Ciprofloxacin - Best antibiotic

        INTRODUCTION:

        Ciprofloxacin Hydrochloride is a second-generation fluoroquinolone antibiotic used to treat infections caused by bacteria      such as pneumonia; bronchitis; prostatitis, anthrax, chancroid; gonorrhea; endocarditis, gastroenteritis and ear, lung, throat, and urinary tract infections. Antibiotics will not work for colds, flu, or other viral infections. Chemically, Ciprofloxacin Hydrochloride is, 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid, monohydrochloride, monohydrate. Its molecular formula is C₁₇H₁₈FN₃O₃·HCl·H₂O, and it has a molecular weight of 385.82.After oral administration, Ciprofloxacin given as an oral tablet is rapidly and well absorbed from the gastrointestinal tract after oral administration. 

The absolute bioavailability is approximately 70% with no substantial loss by first pass metabolism. Ciprofloxacin maximum serum concentrations and area under the curve are shown in the chart for the 250 mg to 1000 mg dose range. 

The pharmacokinetics of Ciprofloxacin in the urine of pediatric patients has not been studied at this time. Until further data are available, the renal pharmacokinetic properties of Ciprofloxacin Hydrochloride established in adults should not be extrapolated to pediatric patients. Because Ciprofloxacin Hydrochloride is renaly excreted, the serum half-life is prolonged in patients with reduced renal function. 

INDICATION:

Ciprofloxacin is used to treat a number of infections, including infections of bones and joints, endocarditis, gastroenteritis, malignant otitis externa, respiratory tract infections, cellulitis, urinary tract infections, prostatitis, anthrax, and chancroid, as well as:

·         Urinary tract infections (recommended as a first-line antibiotic)

·         Chronic bacterial prostatitis (recommended as a first-line antibiotic choice)

·         Lower respiratory tract infections (not recommended as a first-line antibiotic choice)

·         Acute sinusitis (not recommended as a first-line antibiotic choice)

·         Skin and skin structure infections

·         Bone and joint infections

·         Infectious diarrhea

SIDE EFFECTS:

Diarrhea, fever, sore throat and headache, pale or yellowed skin, dark colored urine, fever, weakness, seizure (convulsions), nausea, vomiting, stomach, pain, dizziness, insomnia, numbness, tingling, or unusual pain anywhere in your body

CONSTITUENTS:

Active Substance:

Active ingredient of Xylobox Powder for Suspension 60 ml is Ciprofloxacin Hydrochloride.

CAS Registry Number: [86393-32-0]

               

 Physical Characteristics of Active Substance:

Ciprofloxacin Hydrochloride is a faintly yellowish to light yellow crystal. Sparingly soluble in water, slightly soluble in acetic acid and methanol, very slightly soluble in dehydrate alcohol, practically insoluble in acetone, in acetonitrile, in ethyl acetate, in hexane, and in methylene chloride.

Compatibility:

As the product is designed for single active substance the incompatibility with other active substances does not arise in this preparation. The active material, Ciprofloxacin Hydrochloride is not incompatible with other excipients used in the formulation. 

Cefpodoxime proxetil - Best Powder for suspension --- For Child

INTRODUCTION:

Cefpodoxime proxetil is a cephalosporin antibiotic used to treat infections caused by bacteria such as pneumonia; bronchitis; gonorrhea; and ear, lung, throat, and urinary tract infections. Antibiotics will not work for colds, flu, or other viral infections. Chemically, Cefpodoxime proxetil is, (6R,7R)-7-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Cefpodoxime proxetil is an orally absorbed broad spectrum third generation cephalosporin antibacterial. It is a prodrug that is de-esterified in vivo to its active metabolite, cefpodoxime. After single- and multiple-dose (12-hourly) administration of cefpodoxime proxetil in the therapeutic dose range of 100 to 400mg of cefpodoxime equivalents, average peak plasma concentrations of cefpodoxime range from 1.0 to 4.5 mg/L and occur between 1.9 and 3.1 hours after administration. The half-life of cefpodoxime ranges from 1.9 to 2.8 hours. The absolute bio-availability of cefpodoxime proxetil tablets is 50%, and absorption is enhanced by concomitant administration of food. Drug not absorbed is degraded in the gastrointestinal tract and excreted in the faeces. As expected for a drug eliminated primarily by renal excretion, the disposition of cefpodoxime is altered in patients with impaired renal function; the half-life increases, while apparent plasma clearance and renal clearance decrease. The pharmacokinetics of cefpodoxime after oral administration of cefpodoxime proxetil are not affected by age.

