scholarly journals A Study On Release Rate From Tramadol HCl Loaded Microspheres Prepared By Using Different Polymers.

2021 ◽  
Vol 23 (07) ◽  
pp. 329-341
Author(s):  
Ritesh Bathe ◽  
◽  
Audumbar Mali ◽  
Sagar Kale ◽  
Jitendra Pande ◽  
...  
Keyword(s):  
Severe Pain ◽  
Opioid Analgesic ◽  
Test Apparatus ◽  
Plasma Drug ◽  
Solvent Evaporation Method ◽  
Tramadol Hydrochloride ◽  
Rate Test ◽  
Μ Opioid Receptor

Tramadol which is an opioid analgesic used to treat moderate to moderately severe pain act primarily by binding to the μ-opioid receptor and secondly by inhibiting the reactivity of norepinephrine and serotonin. The emulsion solvent evaporation method was used to encapsulate the polymers EC, HPMC K4M, and CAP, and characterization of formulations was performed. The microspheres obtained were white and spherical. The in vitro studies of the microspheres was performed using phosphate buffer of pH 6.8 at a temperature of 37 degrees Celsius and 100 rpm in 900ml USP basket type dissolution rate test apparatus for 8 hours and various parameters of the formulation were evaluated. Formulation F6 exhibited a higher yield and formulation of F3 entrapped maximum drug. The effect of the nature of polymer and polymer content was clearly visible on the drug release. The controlled release of the drug from the tramadol hydrochloride microsphere provides enhanced plasma drug content and higher bioavailability.

scholarly journals Design and Characterization of Mucoadhesive Microspheres of Etodolac

2019 ◽  
Vol 11 (03) ◽  
Author(s):  
A R Shabaraya ◽  
A S Parulkar ◽  
D Shripathy ◽  
P Shetty
Keyword(s):  
Drug Targeting ◽  
Entrapment Efficiency ◽  
Specific Region ◽  
Zero Order ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Central Composite

Mucoadhesive microspheres are drug delivery system intended for drug targeting to a specific region. Etodolac is a Non-steroidal anti-inflammatory drug. Sustain released Etodolac loaded mucoadhesive microspheres were prepared to overcome the relatively short residence time of Etodolac in the GIT tract before elimination. Solvent evaporation method was used for preparation of mucoadhesive microspheres with the help of Carbopol 974P, HPMC K100M and HPMC K4M as the polymers. Central composite design was selected for the development of the formulation. The formulations were evaluated for their particle size, surface morphology, degree of swelling, entrapment efficiency, drug content and in-vitro drug release study was done. Based on the results obtained from the preliminary formulations three optimized formulations were designed. The percentage mucoadhesion and swelling index of these formulations were obtained in the range of 66-70% and 82.50-83.84% respectively. Optimized formulation releases 90.94% to 92.11% of drug after 10 hours and follows zero order kinetics.

scholarly journals Formation of Andrographlolide-BetaCyclodextrin Inclusion to Increase Solubility and Dissolution Rate

2018 ◽  
Vol 5 (2) ◽  
pp. 49
Author(s):  
Bayu Febram Prasetyo ◽  
Ietje Wientarsih ◽  
Dondhin Sajuthi ◽  
Vetnizah Juniantito
Keyword(s):  
Physical Chemistry ◽  
Inclusion Complex ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Pharmacological Properties ◽  
Solvent Evaporation Method ◽  
Solubility Test ◽  
Beta Cyclodextrin ◽  
Rate Test

Andrographolide (AG) is a pure isolate of the chemical synthesis of sambiloto (Andrographis paniculata Nees.) which has various pharmacological properties such as anti-inflammatory and antimicrobial. In order to improve the ability of AG to penetrate the membrane in transdermal use, an inclusion complex was formed using beta-cyclodextrin (BCD) by modifying the physical chemistry properties of AG, particularly the solubility in its base, partition, and distribution on the skin, as well as by changing the permeability of the stratum corneum. The inclusion complexes of AG with BCD were prepared by the solvent evaporation method in the mole ratios of 1:1, 1:2, and 2:1. The solid of the yield of AG inclusion complex in BCD has been tested with a solubility test until it reached equilibrium at 37 ± 5 °C for 24 hours and In vitro dissolution rate test using the II USP method (paddle type), then compared to a single AG compound, and a physical mixture of AG-BCD. Based on the solubility and dissolution rate tests, it showed that the formation of AG-BCD inclusion complex was obtained at the mole ratio of 1:2. Moreover, the AG solubility increased 38 timesand the dissolution rate in the 60th minute increased twice  in the inclusion complex with BCD.Key words: andrographolide, inclusion complex, beta cyclodextrin, solubility, dissolution rate 

Development, Solubility Enhancement and Characterization of Nimodipine Solid Dispersions

