Lecture 8 & 9 Parenteral products of peptide and proteins.pptx

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1. Parenteral products of peptide and proteins

2. Content Introduction Characteristics of protein and peptides. Isoelectric points Common stabilizer Compatibility with packaging components and infusion sets Formulation of market products.

3. Characteristics of protein and peptides Proteins: Large molecules Made of one or more polypeptide chains Comprised of 50 or more amino acids Have specific three-dimensional structures Functionally diverse (e.g., enzymes, hormones, structural roles) Peptides: Short chains of amino acids Generally contain fewer than 50 amino acids Can act as hormones, neurotransmitters, or signaling molecules

4. isoelectric point The concept of isoelectric point ( pI ) refers to the pH at which a particular molecule, like a protein or peptide, carries no net electrical charge. This occurs when the number of positive charges equals the number of negative charges in the molecule. Here are a few key points: pI and pH Relationship : At a pH below the pI , the molecule is positively charged. At a pH above the pI , the molecule is negatively charged. Protein Behavior at pI : At the isoelectric point, proteins are least soluble in water and may precipitate out of solution. Determination of pI : The pI can be calculated based on the pKa values of the ionizable groups within the protein or peptide.

5. PROTEINS AND PEPTIDES

6. Protein drugs Recombinant proteins have become the fastest growing class of pharmaceuticals and have quickly replaced many animal sources for therapeutic agents, such as bovine insulin. Recombinant proteins such as recombinant human insulin are used to supplement or replace proteins that are inactive or expressed in insufficient quantity in the body. Some proteins may be naturally expressed in the body, but also given pharmacologically in therapeutic doses to elicit a desired therapeutic effect, such as thrombolysis . Clinicians should understand recombinant proteins’ unique properties and requirements for storage, use, and administration because—as biological molecules—they are large, complex, and unstable compared to traditional small-molecule drugs.

7. PACKAGING OF PARENTERAL PRODUCTS 1. Ampoules , the oldest type of parenteral product containers, are made entirely of glass a. Intended for single use only , ampoules are opened by breaking the glass at a scored line on the neck. b. Disadvantages. Because glass particles may become dislodged during ampoule opening, the product must be filtered before it is administered. Their unsuitability for multiple-dose use, the need to filter solutions before use, and other safety considerations have markedly reduced the ampoule as a package form.

8. PACKAGING OF PARENTERAL PRODUCTS 2. Vials are glass or plastic containers closed with a rubber stopper and sealed with an aluminum crimp a. Vials have several advantages over ampoules. (1) Vials can be designed to hold multiple doses (if prepared with a bacteriostatic agent). (2) Th e drug product is easier to remove from vials than from ampoules. (3) Vials eliminate the risk of glass particle contamination during opening. b. However, vials also have certain disadvantages . (1) Th e rubber stopper can become cored , causing a small bit of rubber to enter the solution (see IV.H).

9. PACKAGING OF PARENTERAL PRODUCTS (2) Multiple withdrawals (as with multiple-dose vials) can result in microbial contamination. c. Some drugs that are unstable in solution are packaged in vials unreconstituted and must be reconstituted with a diluent before use. Sterile water or sterile sodium chloride for injection are the most commonly used drug diluents. (1) To accelerate the dissolution rate and permit rapid reconstitution, many powders are lyophilized (freeze dried). (2) Some of these drugs come in vials that contain a double chamber. (a) Th e top chamber, containing sterile water for injection, is separated from the unreconstituted drug by a rubber closure. (b) To dislodge the inner closure and mix the contents of the compartments, external pressure is applied to the outer rubber closure. Th is system eliminates the need to enter the vial twice, thereby reducing the risk of microbial contamination.

10. PACKAGING OF PARENTERAL PRODUCTS 3. Some drugs come in vials that may be attached to a diluent-containing bag for reconstitution and administration, such as the ADD-Vantage System by Abbott or the Mini-Bag Plus System by Baxter ( Figure 17-12 ). Premeasured drug and diluent may also be stored in separate compartments within a delivery system and then combined at the point of use, such as the Duplex System by B. Braun. a. Th e ADD-Vantage vial is screwed into the top of an ADD-Vantage diluent bag, and the rubber diaphragm is dislodged from the vial, allowing the diluent solution to dissolve the drug prior to administration.

11. PACKAGING OF PARENTERAL PRODUCTS b. The Mini-Bag Plus System contains an adaptor that links standard 20 mm powdered drug vials with Baxter’s Mini-Bag containers, allowing vial and bag to be attached without activation until time of administration. c. The Duplex systems has two compartments where a seal is broken and drug and diluent are mixed to form a solution prior to administration. d. The premixed piggyback contains drug solution that is prediluted and ready to be administered with no further preparation needed.

12. PACKAGING OF PARENTERAL PRODUCTS 4. Prefilled syringes and cartridges are designed for maximum convenience ( Figure 17-13 ). a. Prefilled syringes. Drugs administered in an emergency (e.g., atropine, epinephrine) are available for immediate injection when packaged in prefilled syringes. b. Prefilled cartridges are ready-to-use parenteral packages that off er improved sterility and accuracy. They consist of a plastic cartridge holder and a prefilled medication cartridge with a needle attached. The medication is premixed and premeasured. Narcotics such as meperidine (Demerol) and hydromorphone ( Dilaudid ) are commonly available in prefilled cartridges.

13. PACKAGING OF PARENTERAL PRODUCTS 5. Infusion solutions are divided into two categories: small-volume parenterals (SVPs), those having a volume less than 100 mL; and large-volume parenterals (LVPs), those having a volume of 100 mL or greater. Infusion solutions are used for the intermittent or continuous infusion of fluids or drugs.