| Title |
Pharmacodynamic testing and new validated HPLC method to assess the interchangeability between multi-source orlistat capsules
|
|---|---|
| Published in |
Drug Design, Development and Therapy, November 2017
|
| DOI | 10.2147/dddt.s138926 |
| Pubmed ID | |
| Authors |
Abdel Naser Zaid, Nihal Zohud, Bushra E’layan, Tasneem Aburadi, Nidal Jaradat, Iyad Ali, Fatima Hussein, Mashhour Ghanem, Aiman Qaddomi, Yara Abu Zaaror |
| Abstract |
Orlistat is an irreversible inhibitor of the lipase enzyme that prevents trigylcerides from being digested, thereby inhibiting triglyceride hydrolysis and absorption. The resultant reduced calorie uptake enables a positive effect on weight control. Systemic absorption of the drug is, therefore, not necessary for its mode of action. An alternative in vitro study (pharmacodynamic) has been introduced for this drug, as in vivo bioavailability studies are irrelevant with regard to the achievement of the product's intended purposes. To develop a new validated high-performance liquid chromatography (HPLC) method for the analysis of orlistat and to assess the potency and equivalence of three orlistat formulations using the pharmacodynamic method as a surrogate indicator of pharmaceutical interchangeability. A new HPLC method was developed for the analysis and for the dissolution studies of orlistat in capsules. Pancreatic lipase activity was measured for three different capsule products: Orlislim®, Slimcare®, and Xenical®, G1, G2, and the brand, respectively. Porcine pancreatic lipase and p-nitrophenyl butyrate (PNPB) were placed in a pH 7.4 reaction buffer at 37°C, and substrate hydrolysis was monitored by measuring absorbance changes at 410 nm; this was repeated on six capsules of each product. The inhibition was expressed by the concentration of product, which inhibited 50% of the activity of pancreatic lipase (IC50). The new analytical method was suitable for orlistat analysis. Values of IC50 from regression lines and equations were 6.14, 8.43, and 7.80 μg/mL for Orlislim®, Xenical®, and Slimcare®, respectively. Pharmacodynamic studies of lipase inhibition could be used to support in vitro dissolution, which demonstrates interchangeability between generic and branded orlistat capsules. Moreover, it could be suggested as an alternative tool to bioequivalence studies for orlistat oral products. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Germany | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 35 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 35 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 8 | 23% |
| Student > Master | 4 | 11% |
| Student > Doctoral Student | 2 | 6% |
| Lecturer | 2 | 6% |
| Student > Ph. D. Student | 1 | 3% |
| Other | 3 | 9% |
| Unknown | 15 | 43% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 10 | 29% |
| Biochemistry, Genetics and Molecular Biology | 3 | 9% |
| Chemistry | 2 | 6% |
| Computer Science | 1 | 3% |
| Chemical Engineering | 1 | 3% |
| Other | 2 | 6% |
| Unknown | 16 | 46% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 18 September 2018.
All research outputs
#22,764,772
of 25,382,440 outputs
Outputs from Drug Design, Development and Therapy
#1,753
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Outputs of similar age
#299,290
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Outputs of similar age from Drug Design, Development and Therapy
#32
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