INDICATION:

Respiratory tract infections, for example, acute and chronic bronchitis, infected bronchiectasis, Acute bacterial pneumonia, lung abscess.

Ear, nose and throat infections, for example, sinusitis, tonsillitis and pharyngitis.

Urinary tract infections, for example, acute and chronic pyelonephritis, cystitis.

Cotitis media, Pharyngitis, and sinusitis.

Uncomplicated Skin and Skin Structure Infections

Uncomplicated Urinary Tract Infections.

SIDE EFFECTS:

Renal dysfunction, toxic nephropathy, hepatic dysfunction including cholestasis, aplastic anemia, hemolytic anemia, serum sickness-like reaction, hemorrhage, agranulocytosis, and pancytopenia.

Physical Characteristics of Active Substance:

Cefpodoxime proxetil is a white to light brownish-white powder, odorless or having faint odor, and has bitter test. very slightly soluble in water, soluble in acetonitrile and in methanol, freely soluble in dehydrated alcohol, slightly soluble in ether.

Mixing substances and its mechanism of Pharmaceutical Science

Mixing

Definition: Process that results in randomization of dissimilar particles within a system.

Mechanisms of mixing:
The most common classification of mixers however is based on the type of dosage form they are used to handle. A brief summary of mixing process in relation to the type of dosage form is presented below

1. Mixing for solids
Physical properties that effect the ease of mixing are:
(a) Material density
(b) Particle size and distribution
(c) Wettability
(d) Stickiness
(e) Particle shape / roughness

The most preferred types of mixers for solid mixing are Tumble mixers and Fixed shell mixers. Tumble mixers operate on the principle of bulk transport and shear. The mixing efficiency has a direct co-relation with the speed of rotation of tumble blender. Three types of most commonly used blenders are illustrated below:

A – Double cone blender, B – V blender and C – Bin blender

Fixed shell mixers are equipments in which the material is held in a stationary container and mixing is brought about by means of moving screws, paddles or blades. The ribbon blender consists of a relatively long trough like shell with a semicircular bottom, usually opening at the top and fitted with helical blades. The blades produce a continuous cutting and shuffling of charge by circulating the charged powder from end to end of the trough as well as rotationally.

2. Mixing of liquids
Mixing occurs in two stages:
(a) Localized mixing which applies sufficient shear to the particles of the fluid
(b) A general movement sufficient to take all parts of the material through the shearing zone and to ensure a uniform final product.

Mixing mechanisms fall essentially into four categories:

1. Bulk Transport – movement of a relatively large portion of material being mixed from one location in the system to another.

2. Turbulent flow – Characterized by the fluid having different instantaneous velocities at the same instant of time. The temporal and spatial velocity differences resulting from turbulence produce randomization of fluid particles.

3. Laminar Flow – Streamline flow that is encountered most commonly in highly viscous liquids.

4. Molecular diffusion – Primary mechanism responsible for mixing at the molecular level which results from the thermal motion of molecules.

Governed by Fick's fist law of diffusion,

dm/dt = - DA dc/dx
Where,
dm/dt – rate of transport of mass across a surface area
D – Diffusion Co-efficient
A – Area across which diffusion is occurring
dc/dx – Concentration gradient

Mixing as a process can either be carried batch to batch or can be continuous. Impellers, Air-jets, Fluid-jets and Baffle mixers are the major types of equipment used for batch mixing. Impellers operate using a combination of radial, axial and tangential flow. These might be classified into two further types, Propellers and Turbines, the former being used for low viscosity liquids while the latter for high viscosity ones.

3. Mixing of semi-solids
The mechanisms involved in mixing semi solids depend on the character of the material which may show considerable variation. Many semi solids form neutral mixtures having no tendency to segregate although sedimentation may occur.

Three most commonly used semi solid mixers are

(a)      Sigma blade mixer – Contains two blades which operate in a mixing vessel which has a double trough shape, the blades moving at different speeds towards each other. Used for products like granulation masses and ointments.

(b)      Triple-roller mill – The differential speed and narrow clearance between the roller develop high shear over small volumes of material. The roller mills are generally used to grind and complete the homogeneity of ointments.

(c)       Planetary mixers – it utilizes a mixing arm rotating about its own axis and also about a common axis usually the centre of the mixing wheel. The blades provide the kneading action, while the narrow passage between the blades and the wall of the can provides shear.

