 3669-3675
Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Divalproex Sodium ◽  
In Vitro Drug Release ◽  
Weight Variation

Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.  

scholarly journals ENHANCEMENT OF THE DISSOLUTION RATE OF NATEGLINIDE TABLETS USING LIQUISOLID COMPACT TECHNIQUE

2017 ◽  
Vol 10 (10) ◽  
pp. 241
Author(s):  
Tirunagari Mamatha ◽  
Nazia Sultana
Keyword(s):  
Propylene Glycol ◽  
In Vitro Release ◽  
Tween 80 ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Oral Drug ◽  
Polyethylene Glycol 400 ◽  
Weight Variation ◽  
Liquisolid Compacts

  Objective: The main objective of this work is to develop new formulation to enhance the solubility of a highly permeable and a poorly soluble oral drug antihyperglycemic agent, nateglinide by liquisolid compacts.Methods: The liquisolid compact technique is based on dissolving the insoluble drug in propylene glycol, polyethylene glycol 400, tween-80 as non-volatile solvents in which drug is having high solubility and admixture of drug loaded solution with microcrystalline cellulose as carrier, aerosil as coating material, crospovidone as disintegrant, and magnesium stearate as lubricant to convert into acceptably flowing and compressible powder. The prepared liquisolid compacts were evaluated for their flowing properties such as bulk density, tapped density, angle of repose, Hausner’s ratio, and Carr’s index. Further tablets were evaluated for hardness, thickness, weight variation, friability, disintegration test, and in vitro release study.Result: Higher drug release profiles due to increased wetting property and surface area of the drug available for dissolution was obtained in case of liquisolid compacts. Among all formulations, liquisolid system prepared by propylene glycol was considered as best formulation which release drug up to 98% in 60 minutes and in comparison to marketed formulation, optimized formulation showed better dissolution profile.Conclusion: It can be concluded that liquisolid compact technique could be a promising strategy in improving the dissolution of poor water soluble drugs.

scholarly journals Preparation and evaluation of tolmetin sodium conventional and sustained-release suppositories

2002 ◽  
Vol 70 (1) ◽  
pp. 77-86
Author(s):  
Baloǧlu B. ◽  
Kirkaǧaçhoǧlu O.
Keyword(s):  
Polyethylene Glycol ◽  
Sustained Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Order Kinetic ◽  
Polyethylene Glycol 400 ◽  
Suppository Base ◽  
Soluble Base ◽  
Preparation And Evaluation

Conventional suppositories of tolmetin sodium were prepared by using two different types of Witepsol as an oily base and two different ratios of polyethylene glycol 400: polyethylene glycol 4000 as an water-soluble base. In addition, sustained- release suppositories were prepared by adding Eudragit L-100 ta the suppositories. The effects of the suppository base and the ratios of the polyethylene glycol 400: polyethylene glycols 4000 on the in vitro release characteristics were investigated. The release rate of tolmetin sodium from the conventional suppositories prepared with polyethylene glycol was slower than the other suppositories prepared with Witepsol. All of the suppositories with Eudragit L-100 showed slow-release profiles and the drug release rates clearly depended on the Eudragit L-100 content. When dissolution results were evaluated kinetically, zero order kinetic was observed with the sustained- release suppositories of tolmetin sodium prepared with polyethyleneglycol 400: polyethyleneglycol 4000 by adding Eudragit L-100.

scholarly journals FORMULATION AND EVALUATION OF METOCLOPRAMIDE HCL RECTAL SUPPOSITORIES

2019 ◽  
Author(s):  
Deborah Ejiogu Chioma ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Weight Variation ◽  
Rectal Suppositories ◽  
Vitro Release

Metoclopramide hydrochloride is a dopamine receptor antagonist, used mostly for stomach and esophageal problems as it is a prokinetic agent. The aim of the present study was to design and evaluate the suppositories of Metoclopramide HCl.  Six different, rectal suppositories were developed by fusion (pour-moulding) method by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent.  Metoclopramide HCl suppositories were evaluated for appearance, weight variation, drug content uniformity, liquefaction time and temperature, micro-melting range, disintegration and in-vitro release study.  The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism. Optimum formulation of batch S1 has shown 83.427% Metoclopramide HCl in a study of 2 hrs. These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. All formulations has shown zero, first and Higuchi release kinetics. The result suggests that the Metoclopramide HCl suppositories can be prepared by employing hydrophilic and hydrophobic polymers.

Sign in / Sign up

Export Citation Format

Share Document