2018 ◽  
Vol 11 (5) ◽  
pp. 4231-4239
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Muralichand G
Keyword(s):  
Solid Dispersions ◽  
In Vitro Release ◽  
Solvent Evaporation Method ◽  
First Order ◽  
Ftir Studies ◽  
Release Data ◽  
Vitro Release ◽  
Excipient Compatibility

The main aim of this study was to formulate and characterize nimodipine solid dispersions using various novel polymers. Solid dispersions were prepared by solvent evaporation method in order to improve the solubility and overall bioavailability of nimodipine. Solubility and dissolution studies indicate that Kolliwax RH 40 is the most suitable polymer. The solubility studies was corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96 ± 5.15% in about 90 minutes. In vitro release data from several formulations containing Nimodipine was determined kinetically using different mathematical models like Zero order, First order, Higuchi, and Korsmeyer–Peppas model. XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. These results confirm the viability of enhancing the solubility of nimodipine by formulating the drug as solid dispersions in Kolliwax. 

Tramadol & Sports

2018 ◽  
Vol 3 (7) ◽  
Keyword(s):  
Nervous System ◽  
Pain Relief ◽  
Prescription Drugs ◽  
Acute Pain ◽  
Severe Pain ◽  
Opioid Analgesic ◽  
Brand Names ◽  
Tramadol Hydrochloride ◽  
The Us ◽  
The Brain

Tramadol hydrochloride is the full name: is a centrally acting opioid analgesic used to treat moderate to moderately severe pain”. It’s sold under a range of brand names .It works on the brain and nervous system to reduce pain and is a medium to strong pain killer, this is not what people take for a headache. Instead it’s used for chronic and acute pain relief. As an opiate it can be addictive. Indeed as well as correct use it is also abused. By some measures prescription drugs, including Tramadol, are abused in greater quantities in the US than illegal drugs from heroin to cocaine etc.

Assays for Phospholipid-Dependent Formation of Thrombin and Xa: A Potential Method for Quantifying Lupus Anticoagulant Activity

1991 ◽  
Vol 66 (04) ◽  
pp. 453-458 ◽  
Author(s):  
John T Brandt
Keyword(s):  
Specific Activity ◽  
Anticoagulant Activity ◽  
Factor Xa ◽  
Clinical Importance ◽  
Potential Method ◽  
Quantitative Expression ◽  
Increased Risk ◽  
Apparent Association

SummaryLupus anticoagulants (LAs) are antibodies which interfere with phospholipid-dependent procoagulant reactions. Their clinical importance is due to their apparent association with an increased risk of thrombo-embolic disease. To date there have been few assays for quantifying the specific activity of these antibodies in vitro and this has hampered attempts to purify and characterize these antibodies. Methods for determining phospholipid-dependent generation of thrombin and factor Xa are described. Isolated IgG fractions from 7 of 9 patients with LAs were found to reproducibly inhibit enzyme generation in these assay systems, permitting quantitative expression of inhibitor activity. Different patterns of inhibitory activity, based on the relative inhibition of thrombin and factor Xa generation, were found, further substantiating the known heterogeneity of these antibodies. These systems may prove helpful in further purification and characterization of LAs.

Characterization of the Original Christmas Disease Mutation (Cysteine 206 → Serine): From Clinical Recognition to Molecular Pathogenesis

1992 ◽  
Vol 67 (01) ◽  
pp. 063-065 ◽  
Author(s):  
Sherryl A M Taylor ◽  
Jacalyn Duffin ◽  
Cherie Cameron ◽  
Jerome Teitel ◽  
Bernadette Garvey ◽  
...  
Keyword(s):  
Nucleotide Substitution ◽  
Novel Mutation ◽  
Factor Ix ◽  
Causative Mutation ◽  
Coding Region ◽  
Body Of Knowledge ◽  
Polymerase Chain ◽  
Splice Junctions

SummaryChristmas disease was first reported as a distinct clinical entity in two manuscripts published in 1952 (1, 2). The eponym associated with this disorder, is the surname of the first patient examined in detail and reported by Biggs and colleagues in a paper describing the clinical and laboratory features of seven affected individuals (3). This patient has severe factor IX coagulant deficiency (less than 0.01 units/ml) and no detectable circulating factor IX antigen (less than 0.01 units/ml). Coding sequence and splice junctions of the factor IX gene from this patient have been amplified in vitro through the polymerase chain reaction (PCR). One nucleotide substitution was identified at nucleotide 30,070 where a guanine was replaced by a cytosine. This mutation alters the amino acid encoded at position 206 in the factor IX protein from cysteine to serine. The non conservative nature of this substitution, the absence of this change in more than 200 previously sequenced factor IX genes and the fact that the remainder of the coding region of this gene was normal, all provide strong circumstantial evidence in favour of this change being the causative mutation in this patient. The molecular characterization of this novel mutation in the index case of Christmas disease, contributes to the rapidly expanding body of knowledge pertaining to Christmas disease pathogenesis.

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