Mixer Selection

Factors to be taken into consideration while selecting a mixing equipment include,
(a) Physical properties of materials to be mixed such as density, viscosity and miscibility
(b) Economic considerations – operating efficiency, cost and maintenance

One of the first things to determine is if the process is intended to be a batch or a continuous process, each of which can have its advantages and drawbacks depending on the load to be used. Size is considered keeping in mind the optimal working volume, fill level and residence time. The optimal working volume would depend on the construction of the mixer. It generally lies between 50 to 70 percent of the maximum. Similarly, too much of fill would lead to low mixing and hence fill level becomes important. Residence time which is defined as the amount of time ingredients are in the mixer and is a particularly important determinant of the size of a continuous mixer. Choice of agitators determines the efficiency in breaking up lumps/agglomerates and serves to add shear aiding the final dispersion.

A brief table showing various agitator types and their respective uses in shown below.

1.      Ribbon - For Powders, granules, some slurries, mainly free flowing

2.      Paddle - For Powders, granules, some slurries, free flowing, light pastes

3.      Sigma - For Sticky materials, thick pastes and slurries

Important features of the gastrointestinal tract

Important features of the gastrointestinal tract

The following are some of the important features of the human gastrointestinal tract.

1. There is a copious blood supply.

2. The entire tract is lined with mucous membrane through which drugs may be readily transferred into the general circulation.

3. The interior surface of the stomach is relatively smooth.

4. The small intestine presents numerous folds and projections.

5. Approximately 8–10 L per day of fluids are produced or secreted into the gastrointestinal tract and an additional 1–2 L of fluid is obtained via food and fluid intake.

6. The gastrointestinal tract is highly perfused by a capillary network, which allows absorption and distribution of drugs to occur. This immediate circulation drains drug molecules into the portal circulation, where absorbed drugs are carried to the liver and may undergo first pass effect.

Omega-3 fatty acids

Omega-3 fatty acids

Omega-3 fatty acids (also called ω−3 fatty acids or n−3 fatty acids) are fats commonly found in marine and plant oils. They are polyunsaturated fatty acids with a double bond (C=C) starting after the third carbon atom from the end of the carbon chain. The fatty acids have two ends—the acid (-COOH) end and the methyl (-CH3) end. The location of the first double bond is counted from the methyl end, which is also known as the omega (ω) end or the n end.

Common sources of omega–3 fatty acids include fish oils, algal oil, squid oils, and some plant oils such as Sacha Inchi oil, echium oil, flaxseed oil and hemp oil.

Cancer

The evidence linking the consumption of fish to the risk of cancer is poor Supplementation with omega-3 fatty acids does not appear to affect this risk either.

A 2006 report in the Journal of the American Medical Association, in their review of literature covering cohorts from many countries with a wide variety of demographics, concluded that there was no link between omega−3 fatty acids and cancer.

Cardiovascular disease

Omega-3 fatty acids also have mild antihypertensive effects. When subjects consumed omega-3 fatty acids from oily fish on a regular basis, their systolic blood pressure was lowered by about 3.5–5.5 mmHg. The 18 carbon α-linolenic acid (ALA) has not been shown to have the same cardiovascular benefits that DHA or EPA may have. 

Omega-3 fatty acids in algal oil, fish oil, fish and seafood have been shown to lower the risk of heart attacks.

Inflammation

Although not confirmed as an approved health claim, current research suggests that the anti-inflammatory activity of long-chain omega−3 fatty acids may translate into clinical effects. For example, there is evidence that rheumatoid arthritis sufferers taking long-chain omega−3 fatty acids from sources such as fish have reduced pain compared to those receiving standard NSAIDs. Some potential benefits have been reported in conditions such as rheumatoid arthritis.

Developmental disorders

Although not supported by current scientific evidence as a primary treatment for ADHD, autism spectrum disorders, and other developmental differences, omega-3 fatty acids have gained popularity for children with these conditions. 

Omega-3 fatty acids offer a promising complementary approach to standard treatments for ADHD and developmental coordination disorder. Fish oils appear to reduce ADHD-related symptoms in some children. Double blind studies have shown "medium to strong treatment effects of omega 3 fatty acids on symptoms of ADHD".

Psychiatric disorders

Though there is some evidence that omega-3 fatty acids are related to a variety of mental disorders. They may tentatively be useful as an add-on for the treatment of depression associated with bipolar disorder and there is preliminary evidence that EPA supplementation are helpful in cases of depression. There however is a significant risk of bias in the literature.

 

Cognitive aging

Epidemiological studies suggest that consumption of omega-3 fatty acids can reduce the risk of dementia, but evidence of a treatment effect in dementia patients is inconclusive. However, clinical evidence suggests benefits of treatment specifically in patients who show signs of cognitive decline but who are not sufficiently impaired to meet criteria for dementia.

