Dissolution-Controlled Salt of Pramipexole for Parenteral Administration: In Vitro Assessment and Mathematical Modeling

Abstract

Parenteral suspensions of poorly water-soluble salts for intramuscular administration retain therapeutic drug concentration over a long duration. In vitro drug dissolution testing is a prerequisite to assess batch-to-batch variability as well as to assure appropriate drug release during formulation development. The purpose of the present work was to compare the drug release kinetics of two salts of pramipexole in powdered and suspension forms. The two salts employed for the dissolution study were commercially available soluble salt-pramipexole dihydrochloride monohydrate (PRP HCl) and in-house synthesized poorly water-soluble salt, pramipexole pamoic acid salt (PRP PAM). Modified USP apparatus 2 (paddle) using dialysis sac and open loop USP apparatus 4 (flow-through cell) were used for the in vitro dissolution studies. The drug release was estimated using high-performance liquid chromatography. The release kinetics were statistically analyzed using various mathematical models. Results obtained from in vitro dissolution testing showed an immediate-release profile for PRP HCl and a sustained-release profile for PRP PAM, indicating its long-acting potential. The developed method could discriminate between different particle sizes of the PRP PAM salt. The results indicated that the release profile of the PRP PAM salt using modified USP apparatus 2 with dialysis sac more closely mimicked the desired in vivo conditions of intramuscular administration as compared to open loop USP apparatus 4. The developed dissolution method can be used as a quality control tool for PRP PAM injectable suspension.

Predicting Drug Release from 3D Printed Oral Medicines Based on the Surface Area to Volume Ratio of Tablet Geometry

“…Formulation 1, referred to as the PVA-PDM formulation, consisted of 5% ( w / w ) pramipexole dihydrochloride monohydrate (PDM, Chr. Olesen, Denmark) as an API of the biopharmaceutics classification system (BCS) class I, declared as good water solubility (c s ≥ 200 mg/mL) [ 49 , 50 ]. Mannitol (Parteck M ® , Merck, Germany) was used as a plasticizer at 10% ( w / w ) content.…”

Assessment of the pharmaceutical equivalence and in vitro dissolution studies of amlodipine tablets marketed in Northern Nigeria

“…This is a crucial parameter to the overall therapeutic process, since the effectiveness of a tablet hinges on its rate of dissolution within the gastrointestinal tract (GIT) prior to absorption into the systemic circulation [10]. Due to adverse conditions prevalent in the retail outlets for pharmaceutical products, in vitro quality control tests are basic necessity to predict the bioavailability through the assessment of the tablet properties [11,12]. It is also necessary to note the organoleptic properties such as colour, taste and odour.…”

3D Printed Mini-Floating-Polypill for Parkinson’s Disease: Combination of Levodopa, Benserazide, and Pramipexole in Various Dosing for Personalized Therapy

“…LD, BZ and PDM exhibit good water solubility (c s (LD) ≥ 12 mg/mL, c s (BZ) ≥ 10 mg/mL, c s (PDM) ≥ 200 mg/mL [ 68 , 69 , 70 ]) and thus belong to the biopharmaceutical classification system (BCS) class I. As HME and FDM 3D printing are heat intensive processes, care was also taken to ensure that the process temperatures were below the decomposition temperatures (260–330 °C) [ 62 , 71 , 72 , 73 , 74 ].…”