DDS: Implant Flashcards

1
Q

Non-degradable polymers are inert, biocompatible and offer a simple means of controlling drug release by? What are some examples of nondegradable polymers?

A

By diffusion or swelling

  • Examples of nondegradable polymers are cellulose derivatives, silicones and acrylics
  • Suitable for long-term applications such as orthopaedic and dental implants
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2
Q

What are diffusion-controlled systems (non-BDG)? What are the two types?

A

Diffusion-controlled systems can be divided into reservoir type (i.e. a drug core is surrounded by a polymer coating) or matrix type (i.e. drug particles are dispersed in a polymer matrix)

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3
Q

What are swelling-controlled systems produced from (non-BDG)?

A

Swelling-controlled systems are produced from water- soluble, cross-linked polymers

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4
Q

What are non-degradable polymers characterised by?

A

Characterised by tissue/blood compatibility, durability, robustness of structure and mechanical strength

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5
Q

What do biodegradable polymers degrade into?

A

biodegradable polymers degrade into non-toxic monomers and by-products, that can be efficiently cleared by the body

  • No invasive surgery needed after therapy is complete
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6
Q

What are approved pharmaceutical implants based on biodegradable polymers?

A

Include hormones, antitumour drugs and antibiotics

  • Complex sequences of drug-releasing steps involving diffusion and erosion (either surface or bulk)
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7
Q

Why do implants have predictable and reproducible drug release and degradation profile for extended periods of time

A

due to their geometric structure

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8
Q

What does formulation involve for performed and injectable implants? What needs to be done at the beginning and end of therapy?

A

Formulation involves extrusion, compression moulding, solvent casting or melt casting of implants into the desired shape

  • Invasive surgery needed to implant and/or remove them at the beginning and end of therapy
  • Injectable implants take shape after implantation
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9
Q

What are the commonly used polymers in injectable implants?

A

Poly lactide glycolic acid (PLGA) and polylactic acid (PLA) are commonly used polymers

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10
Q

What is a gliadel (carmustine implant) wafer?

A

Gliadel® Wafer is an implant for intracranial use, containing carmustine [1, 3-bis (2-chloroethyl)-1-nitrosourea, or BCNU] homogeneously distributed in polifeprosan 20, a biodegradable polyanhydride copolymer (consists of poly [bis (pcarboxyphenoxy)] propane and sebacic acid in a 20:80 molar ratio), providing controlled release of carmustine

  • It is a sterile, off-white to pale yellow wafer approximately 1.45 cm in diameter and 1 mm thick. Each wafer contains 7.7 mg of carmustine and 192.3 mg of polifeprosan 20
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11
Q

What is an eligard injectable implant?

A

Injectable PLGA suspension formulation containing leuprolide acetate, for subcutaneous injection at 1 to 6-month intervals (based on dose injected: 7.5 – 45 mg LA), to suppress testosterone levels for inhibiting prostatic tumour growth

  • Injected into SC Space
  • Polymers respond to water by precipitating and trapping leuprolide acetate in a solid implant
  • Biodegradable polymers degrade by hydrolysis –> slowly releasing leuprolide acetate
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12
Q

How do azlet osmotic pumps work?

A
  • ALZET pumps operate because of an osmotic pressure difference within the pump and tissue environment in which the pump is implanted
  • The high osmolality causes water to flux into the pump through a semipermeable membrane which forms the outer surface of the pump
  • The expanded osmotic layer compresses the flexible reservoir, displacing the test solution from the pump at a controlled, predetermined rate

The compressed reservoir cannot be refilled, therefore the pumps are designed for single-use only

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13
Q

For an azlet pump;

A) What is the rate of delivery?

B) What drugs is it suitable for?

C) What is the volume delivery rate? How long do they last for?

A

A)

  • The rate of delivery is controlled by the water permeability of the pump’s outer membrane (semi-permeable membrane)
  • Thus, the delivery profile of the pump is independent of the drug properties/formulation dispensed

B)

  • Suitable for drugs of various molecular configurations, including ionized drugs and macromolecules

C)

  • The volume delivery rate of ALZET pumps is fixed at manufacture: available with delivery rates between 0.11 and 10 μL/hr
  • delivery durations between 1 day and 6 weeks
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14
Q

What are some applications of azlet pump?

A
  • Primary use is research.
  • ALZET osmotic pumps can be implanted subcutaneously or intraperitoneally following the animal size guidelines.
  • Can also be connected to a catheter to deliver the pump contents directly into the venous or arterial systems, the brain, or into any organ or tissue
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15
Q

For Implanon NXT (progestion only implant);

A) What does it consist of?

B) How is the contraceptive effect achieved?

C) How is it inserted?

D) When to replace?

A

A)

  • IMPLANON consists of a soft, flexible, rod-shaped implant, containing 68 mg etonogestrel, pre-loaded in the needle of a sterile disposable applicator

B)

  • Contraceptive effect is achieved by suppression of ovulation, increased viscosity of the cervical mucus, and alterations in the endometrium.
  • Efficacy >99.9%

C)

  • Inserted subdermally, just under the skin at the inner side of the non-dominant upper arm. Inserted under aseptic conditions

D)

  • IMPLANON must be removed no later than by the end of the third year
  • Can be replaced with a new implant
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16
Q

How is implanon formulated? What does it consist of? What is the release rate?

A
  • IMPLANON is off-white, non-biodegradable and 4 cm in length with a diameter of 2 mm
  • Implant consists of an ethylene vinyl acetate (EVA) copolymer core, containing 68 mg of the synthetic progestin etonogestrel, surrounded by an EVA copolymer skin
  • Once inserted subdermally, the release rate is 60 to 70 μg/day in Week 5 to 6 and decreases to approximately 35 to 45 μg/day at the end of the first year, to approximately 30 to 40 μg/day at the end of the second year, and then to approximately 25 to 30 μg/day at the end of the third year.
17
Q

For testopel testosterone pellets;

A) How are they given?

B) What do they contain?

C) What are they used for?

D) Doses?

A

A)

  • Testopel testosterone pellets for subcutaneous implantation

B)

  • Each pellet contains 75mg crystalline testosterone; stearic acid and polyvinyl pyrrolidone (PVP).

C)

  • Replacement therapy in conditions associated with deficiency or absence of endogenous testosterone

D)

  • Dosage: 2 x 75mg pellets equivalent to weekly 25mg testosterone dipropionate injection
  • Dosage guideline for replacement therapy in androgen deficient males: 150-450mg pellets every 3-6 months
18
Q

How are microchips used?

A
  • The microchips consist of hundreds of pinhead-sized reservoirs, each capped with a metal membrane, that store tiny doses of therapeutics or chemicals. An electric current delivered by the device removes the membrane, releasing a single dose
  • The device can be programmed wirelessly to release individual doses for up to 16 years to treat
  • diabetes, cancer, multiple sclerosis, and osteoporosis