 

List of omega−3 fatty acids

This table lists several different names for the most common omega−3 fatty acids found in nature.

Common name	Lipid name	Chemical name
Hexadecatrienoic acid (HTA)	16:3 (n−3)	all-cis-7,10,13-hexadecatrienoic acid
α-Linolenic acid (ALA)	18:3 (n−3)	all-cis-9,12,15-octadecatrienoic acid
Stearidonic acid (SDA)	18:4 (n−3)	all-cis-6,9,12,15-octadecatetraenoic acid
Eicosatrienoic acid (ETE)	20:3 (n−3)	all-cis-11,14,17-eicosatrienoic acid
Eicosatetraenoic acid (ETA)	20:4 (n−3)	all-cis-8,11,14,17-eicosatetraenoic acid
Eicosapentaenoic acid (EPA)	20:5 (n−3)	all-cis-5,8,11,14,17-eicosapentaenoic acid
Heneicosapentaenoic acid (HPA)	21:5 (n−3)	all-cis-6,9,12,15,18-heneicosapentaenoic acid
Docosapentaenoic acid (DPA), Clupanodonic acid	22:5 (n−3)	all-cis-7,10,13,16,19-docosapentaenoic acid
Docosahexaenoic acid (DHA)	22:6 (n−3)	all-cis-4,7,10,13,16,19-docosahexaenoic acid
Tetracosapentaenoic acid	24:5 (n−3)	all-cis-9,12,15,18,21-tetracosapentaenoic acid
Tetracosahexaenoic acid (Nisinic acid)	24:6 (n−3)	all-cis-6,9,12,15,18,21-tetracosahexaenoic acid

The omega−6 to omega−3 ratio (Most Important)

Some clinical studies indicate that the ingested ratio of omega−6 to omega−3 (especially linoleic vs alpha-linolenic) fatty acids is important to maintaining cardiovascular health. However, two studies published in 2005 and 2007 found that while omega−3 polyunsaturated fatty acids are extremely beneficial in preventing heart disease in humans, the levels of omega−6 polyunsaturated fatty acids (and therefore the ratios) were insignificant. 

Both omega−6 and omega−3 fatty acids are essential; i.e., humans must consume them in the diets. Omega−6 and omega−3 eighteen-carbon polyunsaturated fatty acids compete for the same metabolic enzymes, thus the omega−6:omega−3 ratio of ingested fatty acids has significant influence on the ratio and rate of production of eicosanoids, a group of hormones intimately involved in the body's inflammatory and homeostatic processes which includes the prostaglandins, leukotrienes, and thromboxanes, among others.

This necessitates that omega−6 and omega−3 be consumed in a balanced proportion; healthy ratios of omega−6:omega−3, according to some authors, range from 1:1 to 1:4 (an individual needs more omega−3 than omega−6). Other authors believe that ratio 4:1 (when the amount of omega-6 is only 4 times greater than that of omega-3) is already healthy. Studies suggest the evolutionary human diet, rich in game animals, seafood, and other sources of omega−3, may have provided such a ratio.

Daily values

As macronutrients, fats are not assigned Dietary Reference Intakes. Macronutrients have acceptable intake (AI) levels and acceptable macronutrient distribution ranges (AMDRs) instead of RDAs. The AI for omega−3 is 1.6 grams/day for men and 1.1 grams/day for women, while the AMDR is 0.6% to 1.2% of total energy.

Grams of omega−3 per 3oz (85g) serving
Common name	grams omega−3
Herring, sardines	1.3–2
Mackerel: Spanish/Atlantic/Pacific	1.1–1.7
Salmon	1.1–1.9
Halibut	0.60–1.12
Tuna	0.21–1.1
Swordfish	0.97
Greenshell/lipped mussels	0.95
Tilefish	0.9
Tuna (canned, light)	0.17–0.24
Pollock	0.45
Cod	0.15–0.24
Catfish	0.22–0.3
Flounder	0.48
Grouper	0.23
Mahi mahi	0.13
Orange roughy	0.028
Red snapper	0.29
Shark	0.83
King mackerel	0.36
Hoki (blue grenadier)	0.41
Gemfish	0.40
Blue eye cod	0.31
Sydney rock oysters	0.30
Tuna, canned	0.23
Snapper	0.22
Eggs, large regular	0.109
Barramundi, saltwater	0.100
Giant tiger prawn	0.100
Lean red meat	0.031
Turkey	0.030
Cereals, rice, pasta, etc.	0.00
Fruit	0.00
Milk regular	0.00
Regular bread	0.00
Vegetables	0.00