Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer based controlled release tablets of aceclofenac to simultaneously enhance the solubility and bioavailability

2021 ◽  
pp. 1-13
Author(s):  
Barkat Ali Khan ◽  
Muhammad Kamran Khan ◽  
Naeem Haider ◽  
Farid Menaa ◽  
Muhammad Khalid Khan

The aim of this study was to enhance the solubility of Aceclofenac with a new polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer (Soloplus ®) and formulate it in controlled release (CR) tablet dosage form by direct compression method with HPMC K-15. Solid dispersions were prepared in different ratio of Aceclofenac and Soloplus ® as F1, F2 and F3 with different polymer ratios i.e. 30%, 50%, and 70% respectively. All the quality control tests were performed for the prepared controlled release tablets. Drug polymer interaction studies of Aceclofenac and Soloplus ® were carried using FTIR and XRD. Dissolution study was carried out against Alkaris ® as a standard reference. The formulation F3 showed optimum results and followed zero order kinetics. The Soloplus ® improved the solubility of the drug and the CR formulation enhanced the delivery in a sustained manner. Hence, the CR formulation enhanced the delivery of aceclofenac in a sustained manner, thereby an efficient drug delivery may lead to an effective anti-inflammatory activity.

Soft Matter ◽  
2019 ◽  
Vol 15 (8) ◽  
pp. 1853-1859 ◽  
Author(s):  
Oliver Werzer ◽  
Stephan Tumphart ◽  
Roman Keimel ◽  
Paul Christian ◽  
Anna Maria Coclite

Temperature-controlled release and study on the effects of the drug–polymer interaction and pH.


Author(s):  
Chowdary KPR ◽  
Murali Krishna MN

The objective of the present investigation is to synthesize starch – urea – borate, a new starch based polymer and to evaluate its application in the design of controlled release matrix tablets of diclofenac and gliclazide. The release rate controlling efficiency of starch – urea – borate was also compared with that of known polymers. Starch – urea – borate (SUB) polymer was synthesized by gelatinization of starch in the presence of urea and borax. Matrix tablets of diclofenac (100 mg) and gliclazide (60 mg) were formulated employing starch – urea – borate polymer in different proportions of drug and polymer and the tablets were evaluated. With both diclofenac and gliclazide, release from the formulated matrix tablets was slow and spread over 24 h and depended on percent polymer in the tablet. Release was diffusion controlled and followed zero order kinetics. Non – fickian diffusion was the drug release mechanism from the formulated tablets. Diclofenac release from matrix tablets formulated employing 33 % SUB (DF3) and Gliclazide release from matrix tablets formulated employing 50 % SUB (GF4) was similar to that from the corresponding commercial SR tablets. Starch – urea – borate polymer was found suitable for the design of oral controlled release tablets of diclofenac and gliclazide. The order of increasing release rate controlling efficiency with various polymers was ethyl cellulose = guar gum > SUB > sodium CMC > HPMC. Starch – urea – borate is a better release rate controlling polymer than HPMC and sodium CMC for obtaining controlled release over    24 hours.


2014 ◽  
Vol 469 (1) ◽  
pp. 159-167 ◽  
Author(s):  
Kateřina Punčochová ◽  
Jerry Y.Y. Heng ◽  
Josef Beránek ◽  
František Štěpánek

Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 442 ◽  
Author(s):  
Yan He ◽  
Hongfei Liu ◽  
Wangqing Bian ◽  
Yue Liu ◽  
Xinyang Liu ◽  
...  

The molecular interactions between compound and polymeric carriers are expected to highly contribute to high drug load and good physical stability of solid dispersions. In this study, a series of amorphous solid dispersions (ASD) of Curcumin (Cur) were prepared with different polymers by the solvent evaporation method. With the carrier polyvinylpyrrolidone (PVP), the amorphous solid dispersion system exhibits a better solubility and stability than that with poloxamers and HP-β-CD due to the strong drug-polymer interaction. The drug/polymer interaction and their binding sites were investigated by combined experimental (XRD, DSC, FTIR, SEM, Raman, and 1H-NMR) and molecular dynamics simulation techniques. The Curcumin ASD demonstrated enhanced bioavailability by 11-fold and improved anti-inflammatory activities by the decrease in cytokine production (MMP-9, IL-1β, IL-6, VEGF, MIP-2, and TNF-α) compared to the raw Curcumin. The integration of experimental and modeling techniques is a powerful tool for the rational design of formulation development.


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