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Design, Development, Manufacturing, and Testing of Transdermal Drug Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Timothy A. Peterson, Steven M. Wick, Chan Ko
Release rate testing for transdermal patches is described in the United States Pharmacopoeia General Chapter <725> (USP 36 2012). The test involves immersion of the patch in a receptor solution (typically aqueous) of specified volume, controlled temperature and consistent agitation with measurement of the drug in the receptor solution as a function of time. Specifications are generally adopted for at least three time points: an early time point to confirm the absence of dose dumping, an intermediate time point or two to characterize the release profile and a final time point to confirm that sufficient drug is released for the intended dose. USP Apparatus 5 (“Paddle over Disk”), Apparatus 6 (“Rotating Cylinder”) and Apparatus 7 (“Reciprocating Holder”) are described as appropriate for transdermal products. The Paddle over Disk apparatus is probably the most popular and easiest to use with a variety of patch constructions and sizes.
Analytical Testing and Evaluation of Capsules
Published in Larry L. Augsburger, Stephen W. Hoag, Pharmaceutical Dosage Forms, 2017
Stuart L. Cantor, Asish K. Dutta
The release of high doses of APIs in a short amount of time or “dose dumping” is a potential safety and efficacy concern. Dose dumping is a particular concern for drugs used to manage pain such as Palladone, an opioid analgesic (hydromorphone HCl). Palladone extended-release capsules were withdrawn from the market in July 2005 because a clinical pharmacology study demonstrated that some patients who took Palladone with alcohol had six times the amount of drug in their blood as those who took Palladone with water (FDA, 2005) [58].
Granulation Approaches for Modified-Release Products
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Neelima Phadnis, Sree Nadkarni
Two additional items relating to dissolution testing of MR products are:In vitro–in vivo correlation (IVIVC)When a predictive mathematical model is able to describe a relationship between an in vitro property of a dosage form, ex., drug dissolution profile, and an in vivo response, ex., drug’s extent of absorption, then an in vitro–in vivo relationship (IVIVR) is said to exist. IVIVR forms the basis for the determination of an IVIVC. The main objective of developing and evaluating an IVIVC is to establish the dissolution test as a surrogate for human bioequivalence studies, which in turn may reduce the number of bioavailability/bioequivalence studies performed during the initial development and approval process as well as with certain scale-up and post-approval changes. Additional details pertaining to bioequivalence are covered in Chapter 22. An example of an IVIVC for a commercial product is depicted in Figure 16.8 as part of the discussion in Case Study 3.Dose Dumping – Food EffectsAs part of the effort to ensure and establish the unique drug release pattern of an MR product, the relationship between food and alcohol effects on the drug dissolution pattern must also be demonstrated. This topic is of particular concern for drugs with a narrow therapeutic window because the complete dose may be more rapidly released from the dosage form than intended, creating a potential safety risk for the study subjects or the ultimate consumer of the MR product.
Nanosuspension coated multiparticulates for controlled delivery of albendazole
Published in Drug Development and Industrial Pharmacy, 2021
Monica R. P. Rao, Rohit Vidyadhar Godbole, Sameer G. Borate, Sanskar Mahajan, Tejal Gangwal
The optimized ALB-NS batch was loaded on Espheres using suspension layering technique and compared with ALB-MS coated Espheres. Preliminary studies were conducted, initially using pan coater and then using fluidized bed coater to fix the operating variables like temperature and spray rate for both stages of coating. The use of Espheres as cores offers many advantages in terms of final product properties such as uniform shape, surface smoothness, adequate mechanical resistance, and ability to be loaded with high drug doses [54]. The biopharmaceutical advantages of Espheres are mainly due to lower variability in the drug absorption profile [55]. The gastric emptying time of multi-unit systems is immune to the digestive phase in which administration takes place. Multiple-unit dosage forms are able to pass the stomach and spread along the gut, thus reducing the gastrointestinal transit variability. Dose dumping is also avoided due to subdivision of the dose [56]. These properties of Espheres are very critical as ALB-NS loaded Espheres were further coated with controlled release polymer. Primary and secondary coating was done using FBP. Presence of TPGS and PVP also ensured adhesivity of the NS on the Espheres and hence no additional excipient was required as binder. The FBP produced uniformly coated Espheres as the statistical residence time of all cores was same and the high kinetic energy provided by pneumatic mass flow caused the moist particles to be separated allowing coating of individual particles [57].
Nose-to-brain delivery of antipsychotics using nanotechnology: a review
Published in Expert Opinion on Drug Delivery, 2020
Madeleine S. A. Tan, Harendra S Parekh, Preeti Pandey, Dan J. Siskind, James R. Falconer
Existing intranasal formulations are marketed for either local or systemic drug delivery [69,71] and presented in the form of gels, solutions, suspensions or powders [7,71]. Currently, there are no U.S. FDA-approved products with antipsychotics. However, there are several other products given intranasally for CNS and systemic diseases, which are listed in Table 4. The strengths given from these products for CNS diseases are still in the milligram range, which shows that these drugs are not targeted for direct brain delivery as quite often only small doses (nanogram range) are required. Due to the small volume of the nasal cavity, only potent drugs are able to utilize this route of administration successfully [72]. When given intranasally, solutions and suspensions may be swallowed while powders may be inhaled, leading to insufficient antipsychotic drug concentration in the brain. There is also a risk of dose dumping with current dosage forms, which may cause toxicity considering its fast onset of action [73].
QuilliChew extended-release chewable tablets for the treatment of ADHD in patients ages 6 years old and above
Published in Expert Opinion on Drug Delivery, 2018
Ann Childress, Bernice Ponce De Leon, Mark Owens
Swallowability is a significant barrier to medication acceptability and adherence for younger patients. Many of the ER compounds require the patient to swallow an intact tablet or capsule. About 70% of five to nine-year-olds are unable to swallow a large pill or small capsule approximately the size of an acetaminophen tablet [29]. Although Concerta® (osmotic release oral system MPH or OROS MPH) must be swallowed whole, the capsules of products such as Adderall XR®, Metadate CD®, Focalin XR®, Aptensio XRTM, and Ritalin LA® may be opened and the contents sprinkled on applesauce [30–35]. Vyvanse® (lisdexamfetamine dimesylate or LDX) capsule contents can also be sprinkled on yogurt or dissolved in water [36]. However, this must be done carefully and the entire mixture should be consumed immediately and cannot be stored for later use. The Ritalin LA® package insert warns that applesauce should not be warm as it may alter the modified release properties of the compound [35]. Chewing the contents of these mixtures may cause dose dumping.