Pharmaceutics
"Future RPh! Pharmaceutics is the art and science of preparing medications. From tablets to injections, understanding dosage forms and drug delivery ensures that patients receive safe, effective, and stable medications. Ito ang hands-on side ng pharmacy!"
1. Dosage Forms Overview 💊
Dosage forms are the physical form of a drug product designed for administration to patients. The choice of dosage form affects drug stability, bioavailability, and patient compliance.
| Category | Dosage Forms | Characteristics | Examples |
|---|---|---|---|
| SOLID | Tablets | Compressed powders, most common form | Paracetamol 500mg tablet |
| Capsules | Hard or soft gelatin shells | Amoxicillin 500mg capsule | |
| Powders | Fine particles for reconstitution | Oral Rehydration Salts | |
| Suppositories | Melt at body temperature | Glycerin suppository | |
| LIQUID | Solutions | Homogeneous, clear mixtures | Paracetamol syrup |
| Suspensions | Particles dispersed in liquid (shake well!) | Amoxicillin suspension | |
| Emulsions | Two immiscible liquids (O/W or W/O) | Cod liver oil emulsion | |
| SEMISOLID | Ointments | Greasy, occlusive (hydrocarbon base) | Petroleum jelly |
| Creams | O/W or W/O emulsions, vanishing | Hydrocortisone cream | |
| Gels | Semisolid, transparent, non-greasy | Clindamycin gel |
💡 Board Exam Tip:
Know the difference between O/W and W/O emulsions! O/W (oil-in-water) is water-washable and less greasy. W/O (water-in-oil) is greasier and provides better occlusion. Test with dilution: O/W dilutes with water, W/O dilutes with oil.
2. Tablet Manufacturing 🏭
Understanding tablet manufacturing processes is essential for quality control and troubleshooting formulation problems.
Direct Compression:
- Simplest method, fewer steps
- Drug + excipients → compress directly
- Best for drugs with good flow properties
- Less heat/moisture exposure
Wet Granulation:
- Most common method
- Powder + binder solution → granules → dry → compress
- Better flow and compressibility
- Not for moisture-sensitive drugs
| Excipient Type | Function | Examples |
|---|---|---|
| Diluent/Filler | Bulk up tablet to practical size | Lactose, MCC, Starch |
| Binder | Hold ingredients together | PVP, Starch paste, HPMC |
| Disintegrant | Help tablet break apart | Croscarmellose, Crospovidone |
| Lubricant | Prevent sticking to dies | Magnesium stearate, Stearic acid |
| Glidant | Improve powder flow | Colloidal silica (Aerosil), Talc |
| Colorant | Identification, aesthetics | FD&C dyes, Iron oxides |
3. Drug Delivery Systems 🚚
Modern drug delivery systems aim to improve efficacy, reduce side effects, and enhance patient compliance through controlled and targeted drug release.
| System Type | Mechanism | Advantages | Examples |
|---|---|---|---|
| Extended Release (ER) | Slow, continuous release over time | Less frequent dosing, steady levels | Metformin XR, Metoprolol ER |
| Delayed Release (DR) | Release after delay (e.g., enteric coating) | Protect stomach, target intestine | Omeprazole DR, Aspirin EC |
| Transdermal | Drug absorption through skin | Bypass first-pass, sustained release | Nicotine patch, Fentanyl patch |
| Osmotic Systems | Water enters, pushes drug out | Zero-order release, food-independent | OROS (Concerta), Glucotrol XL |
| Liposomes | Phospholipid vesicles carrying drug | Targeted delivery, reduced toxicity | Doxil (liposomal doxorubicin) |
⚠️ Important Warning:
Extended-release tablets should NOT be crushed, chewed, or split (unless scored). Doing so destroys the release mechanism and can cause dose-dumping, leading to toxicity!
4. Sterile Products and Parenterals 💉
Parenteral products are administered by injection and must be sterile, pyrogen-free, and isotonic for safe administration.
Routes of Injection:
- IV (Intravenous): Fastest onset, 100% bioavailability
- IM (Intramuscular): Deltoid, gluteus, vastus lateralis
- SC (Subcutaneous): Slower absorption, insulin
- ID (Intradermal): Tuberculin test, allergy testing
Quality Requirements:
- Sterility: No microorganisms
- Pyrogen-free: No fever-causing substances
- Isotonicity: 0.9% NaCl equivalent (285-310 mOsm/L)
- Particulate-free: No visible particles
- Correct pH: Minimize tissue irritation
| Sterilization Method | Conditions | Applications |
|---|---|---|
| Autoclaving (Steam) | 121°C, 15 min, 15 psi | Heat-stable solutions, equipment |
| Dry Heat | 160-180°C, 1-2 hours | Glassware, powders, oils |
| Filtration | 0.22 μm membrane filter | Heat-sensitive solutions |
| Gamma Radiation | 2.5 Mrad | Disposables, some drugs |
5. Compounding Calculations 📐
Accurate calculations are critical in compounding to ensure patient safety and therapeutic effectiveness.
Essential Compounding Calculations:
Percentage Concentration:
- %w/w: g solute / 100g preparation (solids)
- %w/v: g solute / 100mL preparation (solutions)
- %v/v: mL solute / 100mL preparation (liquids)
Dilution Formula:
C₁V₁ = C₂V₂
Where C = concentration, V = volume
Alligation Method:
Used to determine proportions when mixing different strengths
Parts of higher = Desired - Lower strength
Parts of lower = Higher strength - Desired
Isotonicity (Sodium Chloride Equivalent):
NaCl needed (g) = 0.9 - (E × drug concentration)
Where E = NaCl equivalent of drug
💡 Quick Reference:
- 1% = 10 mg/mL = 1 g/100mL
- 1:1000 = 0.1% = 1 mg/mL
- 1:10,000 = 0.01% = 0.1 mg/mL
- Normal saline = 0.9% NaCl = isotonic
6. Practice Questions 📝
Question 1: Dosage Forms
What is the main difference between an ointment and a cream?
Answer: Ointments have a hydrocarbon (greasy) base and are occlusive, while creams are emulsions (O/W or W/O) that are less greasy and water-washable. Ointments provide better barrier protection and are preferred for dry, scaling conditions. Creams are cosmetically more acceptable and preferred for wet, weeping lesions.
Question 2: Excipients
Why is magnesium stearate added in small amounts (0.5-2%) to tablet formulations?
Answer: Magnesium stearate is a lubricant that prevents sticking of tablet powder to dies and punches. However, excess amounts can form a hydrophobic film around drug particles, reducing dissolution rate and bioavailability. It's used in minimal effective amounts.
Question 3: Drug Delivery
Why are enteric-coated tablets designed to resist gastric acid?
Answer: Enteric coatings protect drugs that are degraded by stomach acid (e.g., omeprazole), protect the stomach from irritating drugs (e.g., aspirin), or target drug release to the intestine for local effect. The coating dissolves at intestinal pH (>5.5) but remains intact in acidic stomach (pH 1-3).
Question 4: Compounding Calculation
How many grams of hydrocortisone powder are needed to prepare 60g of 2.5% hydrocortisone cream?
Answer: 1.5 grams. Calculation: 2.5% w/w = 2.5g per 100g. For 60g: (2.5g/100g) × 60g = 1.5g of hydrocortisone powder.
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